会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 10. 发明授权
    • Bicyclic benzo fused pyran compounds used for nausea treatment and
prevention
    • 用于恶心治疗和预防的双环苯并稠合吡喃化合物
    • US4870084A
    • 1989-09-26
    • US278635
    • 1988-12-01
    • James F. EgglerMichael R. JohnsonLawrence S. Melvin, Jr.
    • James F. EgglerMichael R. JohnsonLawrence S. Melvin, Jr.
    • C07C37/055C07C39/08C07C43/23C07C61/39C07D311/22C07D311/58C07D405/12C07D407/12C07D417/12C07D491/10C07D493/06C07D493/10
    • C07D405/12C07C255/00C07C37/055C07C41/30C07C61/39C07D311/22C07D311/58C07D407/12C07D417/12C07D491/10C07D493/06C07D493/10
    • 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.
    • 式(I')的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐,其中M为O,CH 2或NR 6; R6是氢,甲酰基,苄氧羰基或某些烷氧基烷基,烷酰基,烷基,芳烷基或芳烷基羰基; A'为:(1)其中A和B之一为氢,使得当A为氢时,B为C(R2R3)(CH2)fQ且f为1或2; 当B为氢时,A为C(R2R3)(CH2)fQ,f为0或1,当A和OR1一起形成内酯或其某些衍生物时; (2)A'是(3)A'是Q3; Q是CO 2 R 7,COR 8,C(OH)R 8 R 9,CN,CONR 12 R 13,CH 2 NR 12 R 13,CH 2 NHCOR 14,CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN,COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢,苄基或某些酰基; R4是氢,某些烷基或某些芳烷基; R5是氢或某些烷基; Z是(C1-C9)亚烷基,任选地被O,S,SO或SO 2中断; W是氢,甲基,某些芳基或环烷基; 因此在哺乳动物中作为止痛剂,镇定剂,止吐剂,利尿剂,抗惊厥药,止泻药,镇咳药,在治疗青光眼中有用。