Compounds and methods for the treatment or prevention of Flavivirus infections

A compound having the formula Ia:

• or a pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-14 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaRb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, provided that R16 is other than methyl or ethyl;
• R1 is C2-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R2 is C2-12 alkyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, N R13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above is unsubtituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, N R13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2,
• R12, Rc, Rd, R13 and R14 are each independently chosen from H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, and C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle,
• with the proviso that:
• i) when X is 4-Chloro-2,6-dimethyl-benzenesulfonamide and, R1 is phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• ii) when X is Toluene-4-sulfonamide and R1 is 4-chloro-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• iii) when X is Toluene-4-sulfonamide and R1 is 4-fluoro-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• iv) when X is Toluene-4-sulfonamide and R1 is 4-methoxy-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• and
• v) when X is Benzamide and R1 is phenyl Y1 is a bond and Y is COOH then R3 is other than hydrogen.

A method for treating or preventing a Flaviviridae viral infection in a host comprising administering to the host a therapeutically effective amount of at least one compound having the formula III:

• or a pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is H or C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-12 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-12 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• and
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl , C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle.

A pharmaceutical composition comprising at least one compound having the formula III:

• or a pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is H or C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-12 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-12 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• and
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl , C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle;
• and
• at least one pharmaceutically acceptable carrier or excipient.

A method for inhibiting or reducing the activity of viral polymerase in a host comprising administering a therapeutically effective amount of a compound having the formula III:

• or a pharmaceutically acceptable salt thereof;
• wherein
• X is:
• M is chosen from:
• R4 is H or C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-12 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-12 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C1-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• and
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl , C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle.

A method for inhibiting or reducing the activity of viral helicase in a host comprising administering a therapeutically effective amount of a compound having the formula III:

• or a pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is H or C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-12 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-12 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• and
• Z is H, halogen, C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl , C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle.

A combination comprising a compound having the formula III:

• or pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is H or C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-12 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-12 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl, or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• and
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C2-6 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amindino or guanido;
• in each above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3RR12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case above heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C6-12 aryloxy, C(O)C1-6 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroaralkyl groups are heteroaralkyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle;
• and
• one or more additional agents chosen from viral serine protease inhibitors, viral polymerase inhibitors, viral helicase inhibitors, immunomudulating agents, antioxidant agents, antibacterial agents and antisense agents.

A process for preparing a compound of formula A:

• said process comprising the steps of adding:
• an enol ether;
• an hydride donating agent;
• and
• an organic carboxylic acid;
• to a compound of formula B:
• wherein,
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaRb, S(O)OR5, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, CON(R9)—SO2—R5, CONR9OH or halogen;
• R9, R5, R10 and R11 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or R10 and R11 are taken together with the nitrogen to form a 3 to 10 membered heterocycle;
• Ra and Rb are each independently H, C1-12 alkyl, C1-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl and C6-18 aralkyl, or Ra and Rb are taken together with the oxygens to form a 5 to 10 membered heterocycle;
• R16 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• R1 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, C6-18 aralkyl or halogen;
• R2 is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl;
• R3 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl or C6-18 aralkyl;
• Z is H, halogen, or C1-6 alkyl;
• wherein
• in each case above alkyl is straight chain, branched chain or cyclic and is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkenyl is unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above alkynyl is unsubstituted or substituted by one or more halogen nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aryl is a carbocyclic moiety containing at least one benzenoid-type ring which are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above aralkyl is an aryl group attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl group;
• in each case heterocyclic groups contain at least one heteroatom selected from oxygen, sulfur or nitrogen, and are unsubstituted or substituted by one or more halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR12R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino or guanido;
• in each case above heteroarakyl groups are heteroaryl groups attached to the adjacent atom by a C1-6 alkyl, C1-6 alkenyl, or C1-6 alkynyl;
• sulfur atoms are in each case above present in the form of S, SO, or SO2;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens from a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen form a 3 to 10 membered heterocycle.

A compound having the formula I:

• or a pharmaceutically acceptable salt thereof;
• wherein,
• X is:
• M is chosen from:
• R4 is C1-6 alkyl;
• R8 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R15 is H or C1-6 alkyl;
• J is chosen from:
• W is O, S or NR7;
• R7 is H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-12 heteroaralkyl, or C6-16 aralkyl;
• R6 is H, C1-12 alkyl, C6-14 aryl or C6-16 aralkyl;
• Y1 is a bond, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl;
• Y is COOR16, COCOOR5, P(O)ORaORb, S(O)2OR5, tetrazole, CON(R9)CH(R5)COOR5, CONR10R11, or CONR9OH;
• R5, Ra, Rb, R9, R10, R11 and R16 are each independently H or C1-6 alkyl, provided that R16 is other than methyl or ethyl;
• R1 is t-butyl, isobutyl, allyl, ethynyl, 2-phenylethenyl, isobutenyl, benzyl, phenyl, phenethyl, benzodioxolyl, thienyl, thiophenyl, pyridinyl, isoxazolyl, thiazolyl, pyrazolyl, tetrazolyl, benzofuranyl, indolyl, furanyl, or benzothiophenyl, which in each case is unsubstituted or substituted by one or more substituent chosen from halogen, nitro, nitroso, SO2R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10 heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino and guanido;
• R2 is thienyl, furanyl, pyridinyl, oxazolyl, thiazolyl, pyrrolyl, benzofuranyl, indolyl, benzoxazolyl, benzothienyl, benzothiazolyl, piperazinyl, pyrrolidinyl, or quinolinyl, which in each case is unsubstituted or substituted by one or more substituent chosen from halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aryl, C(O)C6-12 aralkyl, C3-10heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino and guanido;
• R3 is H, methyl, ethyl, i-propyl, cyclopropyl, cyclohexyl, allyl, piperidinyl, piperazinyl, pyrrolidinyl, azetidinyl, aziridinyl, pyridinyl, piperidinylmethyl, dioxanyl, dioxolanyl, azepanyl or benzyl, which is each case is unsubstitued or substituted by one or more substituent chosen from halogen, nitro, nitroso, SO3R12, PO3RcRd, CONR13R14, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aralkyl, C6-12 aryl, C1-6 alkyloxy, C2-6 alkenyloxy, C2-6 alkynyloxy, C6-12 aryloxy, C(O)C1-6 alkyl, C(O)C2-6 alkenyl, C(O)C2-6 alkynyl, C(O)C6-12 aralkyl, C3-10heterocycle, hydroxyl, NR13R14, C(O)OR12, cyano, azido, amidino and guanido;
• and
• Z is methyl, trifluoromethyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, isobutyl, cyclobutyl, pentyl, neopentyl, cyclopentyl, hexyl or cyclohexyl;
• and
• R12, Rc, Rd, R13 and R14 are each independently H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-14 aryl, C3-12 heterocycle, C3-18 heteroaralkyl, or C6-18 aralkyl, or Rc and Rd are taken together with the oxygens to form a 5 to 10 membered heterocycle, or R13 and R14 are taken together with the nitrogen to form a 3 to membered 10 membered heterocycle;
• with the proviso that:
• i) when X is 4-Chloro-2,6-dimethyl-benzenesulfonamide and, R1 is phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• ii) when X is Toluene-4-sulfonamide and R1 is 4-chloro-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• iii) when X is Toluene-4-sulfonamide and R1 is 4-fluoro-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• iv) when X is Toluene-4-sulfonamide and R1 is 4-methoxy-phenyl, and R3 is H, and Y1 is a bond, then Y is other than CONH2;
• and
• v) when X is Benzamide and R1 is phenyl Y1 is a bond and Y is COOH then R3 is other than hydrogen.

A compound chosen from:

• 3-[(4-chloro-2,5-dimethyl-benzenesulfonyl)-(3-iodo-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-benzofuran-2-yl-benzyl)-(4-chloro-2,5-dimethyl-benzenesulfonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-{(2,4-dichloro-benzoyl)-[5-(3-trifluoromethyl-phenyl)-furan-2-ylmethyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2,5-dimethyl-benzenesulfonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-fluoro-phenyl)-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,4-dichloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-tert-butyl-3-(4-chloro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 4-(toluene-4-sulfonylamino)-[2,3′]bithiophenyl-5-carboxylic acid;
• 3-[(5-benzofuran-2-yl-thiophen-2-ylmethyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-5-(4-chloro-phenyl)-thiophene-2-carboxylic acid;
• 5-phenyl-3-(toleune-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenyl-3-(toluene-3-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-benzenesulfonylamino-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-5-(4-isobutyl-phenyl)-thiophene-2-carboxylic acid;
• 5-tert-butyl-3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,5-dimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-methoxy-2,3,6-trimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(thiophene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 4-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-[2,3′]bithiophenyl-5-carboxylic acid;
• 5-(3,5-bis-trifluoromethyl-phenyl)-3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 8-chloro-3-(4-chloro-2,5-dimethyl-benzenesulfonylamino)-4H-1,5-dithia-cyclopenta[A]naphthalene-2-carboxylic acid;
• 3-(2,4-difluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[3-(2,6-dichloro-pyridin-4-yl)-ureido]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-chloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-fluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2-trifluoromethoxy-benzenesulfonylamino)-thiophene-2-carboxylic acid
• 3-(4-tert-butyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-phenoxycarbonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3,4-dichloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2-trifluoromethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(5-bromo-6-chloro-pyridine-3-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(5-chloro-thiophene-2-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(5-chloro-3-methyl-benzo[b]thiophene-2-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-bromo-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3-chloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3-bromo-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-isopropyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2,6-dichloro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-nitro-benzenesulfonylamino)-5-phenyl-thiphene-2-carboxylic acid;
• 5-phenyl-3-(5-[1,2,3]thiadiazol-4-yl-thiophene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenyl-3-(pyridine-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,4-dichloro-benzylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3-fluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(3-trifluoromethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2-carboxy-benzoylamino)-5-phenyl-thiophene-2-carboxylic acid methyl ester;
• 5-phenyl-3-(4-trifluoromethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,5-difluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-cyano-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2,5-dichloro-thiophene-3-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 4-(toluene-2-sulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 5′-chloro-4-(toluene-2-sulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 5-(2,4-dichloro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-nitro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-(4-trifluoromethoxy-phenyl)-thiophene-2-carboxylic acid;
• 5-quinolin-8-yl-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenyl-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-nitro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-m-tolyl-thiophene-2-carboxylic acid;
• 5-(3-chloro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-fluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-fluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-chloro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3,5-difluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3,4-difluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-vinyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-benzoylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-[(thiophene-2-carbonyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(thiophene-2-carbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-bromo-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2,4-difluoro-benzoylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-difluoro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-trimethylsilanylethynyl-thiophene-2-carboxylic acid;
• 5-ethynyl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-(3-trifluoromethoxy-phenyl)-thiophene-2-carboxylic acid;
• 5-benzoyl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-cyano-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-chloro-4-fluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3,4-dichloro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-pyridin-4-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-pyridin-3-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-(4-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-methanesulfonyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-acetylamino-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-chloro-4-fluoro-phenyl)-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-methyl-benzoylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3,5-dimethyl-isoxazole-4-sulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-methyl-benzoylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(2-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(5-trifluoromethyl-pyridine-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenylethynyl-3-(toluene-2-sulfonylamino)thiophene-2-carboxylic acid;
• 3-(2,5-dimethyl-benzenesulfonylamino)-5-(4-nitro-phenyl)-thiophene-2-carboxylic acid;
• 5-(2-fluoro-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(2-cyano-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 103 5-(2-ethoxycarbonyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(2-methoxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3′-methyl-4-(toluene-2-sulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-(toluene-2-sulfonylamino)-5-(2-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-(2,5-dimethyl-benzenesulfonylamino)-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;
• 5-styryl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,4-difluoro-benzenesulfonylamino)-5-(4-nitro-phenyl)-thiophene-2-carboxylic acid;
• 3-(2,4-difluoro-benzenesulfonylamino)-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;
• 3-[[5-(3-chloro-4-fluoro-phenyl)-thiophen-2-ylmethyl]-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-oxo-1-phenyl-1,3,8-triaza-spiro[4.5]decane-8-carbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(4-nitro-phenyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 5-(2-carboxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-chloro-phenyl)-3-(pyridine-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-cyano-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,5-dimethyl-benzenesulfonylamino)-5-p-tolyl-thiophene-2-carboxylic acid;
• 3-(2,4-difluoro-benzenesulfonylamino)-5-p-tolyl-thiophene-2-carboxylic acid;
• 5-phenethyl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-ethoxycarbonyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-methoxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-methoxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid
• 5-(4′-bromo-biphenyl-4-yl)-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-hydroxymethyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-furan-3-yl-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-benzofuran-2-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-pyridin-2-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-nitro-phenyl)-3-(pyridine-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(benzofuran-2-carbonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dimethyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[[5-(2-cyano-phenyl)-thiophenyl-2-ylmethyl]-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-fluoro-phenyl)-3-(pyridine-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-[2-(4-chloro-phenyl)-vinyl]-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-benzenesulfonylamino-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;
• 3-(2,4-dimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2-vinyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-bromo-2,5-difluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-acetylamino-4-methyl-thiazole-5-sulfonylamino)-5-phenyl-thiophene-2-thiophene-2-carboxylic acid;
• 3-(4-acetyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-fluoro-2-trifluoromethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-methoxy-4-methyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3,4-difluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 4-(2-carboxy-5-phenyl-thiophen-3-ylsulfamoyl)-5-(4-chloro-phenyl)-2-methyl-furan-3-carboxylic acid ethyl ester;
• 3-(4-fluoro-3-trifluoromethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-amino-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(3-nitro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-nitro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(3-cyano-benzyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2,4,6-trifluoro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-methoxy-2-nitro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2,3,4-trichloro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 5-(2-carboxy-5-phenyl-thiophen-3-ylsulfamoyl)-2-methyl-furan-3-carboxylic acid methyl ester;
• 4-(2-carboxy-5-phenyl-thiophen-3-ylsulfamoyl)-2-methyl-1,5-diphenyl-1H-pyrrole-3-carboxylic acid ethyl ester;
• 5-phenyl-3-{[4-(3-trifluoromethyl-phenyl)-piperazine-1-carbonyl]-amin}-thiophene-2-carboxylic acid;
• 3-{[4-(4-fluoro-phenyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(2,6-dimethyl-phenyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(2-chloro-phenyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(3-chloro-phenyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 4,4′-bis-(toluene-2-sulfonylamino)-[2,2′]-bithiophenyl-5,5′-dicarboxylic acid;
• 3-[allyl-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(1-dimethylsulfamoyl-1H-pyrazol-4-yl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-amino-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-amino-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 4-(2-carboxy-5-phenyl-thiophen-3-ylsulfamoyl)-2,5-dimethyl-1H-pyrrole-3-carboxylic acid ethyl ester;
• 4-(2-carboxy-5-phenyl-thiophen-3-ylsulfamoyl)-5-(4-chloro-phenyl)-3-methyl-1-phenyl-1H-pyrrole-2-carboxylic acid ethyl ester;
• 3-(3,5-dichloro-4-hydroxy-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-(1H-pyrazol-4-yl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(3-hydroxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[methyl-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-{[2-(4-fluoro-phenyl)-acetyl]-methyl-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-pentyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(methyl-phenylacetyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[2,5-bis-(2,2,2-trifluoro-ethoxy)-benzenesulfonylamino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-methyl-2nitro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-thiazol-2-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-phenyl-3-[3-(3-phenyl-propyl)-ureido]-thiophene-2-carboxylic acid;
• 3-[(3,4-dihydro-1H-isoquinoline-2-carbonyl)-amino]-5-phenyl-thoiphene-2-carboxylic acid;
• 3-{[4-(4-methoxy-phenyl)-piperazine-1-carbonyl]-amino}-phenyl-thiophene-2-carboxylic acid;
• 3-{[4-(6-methyl-pyridin-2-yl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid hydrochloride;
• 3-{[4-(4-chloro-benzyl)-piperazine-1-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid hydrochloride;
• 5-(5-methyl-pyridin-2-yl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[ethyl-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-thiophene-2-carbonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-bromo-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-butyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2-chloromethyl-benzenesulfonylamino-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-hydroxy-phenyl)-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(5-chloro-pyridin-2-yl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-chloro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(4-cyano-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-(4-nitro-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-hydroxymethyl-phenyl)-3-[methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-(3-nitro-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-fluoro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(4-methoxy-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-p-tolyl-thiophene-2-carboxylic acid;
• 5-(4-amino-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[cyclopentyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-benzo[1,3]dioxol-5-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-ethyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isobutyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-methoxy-4-methyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(3-cyano-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(2-chloro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-phenyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-(trifluoromethyl-benzoyl)methylamine]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(3,5-difluoro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(3-fluoro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(2,4-difluoro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(4-hydroxy-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-(4-trifluoromethoxy-phenyl)-thiophene-2-carboxylic acid;
• 5-(2-hydroxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3,5-dichloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-bromo-2-methyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(5-carboxy-4-chloro-2-fluoro-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2,3,4-triflouro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-bromo-2-fluoro-benzenesulfonylamino)-5-(4-isobutyl-phenyl)-thiophene-2-carboxylic acid;
• 3-(4-bromo-2-methyl-benzenesulfonylamino)-5-(4-isobutyl-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-isobutyl-phenyl)-3-(3-methoxy-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(4-fluoro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[2,5-bis-(2,2,2-trifluoro-ethoxy)-benzenesulfonylamino]-5-(4-isobutyl-phenyl)-thiophene-2-carboxylic acid;
• 3-(2-chloro-4-cyano-benzenesulfonylamino)-5-(4-isobutyl-phenyl)-thiophene-2-carboxylic acid;
• 5′-acetyl-4-(toluene-2-sulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 5-benzo[b]thiophen-2-yl-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-butyl-phenyl)-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-ethyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[benzyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dimethyl-benzenesulfonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-(4-chloro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-carboxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid tert-butyl ester;
• 3-[(2,4-dimethyl-benzenesulfonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(4-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-ethanesulfonylamino-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-trifluoromethyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(3-methyl-but-2-enyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,6-dichloro-pyridine-3-carbonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(6-chloro-pyridine-3-carbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-carboxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-ethoxy-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(2,6-dichloro-pyridine-3-carbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(benzo[b]thiophene-2-carbonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(napthalene-2-carbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3,4-dichloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3,5-dichloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-bromo-3-methyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzo[b]thiophene-2-carbonyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-3-nitro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-carbamoyl-phenyl)-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-carbamoyl-phenyl)-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(1H-indol-5-yl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[sec-butyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dimethyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-azido-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(1-phenyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-carbamoyl-phenyl)-3-(4-chloro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 5-(2-fluoro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-o-tolyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-m-tolyl-thiophene-2-carboxylic acid;
• 5-(3-chloro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(3,4-diflouro-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(3-amino-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(3-acetyl-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 5-(3-hydroxy-phenyl)-3-[methyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-(4-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[(3,4-dimethoxy-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(2,4,6-trifluoro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,3-difluoro-4-trifluoromethyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-fluoro-4-trifluoromethyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,3-diflouro-4-methyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-fluoro-4-trifluoromethyl-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-carbamoyl-phenyl)-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 5-(4-fluoro-phenyl)-3-[isopropyl-(4-methyl-benzoyl)-amino]-thiophene-2-carboxylic acid;
• 3-[(2-bromo-4-chloro-benzoyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2,6-dimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid methyl ester;
• 5-(4-cyano-phenyl)-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-chloro-benzenesulfonylamino)-5-(4-cyano-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-cyano-phenyl)-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid;
• 5′-acetyl-4-(2,4-dimethyl-benzenesulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 5′-acetyl-4-(2,6-dimethyl-benzenesulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-[methyl-(4-methyl-thiophene-2-carbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(3-chloro-phenyl)-3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 5′-cyano-4-(toluene-2-sulfonylamino)-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-pyridin-2-yl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-thiobenzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-(2,4,6-trimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(1-carboxy-ethyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-benzoyl)-(3-methyl-but-2-enyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-benzoyl)-amino]-5-pyridin-3-yl-thiophene-2-carboxylic acid;
• 5′-acetyl-4-[methyl-(4-methyl-benzoyl)-amino]-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-[isopropyl-(4-methyl-benzoyl)-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-benzoyl)-amino]-5-m-tolyl-thiophene-2-carboxylic acid;
• 3-[(2-bromo-4-chloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2-fluoro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(2,4-dimethyl-benzenesulfonylamino)-4-methyl-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-bromo-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2-iodo-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-cyano-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[allyl-(4-methyl-benzoyl)-amino]-5-[4-(2-carboxy-vinyl)-phenyl]-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2-hydroxy-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-4-methyl-5-phenyl-thiophene-2-carboxylic acid;
• 5-tert-butyl-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-[4-(2-carboxy-ethyl)-phenyl]-3-[(4-methyl-benzoyl)-propyl-amino]-thiophene-2-carboxylic acid;
• 5-benzofuran-2-yl-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-(2,4-dimethyl-benzenesulfonylamino)-5-(4-hydroxymethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-(2,4-dimethyl-benzenesulfonylamino)-5-(4-methanesulfonyl-phenyl)-thiophene-2-carboxylic acid;
• 5-[4-(2-carboxy-vinyl)-phenyl]-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[allyl-(4-methyl-benzoyl)-amino]-5-[3-(2-carboxy-vinyl)-phenyl]-thiophene-2-carboxylic acid;
• 3-[isopropyl-(2,4,6-trimethyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-[3-(2-carboxy-ethyl)-phenyl]-3-[(4-methyl-benzoyl)-propyl-amino]-thiophene-2-carboxylic acid;
• 3-[(2-fluoro-4-trifluoromethyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[tert-butyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-amino-4-chloro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2-nitro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-benzoyl)-(3-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-fluoro-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-carboxy-phenyl)-3-(2,4-dimethyl-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[cyclopropyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-tert-butyl-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-difluoro-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-2,5-difluoro-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(2-methyl-allyl)-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(4-chloro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-[benzyl-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-benzoyl)-(4-nitro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-benzoyl)-(2-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-methoxy-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-(4-methyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-isobutyl-thiophene-2-carboxylic acid;
• 3-[allyl-(2-naphthalen-2-yl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(2,4-dichloro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(2-chloro-4-fluoro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(3,4-dichloro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(2,4-difluoro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(4-trifluoromethyl-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(2,6-dichloro-phenyl)-acetyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-[allyl-(2-m-tolyl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-m-tolyl-thiophene-2-carboxylic acid;
• 5′-acetyl-4-[(2,4-dichloro-benzoyl)-isopropyl-amino]-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 4-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5′-methyl-[2,2′]bithiophenyl-5-carboxylic acid;
• 3-(2,4-dimethyl-benzenesulfonylamino)-5-(4-methoxy-phenyl)-thiophene-2-carboxylic acid;
• 3-(cyclohexanecarbonyl-isopropyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-{(2,4-dichloro-benzoyl)-[1-(2,4-dichloro-benzoyl)-piperidin-4-yl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 4-[(2-carboxy-5-phenyl-thiophen-3-yl)-(4-methyl-benzoyl)-amino]-piperadine-1-carboxylic acid tert-butyl ester;
• 4-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-piperadine-1-carboxylic acid tert-butyl ester;
• 3-[(4-methyl-benzoyl)-piperadin-4-yl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5′-acetyl-4-(2,4-dimethyl-benzenesulfonylamino)-[2,3′]bithiophenyl-5-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-piperidin-4-yl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-methanesulfonylamino-phenyl)-3-toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-(4-fluoro-2-methyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(4-chloro-2-methyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(4-methanesulfonyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(4-methanesulfinyl-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-carboxy-phenyl)-3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 5-benzofuran-2-yl-3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 3-[(2-acetoxy-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(2-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(2-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(cycloheptanecarbonyl-isopropyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-methyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-(3-nitro-phenyl)-thiophene-2-carboxylic acid;
• 3-[(3-cyclopentyl-propionyl)-methyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(butyryl-methyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(methyl-pent-4-enoyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(5-methyl-3-oxo-3H-isoindol-1-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(methyl-pentanoyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[methyl-(4-methyl-pentanoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(cyclopentanecarbonyl-ethyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-cyclopentyl-propionyl)-ethyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(cyclobutanecarbonyl-ethyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(but-2-enonyl-ethyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-2-vinyl-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohex-1-enecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(allyl-hexanol-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(allyl-cyclobutanecarbonyl-amino)-5-phenyl-thiophene-2-cabroxylic acid;
• 3-(allyl-pentanoyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[allyl-(4-methyl-pentanoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[allyl-(2-cyclopentyl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-4-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(1-phenyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(1-phenyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(3-methyl-cyclopent-3-enecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-benzyloxy-4-methyl-benzoyl)-isopropyl-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dimethyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(3-methyl-cyclopentanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-4-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-phenyl-3-[propionyl-(4-trifluoromethyl-benzyl)-amino]-thiophene-2-carboxylic acid;
• 3-[isobutyryl-(4-trifluormethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[3-methyl-butyryl)-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclopropanecarbonyl-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclobutanecarbonyl-(4-triofluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-cyclopentyl-acetyl)-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-nitro-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-methyl-butyryl)-(4-nitro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclopropanecarbonyl-(4-nitro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-isobutyryl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-cyclopropanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(adamantane-1-carbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-cyclobutanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(2-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-methyl-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-4-methyl-benzoyl)-isopropyl-amino]-5-(3-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 3-[(1-acetyl-piperidin-4-yl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-[4-(1H-tetrazol-5-yl)-phenyl]-thiophene-2-carboxylic acid;
• 3-[(2-cyano-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclobutanecarbonyl-(2-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(2-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(3-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclobutanecarbonyl-(4-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclohexanecarbonyl-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-isobutyryl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-cyclopropanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-cyclobutanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-butyryl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-cyclohexanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-tert-butyl-benzyl)-cyclopentyl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-cyclopentyl-acetyl)-(4-nitro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzyl)-cyclohexanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-cyclopentyl-acetyl)-(3-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(3-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(2-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-m-tolyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-thiazol-2-yl-thiophene-2-carboxylic acid;
• 3-(acetyl-benzyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(benzyl-propionyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[benzyl-(2-methoxy-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[benzyl-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(benzyl-cyclopropanecarbonyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(4-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-isobutyryl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-cyclopropanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-acetyl-phenyl)-3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-cyclobutanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(4-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-benzyl)-(2-cyclopentyl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(4-trifluoromethyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isobutyryl-(3-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclopropanecarbonyl-(3-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isobutyryl-(4-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclopropanecarbonyl-(4-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(4-methyl-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-methoxy-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-methoxy-benzyl)-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclobutanecarbonyl-(3-methoxy-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-carbamoyl-4-methyl-benzoyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(3-methoxy-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(3-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-propionyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-(2-methoxy-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-cyclopropanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-chloro-benzyl)-cyclobutanecarbonyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(3-chloro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[acetyl-(2,4-diflouro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-difluoro-benzyl)-(2-methoxy-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-difluoro-benzyl)-isobutyryl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-difluoro-benzyl)-(3-methyl-butyryl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[benzyl-(2-cyclopenyl-acetyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-(1H-indol-5-yl)-thiophene-2-carboxylic acid;
• 3-(benzyl-cyclobutanecarbonyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclohexanecarbonyl-(2,4-difluoro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-{allyl-[2-(4-methoxy-phenyl)-acetyl]-amino}-phenyl-thiophene-2-carboxylic acid;
• 3-(ethyl-hexanoyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(butyryl-ethyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[ethyl-(4-methyl-pentanoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclobutanecarbonyl-(2,4-difluoro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[butyryl-(2,4-difluoro-benzyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(cyclopentanecarbonyl-methyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-(cyclohexanecarbonyl-methyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-carboxy-5-phenyl-thiophene-3-yl)-(2,4-dichloro-benzoyl)-amino]-pyrrolidine-1-carboxylic acid tert-butyl ester;
• 3-[(1,4-dimethyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-ethyl-phenyl)-3-[(2-hydroxy-4-methyl-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 3-[(2-hydroxy-4-methyl-benzoyl)-isopropyl-amino]-5-m-tolyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-pyrrolidin-3-yl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-{5-carboxy-4-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophen-2-yl}-3,6-dichydro-2H-pyridine-1-carboxylic acid benzyl ester;
• 3-{[2-(hydroxyimino-methyl)-4-methyl-benzoyl]-isopropyl-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(1-carbamimidoyl-piperidin-4-yl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-azepane-1-azephane-1-carboxylic acid tert-butyl ester;
• 4-{[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-methyl}-piperidine-1-carboxylic acid benzyl ester;
• 3-[azepan-4-yl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-cyclohexanecarbonyl)-piperidin-4-yl-amino]-5-phenyl-thiophene-2-carboxylic acid lithium salt;
• 3-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester;
• 3-[(4-benzyloxycarbonylamino-cyclohexyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-2-oxo-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-piperidin-3-yl-amino]-5-phenyl-thiophene-2-carboxylic;
• 3-[(4-benzyloxycarbonylamino-cyclohexyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-benzyloxy-1-methyl-ethyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,2-dimethyl-[1,3]dioxan-5-yl)-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2-hydroxy-1-hydroxymethyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-piperidin-4-ylmethyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2-chloro-benzoyl)-piperidin-4-ylmethyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4,6-dichloro-1H-indole-2-carbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2-hydroxy-1-methyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-{1-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-ethyl}-piperidine-1-carboxylic acid benzyl ester;
• 4-{5-carboxy-4-[isopropyl-(4-methyl-cyclohexanecarbonyl)amino]-thiophene-2-yl}-3,6-dihydro-2H-pyridine-1-carboxylic acid benzyl ester;
• 3-[(4-methyl-cyclohexanecarbonyl)-pyridin-4-yl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-5-piperidin-4-yl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-propyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]cyclohexyl-ammonium;
• trifluoro-acetate;
• 3-[(2,4-dichloro-benzoyl)-(1-piperidin-4-yl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(cyclohex-3-enecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-ethyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-chloro-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-3-methyl-piperidime-1-carboxylic acid benzyl ester;
• 3-[(2,4-dichloro-benzoyl)-(2-methoxy-cyclohexyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2,2-dimethyl-[1,3]dioxan-5-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-(1-methyl-piperidin-4-yl)-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(3-methyl-piperidin-4-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2-hydroxy-cyclohexyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-{[(2-carboxy-5-phenyl-thiophen-3-yl)-(4-methylcyclohexane carbonyl)-amino]-methyl}-piperidine-1-carboxylic acid benzyl ester;
• 3-[((1R,2S,4R)-2-hydroxy-4-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-{isopropyl-[1-(4-methoxy-2,3,6-trimethyl-benzenesulfonyl)-5-methyl-1,2,3,6-tetrahydro-pyridine-2-carbonyl]-amino}-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-4-fluoro-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(1-methyl-piperidin-4-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 4-{[(2-carboxy-5-phenyl-thiophen-3-yl)-(4-methycyclohexane carbonyl)-amino]-methyl}-piperidinium;
• trifluoro-acetate;
• 3-[(2-tert-butoxycarbonylamino-1-methyl-ethyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 2-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-propyl-amine trifluoroacetic acid salt;
• 3-[(3-carboxy-cyclopentyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(3-carboxy-cyclopentyl)-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 2-[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-cyclohexyl-ammonium chloride;
• 3-(benzoyl-methyl-amino)-5-phenyl-thiophene-2-carboxylic acid;
• {[5-phenyl-3-(toluene-4-sulfonylamino)-thiophene-2-carbonyl]-amino}-acetic acid;
• 5-bromo-3-(toluene-2-sulfonylamino)-thiophene-2-carboxylic acid;
• 3-[cyclohexyl-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[[1,3]dioxan-5-yl-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[[2-(tert-butyl-dimethyl-silanyloxy)-1-methyl-2-phenyl-ethyl]-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[[2-(tert-butyl-dimethyl-silanyloxy)-1-methyl-2-phenyl-ethyl]-(2,4-dichloro-benzoyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2-diethylamino-thiazol-5-ylmethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• (5-{[(2-carboxy-5-phenyl-thiophen-3-yl)-(2,4-dichloro-benzoyl)-amino]-methyl}-thiazol-2-yl)-diethyl-ammonium;
• chloride;
• 5-(4-fluoro-phenyl)-3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-thiophene-2-carboxylic acid;
• 3-[((1S,2R,4S)-2-hydroxy-4-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-dichloro-benzoyl)-(2-methoxy-1-methyl-ethyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4S)-isopropyl-(4-methyl-cyclohex-1-enecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-methyl-(4-methylbenzoyl)-amino)5-phenyl thiophene-2-carboxylic acid (2-hydroxy-ethyl)amide;
• 5-phenyl-3-(toluene-4-sulfonylamino)-thiophene-2-carboxylic acid cyclobutylamide;
• 3-(2,4-dimethyl-benzenesulfonylamino)-5-phenyl-thiophene-2-carboxylic acid amide;
• 5-bromo-3-[(2,4-dichloro-benzoyl)-isopropyl-amino]-thiophene-2-carboxylic acid;
• 5-(4-chloro-phenyl)-3-[isopropyl-(4-methyl-cylcohexane-carbonyl)-amino]-thiophene-2-carboxylic acid;
• 5-(4′-chloro-biphenyl-4-yl)-3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-thiophene-2-carboxylic acid;
• 3-[(4-methyl-cyclohexanecarbonyl)-(tetrahydro-pyran-4-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-cyclohexanecarbonyl)-(1-methyl-piperidin-4-yl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(4-methyl-cyclohexanecarbonyl)-piperidin-4-yl-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-(4-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid;
• 5-(4-cyano-phenyl)-3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-thiophene-2-carboxylic acid;
• 3-[isopropyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-(4-methoxy-phenyl)-thiophene-2-carboxylic acid;
• 3-[(2-methoxy-1-methyl-ethyl)-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 3-[cyclohexyl-(4-methyl-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid;
• 5-(4-Isobutyl-phenyl)-3-[5-(5-trifluoromethyl-isoxazol-3-yl)-thiophene-2-sulfonylamino]-thiophene-2-carboxylic acid;
• 5-(4-Isobutyl-phenyl)-3-(2,3,4-trifluoro-benzenesulfonylamino)-thiophene-2-carboxylic acid;
• 3-[(2,4-Dichloro-phenyl)-isopropyl-carbamoyl]-5-phenyl-thiophene-2-carboxylic acid;
• 3-(Methyl-p-tolyl-carbamoyl)-5-phenyl-thiophene-2-carboxylic acid;
• 3-[(2,4-Dichloro-phenyl)-methyl-carbamoyl]-5-phenyl-thiophene-2-carboxylic acid;
• or pharmaceutically acceptable salts thereof.