Back to results
US 2003/0153560 A1Published application
Inhibitors of c-Jun N-terminal kinases (JNK)
OwnerFrancesco G. Salituro, Guy W. Bemis +5inventors
InventorsFrancesco G. Salituro, Guy W. Bemis, Susanne Wilke, Jeremy Green, Jingrong Cao, Huai Gao, Edmund Martin Harrington
Life of this patent
Estimating the term…
Abstract
The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Claims13
A compound of the formula:
- 363
- or a pharmaceutically acceptable derivative or prodrug thereof;
- wherein
- Y is selected from —(CH2)—Q1;
- —(CO)—Q1;
- —(CO)NH—Q1;
- —(CO)—O—Q1;
- —(SO2)—Q1 or —(SO2)NH—Q1;
- Q1 is a C1-C6 straight chain or branched alkyl or alkenyl group;
- a 5-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring;
- or a 9-14 membered bicyclic or tricyclic aromatic or non-aromatic carbocyclic or heterocyclic ring system, wherein said alkyl, alkenyl, ring or ring system is optionally substituted with one to four substituents, each of which is independently selected from NH2, NH—R, N(R)2, NO2, OH, OR, CF3, halo, CN, CO2H, C(O)—NH2, C(O)—NH—R, C(O)—N(R)2, C(O)—R, SR, S(O)—R, S(O)2—R, S(O)2—NH—R or —R;
- W is N or C;
- wherein when W is N, R8 is a lone pair of electrons;
- and
- wherein when W is C, R8 is R7.
- A1 is N or CR1;
- A2 is N or CR2;
- A3 is N or CR3;
- A4 is N or CR4;
- provided that at least one of A1, A2, A3 and A4 must not be N;
- R1 is —NHR5, —OR5, —SR5, or —R5;
- R2, R3, and R4 are independently selected from —(CO)NH2, —(CO)NHR, —(CO)N(R)2, —NHR5, —NHCH2R5, —OR5, —SR5, —R5, —NH(CO)—R6, —NH(CO)—NHR6, —NH(CO)—NH(CO)R6, —NH(CO)—OR6, —NH(SO2)—R6, —NH(SO2)—NHR6, —C(O)OH, —C(O)OR, —(CO)—Q1, —(CO)NH—Q1, —(CO)NR—Q1, —(CO)—O—Q1, —(SO2)—Q1 or —(SO2)NH—Q1;
- R5 and R6 are each independently selected from H;
- N(R)2, NHOH, NO2, C(O)OR or halo;
- a C1-C6 straight chain or branched alkyl, alkenyl or alkynyl group;
- a 5-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring;
- or a 9-14 membered bicyclic or tricyclic aromatic or non-aromatic carbocyclic or heterocyclic ring;
- wherein said alkyl, alkenyl, ring or ring system is optionally substituted with one to four substituents, each of which is independently selected from NH2, NHR, NHC(O)OR, N(R)2, NO2, OH, OR, CF3, halo, CN, Si(R)3, CO2H, COOR, CONH2, CONHR, CON(R)2, COR, SR, S(O)R, S(O)2R, S(O)2NHR or R;
- R7 is H;
- a C1-C6 straight chain or branched alkyl or alkenyl group;
- a 5-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring;
- or a 9-14 membered bicyclic or tricyclic aromatic or non-aromatic carbocyclic or heterocyclic ring;
- wherein said alkyl, alkenyl, ring or ring system is optionally substituted with one to four substituents, each of which is independently selected from NH2, NHR, N(R)2, NO2, OH, OR, CF3, halo, CN, CO2H, CONH2, CONHR, CON(R)2, COR, SR, S(O)R, S(O)2R, S(O)2NHR or R;
- R is a C1-C6 straight chain or branched alkyl or alkenyl group, a 5-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring, or a 9-10 membered bicyclic aromatic or non-aromatic carbocyclic or heterocyclic ring system;
- and
- Z is CH or N.
33 more elements
Dependencies are inferred from the claim text.