Patent ID: 6433171
Filing Date: 2002-08-13
Classification: A61K,A61P,C07D,C07K

Abstract:
A compound of the formula where R1 is hydrogen, â€”CN, â€”(CH2)qN(X6)C(O)X6, â€”(CH2)qN(X6)C(O)(CH2)tâ€”A1, â€”(CH2)qN(X6)S(O)2(CH2)tâ€”A1, â€”(CH2)qN(X6)S(O)2X6, â€”(CH2)qN(X6)C(O)N(X6)(CH2)tâ€”A1, â€”(CH2)qN(X6)C(O)N(X6)(X6), â€”(CH2)qC(O)N(X6)(X6), â€”(CH2)qC(O)N(X6)(CH2)tâ€”A1, â€”(CH2)qC(O)OX6, â€”(CH2)qC(O)O(CH2)tâ€”A1, â€”(CH2)qOX6, â€”(CH2)qOC(O)X6, â€”(CH2)qOC(O)(CH2)tâ€”A1, â€”(CH2)qOC(O)N(X6)(CH2)tâ€”A1, â€”(CH2)qOC(O)N(X6)(X6), â€”(CH2)qC(O)X6, â€”(CH2)qC(O)(CH2)tâ€”A1, â€”(CH2)qN(X6)C(O)OX6, â€”(CH2)qN(X6)S(O)2N(X6)(X6), â€”(CH2)qS(O)mX6, â€”(CH2)qS(O)m(CH2)tâ€”A1, â€”(C1-C10)alkyl, â€”(CH2)tâ€”A1, â€”(CH2)qâ€”(C3-C7)cycloalkyl, â€”(CH2)qâ€”Y1â€”(C1-C6)alkyl, (CH2)qâ€”Y1â€”(CH2)tâ€”A1 or â€”(CH2)qâ€”Y1â€”(CH2)tâ€”(C3-C7)cycloalkyl; where the alkyl and cycloalkyl groups in the definition of R1 are optionally substituted with (C1-C4)alkyl, hydroxy, (C1-C4)alkoxy, carboxyl, â€”CONH2, â€”S(O)m(C1-C6)alkyl, â€”CO2(C1-C4)alkyl ester, 1H-tetrazol-5-yl or 1, 2 or 3 fluoro groups; Y1 is O, S(O)m, â€”C(O)NX6â€”, â€”CH&boxH;CHâ€”, â€”Câ‰¡Câ€”, â€”N(X6)C(O)â€”, â€”C(O)NX6â€”, â€”C(O)Oâ€”, â€”OC(O)N(X6)â€” or â€”OC(O)â€”; m for each occurrence is 0, 1 or 2; q is 0, 1, 2, 3 or 4; t is 0, 1, 2 or 3; said (CH2)q group and (CH2)t group in the definition of R1 are optionally independently substituted with hydroxy, (C1-C4)alkoxy, carboxyl, â€”CONH2, â€”S(O)m(C1-C6)alkyl, â€”CO2(C1-C4)alkyl ester, 1H-tetrazol-5-yl, 1, 2 or 3 fluoro groups or 1 or 2 (C1-C4)alkyl groups; A1 for each occurrence is independently selected from the group consisting of (C5-C7)cycloalkenyl, phenyl, a partially saturated, fully saturated or fully unsaturated 4- to 8-membered ring optionally having 1 to 4 heteroatoms independently selected from the group consisting of oxygen, sulfur and nitrogen and a bicyclic ring system consisting of a partially saturated, fully unsaturated or fully saturated 5- or 6-membered ring, optionally having 1 to 4 heteroatoms independently selected from the group consisting of nitrogen, sulfur and oxygen, fused to a partially saturated, fully saturated or fully unsaturated 5- or 6-membered ring, optionally having 1 to 4 heteroatoms independently selected from the group consisting of nitrogen, sulfur and oxygen; A1 for each occurrence is independently optionally substituted, on one or optionally both rings if A1 is a bicyclic ring system, with up to three substituents, each substituent independently selected from the group consisting of F, Cl, Br, I, OCF3, OCF2H, CF3, CH3, OCH3, â€”OX6, â€”C(O)N(X6)(X6), â€”C(O)OX6, oxo, (C1-C6)alkyl, nitro, cyano, benzyl, â€”S(O)m(C1-C6)alkyl, 1H-tetrazol-5-yl, phenyl, phenoxy, phenylalkyloxy, halophenyl, methylenedioxy, â€”N(X6)(X6), â€”N(X6)C(O)(X6), â€”S(O)2N(X6)(X6), â€”N(X6)S(O)2-phenyl, â€”N(X)S(O)2X6, â€”CONX11X12, â€”S(O)2NX11X12, â€”NX6S(O)2X12, â€”NX6(CONX11X12, â€”NX6S(O)2NX11X12, â€”NX6C(O)X12, imidazolyl, thiazolyl and tetrazolyl, provided that if A1 is optionally substituted with methylenedioxy then it can only be substituted with one methylenedioxy; where X11 is hydrogen or optionally substituted (C1-C6)alkyl; the optionally substituted (C1-C6)alkyl defined for X11 is optionally independently substituted with phenyl, phenoxy, (C1-C6)alkoxycarbonyl, â€”S(O)m(C1-C6)alkyl, 1 to 5 halo groups, 1 to 3 hydroxy groups, 1 to 3 (C1-C10)alkanoyloxy groups or 1 to 3 (C1-C6)alkoxy groups; X12 is hydrogen, (C1-C6)alkyl, phenyl, thiazolyl, imidazolyl, furyl or thienyl, provided that when X12 is not hydrogen, the X12 group is optionally substituted with one to three substituents independently selected from the group consisting of Cl, F, CH3, OCH3, OCF3 and CF3; or X11 and X12 are taken together to form â€”(CH2)râ€”L1â€”(CH2)râ€”; L1 is C(X2)(X2), O, S(O)m or N(X2); X6 for each occurrence is independently hydrogen, optionally substituted (C1-C6)alkyl, (C2-C6)halogenated alkyl, optionally substituted (C3-C7)cycloalkyl, (C3-C7)-halogenated cycloalkyl, where optionally substituted (C1-C6)alkyl and optionally substituted (C3-C7)cycloalkyl in the definition of X6 is optionally independently mono-or di-substituted with (C1-C4)alkyl, hydroxy, (C1-C4)alkoxy, carboxyl, CONH2, â€”S(O)m(C1-C6)alkyl, carboxylate (C1-C4)alkyl ester or 1H-tetrazol-5yl; or when there are two X6 groups on one atom and both X6 are independently (C1-C6)alkyl, the two (C1-C6)alkyl groups may be optionally joined and, together with the atom to which the two X6 groups are attached, form a 4- to 9-membered ring optionally having oxygen, sulfur or NX7 as a ring member; and R2 is hydrogen, (C1-C8)alkyl, â€”(C0-C3)alkyl-(C3-C8)cycloalkyl, â€”(C1-C4)alkyl-A1 or A1; where the alkyl groups and the cycloalkyl groups in the definition of R2 are optionally substituted with hydroxy, â€”C(O)OX6, â€”C(O)N(X6)(X6), â€”N(X6)(X6), â€”S(O)m(C1-C6)alkyl, â€”C(O)A1, â€”C(O)(X6), CF3, CN or 1, 2 or independently selected halo groups.