发明授权
US4870084A Bicyclic benzo fused pyran compounds used for nausea treatment and
prevention
失效
用于恶心治疗和预防的双环苯并稠合吡喃化合物
- 专利标题： Bicyclic benzo fused pyran compounds used for nausea treatment and prevention
- 专利标题（中）： 用于恶心治疗和预防的双环苯并稠合吡喃化合物
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申请号： US278635申请日： 1988-12-01
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公开(公告)号： US4870084A公开(公告)日： 1989-09-26
- 发明人: James F. Eggler , Michael R. Johnson , Lawrence S. Melvin, Jr.
- 申请人： James F. Eggler , Michael R. Johnson , Lawrence S. Melvin, Jr.
- 申请人地址： NY New York
- 专利权人： Pfizer Inc.
- 当前专利权人： Pfizer Inc.
- 当前专利权人地址： NY New York
- 主分类号： C07C37/055
- IPC分类号： C07C37/055 ; C07C39/08 ; C07C43/23 ; C07C61/39 ; C07D311/22 ; C07D311/58 ; C07D405/12 ; C07D407/12 ; C07D417/12 ; C07D491/10 ; C07D493/06 ; C07D493/10
摘要：
Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9) alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, antiemetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.