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41. 发明授权

US4250176A Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US4250176A
公开(公告)日：1981-02-10
申请号：US49779
申请日：1979-06-18
申请人： Jan Vandenberk , Ludo E. J. Kennis , Marcel J. M. C. Van der Aa , Albert H. M. T. Van Heertum
发明人： Jan Vandenberk , Ludo E. J. Kennis , Marcel J. M. C. Van der Aa , Albert H. M. T. Van Heertum
IPC分类号： C07C17/16 , C07D211/46 , C07D213/26 , C07D213/30 , C07D213/50 , C07D235/06 , C07D235/08 , C07D235/18 , C07D235/26 , C07D235/28 , C07D295/073 , C07D295/13 , A61K31/495 , C07D403/06 , C07D413/06 , C07D417/06
CPC分类号： C07D213/30 , C07C17/16 , C07D211/46 , C07D213/26 , C07D213/50 , C07D235/06 , C07D235/08 , C07D235/18 , C07D235/26 , C07D235/28 , C07D295/073 , C07D295/13 , Y10S514/826
摘要： Novel 1-substituted 4-(diarylmethyl)piperazine derivatives having antianaphylactic and antihistaminic properties, in which the 1-substituent is optionally substituted 2(3H) benzimidazol-2-one, 2(3H) benzothiazol-2-one, or 2(3H) benzoxazol-2-one.
摘要翻译：具有抗过敏和抗组胺性质的新颖的1-取代的4-（二芳基甲基）哌嗪衍生物，其中1-取代基是任选取代的2（3H）苯并咪唑-2-酮，2（3H）苯并噻唑-2-酮或2（3H ）苯并恶唑-2-酮。

42. 发明授权

US4221805A Method of inducing platelet antiaggregation activity 失效
标题翻译：诱导血小板抗聚集活性的方法
公开(公告)号：US4221805A
公开(公告)日：1980-09-09
申请号：US927726
申请日：1978-07-24
申请人： Giuseppe Quadro
发明人： Giuseppe Quadro
IPC分类号： C07D295/073 , A61K31/40
CPC分类号： C07D295/073 , Y10S514/822
摘要： Compositions useful for platelet antiaggregation activity are described, which contain as the active ingredient N-(2-chlorobenzyl)-pyrrolidine or a pharmacologically compatible salt thereof with an organic or an inorganic acid, and at least one pharmaceutically acceptable carrier or excipient. The compositions in the form of an aqueous solution are administered orally in the dose of 2-8 mgs/kg, preferably 3 mgs/kg body weight twice a day. The compositions may also be administered intravenously or endoperitoneally. The compositions may be administered in the form of capsules, ampoules or in the form of oily suspensions, solutions or emulsions.
摘要翻译：描述了可用于血小板抗聚集活性的组合物，其含有作为活性成分的N-（2-氯苄基） - 吡咯烷或其与有机或无机酸的药理学上相容的盐，以及至少一种药学上可接受的载体或赋形剂。水溶液形式的组合物以2-8mgs / kg，优选3mgs / kg体重的剂量每天两次口服给药。组合物也可以静脉内或腹膜内给药。组合物可以以胶囊，安瓿或油性混悬剂，溶液或乳剂的形式施用。

43. 发明授权

US4198510A Piperidenylmethylidene phosphonylamidines 失效
标题翻译：哌啶基亚甲基膦酰脒
公开(公告)号：US4198510A
公开(公告)日：1980-04-15
申请号：US922524
申请日：1978-07-07
申请人： Takayuki Shioiri , Nobutaka Kawai , Masatoshi Ban
发明人： Takayuki Shioiri , Nobutaka Kawai , Masatoshi Ban
IPC分类号： C07C45/46 , C07C49/76 , C07C51/00 , C07D295/02 , C07D295/03 , C07D295/073 , C07D295/096 , C07D295/112 , C07D307/91 , C07F9/572 , C07F9/59 , C07F9/6533 , C07F9/24
CPC分类号： C07D295/03 , C07C45/46 , C07C49/76 , C07C51/00 , C07D295/073 , C07D295/096 , C07D295/112 , C07D307/91 , C07F9/5721 , C07F9/591 , C07F9/6533
摘要： A process for the preparation of carboxylic acids represented by a formula ##STR1## wherein R.sub.1 represents hydrogen atom or a lower alkyl radical, R.sub.2 represents hydrogen atom, lower alkyl or allyl radical and R.sub.3 represents phenyl, substituted phenyl, substituted naphthyl, dibenzofuranyl or substituted biphenyl. Following novel enamine and amidine compounds as intermediates for manufacturing the carboxylic acids and processes for the manufacture of said enamine and amidine compounds ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 represent the meanings as referred to and R.sub.4 represents dimethylamino, pyrrolidyl, piperidyl or morpholyl.
摘要翻译：其中R1代表氢原子或低级烷基，R2代表氢原子，低级烷基或烯丙基，R3代表苯基，取代苯基，取代萘基，二苯并呋喃基或取代的联苯。以下新颖的烯胺和脒化合物作为制备羧酸的中间体以及制备所述烯胺和脒化合物的方法，其中R1，R2和R3代表所指的含义，R 4代表二甲基氨基，吡咯烷基，哌啶基或吗啉基。

44. 发明授权

US4168153A Cycloalkanecarboxanilide derivative herbicides 失效
标题翻译：环烷基甲酰苯胺衍生物除草剂
公开(公告)号：US4168153A
公开(公告)日：1979-09-18
申请号：US876594
申请日：1978-02-10
申请人： Kurt H. G. Pilgram , Richard D. Skiles
发明人： Kurt H. G. Pilgram , Richard D. Skiles
IPC分类号： A01N37/22 , A01N37/36 , A01N37/44 , A01N39/00 , A01N41/06 , A01N41/10 , A01N51/00 , A01N53/00 , C07C43/205 , C07D211/26 , C07D295/073 , C07D295/135 , C07C103/19 , A01N9/12 , A01N9/14 , A01N9/20
CPC分类号： C07D295/073 , A01N37/22 , A01N37/36 , A01N37/44 , A01N39/00 , A01N41/06 , A01N41/10 , A01N51/00 , A01N53/00 , C07C309/00 , C07C323/00 , C07C43/205 , C07D211/26 , C07D295/135
摘要： Certain cycloalkanecarboxanilide derivatives are useful as herbicides.
摘要翻译：某些环烷烃甲酰苯胺衍生物可用作除草剂。

45. 发明授权

US4140775A Piperazino methyl phenyl aminoquinolines 失效
标题翻译：哌嗪基甲基苯基氨基喹啉
公开(公告)号：US4140775A
公开(公告)日：1979-02-20
申请号：US903199
申请日：1978-05-05
申请人： John M. McCall
发明人： John M. McCall
IPC分类号： A61K31/495 , A61P9/12 , C07D215/44 , C07D295/073 , C07D295/096 , C07D295/135 , C07D295/12
CPC分类号： C07D295/073 , C07D215/44 , C07D295/096 , C07D295/135
摘要： Antihypertensive compounds of the formula III ##STR1## wherein X is chloro or trifluoromethyl; wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is phenyl or phenyl substituted with one or two alkyl, alkoxy, trifluoromethyl or halo substituents, in which alkyl and alkoxy are each of 1 to 3 carbon atoms, inclusive, and halo is fluoro, chloro or bromo, are prepared by reacting a 4-chloro-7-substituted quinoline of formula I with a compound of the formula II ##STR2## wherein R and R.sub.1 are defined as above. The pharmacologically acceptable acid addition salts of compounds of formula III can also be used as antihypertensive agents.
摘要翻译：式III的抗高血压化合物其中X是氯或三氟甲基; 其中R是氢或含有1至3个碳原子的烷基; 其中R1是苯基或被一个或两个烷基，烷氧基，三氟甲基或卤素取代基取代的苯基，其中烷基和烷氧基各自为1-3个碳原子，包括端基，卤素是氟，氯或溴，是通过使具有式II化合物的式I的4-氯-7-取代喹啉其中R和R 1如上定义。式III化合物的药学上可接受的酸加成盐也可以用作抗高血压药。

46. 发明授权

US4125612A N-1-(p-Biphenylalkyl)piperazines and their use as anti-inflammatory agents 失效
标题翻译： N-1-（对联苯基烷基）哌嗪及其作为抗炎剂的用途
公开(公告)号：US4125612A
公开(公告)日：1978-11-14
申请号：US807846
申请日：1977-06-20
申请人： Margaret H. Sherlock
发明人： Margaret H. Sherlock
IPC分类号： C07C29/40 , C07C45/46 , C07C49/813 , C07C309/66 , C07D295/073 , C07D295/088 , C07D295/185 , C07D295/205 , A61K31/495 , C07D295/08 , C07D295/14 , C07D295/18
CPC分类号： C07D295/185 , C07C29/40 , C07C309/66 , C07C45/46 , C07C49/813 , C07D295/073 , C07D295/088 , C07D295/205 , Y10S514/825
摘要： This invention relates to N-1(p-biphenylalkyl) piperazines, to the processes for making such compounds and to the use of such compounds as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis.
摘要翻译：本发明涉及N-1（对联苯基烷基）哌嗪，涉及制备这些化合物的方法以及使用这类化合物作为抗炎剂，特别可用于治疗类风湿性关节炎。

47. 发明授权

US4049422A Herbicidal morpholinobenzimidazoles 失效
标题翻译：除草剂吗啉代苯并咪唑
公开(公告)号：US4049422A
公开(公告)日：1977-09-20
申请号：US671452
申请日：1976-03-29
申请人： Kelvin Kei-Wei Shen , Wayne Stuart Belles
发明人： Kelvin Kei-Wei Shen , Wayne Stuart Belles
IPC分类号： A01N43/52 , A01N43/90 , C07D295/073 , C07D295/135 , C07D498/04 , A01N9/22
CPC分类号： C07D295/073 , A01N43/90 , C07D295/135
摘要： Tricyclic 1,2-morpholinobenzimidazoles having a haloalkyl, alkylsulfonyl, haloalkylsulfonyl, halo or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The aromatic ring and morpholino ring may also have other substituents. The compounds are herbicidal, useful as pre-emergence or post-emergence treatments.
摘要翻译：在吗啉代氮对位的芳环上具有卤代烷基，烷基磺酰基，卤代烷基磺酰基，卤代或低级烷基取代基的三环1,2-吗啉代苯并咪唑。芳环和吗啉环也可以具有其它取代基。这些化合物是除草剂，可用作出苗前或出苗后处理。

48. 发明授权

US3960961A 4'-Fluoro-4-{[4-(phenyl)cyclohexyl]amino}butyrophenones and the salts thereof 失效
标题翻译： 4 {40-氟-4- {55 {8 4-（苯基）环己基{9氨基{56丁基苯及其盐
公开(公告)号：US3960961A
公开(公告)日：1976-06-01
申请号：US329044
申请日：1973-02-02
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07C45/29 , C07C45/62 , C07C45/66 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07D295/073 , C07C97/10
CPC分类号： C07D295/073 , C07C247/00 , C07C45/292 , C07C45/62 , C07C45/66 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747
摘要： This invention relates to novel 4-phenylcyclohexylamines embraced by the formula ##SPC1##Wherein .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof; R is selected from the group consisting of alkyl of from one through four carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, nitro and alkoxy of from one through four carbon atoms; R' and R.sup.1 are selected from the group consisting of hydrogen and alkyl of from one through four carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, alkyl of from one through four carbon atoms, alkanoyl of from one through three carbon atoms, alkylsulfonyl of from one through three carbon atoms, arylsulfonyl of from six through ten carbon atoms, alkylcarbamoyl wherein alkyl is from one through four carbon atoms, alkoxycarbonyl wherein alkyl is from one through four carbon atoms, ring monosubstituted aroylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms and bis (ring monosubstituted) arylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms; R.sup.1 and R.sup.2 when taken together with --N
摘要翻译：本发明涉及以下式所表示的新型4-苯基环己胺：其中差异是一般性表达式，其特征在于其独特的化学反应和其混合物及其混合物; R选自1至4个碳原子的烷基，1至4个碳原子的氟，氯，溴，三氟甲基，硝基和烷氧基; R'和R 1选自氢和一至四个碳原子的烷基; R2选自氢，一至四个碳原子的烷基，一至三个碳原子的烷酰基，一至三个碳原子的烷基磺酰基，六至十个碳原子的芳基磺酰基，其中烷基是一个至四个碳原子，其中烷基是一个至四个碳原子的烷氧基羰基，其中取代基具有与上述R相同的含义的环单取代的芳酰基烷基，芳基是六至十个碳原子，烷基是一至六个碳原子和双（环单取代）芳烷基，其中取代基具有与上述R相同的含义，芳基为6至10个碳原子，烷基为1至6个碳原子; R 1和R 2与-N'一起是选自未取代的和单取代的吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代和哌嗪基的饱和杂环氨基; 及其酸加成盐。它还涉及制备上述新化合物（1）的中间体和方法及其新颖的衍生物。新化合物（1）对人和动物的全身给药抑制其中枢神经系统。

49. 发明授权

US3917703A 4-(Aminoalkylamino)-2-halobenzyl lower-alkyl ethers 失效
标题翻译： 4-（氨基烷基氨基）-2-卤代苄基低级烷基醚
公开(公告)号：US3917703A
公开(公告)日：1975-11-04
申请号：US45350274
申请日：1974-03-21
申请人： STERLING DRUG INC
发明人： ARCHER SYDNEY , ROSI DAVID
IPC分类号： C07D295/073 , C07D295/096 , C07D295/112 , C07C87/48
CPC分类号： C07D295/073 , C07D295/096 , C07D295/112 , Y10S435/913
摘要： 4-(Amino-(polycarbon-lower-alkyl)-amino)-2-halobenzyl alcohols and lower-alkyl ethers thereof have schistosomacidal activity. The benzyl alcohols are prepared: by reduction of the corresponding benzaldehydes or lower-alkyl benzoates; by microbiological oxidation of the corresponding 4-substitutedamino-2-halotoluenes; or, for the compounds where polycarbonlower-alkyl is ethylene, by reducing the corresponding loweralkyl 4-(aminoacetylamino)-2-halobenzoates or by reducing the corresponding 4-(aminoacetylamino)-2-halobenzyl alcohols. The ethers are prepared by heating the benzyl alcohols with a loweralkanol in the presence of an acid.
摘要翻译： 4- [氨基 - （聚碳 - 低级 - 烷基） - 氨基] -2-卤代苄醇及其低级烷基醚具有血吸虫活性。制备苄醇：通过还原相应的苯甲醛或苯甲酸低级烷基酯; 通过相应的4-取代 - 氨基-2-卤代甲苯的微生物氧化; 或通过还原相应的4-（氨基乙酰基氨基）-2-卤代苯甲酸的低级烷基酯或通过还原相应的4-（氨基乙酰基氨基）-2-卤代苄醇，对于聚碳 - 低级 - 烷基是亚乙基的化合物。醚通过在酸存在下用低级链烷醇加热苄醇来制备。

50. 发明授权

US3901889A 1,2-bis-(4-phenyl-1-piperazinyl)-ethanes 失效
标题翻译： 1,2-BIS-（4-苯基-1-哌嗪基）-ETHANES
公开(公告)号：US3901889A
公开(公告)日：1975-08-26
申请号：US36432873
申请日：1973-05-29
申请人： BOUCHARA EMILE
发明人： BOUCHARA EMILE
IPC分类号： C07D295/06 , A61K31/495 , A61P3/06 , A61P25/04 , A61P29/00 , C07D295/073 , C07D295/12
CPC分类号： C07D295/073
摘要： This invention relates to therapeutically useful 1,2-bis-(4phenyl-1-piperazinyl)-ethane derivatives having the formula:

IN WHICH R1 and R2 represent independently from each other a radical selected from the halogens, the trifluoromethyl radical and the lower alkyl radicals.

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