Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-12-14
1995-06-06
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514252, 514290, 514291, 514318, 544360, 544361, 546 80, 546 89, 546 93, 546194, A61K 31495, A61K 3144, C07D40100, C07D49100
Patent
active
054223512
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds and to pharmaceutical compositions and methods of using such compounds.
U.S. Pat. Nos. 3,326,924, 3,717,647 and 4,282,233, European published Application No. 0042544 and Villani et al., Journal of Medicinal Chemistry, Vol. 15, No. 7, pp 750-754 (1972) and Arzn. Forsh 36 1311-1314 (1986) describe certain 11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridines as antihistamines. U.S. Pat. No. 4,355,036 describes certain N-substituted piperidylidene compounds.
International Publication Number WO 89/10369 discloses compounds of the formula: ##STR3## wherein: one of a, b, c and d represents nitrogen or --NR.sup.11 --, wherein R.sup.11 is O.sup.-, --CH.sub.3 or --(CH.sup.2).sub.p CO.sub.2 H wherein p is 1 to 3, and the remaining a, b, c and d groups are CH which may be substituted with R.sup.1 or R.sup.2 ; represents halo, --CF.sub.3, --OR.sup.10, --C(O)R.sup.10, --S(O).sub.e R.sup.12 wherein e is 0, 1, or 2, --N(R.sup.10).sub.2, --NO.sub.2, --SH, --CN, --OC(O)R.sup.10, --CO.sub.2 R.sup.10, --OCO.sub.2 R.sup.12, --NR.sup.10 C(O)R.sup.10, alkyl, alkenyl or alkynyl, which alkyl or alkenyl groups may be substituted with halo, --OR.sup.10 or --CO.sub.2 R.sup.10, or R.sup.1 and R.sup.2 may together form a benzene ring fused to the pyridine ring; represents H or any of the substituents of R.sup.1 and R.sup.2, or R.sup.3 and R.sup.4 may be taken together to represent a saturated or unsaturated C.sub.5 to C.sub.7 ring fused to the benzene ring; --CF.sub.3, --CO.sub.2 R.sup.10, --C(O)R.sup.10, alkyl or aryl, which alkyl or aryl may be substituted with --OR.sup.10, --SR.sup.10, --N(R.sup.10).sub.2, --NO.sub.2, --C(O)R.sup.10, --OC(O)R.sup.12, --CO.sub.2 R.sup.10 and --OPO.sub.3 (R.sup.10).sub.2, or one of R.sup.5, R.sup.6, R.sup.7, and R.sup.8 may be taken in combination with R as defined below to represent --(CH.sub.2).sub.r wherein r is 1 to 4, said combination being optionally substituted with lower alkyl, lower alkoxy, --CF.sub.3 or aryl, or R.sup.5 may be combined with R.sup.6 to represent .dbd.O or .dbd.S, and/or R.sup.7 may be combined with R.sup.8 to represent .dbd.O or .dbd.S; representing an optional double bond when T is carbon; to 3; 1 or 2, --NR.sup.10 --, --C(O)NR.sub.10 --, --NR.sup.10 C(O)--, --C(S)NR.sup.10 --, --NR.sup.10 C(S)--, --C(O).sub.2 -- or --O.sub.2 C--, wherein R.sup.10 is as defined above; or 2, or --NR.sup.10 --; 1 and X can also be a direct bond, cyclopropylene or propenylene; represents H, lower alkyl or phenyl; R.sup.10 or --CN, wherein R.sup.10 is as defined above, such that R.sup.7 or R.sup.8 as defined above, or R represents H, alkyl, aryl, --SR.sup.12, --N(R.sup.10).sub.2, cycloalkyl, alkenyl, alkynyl or --D wherein --D represents heterocycloalkyl, ##STR4## wherein R.sup.3 and R.sup.4 are as previously defined, and W is O, S or NR.sup.10, and wherein Y is N or NR.sup.11, said cycloalkyl, alkyl, alkenyl and alkynyl being optionally substituted with from 1-3 groups selected from halo, --CON(R.sup.10).sub.2, aryl, --CO.sub.2 R.sup.10, --OR.sup.14, --SR.sup.14, --N(R.sup.10).sub.2, --N(R.sup.10)CO.sub.2 R.sup.10, --COR.sup.14, --NO.sub.2 or --D, wherein --D and R.sup.10 are as defined above and R.sup.14 represents R.sup.10, --(CH.sub.2).sub.r OR.sup.10 or --(CH.sub.2).sub.q CO.sub.2 R.sup.10 wherein r is 1 to 4, q is 0 to 4; said alkenyl and alkynyl R groups not containing --OH, --SH, or --N(R.sup.10).sub.2 on a carbon in a double or triple bond respectively; and above, aryloxy or alkoxy; and N(R.sup.10).sub.2, cycloalkyl, alkenyl or alkynyl.
WO 89/10369 generically discloses compounds which can have the structure: ##STR5## wherein Z can be O and R can be: ##STR6## wherein Y can be NR.sup.11 and R.sup.11 can be --O.sup.- ; however, no specific compounds are disclosed with this structure.
U.S. Pat. No. 4,826,853 issued to Piwinski et al. on May 2, 1989 is the priority document for WO 88/03138 which published on May 5, 1988. WO 88/03138 discloses co
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Green Michael J.
Piwinski John J.
Wong Jesse
Jeanette Henry C.
Nelson James R.
Schering Corporation
Tsang Cecilia
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