Patent ID: 6329421
Filing Date: 2001-12-11
Classification: A61P,C07D

Abstract:
A compound of Formula ##STR62##or a pharmaceutically acceptable salt thereof wherein:X is O or S;R.sup.1 is selected from the group consisting of(a) S(O).sub.2 CH.sub.3,(b) S(O).sub.2 NH.sub.2,(c) S(O).sub.2 NHCOCF.sub.3,(d) S(O)(NH)CH.sub.3,(e) S(O)(NH)NH.sub.2,(f) S(O)(NH)NHCOCF.sub.3,(g) P(O)(CH.sub.3)OH, and(h) P(O)(CH.sub.3)NH.sub.2,R.sup.2 is selected from the group consisting of(a) C.sub.1-6 alkyl,(b) C.sub.3-7, cycloalkyl,(c) mono- or di-substituted phenyl or naphthyl wherein the substituent is selected from the group consisting of(1) hydrogen,(2) halo, including F, Cl, Br, I,(3) C.sub.1-6 alkoxy,(4) C.sub.1-6 alkylthio,(5) CN,(6) CF.sub.3,(7) C.sub.1-6 alkyl,(8) N.sub.3,(9) --CO.sub.2 H,(10) --CO.sub.2 --C.sub.1-4 alkyl,(11) --C(R.sup.5)(R.sup.6)--OH,(12) --C(R.sup.5)(R.sup.6)--O--C.sub.1-4 alkyl, and(13) --C.sub.1-6 alkyl-CO.sub.2 -R.sup.7 ;(d) mono- or di-substituted heteroaryl wherein the heteroaryl is a monocyclic aromatic ring of 5 atoms, said ring having one hetero atom which is S, O, or N, and optionally 1, 2, or 3 additional N atoms; orthe heteroaryl is a monocyclic ring of 6 atoms, said ring having one hetero atom which is N, and optionally 1, 2, 3, or 4 additional N atoms; said substituents are selected from the group consisting of(1) hydrogen,(2) fluoro, chloro, bromo and iodo,(3) C.sub.1-6 alkyl,(4) C.sub.1-6 alkoxy,(5) C.sub.1-6 alkylthio,(6) CN,(7) CF.sub.3,(8) N.sub.3,(9) --C(R.sup.5)(R.sup.6)--OH, and(10) --C(R.sup.5)(R.sup.6)--O--C.sub.1-4 alkyl;(e) benzoheteroaryl which includes the benzo fused analogs of (d);R.sup.3 and R.sup.4 are independently selected from the group consisting of:(a) hydrogen,(b) CF.sub.3,(c) CN,(d) C.sub.1-6 alkyl,(e) --Q.sup.1 wherein Q.sup.1 is Q.sup.2, CO.sub.2 H, C(R.sup.5)(R.sup.6)OH,(f) --O--Q.sup.2,(g) --S--Q.sup.2, and(h) optionally substituted(1) --C.sub.1-5 alkyl-Q.sup.1,(2) --O--C.sub.1-5 alkyl-Q.sup.1,(3) --S--C.sub.1-5 alkyl-Q.sup.1,(4) --C.sub.1-3 alkyl-O--C.sub.1-3 alkyl-Q.sup.1,(5) --C.sub.1-3 alkyl-S--C.sub.1-3 alkyl-Q.sup.1,(6) --C.sub.1-5 alkyl-O--Q.sup.2,(7) --C.sub.1-5 alkyl-S--Q.sup.2,wherein the substituent resides on the alkyl chain and the substituent is C.sub.1-3 alkyl, and Q.sup.1 is Q.sup.2, CO.sub.2 H, C(R.sup.5)(R.sup.6)OH Q.sup.2 is CO.sub.2 --C.sub.1-4 alkyl, tetrazolyl-5-yl, or C(R.sup.5)(R.sup.6)O--C.sub.1-4 alkyl;R.sup.5, R.sup.6 and R.sup.7 are each independently selected from the group consisting of(a) hydrogen,(b) C.sub.1-6 alkyl,or R.sup.5 and R.sup.6 together with the carbon to which they are attached form a saturated monocyclic carbon ring of 3, 4, 5, 6 or 7 atoms.