Patent ID: 6664291
Filing Date: 2003-12-16
Classification: C07C,C07D

Abstract:
A compound of Formula I an isomer thereof, a prodrug of said compound or isomer, or a pharmaceutically acceptable salt of said compound, isomer or prodrug;whereinW is â€”Oâ€”: R0 is hydrogen; R1 and R2 are each independently hydrogen, â€”(C1-C6)alkyl, halogen or CN; R1 is located at the 5-position and R2 is located at the 3-position; R3 is hydrogen, â€”(C1-C4)alkyl or halogen; R4 is (a) â€”(C1-C10)alkyl substituted with zero to three substituents dependently selected from F, hydroxy, oxo, aryl, heteroaryl, â€”(C3-C8)cycloalkyl, or heterocycloalkyl, (b) â€”(C3-C8) cycloalkyl, (c) heterocycloalkyl, (d) â€”C(O)Rc, (e) â€”ORb, (f) â€”NRaC(O)Rd, (g) â€”NRaC(O)NRcRd or (h) â€”NRaS(O)2Rd; or R3 and R4 are taken together along with the carbon atoms to which they are attached to form a carbocyclic ring of formula â€”(CH2)iâ€” or a heterocyclic ring of formula â€”(CH2)kâ€”Qâ€”(CH2)1â€” wherein Q is â€”Oâ€”, â€”Sâ€” or â€”NRaâ€”; i is 3, 4, 5 or 6; k is 0, 1, 2, 3, 4 or 5; and l is 0, 1, 2, 3, 4 or 5; and wherein the carbocyclic ring and the heterocyclic ring are each substituted with zero to four substituents independently selected from (a) â€”(C1-C4)alkyl, (b) â€”ORb,(c) oxo, (d) â€”CN, (e) phenyl or (f) â€”NRRR8; provided that when the substituent R4 is â€”(C1-C10)alkyl substituted with zero to three substituents, the oxo group is substituted on a carbon atom other than the C1 carbon atom in â€”(C1-C10)alkyl; R5 is (a) â€”OH, (b) â€”O(C1-C6)alkyl, (c) â€”OC(O)Rf, (d) F, or (e) â€”C(O)ORc; or R4 and R5 are taken together along with the carbon atoms to which they are attached to form a heterocyclic ring selected from the group consisting of â€”CRc&boxH;CRaâ€”NHâ€”, â€”N&boxH;CRaâ€”NH, â€”CRo&boxH;CRaâ€”Oâ€”, â€”CRc&boxH;CRaâ€”NHâ€” and â€”CRa&boxH;CRaâ€”CRa&boxH;Nâ€”; R6 is (a) hydrogen, (b) halogen, (c) â€”(C1-C8)alkyl, (d) â€”CF3, (e) â€”OCF3, (f) â€”O(C1-C8)alkyl, or (g) â€”CN; R7 is (a) hydrogen or (b) â€”(C1-C6)alkyl; R8 and R9 are each independently (a) hydrogen, (b) â€”(C1-C6)alkyl, (c) aryl, or (d) halogen; R10 is (a) â€”(C0-C1)alkyl-C(O)OH, (b) â€”(C0-C1)alkyl-C(O)ORf, (c) â€”(C0-C1)alkyl â€”C(O)NRcRd, or (d) â€”(C0-C1)alkyl-OH; Ra for each occurrence is independently (a) hydrogen or (b) â€”(C1-C6)alkyl substituted with zero or one â€”(C3-C6)cycloalkyl or methoxy; Rb for each occurrence is independently (a) hydrogen, (b) â€”(C1-C12)alkyl substituted with zero to three substituents independently selected from Group V, (c) aryl, (d) heteroaryl, (e) â€”(C3-C10) cycloalkyl, (f) heterocycloalkyl, (g) â€”C(O)NRcRd, or (h) â€”C(O)Rf; Rc and Rd for each occurrence are each independently (a) hydrogen, (b) â€”(C1-C12)alkyl substituted with zero to three substituents independently selected from Group VI, (c) â€”(C2-C12)alkenyl, (d) â€”(C2-C12)alkynyl, (e) aryl, (f) heteroaryl, (g) â€”(C3-C10)cycloalkyl or (h) heterocycloalkyl; or Rc and Rd are taken together along with the atom(s) to which they are attached to form a 3-10 membered heterocyclic ring which may optionally contain a second heterogroup selected from â€”Oâ€”, â€”NReâ€” or â€”Sâ€”; and wherein the heterocyclic ring is substituted with zero to four substituents independently selected from (a) â€”(C1-C4)alkyl, (b) â€”ORb, (c) oxo, (d) â€”CN, (e) phenyl or (f) â€”NRaRb; Re for each occurrence is (a) hydrogen, (b) â€”CN, (c) â€”(C1-C10)alkyl substituted with zero to three substitutents independently selected from Group V, (d) â€”(C2-C10)alkenyl, (e) â€”(C2-C10) alkoxy, (f) â€”(C3-C10)cycloalkyl, (g) aryl, (h) heteroaryl, (i) â€”C(O)Rf, (j) â€”C(O)ORf, (k) â€”C(O)NRaRf or (l) â€”S(O)2Rf; Rf for each occurrence is independently (a) â€”(C1-C10)alkyl substituted with zero to three substituents independently selected from the Group VI, (b) â€”(C2-C10)alkenyl, (c) â€”(C2-C10)alkynyl, (d) â€”(C3-C10)cycloalkyl, (e) aryl, (f) heteroaryl or (g) heterocycloalkyl; R8 for each occurrence is independently (a) hydrogen, (b) â€”(C1-C6)alkyl, (c) â€”(C2-C6)alkenyl, (d) aryl, (e) â€”C(O)Rf, (f) â€”C(O)ORf, (g) â€”C(O)NRaRf, (h) â€”S(O)2Rf or (i) â€”(C3-C8)cycloalkyl; Rb is (a) â€”(C1-C6)alkyl substituted with zero or one substituent selected from the group consisting of (1) â€”(C3-C6)cycloalkyl, (2) heterocycloalkyl and (3) phenyl substituted with zero or one substituent selected from the group consisting of (i) â€”(C1-C4)alkyl, (ii) halogen, (iii) â€”CF3 and (iv) â€”OCF3; (b) phenyl substituted with zero to two substituents independently selected from the group consisting or (1) â€”(C1-C4)alkyl, (2) halogen, (3) â€”CF3, and (4) â€”OCF3; (c) â€”(C3-C6)cycloalkyl or (d) heterocycloalkcyl; Group V is (a) halogen, (b) â€”CF3, (c) â€”OCF3, (d) â€”OH, (e) -oxo, (f) â€”(C1-C6)alkoxy, (g) â€”CN, (h) aryl, (i) heteroaryl, (j) â€”(C3-C10)cycloalkyl, (k) heterocycloalkyl, (l) â€”SRf, (m) â€”S(O)Rf, (n) â€”S(O)2Rf, (o) â€”S(O)2NRaRf (p) â€”NRaRg or (q) â€”C(O)NRaRf; Group VI is (a) halogen, (b) hydroxy, (c) oxo, (d) â€”(C1-C6)alkoxy, (e) aryl, (f) heteroaryl, (g) â€”(C3-C8)cycloalkyl, (h) heterocycloalkyl, (i) â€”CN, or (j) â€”OCF3; aryl for each occurrence is independently phenyl or naphthyl substituted with zero to four substituents independently selected from (a) halogen, (b) â€”(C1-C6)alkyl, (c) â€”CN, (d) â€”SRf, (e) â€”S(O)Rf, (f) â€”S(O)2Rf, (g) â€”(C3-C6)cycloalkyl, (h) â€”S(O)2NRaRf, (i) â€”NRaRg, (j) â€”C(O)NRaRf, (k) â€”ORb, (l)-perfluoro-(C1-C4)alkyl, or (m) â€”COORf; provided that when the substituent(s) on aryl are â€”SRf, â€”S(O)Rf, â€”S(O)2Rf, â€”S(O)2NRaRf, â€”NRaRg, â€”C(O)NRaRf, â€”ORb, or â€”COORf, the substituents Rb, Rf and Rg are other than aryl or heteroaryl; heteroaryl for each occurrence is independently a 5-, 6-, 7-, 8-, 9- or 10-membered monocyclic or bicyclic ring having from 1 to 3 heteroatoms selected from O, N or S; wherein in the bicyclic ring, a monocyclic heteroaryl ring is fused to a benzene ring or to another heteroaryl ring; and having zero to three substituents independently selected from (a) halogen, (b) â€”(C1-C4)alkyl, (c) â€”CF3, (d) â€”ORb, (e) â€”NRaRg, or (f) â€”CO2Rf; provided that when the substituent(s) on heteroaryl are â€”ORb, â€”NRaRg or â€”CO2Rf, the substituents Rb, Rf and Rg are other than aryl or heteroaryl; heterocycloalkyl for each occurrence is independently a 4-, 5-, 6-, 7-, 8-, 9- or 10-membered monocyclic or bicyclic cycloalkyl ring having from 1 to 3 heteroatoms selected from O, NRc or S; and having zero to four substituents independently selected from (a) â€”(C1-C4)alkyl, (b) â€”ORb, (c) oxo, (d) â€”CN, (e) phenyl or (f) â€”NRaRg.