Patent ID: 6642231
Filing Date: 2003-11-04
Classification: A61P,C07D

Abstract:
A compound of the formula wherein R is selected from the group consisting of R2, R2NHâ€”, or R3R4Nâ€”R5â€” wherein R2 is selected from the group consisting of C9-C12 alkyl, wherein each R6 is independently selected from the group consisting of hydrogen, C3-C8 cycloalkyl, C1-C4 alkyl, and (CH2)m-phenyl, wherein m is an integer 0-8; x is an integer 1-8; n is an integer 1-8; Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthyl, where heterocycle is piperidinyl, pyridinyl, isoxazolyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, benzimidazolyl, thiazolyl, thiophene, furanyl, indolyl, 1,3-benzodioxolyl, tetrahydropyranyl, imidazolyl, tetrahydrothiophene, pyranyl, dioxanyl, pyrrolyl, pyrimidinyl, pyrazinyl, triazinyl, oxazolyl, purinyl, quinolinyl, or isoquinolinyl; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, â€ƒwherein each R6â€² is independently selected from the group consisting of hydrogen, C3-C8 cycloalkyl, C1-C4 alkyl, and (CH2)mâ€²-phenyl, wherein mâ€² is an integer 0-8; nâ€² is an integer 0-8; xâ€² is an integer 1-8; Q is hydrogen or C1-C4 alkyl; and Zâ€² is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthyl, where heterocycle is piperidinyl, pyridinyl, isoxazolyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, benzimidazolyl, thiazolyl, thiophene, furanyl, indolyl, 1,3-benzodioxolyl, tetrahydropyranyl, imidazolyl, tetrahydrothiophene, pyranyl, dioxanyl, pyrrolyl, pyrimidinyl, pyrazinyl, triazinyl, oxazolyl, purinyl, quinolinyl, or isoquinolinyl; and wherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, C2-C6 alkenyl, and C1-C8 alkyl; b is an integer 0-2; Zâ€³ is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthyl, where heterocycle is piperidinyl, pyridinyl, isoxazolyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, benzimidazolyl, thiazolyl, thiophene, furanyl, indolyl, 1,3-benzodioxolyl, tetrahydropyranyl, imidazolyl, tetrahydrothiophene, pyranyl, dioxanyl, pyrrolyl, pyrimidinyl, pyrazinyl, triazinyl, oxazolyl, purinyl, quinolinyl, or isoquinolinyl; each R6â€³ is independently selected from the group consisting of hydrogen, C3-C8 cycloalkyl, C1-C4 alkyl, and (CH2)mâ€³-phenyl, wherein mâ€³ is an integer 0-8; nâ€³ is an integer 0-8; xâ€³ is an integer 1-8; and Mâ€² is selected from the group consisting of hydrogen, C1-C4 alkyl, wherein each R6â€²â€³ is independently selected from the group consisting of hydrogen, C3-C8 cycloalkyl, C1-C4 alkyl, and (CH2)mâ€²â€³-phenyl, wherein mâ€²â€³ is an integer 0-8; nâ€²â€³ is an integer 0-8; xâ€²â€³ is an integer 1-8; Qâ€² is hydrogen or C1-C4 alkyl; and Zâ€²â€³ is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthyl, where heterocycle is piperidinyl, pyridinyl, isoxazolyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, benzimidazolyl, thiazolyl, thiophene, furanyl, indolyl, 1,3-benzodioxolyl, tetrahydropyranyl, imidazolyl, tetrahydrothiophene, pyranyl, dioxanyl, pyrrolyl, pyrimidinyl, pyrazinyl, triazinyl, oxazolyl, purinyl, quinolinyl, or isoquinolinyl, wherein the groups Mâ€² and Zâ€³ may be optionally substituted with the groups Dâ€², Eâ€² or provided Mâ€² is not hydrogen, wherein each R6â€³â€³ is independently selected from the group consisting of hydrogen, C3-C8 cycloalkyl, C1-C4 alkyl, and (CH2)mâ€³â€³-phenyl, wherein mâ€³â€³ is an integer 0-8; xâ€³â€³ is an integer 0-8; Qâ€³ is hydrogen or C1-C4 alkyl or phenyl; each Dâ€² is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each Eâ€² is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl; R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen; R5 is C1-C8 alkylene; and R1 is isopropyl, or a pharmaceutically acceptable salt, an optical isomer, or a hydrate thereof,with the proviso that when R2 is the group wherein n is 1 or greater; R6 is hydrogen, C1-C4 alkyl, or (CH2)m-phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of wherein D, b, R6â€³, xâ€³, nâ€³, Mâ€², and Zâ€³ are as previously defined.