Compounds

A compound of the formula:

• wherein
• G3 is CH2;
• G4 is CH;
• R1 is C(Z)N(R10′)(CR10R20)vRb;
• R1′ is independently selected at each occurrence from hydrogen, halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v′NRdRd′, (CR10R20)v′C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v′OR13;
• Rb is an optionally substituted heteroaryl, an optionally substituted heteroaryl C1-10 alkyl, an optionally substituted heterocyclic, or an optionally substituted heterocyclic C1-10 alkyl;
• X is R2, OR2′, S(O)mR2′, (CH2)n′N(R10′)S(O)mR2′, (CH2)n′N(R10′)C(O)R2′, (CH2)n′NR4R14, (CH2)n′N(R2′)(R2″), or N(R10′)RhNH—C(═N—CN)NRqRq′;
• X1 is N(R11), O, S(O)m, or CR10R20;
• Rh is selected from an optionally substituted C1-10 alkyl-, —CH2—C(O)—CH2—, —CH2—CH2—O—CH2—CH2—, —CH2—C(O)N(R10′)CH2—CH2—, —CH2—N(R10′)C(O)CH2—, —CH2—CH(OR10′)—CH2—, —CH2—C(O)O—CH2—CH2—, or —CH2—CH2—O—C(O) CH2—;
• Rq and Rq′ are independently selected from hydrogen, C1-10 alkyl , C3-7cycloalkyl, C3-7cycloalkylC1-10alkyl, C5-7 cycloalkenyl, C5-7 cycloalkenyl-C1-10alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, wherein all of the moieties are optionally substituted, or Rq and Rq′ together with the nitrogen to which they are attached form a 5 to 7 membered optionally substituted ring, which ring may contain an additional heteroatom selected from O/N/S;
• R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or
• R2 is the moiety (CR10R20)q′X1(CR10R20)qC(A1)(A2)(A3), or (CR10R20)q′C(A1)(A2)(A3);
• R2′ is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• R2″ is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and
• wherein these moieties, excluding hydrogen, may be optionally substituted 1 to 4 times, independently, by C1-10 alkyl, halo-substituted C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl, C3-7cycloalkylC1-10alkyl, C5-7cycloalkenyl, C5-7 cycloalkenyl C1-10 alkyl, halogen, —C(O), cyano, nitro, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nN(R10′)S(O)2R7, (CR10R20)nNReRe′, (CR10R20)nCN, (CR10R20)nS(O)2NReRe′, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NReRe′, (CR10R20)nN(R10′)C(Z)R6, (CR10R20)nN(R10′)C(═N(R10′))NReRe′, (CR10R20)nC(═NOR6)NReRe′, (CR10R20)nOC(Z) NReRe′, (CR10R20)nN(R10′)C(Z)NReRe′, or (CR10R20)nN(R10′)C(Z)OR7;
• or
• wherein R2″ is the moiety (CR10R20)tX1(CR10R20)qC(A1)(A2)(A3);
• A1 is an optionally substituted C1-10 alkyl, heterocyclic, heterocyclic C1-10 alkyl, heteroaryl, heteroaryl C1-10 alkyl, aryl, or aryl C1-10 alkyl;
• A2 is an optionally substituted C1-10 alkyl, heterocyclic, heterocyclic C1-10 alkyl, heteroaryl, heteroaryl C1-10 alkyl, aryl, or aryl C1-10 alkyl;
• A3 is hydrogen or is an optionally substituted C1-10 alkyl;
• R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted;
• R4 and R14 are each independently selected at each occurrence from hydrogen, C1-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylC1-4alkyl, aryl, aryl-C1-4 alkyl, heterocyclic, heterocyclic C1-4 alkyl, heteroaryl or a heteroaryl C1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or the R4 and R14 together with the nitrogen which they are attached form an optionally substituted heterocyclic ring of 4 to 7 members, which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9;
• R4′ and R14′ are each independently selected at each occurrence from hydrogen or C1-4 alkyl, or R4′ and R14′ together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members, which ring optionally contains an additional heteroatom which is NR9′;
• R5 is independently selected at each occurrence from hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl or NR4′R14′, excluding the moieties SR5 being SNR4′R14′, S(O)2R5 being SO2H and S(O)R5 being SOH;
• R6 is independently selected at each occurrence from hydrogen, C1-10 alkyl, C3-7 cycloalkyl, heterocyclyl, heterocyclyl C1-10alkyl, aryl, arylC1-10 alkyl, heteroaryl or heteroarylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• R9 is independently selected at each occurrence from hydrogen, C(Z)R6, optionally substituted C1-10 alkyl, optionally substituted aryl, or an optionally substituted aryl-C1-4 alkyl;
• R9′ is independently selected at each occurrence from hydrogen, or C1-4 alkyl;
• R10 and R20 are independently selected at each occurrence from hydrogen or C1-4alkyl;
• R10′ is independently selected at each occurrence from hydrogen or C1-4alkyl;
• R11 is independently selected at each occurrence from hydrogen or C1-4alkyl;
• R12 is independently selected at each occurrence from hydrogen, C1-4 alkyl, halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-7 cycloalkyl, C3-7cycloalkylC1-4 alkyl, C5-7 cycloalkenyl, C5-7cycloalkenyl C1-4 alkyl, aryl, arylC1-4 alkyl, heteroaryl, heteroarylC1-4 alkyl, heterocyclyl, or a heterocyclylC1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• R13 is independently selected at each occurrence from hydrogen, C1-4 alkyl, halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-7 cycloalkyl, C3-7cycloalkylC1-4 alkyl, C5-7 cycloalkenyl, C5-7cycloalkenyl C1-4 alkyl, aryl, arylC1-4 alkyl, heteroaryl, heteroarylC1-4 alkyl, heterocyclyl, or a heterocyclylC1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• Rd and Rd′ are each independently selected from hydrogen, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkylC1-4alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or Rd and Rd′ together with the nitrogen which they are attached form an optionally substituted heterocyclic ring of 5 to 6 members, which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9′;
• g is 0, or integer having a value of 1, 2, 3, or 4;
• n is independently selected at each occurrence from 0 or an integer having a value of 1 to 10;
• n′ is independently selected at each occurrence from 0 or an integer having a value of 1 to 10;
• m is independently selected at each occurrence from 0 or an integer having a value of 1 or 2;
• q is 0 or an integer having a value of 1 to 10;
• q′ is 0, or an integer having a value of 1 to 6;
• v is 0 or an integer having a value of 1 or 2;
• v′ is independently selected at each occurrence from 0 or an integer having a value of 1 or 2;
• s is independently selected at each occurrence from an integer having a value of 1, 2, or 3;
• t is an integer having a value of 2 to 6;
• Z is independently selected at each occurrence from oxygen or sulfur;
• or
• a pharmaceutically acceptable salt thereof.

A compound of the formula:

• wherein
• G1, and G2 are independently nitrogen;
• G3 is CH2;
• G4 is CH;
• R1 is C(Z)N(R10′)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10′)C(Z)(CR10R20)vRb, N(R10′)C(Z)N(R10′)(CR10R20)vRb, or N(R10′)OC(Z)(CR10R20)vRb;
• R1′ is independently selected at each occurrence from halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v′NRdRd′, (CR10R20)v′C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v′OR13;
• Rb is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or heterocyclylC1-10 alkyl moiety, which moieties, excluding hydrogen, may all be optionally substituted;
• X is R2, OR2′, S(O)mR2′, (CH2)n′N(R10′)S(O)mR2′, (CH2)n′N(R10′)C(O)R2′, (CH2)n′NR4R14, (CH2)n′N(R2′)(R2″), or N(R10′)RhNH—C(═N—CN)NRqRq′;
• X1 is N(R11), O, S(O)m, or CR10R20;
• Rh is selected from an optionally substituted C1-10 alkyl-, —CH2—C(O)—CH2—, —CH2—CH2—O—CH2—CH2—, —CH2—C(O)N(R10′)CH2—CH2—, —CH2—N(R10′)C(O)CH2—, —CH2—CH(OR10′)—CH2—, —CH2—C(O)O—CH2—CH2—, or —CH2—CH2—O—C(O) CH2—;
• Rq and Rq′ are independently selected at each occurrence from hydrogen, C1-10 alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-10alkyl, C5-7 cycloalkenyl, C5-7 cycloalkenyl-C1-10alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, wherein all of the moieties except for hydrogen, are optionally substituted, or Rq and Rq′ together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring of 5 to 7 members, which ring may contain an additional heteroatom selected from oxygen, nitrogen or sulfur;
• R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or
• R2 is the moiety (CR10R20)q′X1(CR10R20)qC(A1)(A2)(A3), or (CR10R20)q′C(A1)(A2)(A3);
• R2′ is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• R2″ is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein these moieties, excluding hydrogen, may be optionally;
• or wherein R2″ is the moiety (CR10R20)tX1(CR10R20)qC(A1)(A2)(A3);
• A1 is an optionally substituted C1-10 alkyl, heterocyclic, heterocyclic C1-10 alkyl, heteroaryl, heteroaryl C1-10 alkyl, aryl, or aryl C1-10 alkyl;
• A2 is an optionally substituted C1-10 alkyl, heterocyclic, heterocyclic C1-10 alkyl, heteroaryl, heteroaryl C1-10 alkyl, aryl, or aryl C1-10 alkyl;
• A3 is hydrogen or is an optionally substituted C1-10 alkyl;
• R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted;
• R4 and R14 are each independently selected at each occurrence from hydrogen, C1-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylC1-4alkyl, aryl, aryl-C1-4 alkyl, heterocyclic, heterocyclic C1-4 alkyl, heteroaryl or a heteroaryl C1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or the R4 and R14 together with the nitrogen which they are attached form an optionally substituted heterocyclic ring of 4 to 7 members, which ring optionally contains an additional heteroatom selected from oxygen, sulfur or nitrogen;
• R4′ and R14′ are each independently selected at each occurrence from hydrogen or C1-4 alkyl, or R4′ and R14′ together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members, which ring optionally contains an additional heteroatom which is NR9′;
• R5 is independently selected at each occurrence from hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl or NR4′R14′, excluding the moieties SR5 being SNR4′R14′, S(O)2R5 being SO2H and S(O)R5 being SOH;
• R9′ is independently selected at each occurrence from hydrogen, or C1-4 alkyl;
• R10 and R20 are independently selected at each occurrence from hydrogen or C1-4alkyl;
• R10′ is independently selected at each occurrence from hydrogen or C1-4alkyl;
• R11 is independently selected at each occurrence from hydrogen or C1-4alkyl;
• R12 is independently selected at each occurrence from hydrogen, C1-4 alkyl, halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-7 cycloalkyl, C3-7cycloalkylC1-4 alkyl, C5-7 cycloalkenyl, C5-7cycloalkenyl C1-4 alkyl, aryl, arylC1-4 alkyl, heteroaryl, heteroarylC1-4 alkyl, heterocyclyl, or a heterocyclylC1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• R13 is independently selected at each occurrence from hydrogen, C1-4 alkyl, halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-7 cycloalkyl, C3-7cycloalkylC1-4 alkyl, C5-7 cycloalkenyl, C5-7cycloalkenyl C1-4 alkyl, aryl, arylC1-4 alkyl, heteroaryl, heteroarylC1-4 alkyl, heterocyclyl, or a heterocyclylC1-4 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• Rd and Rd′ are each independently selected from hydrogen, C1-4 alkyl, C3-6 cycloalkyl, C3-6cycloalkylC1-4alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
• or Rd and Rd′ together with the nitrogen which they are attached form an optionally substituted heterocyclic ring of 5 to 6 members, which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9′;
• g is 0 or an integer having a value of 1, 2, 3, or 4;
• n′ is independently selected at each occurrence from 0 or an integer having a value of 1 to 10;
• m is independently selected at each occurrence from 0 or an integer having a value of 1 or 2;
• q is 0 or an integer having a value of 1 to 10;
• q′ is 0, or an integer having a value of 1 to 6;
• t is an integer having a value of 2 to 6;
• v is 0 or an integer having a value of 1 or 2;
• v′ is independently selected at each occurrence from 0 or an integer having a value of 1 or 2;
• Z is independently selected at each occurrence from oxygen or sulfur;
• or
• a pharmaceutically acceptable salt thereof.