Patent ID: 6180627
Filing Date: 2001-01-30
Classification: A61K,A61P,C07D,C07K

Abstract:
A compound of formula 1 ##STR239##wherein:R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, perfluoro C.sub.1 -C.sub.4 alkyl, OC.sub.1 -C.sub.4 alkyl, fluoro or chloro;R.sup.2 is hydrogen, CH.sub.3, or CF.sub.3 ;R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, perfluoro C.sub.1 -C.sub.4 alkyl, OC.sub.1 -C.sub.4 alkyl, fluoro or chloro;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is hydrogen, fluoro or chloro;C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 carbocyclic, C.sub.3 -C.sub.6 carbocyclic, or C.sub.1 -C.sub.4 alkyl wherein the alkyl and carbocyclic may optionally be substiututed by C.sub.1 -C.sub.4 alkyl or fluoro, and wherein the carbocycle contains zero, one or more double bonds;or R.sup.5 and R.sup.6 together form a bridging chain containing 2 or 3 carbon atoms;Y is hydrogen, chloro, fluoro, bromo, methyl or CF.sub.3 ;V is C or N;W is CH, CF, CCl, or N, and X is N;B--A-- is any one of the following fragments:B--C(R.sup.8)(R.sup.9)--B--CH.sub.2 --C(R.sup.8)(R.sup.9)--B--C(R.sup.8)(R.sup.9)--CH.sub.2 --B--CH.sub.2 --(R.sup.8)(R.sup.9)--CH.sub.2 --B--C(R.sup.8)(R.sup.9)--CH.sub.2 --CH.sub.2 --B--CH.sub.2 --CH.sub.2 --C(R.sup.8)(R.sup.9)--wherein:R.sup.8 and R.sup.9 are independently hydrogen, --(CH.sub.2).sub.m N(R.sup.10)(R.sup.11), --CH.sub.2 O--(CH.sub.2).sub.2 N(R.sup.10)(R.sup.11), or R.sup.8 and R.sup.9 together form a 4 to 6 membered ring containing N(R.sup.12); andm is 0, 1 and 2 except where A represents --C(R.sup.8)(R.sup.9)-- when m is 1 or 2;R.sup.10 and R.sup.11 are independently selected from hydrogen or C.sub.1 -C.sub.4 alkyl optionally containing an oxygen in the chain or at the end of the chain;or R.sup.10 and R.sup.11 together with the nitrogen atom to which they are bonded form a 4 to 6 membered saturated heterocyclic ring wherein when the ring is six membered it may optionally contain one oxygen or an additional nitrogen atom present as N(R.sup.12);R.sup.12 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally containing an oxygen atom in the chain or at the end of the chain;B is phenyl or a 5 to 6 membered aromatic heterocyclic ring containing up to two heteroatoms independently selected from oxygen, sulphur and nitrogen; when B is phenyl or an aromatic heterocycle, R.sup.7 is one or more of hydrogen, C.sub.1 -C.sub.6 alkyl, perfluoro C.sub.1 -C.sub.6 alkyl, OC.sub.1 -C.sub.6 alkyl perfluoro OC.sub.1 -C.sub.6 alkyl, fluoro, chloro, or any one of the following fragments:(CH.sub.2).sub.p --O--(CH.sub.2).sub.2 N(R.sup.10)(R.sup.11) where R.sup.10 and R.sup.11 are as defined above, p is 0 or 1; ##STR240##where Q, together with the C atom to which it is joined, is a 5 or 6 membered heterocyclic ring containing one nitrogen atom, said heterocyclic ring being optionally substituted by C.sub.1 -C.sub.4 alkyl, and q is 1 or 2;--(CH.sub.2).sub.r --C(R.sup.13)(R.sup.14)--(CH.sub.2).sub.s --N(R.sup.15)(R.sup.16) where r and s are independently=0, 1 or 2 R.sup.13 and R.sup.14 are independently hydrogen or C.sub.1 -C.sub.4 alkyl optionally containing one oxygen atom in the chain or at the end of the chain, or R.sup.13 and R.sup.14 together with the carbon atom to which they are bonded form a 4 to 6 membered carbocyclic saturated ring;R.sup.15 and R.sup.16 are independently selected from hydrogen or C.sub.1 -C.sub.4 alkyl optionally containing an oxygen atom in the chain or at the end of the chain, or R.sup.15 and R.sup.16 together with the nitrogen atom to which they are bonded form a 4 to 6 membered saturated heterocyclic ring;or one of R.sup.13 or R.sup.14 and one of R.sup.15 or R.sup.16 together with the carbon and nitrogen atoms to which they are bonded form a 4 to 6 membered saturated heterocyclic ring in which case the other of R.sup.13 or R.sup.14 is hydrogen or C.sub.1 -C.sub.4 alkyl, and the others of R.sup.15 or R.sup.16 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally containing an oxygen atom in the chain or at the end of the chain;or wherein R.sup.7 --B represents the following bicyclic fragments where R.sup.12 is as defined above ##STR241##with the proviso that R.sup.7, R.sup.8 and R.sup.9 cannot all be hydrogen, and only one of R.sup.7, R.sup.8 and R.sup.9 contains one nitrogen atom or, when R.sup.8 and R.sup.9 together form a ring, said ring contains only one nitrogen atom with the proviso that one of R.sup.8 or R.sup.9 may be the following fragment which contains two nitrogen atoms: ##STR242##or, B is a 4 to 7 membered saturated or partially saturated heterocyclic ring containing one or two heteroatoms wherein at least one is a nitrogen and the other is independently selected from oxygen, sulphur and nitrogen; and wherein B is a saturated or partially saturated heterocycle, R.sup.7 is one or more of C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 carbocyclic or C.sub.3 -C.sub.6 carbocyclic C.sub.1 -C.sub.4 alkyl said carbocyclic containing zero, one or more double bonds wherein said alkyl and cycloalkyl optionally contain one heteratom selected from oxygen, sulphur and nitrogen and are further optionally substituted by one or more fluoro, or C.sub.1 -C.sub.4 alkyl optionally containing an oxygen in the alkyl chain or at the end of the chain;and pharmaceutically acceptable salts thereof.