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1. 发明授权

US5049559A Thieno-triazolo-diazepine derivatives useful as anti-ischemic agents 失效
标题翻译：可用作抗缺血剂的噻吩并三唑并二氮杂衍生物
公开(公告)号：US5049559A
公开(公告)日：1991-09-17
申请号：US522235
申请日：1990-05-11
申请人： Pierre Braquet , Andre Esanu , Jean-Pierre Laurent , Jacques Pommier
发明人： Pierre Braquet , Andre Esanu , Jean-Pierre Laurent , Jacques Pommier
IPC分类号： A61K31/55 , A61P7/02 , C07D495/22
CPC分类号： C07D495/22
摘要： The invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting in the treatment of ischemia.
摘要翻译：本发明涉及式IMA的噻吩并三唑并二氮杂衍生物，其中Y代表氧或硫，R代表各种取代基，所述化合物的制备方法以及含有该取代基的治疗组合物。该化合物在治疗缺血方面特别有意义。

2. 发明授权

US5492906A Derivatives of thieno-triazolo-diazepine and therapeutic compositions containing them 失效
标题翻译：噻吩并三唑并二氮杂的衍生物和含有它们的治疗组合物
公开(公告)号：US5492906A
公开(公告)日：1996-02-20
申请号：US837580
申请日：1992-02-18
申请人： Pierre Braquet , Andre Esanu , Jean-Pierre Laurent , Alain Rolland
发明人： Pierre Braquet , Andre Esanu , Jean-Pierre Laurent , Alain Rolland
IPC分类号： A61K31/55 , A61P1/00 , A61P11/00 , A61P11/08 , A61P37/08 , C07D495/22
CPC分类号： C07D495/22
摘要： The invention relates to thieno-triazolo-diazepine derivatives of the formula: ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-asthmatic, anti-allergic and gastro-intestinal protectors.
摘要翻译：本发明涉及下式的噻吩并三氮唑并二氮杂衍生物：其中Y代表氧或硫，R代表各种取代基，所述化合物的制备方法和含有它们的治疗组合物。这些化合物作为抗哮喘，抗过敏和胃肠保护剂是特别有趣的。

3. 发明授权

US5049560A Sulfonyl derivatives of thieno-triazolo-diazepines useful as anti-PAF and anti-ischemic agents 失效
标题翻译：噻吩并三唑并二氮杂的磺酰基衍生物可用作抗PAF和抗缺血剂
公开(公告)号：US5049560A
公开(公告)日：1991-09-17
申请号：US496410
申请日：1990-03-20
申请人： Andre Esanu , Pierre Braquet , Christiane Martin , Jean-Pierre Laurent
发明人： Andre Esanu , Pierre Braquet , Christiane Martin , Jean-Pierre Laurent
IPC分类号： C07D495/04 , A61K31/55 , A61P7/02 , C07D495/14 , C07D495/22
CPC分类号： C07D495/22
摘要： This invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein R represents various substituents, to a preparation process of these compounds consisting in reacting the thieno-triazolo-diazepine compound of the formula ##STR2## on RSO.sub.2 Cl and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-PAF and anti-ischemic agents.
摘要翻译：本发明涉及通式为“IMAGE”的噻吩并三唑并二氮杂衍生物，其中R代表各种取代基，这些化合物的制备方法包括使式ⅩⅥ的噻吩并三唑并哒嗪化合物与RSO2Cl反应，含有其的治疗组合物。这些化合物作为抗PAF和抗缺血剂特别有意义。

4. 发明授权

US4904693A Octahydro indenofuran derivatives and their therapeutic compositions 失效
标题翻译：八氢吲哚呋喃衍生物及其治疗组合物
公开(公告)号：US4904693A
公开(公告)日：1990-02-27
申请号：US267438
申请日：1988-11-04
申请人： Pierre Braquet , Andre Esanu
发明人： Pierre Braquet , Andre Esanu
IPC分类号： C07D307/94 , A61K31/365 , A61P11/08 , A61P37/08 , C07D307/77 , C07D307/93
CPC分类号： C07D307/93
摘要： This invention relates to indenofuran derivatives of the formula: ##STR1## wherein R stands for H or for a ##STR2## group optionally substituted on the phenyl ring by Alk, OH or OAlk, Alk being a lower straight or branched alkyl group up to C.sub.5, to the preparation of these compounds and to therapeutic compositions containing the same in the field of anaphylaxis.
摘要翻译：本发明涉及下式的茚诺呋喃衍生物：其中R代表H或任选在苯环上被Alk，OH或OAlk取代的基团，Alk是直至C5的低级直链或支链烷基，涉及这些化合物的制备及其在过敏反应领域中含有该组合物的治疗组合物。

5. 发明授权

US5168098A Pyrrolo-pyridine derivatives and therapeutic compositions containing them 失效
标题翻译：吡咯并吡啶衍生物和含有它们的治疗组合物
公开(公告)号：US5168098A
公开(公告)日：1992-12-01
申请号：US708675
申请日：1991-05-31
申请人： Andre Esanu , Pierre Braquet
发明人： Andre Esanu , Pierre Braquet
IPC分类号： A61K31/435 , A61P37/08 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to pyrrolo-pyridine derivatives of the formula: ##STR1## wherein R represents a phenyl group, optionally substituted by one or more of various groups and therapeutically acceptable salts of these compounds, to a preparation process of the same comprising reacting, in an inert atmosphere and in a protic solvent, the 2-methyl 3-hydroxy 4,5-diboromomethyl pyridine, on a stoichiometric excess of the compound of the formula NH.sub.2 -R.The invention relates also to therapeutic compositions containing said derivatives as active ingredient.The compounds according to the invention have antiallergic activity.
摘要翻译：本发明涉及下式吡咯并吡啶衍生物：其中R表示苯基，任选被一种或多种各种基团和这些化合物的可治疗可接受的盐取代，其制备方法包括在惰性气氛和质子溶剂中，在化学计量过量的式NH 2 -R的化合物上使2-甲基3-羟基4,5-二溴甲基吡啶反应。本发明还涉及含有所述衍生物作为活性成分的治疗组合物。根据本发明的化合物具有抗过敏活性。

6. 发明授权

US5047537A Separation of isomers of furo (3,4-C) pyridine derivatives 失效
标题翻译：分离呋喃（3,4-C）吡啶衍生物的异构体
公开(公告)号：US5047537A
公开(公告)日：1991-09-10
申请号：US598653
申请日：1990-10-18
申请人： Andre Esanu , Charles Eck
发明人： Andre Esanu , Charles Eck
IPC分类号： C07D491/04 , C07D491/048 , C07H17/00
CPC分类号： C07D491/04 , C07H17/00
摘要： This invention relates to a method for the separation of stereoisomers of 7-hydroxy-furo[3,4-c]pyridine derivatives of the formula ##STR1## wherein R.sub.3, R.sub.4 and R.sub.6 represent various substitutents, which comprises reacting a fully O-acetylated monosaccharide halogenide with a racemate of the selected 7-hydroxy-furo[3,4-c]pyridine derivative, to form the (+) and (-) (O-acetylated monosaccharide) (furo[3,4-c] pyridine 7-yl derivative) ethers, then separating the (+) and the (-) ethers by selective crystallization, in an hydroalcoholic medium, either of the acetylated forms or of the corresponding desacetylated forms and, finally, working up each of the separated derivatives by the usual routes. The compounds are known pharmaceuticals.
摘要翻译： PCT No.PCT / FR90 / 00228 Sec。 371 1990年10月18日第 102（e）1990年10月18日的PCT 1990年4月2日提交的PCT。本发明涉及分离下式的7-羟基 - 呋喃并[3,4-c]吡啶衍生物的立体异构体的方法：其中R3，R4和R6代表各种取代基，其包括使完全O-乙酰化的单糖卤化物与所选择的7-羟基 - 呋喃并[3,4-c]吡啶衍生物的外消旋体反应形成（+）和（ - ）（O-乙酰化单糖）（呋喃并[3,4-c]吡啶-7-基衍生物）醚，然后通过选择性结晶在水醇介质中分离（+）和（ - ）醚，任一种乙酰化形式或相应的去乙酰化形式，最后通过通常的路线处理每个分离的衍生物。这些化合物是已知的药物。

7. 发明授权

US4782068A New quinoline derivatives, their preparation and therapeutic compositions containing the same 失效
标题翻译：新喹啉衍生物，其制备方法和含有其的治疗组合物
公开(公告)号：US4782068A
公开(公告)日：1988-11-01
申请号：US22620
申请日：1987-03-04
申请人： Andre Esanu
发明人： Andre Esanu
IPC分类号： A61K31/47 , A61P31/04 , C07D215/56 , C07D405/06 , C07D215/18
CPC分类号： C07D405/06 , C07D215/56
摘要： The invention relates to new quinoline derivatives of the formula: ##STR1## wherein R stands for C.sub.2 H.sub.5, C.sub.2 H.sub.4 F, CH.sub.2 --O--CH.sub.2 --CH.sub.2 OH, ##STR2## to a process for their preparation comprising reacting, for 12-24 hours, at 70.degree.-95.degree. C., in dimethylformamide, the 1,4-dihydro- 3-ethoxycarbonyl- 6,8- difluoro-4-oxo-quinoline with an excess of RX (2-5 mol of RX for one mol of quinoline), in the presence of K.sub.2 CO.sub.3 and subsequently hydrolyzing the obtained 3-ester by HCl under reflux conditions and to pharmaceutical compositions comprising at least one 1,4-dihydro- 3-carboxy- 6,8-difluoro- 1-R-4-oxo-quinoline derivative in admixture with a pharmaceutically acceptable diluent or carrier.
摘要翻译：本发明涉及下式的新喹啉衍生物：其中R代表C 2 H 5，C 2 H 4 F，CH 2 -O-CH 2 -CH 2 OH，其中R 3代表其制备方法，包括使12 -24小时，在70℃-95℃，在二甲基甲酰胺中，将1,4-二氢-3-乙氧基羰基-6,8-二氟-4-氧代喹啉与过量的RX（2-5摩尔RX 对于一摩尔喹啉），在K 2 CO 3的存在下，然后在回流条件下用HCl将所得的3-酯水解，并包含至少一种1,4-二氢-3-羧基-6,8-二氟-1- -R-4-氧代 - 喹啉衍生物与药学上可接受的稀释剂或载体混合。

8. 发明授权

US4735950A Furo-(3,4-C)-pyridine derivatives and therapeutic composition containing the same 失效
标题翻译：呋喃 - （3,4-C） - 吡啶衍生物和含有它们的治疗组合物
公开(公告)号：US4735950A
公开(公告)日：1988-04-05
申请号：US32947
申请日：1987-03-30
申请人： Andre Esanu
发明人： Andre Esanu
IPC分类号： C07D491/04 , C07D491/048 , A61K31/44
CPC分类号： C07D491/04
摘要： This invention relates to 1,3-dihydro-6-methyl-7-hydroxy-furo-(3,4-c)-pyridine derivatives of the general formula I ##STR1## wherein each of A.sub.1 and A.sub.2 independently represents various hydrocarbon groups and therapeutically acceptable addition salts thereof; to a process for the preparation of the same comprising oxidizing the secondary alcohol .alpha..sup.4, 3-o-isopropylidene-1-methyl-5-(1-hydroxy-1-A.sub.1)-methyl pyridine by any usual technique, reacting the resultant ketone with a compound of the general formula XA.sub.2 wherein X stands for Br or I in the presence of magnesium in diethyl ether at the boil and treating the resultant tertiary alcohol with an acidic agent to provoke breaking of the isopropylidene ring and 3,4-cyclisation; and to pharmaceutical compositions containing these derivatives useful for example in diuresis.
摘要翻译：本发明涉及通式Ⅰ的1,3-二氢-6-甲基-7-羟基 - 呋喃 - （3,4-c） - 吡啶衍生物，其中A1和A2各自独立地表示各种烃基和其治疗上可接受的加成盐; 涉及其制备方法，包括用任何常规技术氧化仲醇α4,3-O-异丙叉-1-甲基-5-（1-羟基-1-A1） - 甲基吡啶，使所得酮与通式XA2的化合物，其中X代表Br或I，在镁存在下在乙醚中沸腾，并用酸性试剂处理所得叔醇以引发异亚丙基环的断裂和3,4-环化; 以及含有可用于例如利尿的这些衍生物的药物组合物。

9. 发明授权

US4681888A Thienopyridine derivatives and anti-thrombotic compositions containing the same 失效
标题翻译：噻吩并吡啶衍生物和含有它们的抗血栓形成组合物
公开(公告)号：US4681888A
公开(公告)日：1987-07-21
申请号：US894780
申请日：1986-08-08
申请人： Andre Esanu
发明人： Andre Esanu
IPC分类号： A61K31/435 , A61P3/00 , A61P3/14 , A61P7/02 , C07D495/04 , A61K31/44
CPC分类号： C07D495/04
摘要： This invention relates to new derivatives of 5-(.omega.-phenethylamino-alkyl) -4,5,6,7-tetrahydro-thieno-(3,2-c)-pyridine of the formula ##STR1## wherein n is an integer of from 2 to 5, R.sub.1 represents a hydrogen atom or a 3,4-dimethoxyphenyl group, R.sub.2 represents a hydrogen atom, an alkyl group having up to 4 carbon atoms or a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group and R.sub.3 represents two or three methoxy groups, to therapeutically acceptable salts thereof, to a process for the preparation of these derivatives comprising condensing a 5-(.omega.-chloroalkyl)-4,5,6,7- tetrahydro- thieno- (3,2-c)-pyridine with the appropriate phenethyl derivative at from 90.degree. to 130.degree. C. under nitrogen circulation and to therapeutic compositions containing said compounds.
摘要翻译：本发明涉及式（IMAGE）的5-（ω-苯乙基氨基 - 烷基）-4,5,6,7-四氢 - 噻吩并 - （3,2-c） - 吡啶的新衍生物，其中n是 2至5，R 1表示氢原子或3,4-二甲氧基苯基，R 2表示氢原子，具有至多4个碳原子的烷基或4-氰基-4-（3,4-二甲氧基苯基） - 5-甲基己基，R3代表两个或三个甲氧基，其代表其治疗上可接受的盐，涉及制备这些衍生物的方法，包括将5-（ω-氯代烷基）-4,5,6,7-四氢噻吩并 - （3,2-c） - 吡啶与适当的苯乙基衍生物在氮气循环下在90°至130℃下加入含有所述化合物的治疗组合物。

10. 发明授权

US4254162A Phenoxy acetic acid derivative, its preparation and therapeutic use 失效
标题翻译：苯氧乙酸衍生物，其制备及治疗用途
公开(公告)号：US4254162A
公开(公告)日：1981-03-03
申请号：US97037
申请日：1979-11-21
申请人： Andre Esanu
发明人： Andre Esanu
IPC分类号： A61K31/38 , A61K31/381 , A61P1/16 , C07D333/22 , C07D333/38
CPC分类号： C07D333/22
摘要： A therapeutic use for a phenoxy acetic acid is disclosed. The compound is effective as a choleretic agent and can be administered orally or intravenously.
摘要翻译：公开了苯氧基乙酸的治疗用途。该化合物作为胆固醇剂是有效的，可以口服或静脉内给药。

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