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公开(公告)号：US3941806A
公开(公告)日：1976-03-02
申请号：US218833
申请日：1972-01-18
IPC分类号： C07D209/08 , C07D223/16 , C07D209/12 , A61K31/40
CPC分类号： C07D223/16 , C07D209/08 , Y10S514/937 , Y10S514/96
摘要： The preparation of compounds of the formula ##SPC1##Wherein R is selected from the group consisting of hydrogen and chlorine is described. The compounds are useful as chemical intermediates and as anti-inflammatory agents.
摘要翻译： 描述式WHEREIN R选自氢和氯的化合物的制备。 该化合物可用作化学中间体和抗炎剂。
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公开(公告)号：US4031245A
公开(公告)日：1977-06-21
申请号：US674706
申请日：1976-04-07
IPC分类号： C07D295/06 , C07D295/08 , A61K31/135
CPC分类号： C07D295/08 , C07D295/06
摘要： Novel alkenyl- and alkanylamines having the formula: ##STR1## wherein Am is lower-alkylamino, di-lower-alkylamino and piperidino; A is methylene and methylidyne; R is hydrogen, lower-alkyl, lower-alkoxy, halogen and trifluoromethyl; m is zero and one; n is one and two; X is halogen and the pharmaceutically acceptable acid addition salts thereof. The alkenylamines are prepared by contacting 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols with strong mineral acids. The alkanylamines are prepared by hydrogenation of the alkenylamines. Some of the compounds exhibit potent antagonism to the depressant effects of tetrabenazine.
摘要翻译： 新的具有下式的烯基和烷基胺：其中Am是低级烷基氨基，二低级烷基氨基和哌啶子基; A是亚甲基和亚甲基; R为氢，低级烷基，低级烷氧基，卤素和三氟甲基; m是零和一; n是一和二; X是卤素及其药学上可接受的酸加成盐。 烯基胺通过使1-环丙基-1-苯基 - ω-氨基-1-链烷醇与强无机酸接触来制备。 链烷胺通过链烯基胺的氢化制备。 一些化合物表现出对丁苯那敏抑制作用的强烈拮抗作用。
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3.发明授权1-Cyclopropyl-1-phenyl-.omega.-amino-1-alkanols and 1-lower-alkylacyl derivatives as analgetics 失效1-环丙基-1-苯基-γ-氨基-1-烷醇和1-低级烷基胆碱衍生物作为分析
公开(公告)号：US4001429A
公开(公告)日：1977-01-04
申请号：US580106
申请日：1975-04-28
IPC分类号： C07D295/08 , A61K31/22 , A61K31/445
CPC分类号： C07D295/08
摘要： Novel 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols and 1-lower-alkylacyl derivatives are described having the formula: ##STR1## wherein; Am is lower-alkylamino, di-lower-alkylamino and piperidino, R is hydrogen and lower alkanoyl, R.sup.1 is hydrogen, halogen, lower-alkoxy, lower-alkyl and trifluoromethyl, and n is two and three. The compounds wherein R is hydrogen have antidepressant properties and those wherein R is lower-alkanoyl have analgetic properties.
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公开(公告)号：US4120969A
公开(公告)日：1978-10-17
申请号：US796264
申请日：1977-05-12
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： 1-R-4-(omega-substituted alkyl)-3,3-diphenyl-2-pyrrolidinones of the formula ##STR1## wherein R is hydrogen, lower alkyl, cyclohexyl or benzyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or lower alkoxy, R.sup.2 is hydrogen, chloro, bromo, or fluoro, A is hydroxy, lower-alkylcarbonyloxy or lower-alkoxycarbonyl and n is 1, 2 or 3 having analgetic and antidiarrheal activity are disclosed. The pharmaceutically acceptable acid addition salts of the bases are within the scope of the present invention.
摘要翻译： 其中R是氢，低级烷基，环己基或苄基，R 1是氢，氯，溴，氟，C 1 -C 4烷基，C 1 -C 4 - （ω-取代的烷基）-3,3-二苯基-2-吡咯烷酮， 三氟甲基或低级烷氧基，R 2是氢，氯，溴或氟，A是羟基，低级烷基羰基氧基或低级烷氧基羰基，n是具有止痛和止泻活性的1,2或3。 碱的药学上可接受的酸加成盐在本发明的范围内。
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公开(公告)号：US3978130A
公开(公告)日：1976-08-31
申请号：US452578
申请日：1974-03-19
IPC分类号： C07D295/08 , C07C91/22
CPC分类号： C07D295/08
摘要： Novel 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols are described having the formula: ##SPC1##Wherein;Am is lower-alkylamino and di-lower-alkylamino and piperidino, R is hydrogen, halogen, lower-alkoxy, lower-alkyl and trifluoromethyl, and n is 2 and 3. The compounds have antidepressant properties.
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公开(公告)号：US4002766A
公开(公告)日：1977-01-11
申请号：US536708
申请日：1974-12-26
IPC分类号： A61K31/40 , A61P9/06 , C07D207/06 , C07D207/08
CPC分类号： C07D207/08 , C07D207/06 , Y10S514/821
摘要： 1-R-3-Pyrrolidinyl-.alpha.,.alpha.-diphenylacetamides, -acetonitriles and -methanes represented by the following formula: ##STR1## wherein R represents hydrogen, lower alkyl, lower cycloalkyl or phenyllower alkyl, R.sup.1 represents hydrogen or lower alkyl, and Y is carbamoyl, di-lower-alkylcarbamoyl, pyrrolidinocarbonyl, morpholinocarbonyl, cyano or hydrogen having antiarrhythmic activity are disclosed. Pharmaceutically acceptable acid addition salts are included as part of the invention.
摘要翻译： 由下式表示的1-R-3-吡咯烷基-α，α-二苯基乙酰胺， - 乙腈和 - 甲烷：其中R表示氢，低级烷基，低级环烷基或苯基低级烷基，R1表示氢或低级烷基， Y是氨基甲酰基，二低级烷基氨基甲酰基，吡咯烷基羰基，吗啉代羰基，具有抗心律不齐活性的氰基或氢。 包括药学上可接受的酸加成盐作为本发明的一部分。
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7.发明授权
公开(公告)号：US3975531A
公开(公告)日：1976-08-17
申请号：US545057
申请日：1975-01-29
IPC分类号： C07D209/08 , C07D209/34 , A61K31/40
CPC分类号： C07D209/08 , C07D209/34
摘要： Novel 4-(5- and 7-)benzoylindolin-2-ones of the formula: ##SPC1##Wherein R is hydrogen, lower-alkyl, or methylthio, R.sup.1 is hydrogen or lower-alkyl, R.sup.2 is lower-alkyl, lower-alkoxy, halogen, nitro or trifluoromethyl, R.sup.3 is hydrogen, halogen or lower-alkoxy, and n is 0, 1 or 2, are prepared by (a) acylation of indolin-2-one to give 5-benzoylindoline-2-one, (b) cyclization of 2-acetamido-3-benzoylphenylacetic acid or ethyl 2-acetamido-3-benzoylphenylacetate to give 7-benzoyindoline-2-one, or (c) by reacting aminobenzophenones with alkyl .alpha.(methylthio)acetates to give alkyl 2-amino-3-(5- or 6-)benzoyl-.alpha.-(methylthio)phenylacetates which are cyclized and demethylthiolated to 4-(5- and 7-)benzoylindolin-2-ones. The novel compounds possess anti-inflammatory activity and are intermediates for the preparation of 2-amino-3-(5- or 6-) benzoylphenylacetic acids which posess anti-inflammatory properties.
摘要翻译： 新的4-（5-和7-）苯并二氢吲哚-2-酮，其具有下式：
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8.发明授权Phenylalkylamines and phenylalkylureas in combinations to suppress gastric bleeding in aspirin therapy 失效苯基烷基胺和苯基烷基脲组合用于抑制阿司匹林治疗中的胃出血
公开(公告)号：US4025624A
公开(公告)日：1977-05-24
申请号：US633042
申请日：1975-11-18
IPC分类号： A61K31/17 , A61K31/625 , A61K31/615
CPC分类号： A61K31/60 , A61K31/621
摘要： Novel pharmaceutical methods, combinations and compositions for reducing gastric bleeding during aspirin therapy for inflammation are disclosed. Compounds used in combination with aspirin are phenylalkylamines and phenylalkylureas having the formula: ##STR1## wherein Z is selected from the group consisting of --NHR.sup.2 or ##STR2## and R is selected from the group consisting of hydrogen, halogen, lower-alkoxy and trifluoromethyl and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower-alkyl, where R.sup.3 and R.sup.4 taken together with the adjacent nitrogen atom may form a heterocyclic ring selected from the group of piperidino, pyrrolidino, piperazino, and morpholino.
摘要翻译： 公开了用于减少阿司匹林治疗炎症期间胃出血的新型药物方法，组合和组合物。 与阿斯匹林组合使用的化合物是具有下式的苯基烷基胺和苯基烷基脲：其中Z选自-NHR2或者“IMAGE”，R选自氢，卤素，低级烷氧基和三氟甲基 并且R 1，R 2，R 3和R 4选自氢和低级烷基，其中R 3和R 4与相邻的氮原子一起形成选自哌啶子基，吡咯烷子基，哌嗪基和吗啉代的杂环 。
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公开(公告)号：US3984557A
公开(公告)日：1976-10-05
申请号：US536521
申请日：1974-12-26
IPC分类号： C07D213/57 , A61K31/44
CPC分类号： C07D213/57
摘要： 1-R-3-Pyrrolidinyl-.alpha.-phenyl-.alpha.-(2-pyridyl)acetamides, -acetonitriles and -methanes represented by the following formula: ##SPC1##Wherein R represents lower alkyl, lower cycloalkyl or phenyllower alkyl and Y is carbamoyl, cyano or hydrogen having antiarrhythmic activity are disclosed. Pharmaceutically acceptable acid addition salts are included as part of the invention.
摘要翻译： 由下式表示的1-R-3-吡咯烷基-α-苯基-α-（2-吡啶基）乙酰胺， - 乙腈和 - 甲烷：
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公开(公告)号：US3978129A
公开(公告)日：1976-08-31
申请号：US221825
申请日：1972-01-28
IPC分类号： C07C211/28 , C07C67/00 , C07C209/00 , C07C211/29 , C07D295/067 , C07D295/084 , C07C87/28 , C07C87/29
CPC分类号： C07D295/067 , C07D295/092
摘要： Novel alkenyl- and alkanylamines having the formula: ##EQU1## WHEREIN Am is lower-alkylamino, di-lower-alkylamino and piperidino; A is methylene and methylidyne; R is hydrogen, lower-alkyl, lower-alkoxy, halogen and trifluoromethyl; m is zero and one; n is one and two; X is halogen and the pharmaceutically acceptable acid addition salts thereof. The alkenylamines are prepared by contacting 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols with strong mineral acids. The alkanylamines are prepared by hydrogenation of the alkenylamines. Some of the compounds exhibit potent antagonism to the depressant effects of tetrabenazine.
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