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1. 发明授权

US4717563A 2-alkoxy-N-(1-azabicyclo(2.2.2)oct-3-yl) benzamides and thiobenzamides in a method for alleviating emesis caused by non-platinum anticancer drugs 失效
标题翻译： 2-烷氧基-N-（1-氮杂双环（2.2.2）辛-3-基）苯甲酰胺和硫代苯甲酰胺在减轻由非铂抗癌药引起的呕吐的方法中
公开(公告)号：US4717563A
公开(公告)日：1988-01-05
申请号：US836518
申请日：1986-03-05
申请人： Reevis S. Alphin , William L. Smith , Harry R. Munson, Jr. , Robert F. Boswell
发明人： Reevis S. Alphin , William L. Smith , Harry R. Munson, Jr. , Robert F. Boswell
IPC分类号： A61K31/435 , A61P1/08 , C07D453/02 , A61K31/44
CPC分类号： C07D453/02 , A61K31/435 , Y10S514/872
摘要： A method of controlling emesis caused by non-platinum anti-cancer drugs with 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is loweralkyl; and R.sub.2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, methylsulfonyl, loweralkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof is disclosed.

2. 发明授权

US4593034A 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides 失效
标题翻译： 2-烷氧基-N-（1-氮杂双环[2.2.2]辛-3-基）苯甲酰胺和硫代苯甲酰胺
公开(公告)号：US4593034A
公开(公告)日：1986-06-03
申请号：US597275
申请日：1984-04-06
申请人： Harry R. Munson, Jr. , Robert F. Boswell, Jr.
发明人： Harry R. Munson, Jr. , Robert F. Boswell, Jr.
IPC分类号： A61K31/435 , A61P1/08 , C07D453/02 , A61K31/445
CPC分类号： C07D453/02 , A61K31/435
摘要： 2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is loweralkyl; and R.sub.2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, alkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof having gastrokinetic and anti-emetic activity are disclosed.
摘要翻译： 2-烷氧基-N-（1-氮杂双环[2.2.2]辛-3-基）苯甲酰胺和具有式的硫代苯甲酰胺，其中X是氧或硫; R1是低级烷基; 并且R 2选自氢，卤素，4,5-苯并，烷氧基或Am，n为1或2，并且公开了其具有胃动力和抗呕吐活性的药学上可接受的酸加成盐。

3. 发明授权

US4585785A Cis and trans-3-aryloxy-4-hydroxypyrrolidines used as anti-arrhythmics 失效
标题翻译：用作抗心律失常药的顺式和反式-3-芳氧基-4-羟基吡咯烷
公开(公告)号：US4585785A
公开(公告)日：1986-04-29
申请号：US128696
申请日：1980-03-10
申请人： David A. Walsh , William J. Welstead, Jr.
发明人： David A. Walsh , William J. Welstead, Jr.
IPC分类号： C07D207/12 , C07D207/20 , C07D491/04 , A61K31/40
CPC分类号： C07D491/04 , C07D207/12 , C07D207/20
摘要： Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, phenylalkyl, benzyloxycarbonyl, carbamoyl, N-loweralkylcarbamoyl, N-diloweralkylcarbamoyl and parafluorobenzoyl-lower-alkyl; Ar is phenyl, substituted phenyl, 1-naphthyl, 2-naphthyl, 1-indenyl and 2-indenyl and pharmaceutically acceptable acid addition and quaternary salts thereof. The compounds have antidepressant, antihypertensive and antiarrythmic activity in animals.
摘要翻译：公开了具有下式的顺式和反式-3-芳氧基-4-羟基吡咯烷及其衍生物：其中R 1是氢，低级烷基，苄氧基羰基和N-低级烷基氨基甲酰基; R2是氢，低级烷基，环烷基，苯基烷基，苄氧基羰基，氨基甲酰基，N-低级烷基氨基甲酰基，N-二低级烷基氨基甲酰基和九氟苯甲酰基 - 低级烷基; Ar是苯基，取代的苯基，1-萘基，2-萘基，1-茚基和2-茚基及其药学上可接受的酸加成盐和季盐。该化合物在动物中具有抗抑郁，抗高血压和抗焦虑作用。

4. 发明授权

US4538001A 1-Aryloxy-4-amino-2-butanols 失效
标题翻译： 1-芳氧基-4-氨基-2-丁醇
公开(公告)号：US4538001A
公开(公告)日：1985-08-27
申请号：US649331
申请日：1984-09-11
申请人： Carl D. Lunsford , Ying-Ho Chen
发明人： Carl D. Lunsford , Ying-Ho Chen
IPC分类号： C07C43/196 , C07C43/23 , C07C45/71 , C07D211/14 , C07D211/70 , C07D213/64 , C07D215/06 , C07D217/04 , C07D295/092 , C07C43/225
CPC分类号： C07D213/64 , C07C43/196 , C07C43/23 , C07C45/71 , C07D211/14 , C07D211/70 , C07D215/06 , C07D217/04 , C07D295/088
摘要： Novel 1-aryloxy-4-amino-2-butanols of the formulaArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenyl-alkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen form a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.
摘要翻译：式ArO-CH2-CHOH-CH2-CH2-NR1R2的新型1-芳氧基-4-氨基-2-丁醇其中Ar为1-萘基，2-萘基，茚-4（或5-）基，3-（苯基，苯基，苯基 - 烷基，2-羟甲基-2-丙基，金刚烷基或低级环烷基，R 2为氢或低级烷基，其中R 1和R 2与相邻的氮一起形成杂环残基，并且其中药学上可接受的酸加成盐具有局部麻醉剂，β-肾上腺素能阻断剂，抗高血压药和抗心律失常药物。该化合物通过新颖的1-芳氧基-4-氯-2-丁醇与胺反应来制备。还公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。

5. 发明授权

US4518603A [2-[(Nitropyridinyl)amino]phenyl]arylmethanones in a process for preparing pyrido[1,4]benzodiazepines 失效
标题翻译： [2 - [（硝基吡啶基）氨基]苯基]芳基甲酮在制备吡啶并[1,4]苯并二氮杂
公开(公告)号：US4518603A
公开(公告)日：1985-05-21
申请号：US541215
申请日：1983-12-23
申请人： Young S. Lo , Chandler R. Taylor, Jr.
发明人： Young S. Lo , Chandler R. Taylor, Jr.
IPC分类号： C07D213/74 , C07D471/04 , A61K31/38 , A61K31/40 , A61K31/44 , A61K31/495
CPC分类号： C07D213/74 , C07D471/04
摘要： [2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: ##STR1## wherein; B is carbonyl, thioxomethyl, ketal or thioketal,R is hydrogen or --alk.sup.1 -Q,Q is hydrogen, --NR.sup.1 R.sup.2 or halogen are disclosed in a process for preparing pyrido[1,4]benzodiazepines.
摘要翻译： [2 - [（硝基吡啶基）氨基]苯基]芳基甲酮作为化学中间体和/或具有下式的抗抑郁活性：其中： B是羰基，硫代甲基，缩酮或硫缩酮，R是氢或-alk1-Q，Q是氢，-NR1R2或卤素在制备吡啶并[1,4]苯并二氮杂的方法中公开。

6. 发明授权

US4377582A 2-Phenyl-4-[cis-2,5-dimethyl-4-(2-pyridinyl)-1-piperazinyl]quinazoline 失效
标题翻译： 2-苯基-4- [顺式-2,5-二甲基-4-（2-吡啶基）-1-哌嗪基]喹唑啉
公开(公告)号：US4377582A
公开(公告)日：1983-03-22
申请号：US266257
申请日：1981-05-22
申请人： Ying-Ho Chen
发明人： Ying-Ho Chen
IPC分类号： C07D239/94 , A61K31/505
CPC分类号： C07D239/94
摘要： Novel hypotensive agents are disclosed which are quinazolines substituted in the 2 and 4 position having the general formula: ##STR1## wherein Q is a secondary amine radical illustrated by loweralkanolylamino or a tertiary amine radical such as pyrrolidinyl, piperidinyl or piperazinyl, any of which may be substituted by various groups such as loweralkanolyl.
摘要翻译：公开了新的降压剂，其在2和4位被喹唑啉取代，具有以下通式：其中Q是由低级烷酰胺基或叔胺基例如吡咯烷基，哌啶基或哌嗪基所示的仲胺基，其中任何一种可以被各种基团取代，例如低级烷酰基。

7. 发明授权

US4362667A Optical isomers of 4-amino-N-(1-cyclohexyl-3-pyrrolidinyl)-N-methylbenzamide 失效
标题翻译： 4-氨基-N-（1-环己基-3-吡咯烷基）-N-甲基苯甲酰胺的光学异构体
公开(公告)号：US4362667A
公开(公告)日：1982-12-07
申请号：US226868
申请日：1981-01-21
申请人： Albert D. Cale, Jr. , Charles A. Leonard
发明人： Albert D. Cale, Jr. , Charles A. Leonard
IPC分类号： C07D207/14 , A61K31/40
CPC分类号： C07D207/14 , Y10S514/872
摘要： The resolution of racemic 4-amino-N-(1-cyclohexyl-3-pyrrolidinyl)-N-methylbenzamide into the optically active (+) and (-) isomers is disclosed.
摘要翻译：公开了将外消旋4-氨基-N-（1-环己基-3-吡咯烷基）-N-甲基苯甲酰胺拆分成光学活性（+）和（ - ）异构体。

8. 发明授权

US4343804A 4-Amino-3-quinolinecarboxylic acids and esters-antisecretory anti-ulcer compounds 失效
标题翻译： 4-氨基-3-喹啉羧酸和酯类抗分泌性抗溃疡化合物
公开(公告)号：US4343804A
公开(公告)日：1982-08-10
申请号：US127153
申请日：1980-03-04
申请人： Harry R. Munson, Jr. , Reevis S. Alphin
发明人： Harry R. Munson, Jr. , Reevis S. Alphin
IPC分类号： A61K31/47 , A61P1/04 , C07D215/54
CPC分类号： C07D215/54 , Y10S514/927
摘要： A method of reducing gastric acidity and treating peptic ulcers and pharmaceutical compositions therefor with certain 4-amino-3-quinolinecarboxylic acids and esters are disclosed. Illustrative of compounds useful in the method which relies on activity as antisecretory activity is the novel compound ethyl 8-methoxy-4-[(2-methylphenyl)amino]-3-quinolinecarboxylate which has the formula: ##STR1##
摘要翻译：公开了一些降低胃酸度并用某些4-氨基-3-喹啉羧酸和酯来治疗消化性溃疡及其药物组合物的方法。可用于依赖于作为抗分泌活性的活性的方法中的化合物的实例是具有下式的新化合物8-甲氧基-4 - [（2-甲基苯基）氨基] -3-喹啉羧酸乙酯，其具有下式：

9. 发明授权

US4327108A Methods useful in the treatment of cardiac arrhythmia using 4-substituted-2-iminoimidazolidine compounds 失效
标题翻译：用于使用4-取代-2-亚氨基咪唑烷化合物治疗心律失常的方法
公开(公告)号：US4327108A
公开(公告)日：1982-04-27
申请号：US146612
申请日：1980-05-05
申请人： Albert D. Cale, Jr.
发明人： Albert D. Cale, Jr.
IPC分类号： C07D233/44 , A61K31/415 , A61K31/445 , A61K31/495
CPC分类号： C07D233/44 , Y10S514/821
摘要： This invention provides a novel class of 2-iminoimidazolidines which include 4-substituted derivatives such as 4-(2-chloroethyl)-1-methyl-2-methylimino-3-phenyl imidazolidine fumarate: ##STR1## This illustrated 4-substituted 2-iminoimidazolidine compound exhibits cardiovascular hypotensive, hypoglycemic (glucose tolerance, and sugar cataract) and anti-inflammatory (pleural effusion) pharmacological activities in test animals.
摘要翻译：本发明提供了一类新的2-亚氨基咪唑烷，其包括4-取代的衍生物如4-（2-氯乙基）-1-甲基-2-甲基亚氨基-3-苯基咪唑烷富马酸盐。亚氨基咪唑烷化合物在试验动物中表现出心血管低血压，低血糖（葡萄糖耐量和糖白内障）和抗炎（胸腔积液）药理活性。

10. 发明授权

US4313949A Method of producing an inhibitory effect on blood platelet aggregation 失效
标题翻译：产生对血小板聚集的抑制作用的方法
公开(公告)号：US4313949A
公开(公告)日：1982-02-02
申请号：US234532
申请日：1981-02-17
申请人： James R. Shanklin, Jr. , Dwight A. Shamblee , David A. Walsh
发明人： James R. Shanklin, Jr. , Dwight A. Shamblee , David A. Walsh
IPC分类号： C07D295/185 , A61K31/535 , A61K31/165
CPC分类号： C07D295/185
摘要： Novel 2-amino-3-benzoyl-phenylacetamides are provided having the formula: ##STR1## wherein R represents hydrogen or lower alkyl, R.sup.1 and R.sup.2 represent hydrogen, lower alkyl, cycloalkyl, phenyl and phenyl substituted by lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen may form a heterocyclic residue; X represents hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; Y represents hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, lower alkylthio, lower alkyloxythio or lower alkyldioxythio; Am is primary amino (--NH.sub.2), methylamino or dimethylamino, and n is 1 to 3 inclusive. The compounds exhibit anti-inflammatory, antipyretic, anti-blood platelet aggregation and analgetic pharmacological activities.
摘要翻译：提供了新的2-氨基-3-苯甲酰基 - 苯基乙酰胺，其具有下式：其中R表示氢或低级烷基，R 1和R 2表示氢，低级烷基，环烷基，苯基和被低级烷基，低级烷氧基，卤素硝基和三氟甲基，当R 1和R 2与相邻的氮原子一起时可以形成杂环残基; X表示氢，低级烷基，低级烷氧基，卤素或三氟甲基; Y代表氢，低级烷基，低级烷氧基，卤素，三氟甲基，低级烷硫基，低级烷硫氧基或低级烷基二氧硫基; Am是伯氨基（-NH 2），甲基氨基或二甲基氨基，n是1〜3。该化合物具有抗炎，解热，抗血小板聚集和止痛药理作用。

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