Patent ID: 6353006
Filing Date: 2002-03-05
Classification: C07D

Abstract:
A compound having the formula whereinR is substituted phenyl, wherein the substituent is selected from T; or substituted pyridyl, wherein the substituent is selected from T; Râ€² is alkyl of 1-10 carbons; cycloalkyl of 3-12 carbons and containing 1-3 rings; alkenyl of 2-10 carbons; cycloalkenyl of 5-12 carbons and containing 1-3 rings; or alkynyl of 3-10 carbons; R2, R3, and R4 are independently selected from the group consisting of H; alkyl of 1-10 carbons; cycloalkyl of 3-12 carbons; alkenyl of 2-10 carbons; cycloalkenyl of 5-12 carbons; and &boxH;O, representing two of the groups R2, R3, and R4; X is S(O)y; wherein y is 0, 1, or 2; n is 2; p is the sum of non-H substituents R2, R3, and R4; T is a substituent selected from the group consisting of alkyl of 1-4 carbons; alkoxy of 1-4 carbons; alkenyl of 2-4 carbons; alkynyl of 2-4 carbons; NO2; CN; and halogen; t is 1-5; provided that when substituent moiety T is alkyl of 1-4 carbons, alkoxy of 1-4 carbons, alkenyl of 2-4 carbons, or alkynyl of 2-4 carbons, then T optionally may bear secondary substituents selected from the group consisting of alkyl of 1-4 carbons; alkoxy of 1-4 carbons; CO2R5; wherein R5 is alkyl of 1-4 carbons, haloalkyl of 1-4 carbons, cycloalkyl of 3-6 carbons, or halocycloalkyl of 3-6 carbons; CO2H; C(O)N(R6)(R7); wherein R6 is H or alkyl of 1-5 carbons; and R7 is H or alkyl of 1-5 carbons; CHO; OH; NO2; CN halogen; S(O)yR8; wherein R8 is alkyl of 1-5 carbons; and &boxH;O, representing two secondary substituents; the number of said secondary substituents being 1 or 2 with the exception of halogen, which may be employed up to the perhalo level; G is a substituent selected from the group consisting of halogen; OR5; alkyl of 1-4 carbons; alkenyl of 1-4 carbons; cycloalkyl of 3-7 carbons; cycloalkenyl of 5-7 carbons; aryl of 6-10 carbons; and CN; g is 0-4, with the exception of halogen, which may be employed up to the perhalo level; provided that when substituent G is alkyl of 1-4 carbons, alkenyl of 1-4 carbons, cycloalkyl of 3-7 carbons, or cycloalkenyl of 5-7 carbons, then G optionally may bear secondary substituents of halogen up to the perhalo level; and when substituent G is aryl, then G optionally may bear secondary substituents independently selected from the group consisting of alkyl of 1-4 carbons and halogen, the number of said secondary substituents being up to 3 for alkyl moieties, and up to the perhalo level for halogen; Q is a substituent selected from the group consisting of alkyl of 1-4 carbons; haloalkyl of 1-4 carbons; cycloalkyl of 3-8 carbons; alkoxy of 1-8 carbons; alkenyl of 2-5 carbons; cycloalkenyl of 5-8 carbons; CO2R5; &boxH;O, representing two substituents Q; OH; halogen; N(R6)(R7); and S(O)yR8; q is 0-4; and with the further provisos that: a) two of (Q)qR1, (Q)qR2 (Q)qR3, and (Q)qR4 may be joined, and taken together with the atom(s) to which they are attached, form a spiro or nonspiro nonaromatic ring of 3-8 members containing 0-2 heteroatoms selected from the group consisting of N, O, and S; b) at least one of R2, R3, and R4 is other than H; c) the sum of non-hydrogen atoms in R1, R2, R3, and R4 is at least 5; and d) when the 4-position of the 1,3-thiazolidine ring bears a carbonyl group, R1 is a substituted methyl group, and G is a phenyl group, then said phenyl group bears a secondary substituent; and pharmaceutically acceptable salts thereof.