Patent ID: 6239142
Filing Date: 2001-05-29
Classification: A61P,C07D

Abstract:
A compound of formula I: ##STR87##or a pharmaceutically acceptable salt thereof wherein,R.sup.1 is(a) Cl,(b) Br,(c) CN,(d) NO.sub.2, or(e) F;R.sup.2 is H;R.sup.3 is(a) H,(b) halo,(c) aryl,(d) S(O).sub.m R.sup.6,(e) (C.dbd.O)R.sup.6,(f) (C.dbd.O)OR.sup.9,(g) cyano,(h) het, wherein said het is bound via a carbon atom,(i) OR.sup.10,(j) Ohet,(k) NR.sup.7 R.sup.8(l) SR.sup.10,(m) Shet,(n) NHCOR.sup.12,(o) NHSO.sub.2 R.sup.12, or(p) C.sub.1-7 alkyl which may be partially unsaturated and optionally substituted by one or more substituents of the group R.sup.11, OR.sup.13, SR.sup.10, SR.sup.13, NR.sup.7 R.sup.8, halo, (C.dbd.O)C.sub.1-7 alkyl, and SO.sub.m R.sup.9 ;R.sup.4 is(a) H,(b) halo,(c) C.sub.1-4 alkyl, or(d) R.sup.4 together with R.sup.3 form a carbocyclic or het, either of which may be optionally substituted by NR.sup.7 R.sup.8, by C.sub.1-7 alkyl which may be optionally substituted by OR.sup.14, or by het, wherein said het is bound via a carbon atom;R.sup.6 is(a) C.sub.1-7 alkyl,(b) NR.sup.7 R.sup.8,(c) aryl, or(d) het, wherein said het is bound via a carbon atom;R.sup.7 and R.sup.8 are independently(a) H,(b) aryl,(c) C.sub.1-7 alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from a group consisting of NR.sup.10 R.sup.10, R.sup.11, SO.sub.m R.sup.9, CONR.sup.10 R.sup.10, and halo, or,(d) R.sup.7 and R.sup.8 together with the nitrogen to which they are attached form a het;R.sup.9 is(a) aryl,(b) het,(c) C.sub.3-8 cycloalkyl, or(d) C.sub.1-7 alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from a group consisting of NR.sup.10 R.sup.10, R.sup.11, SH, CONR.sup.10 R.sup.10, and halo;R.sup.10 is(a) H, or(b) C.sub.1-7 alkyl optionally substituted by OH;R.sup.11 is(a) OR.sup.10,(b) Ohet,(c) Oaryl,(d) CO.sub.2 R.sup.10,(e) het,(f) aryl, or(g) CN;R.sup.12 is(a) H,(b) het,(c) aryl,(d) C.sub.3-8 cycloalkyl, or(e) C.sub.1-7 alkyl optionally substituted by NR.sup.7 R.sup.8 or R.sup.11 ;R.sup.13 is(a) (P.dbd.O)(OR.sup.14).sub.2,(b) CO(CH.sub.2).sub.n CON(CH.sub.3)--(CH.sub.2).sub.n SO.sub.3.sup.- M.sup.+,(c) an amino acid,(d) C(.dbd.O)aryl, or(e) C(.dbd.O)C.sub.1-7 alkyl optionally substituted by NR.sup.7 R.sup.8, aryl, het, CO.sub.2 H, or O(CH.sub.2).sub.n CO.sub.2 R.sup.14);R.sup.14 is(a) H, or(b) C.sub.1-7 alkyl;each i is independently 2, 3, or 4;each n is independently 1, 2, 3, 4 or 5;each m is independently 0, 1, or 2; andM is sodium, potassium, or lithium;wherein any aryl is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, CO.sub.2 R.sup.14, CF.sub.3, C.sub.1-6 alkoxy, and C.sub.1-6 alkyl which maybe further substituted by one to three SR.sup.14, NR.sup.14 R.sup.14, OR.sup.14, het, or CO.sub.2 R.sup.14 ; andwherein any het is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, phenyl, CO.sub.2 R.sup.14, CF.sub.3, C.sub.1-6 alkoxy, oxo, oxime, and C.sub.1-6 alkyl which maybe further substituted by one to three SR.sup.14, NR.sup.14 R.sup.14, OR.sup.14, or CO.sub.2 R.sup.14.