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公开(公告)号：US5041442A
公开(公告)日：1991-08-20
申请号：US560528
申请日：1990-07-31
IPC分类号： C07D497/04
CPC分类号： C07D497/04 , Y10S514/927
摘要： This invention is directed to compounds of formula (I): ##STR1## wherein R.sup.1 is thiocyano, --CH.sub.2 CN, --NH.sub.2, --NHR.sup.5, or --CH.sub.2 OR.sup.5 where R.sup.5 is lower alkyl;R.sup.2 is hydrogen, halo, lower alkyl, or lower alkylthio;R.sup.3 is hydrogen, halo, lower alkyl, lower alkylthio, or thiocyano;R.sup.4 is hydrogen, halo, lower alkyl, lower alkoxy, lower alkylthio, or lower alkylsulfonyl; andY is --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.dbd.CH--, or --(CH.sub.2).sub.n -- where n is 0, 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof. These compounds are useful in treating mammals having disease-states characterized by excessive gastric acid secretion.
摘要翻译： 本发明涉及式（I）的化合物：其中R 1是硫氰基，-CH 2 CN，-NH 2，-NHR 5或-CH 2 OR 5，其中R 5是低级烷基; R2是氢，卤素，低级烷基或低级烷硫基; R3是氢，卤素，低级烷基，低级烷硫基或硫氰基; R4是氢，卤素，低级烷基，低级烷氧基，低级烷硫基或低级烷基磺酰基; 并且Y是-O-CH 2 - ， - S-CH 2 - ， - CH = CH-或 - （CH 2）n - ，其中n是0,1,2,3或4; 或其药学上可接受的盐。 这些化合物可用于治疗以过度胃酸分泌为特征的疾病状态的哺乳动物。
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32.发明授权Intermediates for preparing 5-aroyl-1,2-dihydro-3H-pyrrolo(1,2-A)pyrrole-1,1-dicarboxylates 失效制备5-芳酰基-1,2-二氢-3H-吡咯并（1,2-A）吡咯-1,1-二羧酸酯的中间体
公开(公告)号：US4988822A
公开(公告)日：1991-01-29
申请号：US386832
申请日：1989-07-27
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-halopyrroles. Hydrolysis and .beta.-decarboxylation of these compounds affords ketorolac and related compounds.
摘要翻译： 由2-卤代吡咯制备式“IMAGE”的5-芳酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1,1-二羧酸酯。 这些化合物的水解和β-脱羧提供酮咯酸和相关化合物。
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公开(公告)号：US4888358A
公开(公告)日：1989-12-19
申请号：US236697
申请日：1988-08-25
申请人： Joan Huguet , Joseph M. Muchowski , Maria T. Lara
发明人： Joan Huguet , Joseph M. Muchowski , Maria T. Lara
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： Novel 13,14-dihydroprostaglandin derivatives of the formula ##STR1## wherein: m is 1 or 3;R.sub.1 is hydrogen or alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 and R.sub.4 are independently hydrogen or methyl;R.sub.5 is alkyl, CF.sub.3 (CH.sub.2).sub.n -- in which n is an integer of 3-5, cycloalkyl, or optionally substituted phenyl, benzyl or phenoxy; orR.sub.4 and R.sub.5 taken together with the carbon to which they are attached is cycloalkyl of 4-8 carbon atoms;X is cis --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 -- when m is 3, orX is --CH.sub.2 CH.dbd.C.dbd.CH-- when m is 1;and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.;or a pharmaceutically acceptable salt thereof,have been prepared. They are useful in particular for their antihypertensive and anti-ulcerogenic properties.
摘要翻译： 式（I）的新型13,14-二氢前列腺素衍生物，其中：m为1或3; R1是氢或烷基; R2是氢或低级烷基; R 3和R 4独立地是氢或甲基; R5是烷基，CF3（CH2）n-，其中n是3-5的整数，环烷基或任选取代的苯基，苄基或苯氧基; 或者R 4和R 5与它们所连接的碳一起是4-8个碳原子的环烷基; 当m为3时，X为顺式-CH = CH-或-CH2CH2-，当m为1时，X为-CH2CH = C = CH-; 而波浪线表示α或β构型，条件是当一条波浪线为α时，另一条波长为β; 或其药学上可接受的盐。 它们特别适用于其抗高血压和抗溃疡性质。
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34.发明授权3-(.omega.-(3,5,-di-t-butyl-4-hydroxyphenyl)-alkanoyl)pyrroles, and anti-inflammatory uses thereof 失效3-（ω-（3,5'-二叔丁基-4-羟基苯基） - 烷酰基）吡咯及其抗炎用途
公开(公告)号：US4833155A
公开(公告)日：1989-05-23
申请号：US936551
申请日：1986-11-25
IPC分类号： A61K31/40 , A61P9/00 , A61P25/04 , A61P29/00 , C07D207/32 , C07D207/333 , C07D207/335 , C07D207/34 , C07D207/36
CPC分类号： C07D207/333 , C07D207/34 , C07D207/36
摘要： 3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkanoyl]-pyrroles and their de-oxy analogs, for example, 3-(3,5-di-t-butyl-4-hydroxybenzyl)pyrrole, 2-chloro-4-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole, 3-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole and 3-[2-(3,5-di-t-butyl-4-hydroxyphenyl)-1-oxoethyl]pyrrole, have high pharmacological potency as anti-inflammatory, analgesic and antipyretic agents.
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35.发明授权+2-[(3,4-Methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hy droxy)-.alpha.-hydroxybenzyl]pyrrolidines 失效+2 - [（3,4-亚甲二氧基）苯乙基] -5 - [（3-甲酰胺基-4-羟基）-α-羟基苄基]吡咯烷
公开(公告)号：US4548949A
公开(公告)日：1985-10-22
申请号：US527716
申请日：1983-08-29
IPC分类号： A61K31/40 , C07D295/108 , C07D317/60 , C07D405/06
CPC分类号： C07D295/108 , C07D317/60 , C07D405/06
摘要： A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators. These compounds are also useful as bronchodilators.
摘要翻译： 式“IMAGE”及其药学上可接受的酸加成盐的化合物是有效的抗高血压药，因此可用作心血管系统调节剂。 这些化合物也可用作支气管扩张剂。
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36.发明授权5-Benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and pharmaceutical use thereof 失效5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸及其药物用途
公开(公告)号：US4505927A
公开(公告)日：1985-03-19
申请号：US339813
申请日：1982-01-15
IPC分类号： C07D207/34 , C07D487/04 , C07D487/06 , A61K31/40
CPC分类号： C07D487/04 , C07D207/34
摘要： 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
摘要翻译： 由式（VII）表示的5-苯甲酰基-7-卤代-1,2-二氢-3H-吡咯并[1,2-a] - 吡咯-1-羧酸和药学上可接受的无毒酯 及其盐，其中：R为氢或低级烷基; X是氢，低级烷基，低级烷氧基，低级烷氧基羰基，羧基，低级烷基羰基，磺酸，磺酸烷基酯，氟，氯或溴; 和Y是氯或溴，它们是新的，由式（VI）表示的5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸， 其中X和R如上所定义，除了X不能是氯或溴以外，是通过相应的1,1-二羧酸脱羧制备的。 还公开了所述制备中的中间体。
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公开(公告)号：US4496577A
公开(公告)日：1985-01-29
申请号：US539197
申请日：1983-10-05
申请人： Joseph M. Muchowski , Angel Guzman
发明人： Joseph M. Muchowski , Angel Guzman
IPC分类号： C07D233/22 , A61K31/415 , A61P7/02 , C07D233/32 , C07D233/34 , C07D309/12 , C07D333/00 , C07D405/06 , C07D409/06 , C07D233/02
CPC分类号： C07C247/00 , C07D233/32 , C07D309/12
摘要： This invention relates to novel imidazolidinone prostaglandin compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen or alkyl of 1 to 4 carbons; R.sup.3 is hydrogen or methyl; and R4 is --(CH.sub.2).sub.n CH.sub.3 wherein n is 3-7, cycloalkyl of 5-7 carbons, a substituent of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, halo or trifluoromethyl. These compounds are inhibitors of blood platelet aggregation.
摘要翻译： 本发明涉及式（I）的新型咪唑啉酮前列腺素化合物及其药学上可接受的盐，其中R 1和R 2独立地是氢或1至4个碳的烷基; R3是氢或甲基; 并且R 4是 - （CH 2）n CH 3，其中n是3-7，5-7个碳的环烷基，式的取代基，其中R5是氢，1至4个碳的烷基，1个烷氧基， 至4个碳，卤素或三氟甲基。 这些化合物是血小板聚集的抑制剂。
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38.发明授权5-Benzoyl-7-halo-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1,1-dicarboxylic acids and esters thereof 失效5-苯甲酰基-7-卤代-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1,1-二羧酸及其酯
公开(公告)号：US4456759A
公开(公告)日：1984-06-26
申请号：US387562
申请日：1982-06-11
IPC分类号： C07D207/34 , C07D487/04 , C07D487/02
CPC分类号： C07D487/04 , C07D207/34
摘要： 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
摘要翻译： 由式（VII）表示的5-苯甲酰基-7-卤代-1,2-二氢-3H-吡咯并[1,2-a] - 吡咯-1-羧酸和药学上可接受的无毒酯 及其盐，其中：R为氢或低级烷基; X是氢，低级烷基，低级烷氧基，低级烷氧基羰基，羧基，低级烷基羰基，磺酸，磺酸烷基酯，氟，氯或溴; 和Y是氯或溴，它们是新的，由式（VI）表示的5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸， 其中X和R如上所定义，除了X不能是氯或溴以外，是通过相应的1,1-二羧酸脱羧制备的。 还公开了所述制备中的中间体。
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39.发明授权3-Substituted-5,6,7,8-tetrahydropyrrolo[1,2-a]-pyridine-and 6,7,8,9-tetrahydro-5H-pyrrolo[1,2-a]-azepine carboxylic acid derivatives useful as blood platelet aggregation inhibitors 失效3-取代的5,6,7,8-四氢吡咯并[1,2-a] - 吡啶和6,7,8,9-四氢-5H-吡咯并[1,2-a] - 吖庚因羧酸衍生物有用 作为血小板聚集抑制剂
公开(公告)号：US4410534A
公开(公告)日：1983-10-18
申请号：US243322
申请日：1981-03-13
IPC分类号： C07D471/04 , C07D487/04 , A61K31/44 , C07D221/02
CPC分类号： C07D471/04 , C07D487/04
摘要： Novel 3-substituted-5,6,7,8-tetrahydropyrrolo[1,2-a]pyridine-8-carboxylic acid and 3-substituted-6,7,8,9-tetrahydro[1,2-a]azepine-9-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 carbon atoms, n is the integer selected from the integers 1 or 2 and Ar is a 6- or 5-member ring. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents, platelet aggregation inhibitors, and as smooth muscle relaxants.
摘要翻译： 新的3-取代-5,6,7,8-四氢吡咯并[1,2-a]吡啶-8-羧酸和3-取代-6,7,8,9-四氢[1,2-a]吖庚因 - 由式
表示的9-羧酸化合物及其药学上可接受的无毒酯及其盐，其中R是氢或含有1至4个碳原子的低级烷基，n是选自整数的整数 1或2，Ar是6-或5-元环。 这些化合物可用作抗炎，镇痛和解热剂，血小板聚集抑制剂和平滑肌松弛剂。 -
公开(公告)号：US4410526A
公开(公告)日：1983-10-18
申请号：US323152
申请日：1981-11-20
申请人： Joseph M. Muchowski , Angel Guzman
发明人： Joseph M. Muchowski , Angel Guzman
IPC分类号： C07D263/20 , C07D263/24 , C07D277/14 , C07D413/12 , C07D417/12 , A61K31/42 , A61K31/425 , C07D263/22
CPC分类号： C07D263/20 , C07C247/00 , C07D277/14
摘要： Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons, ##STR2## R.sup.2 is hydrogen or methyl; exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.
摘要翻译： 式（I）化合物及其药学上可接受的无毒盐和酯（烷基，1-6C），其中：X是O或S; R1选自：（a）3-8个碳原子的烷基或环烷基，（b）
CH2，Y是低级烷基（1-4C），低级烷氧基（1-4C），卤素， 或CF3，和（c）本文定义的 并且R 2是氢或甲基; 表现出前列腺素样活性，因此可用作血小板聚集抑制剂。
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