Patent ID: 6713508
Filing Date: 2004-03-30
Classification: A61K,A61P,C07D

Abstract:
A compound having the formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein:Z is selected from the group consisting of CH2 and C&boxH;O; R1 is selected from the group consisting of Cl, Br, F and C1-4 alkyl, wherein said C1-4alkyl is linear or branched and is optionally substituted with 1-3 halogens independently selected from F and Cl, 1 phenyl which is optionally substituted with 1-3 halogens, or a mixture thereof; Ar is Aryl, wherein Aryl is in each instance optionally substituted with 1-5 substituents independently selected from (a) halogen, (b) C1-5alkyl, (c) C2-5alkenyl, (d) C2-5alkynyl, (e) â€”OC1-5alkyl, (f) â€”OC2-5alkenyl, (g) â€”OC2-5alkynyl, (h) â€”SOxC1-5alkyl, (i) â€”SOxNRaRb, (j) â€”SOxphenyl, (k) â€”C(O)C1-3alkyl, and (l) â€”C(O)NRaRb, wherein in each instance, each alkyl, alkenyl and alkynyl is linear or branched and is optionally substituted with (a) 1-5 halogen atoms, (b) 1-2 groups independently selected from â€”OC1-3alkyl, which is linear or branched and is optionally substituted with 1-5 halogens, or (c) a mixture thereof, and wherein phenyl is optionally substituted with 1-3 substituents independently selected from halogen, C1-3alkyl, and C1-3alkoxy, wherein C1-3alkyl and C1-3alkoxy are linear or branched and are optionally substituted with 1-5 halogen; x is selected from 0, 1 and 2; Aryl is a carbocyclic 6-10 membered monocyclic or bicyclic aromatic ring system; Hetcyc is a 5- or 6-membered saturated or partly saturated monocyclic heterocycle having 1-4 heateroatoms independently selected from N, S, and O in the ring, wherein N may optionally be NRa and S may optionally be SO or SO2; Benzoheterocycle contains a 5 or 6-membered heterocyclic ring which may be saturated, partly unsaturated or aromatic, and a benzene ring, wherein said heterocyclic ring and said benzene ring are fused together, wherein said heterocyclic ring contains 1-3 heteroatoms independently selected from O, S, and N in the ring, where N may optionally be NRa, and S may optionally be SO or SO2; Ra Rb are independently selected from the group consisting of H, C1-5alkyl, C2-5alkenyl, C2-5alkynyl, â€”C(O)C1-5alkyl, â€”C(O)C2-5alkenyl, â€”C(O)C2-5alkynyl, SOxC1-5alkyl, SOxphenyl, SOxNRdRe, â€”C(O)NRdRe, halogen, and phenyl, wherein in all instances, alkyl, alkenyl, and alkynyl are linear or branched and are optionally substituted with (a) 1-5 halogen atoms, (b) 1-3 groups independently selected from â€”OCH3, â€”OCF3 and phenyl, or (c) a mixture thereof wherein phenyl in all occurrences is optionally substituted with 1-3 substituents independently selected from halogen, C1-3alkyl, and C1-3alkoxy, said C1-3alkyl and C1-3alkoxy being linear or branched and optionally substituted with 1-5 halogens; Rd and Re are independently selected from H, C1-5alkyl, C2-5alkenyl, C2-5alkynyl, and phenyl, wherein said alkyl, alkenyl, and akynyl are linear or branched and are optionally substituted with (a) 1-5 halogen atoms, (b) 1-3 groups independently selected from â€”OCH3, â€”OCF3 and phenyl, or (c) a mixture thereof, wherein phenyl in all occurrences is optionally substituted with 1-3 substituents independently selected from halogen, C1-3alkyl, and C1-3alkoxy, said C1-3alkyl and C1-3alkoxy being linear or branched and optionally substituted with 1-5 halogens; X and Y are independently selected from the group consisting of O and S; n is an integer from 1-6; R2 is selected from the group consisting of Cl, Br, F and C1-4alkyl, wherein said C1-4alkyl is optionally substituted with 1-3 halogens; R3, R5, R6, R7, R8, R9 and R10 are H; R4 is selected from the group consisting of Benzoheterocycle, C3-8Cycloalkyl, Hetcyc, â€”OC3-8Cycloalkyl and Rc; wherein Benzoheterocycle, C3-8Cycloalkyl, Hetcyc and â€”OC3-8Cycloalkyl are each optionally substituted with 1-3 groups independently selected from halogen, C1-5alkyl, C2-5alkenyl, C2-5alkynyl, â€”OC1-5alkyl, â€”OC2-5alkenyl, â€”OC2-5alkynyl, C3-8Cycloalkyl, â€”SOxC1-5alkyl, â€”SOxNRaRb, â€”SOxphenyl, C(O)C1-3alkyl and â€”C(O)NRaRb, wherein in all instances, said C1-5alkyl, C2-5alkenyl, and C2-5alkynyl groups are linear or branched and are optionally substituted with 1-3 halogens, and wherein Hetcyc, â€”OC3-8Cycloalkyl and C3-8Cycloalkyl may optionally have a C3-6-spiro-cycloalkyl substituent on the ring, wherein the spiro-cycloalkyl group is optionally substituted with 1-2 groups independently selected from methyl, trifluoromethyl, methoxy, trifluoromethoxy and halogen; wherein Rc is selected from the group consisting of halogen, â€”OH, â€”OSO2C1-8alkyl, â€”OSO2C3-8Cycloalkyl, â€”OSO2Ar, C1-8alkyl, C2-8alkenyl, C2-8alkynyl, â€”OC1-8alkyl, â€”OC2-8alkenyl, â€”OC2-8alkynyl, and Aryl, wherein said â€”OSO2C1-8alkyl, C1-8alkyl, C2-8alkenyl, C2-8alkynyl, â€”OC1-8alkyl, â€”OC2-8alkenyl, and â€”OC2-8alkynyl are linear or branched, and are optionally substituted with (a) 1-5 halogens, (b) 1-2 groups independently selected from â€”OC1-3alkyl, which are linear or branched and which are optionally substituted with 1-5 halogens, (c) 1 group selected from Aryl and C3-8Cycloalkyl, or (d) a mixture of one or more of (a), (b) and (c), and Aryl and C3-8Cycloalkyl are each optionally substituted as defined under Ar for Aryl and R4 for C3-8Cycloalkyl; or alternatively R4 and the adjacent substituent R3 or R5 may be connected to foam a 5- or 6-membered heterocyclic ring that may he saturated, partly unsaturated or aromatic fused to the benzene ring, wherein the 5- or 6-membered fused ring contains 1-3 heteroatoms independently selected from O, S, and N, where N may optionally be NRa and S may optionally be SO or SO2, said fused ring optionally also containing 1-2 C&boxH;O groups in the ring, wherein said 5- or 6-membered heterocyclic fused ring is optionally substituted with 1-2 groups independently selected from R3.