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    • 26. 发明授权
    • Benzopyrans
    • 苯并吡喃
    • US4841078A
    • 1989-06-20
    • US639038
    • 1984-08-09
    • James F. EgglerMichael R. JohnsonLawrence Sherman
    • James F. EgglerMichael R. JohnsonLawrence Sherman
    • 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, anteimetic 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,止痛剂,促炎剂,利尿剂,抗惊厥药,止泻药,镇咳药,治疗青光眼有用。
    • 28. 发明授权
    • Substituted dibenzo[b,d]pyran analgesics
    • 取代的二苯并[b,d]吡喃镇痛药
    • US4454144A
    • 1984-06-12
    • US390418
    • 1982-06-21
    • Lawrence S. Melvin, Jr.Michael R. Johnson
    • Lawrence S. Melvin, Jr.Michael R. Johnson
    • C07D311/80C07D405/12A61K31/35A61K31/44C07D311/78C07D405/02
    • C07D405/12C07D311/80
    • The present invention comprises novel compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: G is hydroxymethylene or carbonyl;R.sub.a and R.sub.b are each methyl or hydrogen;R.sub.1 is hydrogen or alkanoyl having one to five carbon atoms;R.sub.2 is hydrogen, bromo, chloro or fluoro;R.sub.3 is hydrogen, bromo, chloro, fluoro, alkyl having one to six carbon atoms, (CH.sub.2).sub.p COOR.sub.4 wherein p is an integer from 0-6 and R.sub.4 is hydrogen, methyl or ethyl, or (CH.sub.2).sub.q OH wherein q is an integer from 1-6; with the proviso that when R.sub.3 is hydrogen or alkyl, R.sub.2 is bromo, chloro or fluoro;Z is (--alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) has from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each zero or 1;X is oxygen or methylene; andW is methyl, pyridyl, piperidyl or ##STR2## wherein W.sub.1 is hydrogen, fluoro, chloro or methoxy. An analgesically producing quantity of the compound when administered to a mammal produces analgesia therein.
    • 本发明包括式IMA的新化合物或其药学上可接受的盐,其中:G是羟基亚甲基或羰基; Ra和Rb各自为甲基或氢; R1是氢或具有1-5个碳原子的烷酰基; R2是氢,溴,氯或氟; R3是氢,溴,氯,氟,具有1-6个碳原子的烷基,(CH2)pCOOR4,其中p是0-6的整数,R4是氢,甲基或乙基,或(CH2)qOH其中q是整数 从1-6开始; 条件是当R3为氢或烷基时,R2为溴,氯或氟; Z是(-alk1)mX-(alk2)n-,其中(alk1)和(alk2)中的每一个具有1至9个碳原子,条件是(alk1)+(alk2)中的碳原子的加成不是 大于9; m和n分别为零或1; X是氧或亚甲基; W是甲基,吡啶基,哌啶基或者其中W1是氢,氟,氯或甲氧基。 给予哺乳动物的化合物的镇痛产生量在其中产生镇痛。
    • 29. 发明授权
    • 9-Amino-1-hydroxyoctahydrobenzo[c]quinolines and derivatives thereof as
analgesics and anti-emetics
    • US4351833A
    • 1982-09-28
    • US296745
    • 1981-08-27
    • Michael R. Johnson
    • Michael R. Johnson
    • C07D215/22C07D215/233C07D221/12
    • C07D215/233C07D221/12Y10S514/85Y10S514/867Y10S514/869Y10S514/872Y10S514/906Y10S514/913
    • 9-Amino-1-hydroxyoctahydrobenzo[c]quinoline derivatives of formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R is hydrogen, COR.sub.7 or SO.sub.2 R.sub.8 where R.sub.7 is hydrogen, alkyl, having from one to five carbon atoms; alkenyl and alkynyl each having from two to six carbon atoms; trifluoromethyl, benzyl, furyl, thienyl, pyridyl or R.sub.9 C.sub.6 H.sub.4 where R.sub.9 is H, NH.sub.2, F, Cl, Br, Ch.sub.3 or OCH.sub.3 ; R.sub.8 is alkyl having from one to five carbon atoms or R.sub.9 C.sub.6 H.sub.4 ; R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.p --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino or N-alkylpiperazino having from one to four carbon atoms in the alkyl group;R.sub.4 is hydrogen, alkyl having from 1 to 6 carbon atoms or --(CH.sub.2).sub.z --C.sub.6 H.sub.5 wherein z is an integer from 1 to 4;R.sub.5 is hydrogen, methyl or ethyl;R.sub.6 is hydrogen, --(CH.sub.2).sub.y --carbalkoxy having from one to four carbon atoms in the alkoxy group and wherein y is 0 or an integer from 1 to 4, carbobenzyloxy, formyl, alkanoyl having from two to five carbon atoms, alkyl having from one to six carbon atoms; --(CH.sub.2).sub.x --C.sub.6 H.sub.5 wherein x is an integer from 1 to 4; or --CO(CH.sub.2).sub.x-1 --C.sub.6 H.sub.5 ;Z is (a) alkylene having from one to nine carbon atoms; (b) -(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from one to nine carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than nine; each of m and n is 0 or 1; X is O, S, SO and SO.sub.2 ; andW is hydrogen, methyl, pyridyl, piperidyl, ##STR2## wherein W.sub.1 is selected from the group consisting of hydrogen, fluoro and chloro; and ##STR3## wherein W.sub.2 is hydrogen or ##STR4## a is an integer from 1 to 5 and b is 0 or an integer from 1 to 5; with the proviso that the sum of a and b is not greater than 5; useful in mammals as analgesics, tranquilizers, anti-emetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.