Patent ID: 6638980
Filing Date: 2003-10-28
Classification: A61P,C07C,C07D

Abstract:
A compound according to the formula:Aâ€”Yâ€”Dâ€”Eâ€”Gâ€”Jâ€”Zâ€”L wherein:A is selected from the group consisting of: (a) C3-C8-cycloalkyl; (b) phenyl, which is independently substituted with 0-2 R1 substituents; and (c) naphthyl, which is independently substituted with 0-2 R1 substituents; R1 is selected from the group consisting of: Halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, â€”NO2, (CH2)mNR2R3, SO2NR2R3, SO2R2, CF3, OR2, and a 5-6 membered aromatic heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O and S, wherein from 1-4 hydrogen atoms on the aromatic heterocyclic system may be independently replaced with a member selected from the group consisting of halo, C1-C4-alkyl, â€”CN, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl and â€”NO2; R2 and R3 are independently selected from the group consisting of: H, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalky, C0-4alkylphenyl and C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, and â€”NO2; m is an integer of 0-2; Y is a direct link; D is a member selected from the group consisting of: (a) phenyl, which is independently substituted with 0-2 R1a substituents; and (b) naphthyl, which is independently substituted with 0-2 R1a substituents; R1a is selected from the group consisting of: Halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, â€”NO2, (CH2)mNR2aR3a, SO2NR2aR3a, SO2R2a, CF3, OR2a, and a 5-6 membered aromatic heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O and S, wherein from 1-4 hydrogen atoms on the aromatic heterocyclic system may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN and â€”NO2; R2a and R3a are independently selected from the group consisting of: H, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, C0-4alkylphenyl and C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN and â€”NO2; E is â€”N(R5)â€”C(&boxH;O)â€”; R5 is selected from the group consisting of: H, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, C0-4alkylphenyl, C0-4alkylnaphthyl, C0-4alkylheteroaryl, C1-4alkylCOOH and C1-4alkylCOOC1-4alkyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl, naphthyl and heteroaryl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3cycloalkyl, â€”CN and â€”NO2; G is selected from the group consisting of: â€”CR7R8â€” and â€”CR7aR8aâ€”CR7bR8bâ€”wherein R7, R8, R7a, R8a, R7b and R8b are independently a member selected from the group consisting of: hydrogen, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkyl-C3-8cycloalkyl, C0-4alkylphenyl, C0-4alkylnaphthyl, C0-4alkylimidazolyl, â€”OR9, â€”C0-4alkylCOOR9, â€”C0-4alkylC(&boxH;O)NR9R10, â€”C0-4alkylC(&boxH;O)NR9â€”CH2â€”CH2â€”Oâ€”R10, â€”C0-4alkylC(&boxH;O)NR9(â€”CH2â€”CH2â€”Oâ€”R10â€”)2, â€”N(R9)COR10, â€”N(R9)C(&boxH;O)R10, â€”N(R9)SO2R10, and a naturally occurring or synthetic amino acid side chain, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkyl-C3-8cycloalkyl, â€”CN, â€”OH, â€”OC1-4alkyl, â€”OC1-4alkyl-OMe, â€”OCH2COOH, and â€”NO2; R9 and R10 are independently selected from the group consisting of: H, C1-4alkyl, C3-8cycloalkyl, C0-4alkylphenyl and C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkyl-C3-8cycloalkyl, â€”CN and â€”NO2, and wherein R9 and R10 taken together can form a 5-8 membered heterocylic ring; J is â€”Oâ€”; Z is a member selected from the group consisting of: (a) phenyl, which is independently substituted with 0-2 R1b substituents; and (b) naphthyl, which is independently substituted with 0-2 R1b substituents; R1b is selected from the group consisting of: Halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, NO2, NR2bR3b, SO2NR2bR3b, SO2R2b, CF3, OR2b, Oâ€”CH2â€”OPh, Oâ€”CH2â€”Ph, Oâ€”CH2CH2â€”OR2b, Oâ€”CH2â€”COOR2b, N(R2b)â€”CH2â€”CH2â€”OR2b, N(â€”CH2â€”CH2â€”OR2b)2, N(R2b)â€”C(&boxH;O)R3b, N(R2b)â€”SO2â€”R3b, and a 5-6 membered aromatic heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O and S, wherein from 1-4 hydrogen atoms on the aromatic heterocyclic system may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN and â€”NO2; R2b and R3b are independently selected from the group consisting of: H, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, C0-4alkylphenyl and C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN and â€”NO2; L is C(&boxH;NR12)NR12 R13; R12 and R13 are independently selected from the group consisting of: hydrogen, â€”OR14, â€”NR14R15, C1-4alkyl, C0-4alkylphenyl, C0-4alkylnaphthyl, COOC1-4alkyl, COOâ€”C0-4alkylphenyl and COOâ€”C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, and â€”NO2; R14 and R15 are independently selected from the group consisting of: H, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, C0-4alkylphenyl and C0-4alkylnaphthyl, wherein from 1-4 hydrogen atoms on the ring atoms of the phenyl and naphthyl moieties may be independently replaced with a member selected from the group consisting of halo, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C0-4alkylC3-8cycloalkyl, â€”CN, and â€”NO2; and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.