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21. 发明授权

US4400384A 5-o-Cyanobenzyl-4,5,6,7-tetrahydrothieno [3,2-c] pyridine methanesulfonate and other novel salts thereof 失效
标题翻译： 5'-氰基苄基-4,5,6,7-四氢噻吩并[3,2-c]吡啶甲磺酸盐及其它新的盐
公开(公告)号：US4400384A
公开(公告)日：1983-08-23
申请号：US193906
申请日：1980-10-06
申请人： Armand Amselem , Fernand Eloy , Jean-Pierre Maffrand
发明人： Armand Amselem , Fernand Eloy , Jean-Pierre Maffrand
IPC分类号： C07D495/04 , C07D513/04 , A61K31/44
CPC分类号： C07D495/04 , Y10S514/821
摘要： The invention concerns novel 5-o-cyanobenzyl-4, 5, 6, 7-tetrahydrothieno-[3,2-c] pyridine acid addition salts having inhibitory action against blood platelet aggregation without anti-inflammatory activity, and the compositions and methods of use therefor.
摘要翻译：本发明涉及对没有抗炎活性的血小板聚集具有抑制作用的新的5-邻氰基苄基-4,5,6,7-四氢噻吩并[3,2-c]吡啶酸加成盐，以及其组合物和方法用于此。

22. 发明授权

US4107437A 2,3-Dihydrobenzofurans 失效
标题翻译： 2,3-二氢苯并呋喃
公开(公告)号：US4107437A
公开(公告)日：1978-08-15
申请号：US792504
申请日：1977-05-02
申请人： Jean-Pierre Maffrand , Jean-Marie Pereillo
发明人： Jean-Pierre Maffrand , Jean-Marie Pereillo
IPC分类号： A61K31/34 , A61K31/343 , A61K31/40 , A61K31/495 , A61K31/535 , A61P9/06 , A61P25/20 , C07D307/80 , C07D405/12
CPC分类号： C07D307/80 , Y10S514/821
摘要： 2,3-Dihydrobenzofuran of formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, a lower alkyl or lower phenylalkyl or form, together with the nitrogen atom to which they are attached, a 4 to 8-membered saturated heterocyclic ring having 3 to 7 cyclic carbon atoms, a 4 to 8-membered saturated heterocyclic ring having 2 to 6 cyclic carbon atoms and two heteroatoms one of which is said nitrogen atom and the other is an oxygen atom, a sulphur atom or another nitrogen atom, said other nitrogen atom being optionally substituted by a phenyl, halophenyl, trifluromethylphenyl, lower alkylphenyl or lower alkoxyphenyl; n is 2 or 3, and the salts thereof.
摘要翻译： 2,3-二氢苯并呋喃，其结构式如下：其中R 1和R 2各自独立地为低级烷基或低级苯基烷基或与其连接的氮原子一起形成4至8元饱和的具有3至7个环状碳原子的杂环，具有2至6个环状碳原子的4至8元饱和杂环和2个杂原子，其中一个为所述氮原子，另一个为氧原子，硫原子或其它氮所述其它氮原子任选被苯基，卤代苯基，三氟甲基苯基，低级烷基苯基或低级烷氧基苯基取代; n为2或3，及其盐。

23. 发明授权

US4065459A Process for the preparation of thieno(3,2-c) pyridine and derivatives thereof 失效
标题翻译：噻吩并（3,2-c）吡啶及其衍生物的制备方法
公开(公告)号：US4065459A
公开(公告)日：1977-12-27
申请号：US655966
申请日：1976-02-06
申请人： Alan Heymes , Jean-Pierre Maffrand
发明人： Alan Heymes , Jean-Pierre Maffrand
IPC分类号： C07D513/04 , A61K20060101 , A61K31/425 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D495/04 , C07D501/00 , C07D501/04 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/56 , C07D501/60 , C07D519/06 , C07D283/00
CPC分类号： C07D495/04 , C07D501/20
摘要： This invention relates to a process for the preparation of compounds having the formula: ##STR1## in which R.sub.1 is H or lower alkyl and R.sub.2 is H or lower alkyl, or phenyl or benzyl optionally substituted with at least one halogen or a lower alkyl, lower alkoxy, trifluoromethyl or nitro group.According to this method, a compound of the formula: ##STR2## in which R.sub.1 and R.sub.2 are as defined above and R.sub.3 is H or optionally substituted alkyl or benzyl, is reacted with a derivative Hal--SO.sub.2 --R (III) in which Hal is halogen and R is optionally substituted alkyl, aryl or aralkyl, to give a derivative of the formula: ##STR3## in which the various symbols have the above-defined meanings, and the sulfonated derivative of the formula (IV) is heated in the presence of an acid, to give the compound of the formula (I).
摘要翻译：本发明涉及一种制备具有下式的化合物的方法：其中R 1为H或低级烷基且R 2为H或低级烷基，或任选被至少一个卤素取代的苯基或苄基，低级烷基，低级烷氧基，三氟甲基或硝基。

24. 发明授权

US4424356A Process for the preparation of 5,6,7,7a-tetrahydro-4H-thieno-�3,2,-c!pyridin-2-one 失效
标题翻译： 5,6,7,7a-四氢-4H-噻吩并[3,2-a]吡啶-2-酮的制备方法
公开(公告)号：US4424356A
公开(公告)日：1984-01-03
申请号：US325795
申请日：1981-11-30
申请人： Jean-Pierre Maffrand , Norio Suzuki , Kynichi Matsubayashi , Shinichiro Ashida
发明人： Jean-Pierre Maffrand , Norio Suzuki , Kynichi Matsubayashi , Shinichiro Ashida
IPC分类号： C07D495/00 , A61K31/381 , A61P7/02 , C07D211/74 , C07D495/04 , C07D513/04
CPC分类号： C07D495/04 , C07D211/74
摘要： The present invention provides a process for the preparation of 5,6,7,7a-tetrahydro-4H-pyridin-2-one derivatives of the general formula: ##STR1## in which R is a hydrogen atom or a phenyl radical optionally substituted by at least one halogen atom, lower alkyl radical, lower alkoxy radical, nitro group, carboxy group, alkoxycarbonyl radical or cyano group; R' is a hydrogen atom or a lower alkyl radical and n is 0, 1, 2, 3 or 4; and of their addition salts with mineral or organic acids, wherein a compound of the general formula: ##STR2## in which R, R' and n have the same meanings as above and R" is a hydrogen atom or an alkyl radical containing up to 4 carbon atoms, is treated in an organic solvent with gaseous hydrogen choloride and gaseous hydrogen sulphide. The compounds have platelet anti-aggregant and anti-thrombotic properties.
摘要翻译：本发明提供了制备通式如下的5,6,7,7a-四氢-4H-吡啶-2-酮衍生物的方法：其中R是氢原子或苯基任选被至少一个卤素原子，低级烷基，低级烷氧基，硝基，羧基，烷氧基羰基或氰基取代; R'是氢原子或低级烷基，n是0,1,2,3或4; 和其与矿物或有机酸的加成盐，其中通式为：其中R，R'和n具有与上述相同的含义的化合物，其中R“是氢原子或烷基含有最多4个碳原子的基团在有机溶剂中用气态氢氯化物和气态硫化氢处理。该化合物具有血小板抗聚集和抗血栓形成特性。

25. 发明授权

US4193997A Thieno[2,3-c] and [3,2-c]pyridines, process for their preparation and therapeutic applications thereof 失效
标题翻译：噻吩并[2,3-c]和[3,2-c]吡啶，其制备方法及其治疗应用
公开(公告)号：US4193997A
公开(公告)日：1980-03-18
申请号：US886688
申请日：1978-03-15
申请人： Robert Boigegrain , Michel Gachon , Jean-Pierre Maffrand , Gerard Maire
发明人： Robert Boigegrain , Michel Gachon , Jean-Pierre Maffrand , Gerard Maire
IPC分类号： A61K31/435 , A61K31/4365 , A61P7/02 , A61P25/04 , A61P29/00 , C07D495/04 , C07D471/04
CPC分类号： C07D495/04
摘要： This invention relates to compounds having the formulae ##STR1## in which: R.sup.1 represents hydrogen, a halogen atom or a lower alkyl radical, a lower alkoxy radical or a lower alkylthio radical;R.sup.2 represents hydrogen or a lower alkyl, aralkyl, aryl, carboxy or alkoxycarbonyl radical;R.sup.3 represents hydrogen, a C.sub.1-12 alkyl radical, or an aralkyl or aryl radical, optionally substituted on the aromatic nucleus with one or more halogen atoms or hydroxy, nitro, cyano, carboxamido, carboxy, alkoxycarbonyl, lower alkyl, lower alkoxy or trifluoromethyl groups; andn is zero or 1.Said new compounds possess therapeutically useful blood-platelet aggregation inhibiting properties and also anti-thrombotic, anti-sludge, antalgic and anti-inflammatory properties.
摘要翻译：本发明涉及具有下式的化合物：其中：R 1表示氢，卤原子或低级烷基，低级烷氧基或低级烷硫基; R 2表示氢或低级烷基，芳烷基，芳基，羧基或烷氧基羰基; R 3表示氢，C 1-12烷基或芳烷基或芳基，任选地在芳族核上被一个或多个卤素原子取代，或羟基，硝基，氰基，甲酰氨基，羧基，烷氧基羰基，低级烷基，低级烷氧基或三氟甲基团体并且n为零或1.所述新化合物具有治疗上有用的血小板聚集抑制性质以及抗血栓形成，抗污泥，止痛和抗炎特性。

26. 发明授权

US4163852A Process for the preparation of tetrahydro-thieno[3,2-c]- and [2,3-c]pyridine derivatives 失效
标题翻译：制备四氢噻吩并[8,2-c {9 - 和{8,2,3- C {9吡啶衍生物）的方法
公开(公告)号：US4163852A
公开(公告)日：1979-08-07
申请号：US860188
申请日：1977-12-13
申请人： Gerard Ferrand , Jean-Pierre Maffrand
发明人： Gerard Ferrand , Jean-Pierre Maffrand
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , Y10S514/822
摘要： This invention relates to a process for the preparation of tetrahydro-thieno[3,2-c]pyridine derivatives of the formula ##STR1## AND THEIR ISOMERIC TETRAHYDRO-THIENO[2,3-C]PYRIDINE DERIVATIVES IN WHICH R.sub.1 represents hydrogen, a lower alkyl or alkoxy radical, an aryl radical or an aralkyl radical; R.sub.2 and R.sub.3 represent hydrogen, halogen, a lower alkyl or alkoxy group, a di(loweralkyl)amino, nitro, cyano or acetamido group or, together with the phenyl nucleus to which they are attached, form a polycyclic aromatic ring, comprising reacting a tetrahydrothieno[3,2-c]pyridine derivative of the formula: ##STR2## OR A DERIVATIVE OF ITS ISOMER, TETRAHYDRO[2,3-C]PYRIDINE, WITH FORMALDEHYDE H-CHO and a phenol of the formula: ##STR3##
摘要翻译：本发明涉及制备式（Ia）的四氢噻吩并[3,2-c]吡啶衍生物及其异构四氢 - 噻吩并[2,3-C]吡啶衍生物的方法，其中R 1表示氢，低级烷基或烷氧基，芳基或芳烷基; R 2和R 3表示氢，卤素，低级烷基或烷氧基，二（低级烷基）氨基，硝基，氰基或乙酰氨基，或与它们所连接的苯基一起形成多环芳环，包括使（IIa）的四氢噻吩并[3,2-c]吡啶衍生物或其异构体衍生物，四氢呋喃并[2,3-C]吡啶与甲醛H-CHO和下式的苯酚：（III）。

27. 发明授权

US4075340A Thieno [2,3-C] pyridine derivatives and therapeutic composition containing same 失效
标题翻译：噻吩并[8,2,3- C {9 {0吡啶衍生物和含有其的治疗组合物
公开(公告)号：US4075340A
公开(公告)日：1978-02-21
申请号：US692186
申请日：1976-06-02
申请人： Jean-Pierre Maffrand
发明人： Jean-Pierre Maffrand
IPC分类号： A61K31/435 , A61K31/4365 , A61P7/02 , A61P9/06 , A61P29/00 , C07D495/04 , A61K31/54 , C07D417/04
CPC分类号： C07D495/04 , Y10S514/821
摘要： This invention relates to derivatives having the formula: ##STR1## in which R.sub.1 is hydrogen or alkyl having 1-6 carbon atoms; X is (CHR.sub.2).sub.m in which m is an integer from 2 to 15, or (CHR.sub.2).sub.n R.sub.3 in which n is an integer from 1 to 15, R.sub.2 is hydrogen, or a hydroxy, acyloxy or alkyl group having 1-6 carbon atoms, and the various symbols R.sub.2 may have different meanings in each radical (CHR.sub.2) when several radicals (CHR.sub.2) are present, R.sub.3 is a trichloromethyl, acetyl, carboxy or alkoxycarbonyl group, or a phenyl, phenoxy, benzoyl, thienyl or pyridyl radical optionally substituted with at least a halogen atom, or a hydroxy, nitro, amino, cyano, carboxy, alkyloxycarbonyl, alkyl having 1-6 carbon atoms, alkoxy having 1-6 carbon atoms or methylenedioxy group, and to the acid addition salts of the derivatives of the formula (I).Said derivatives have useful anti-inflammatory and anti-arrhythmic activities and an inhibiting action on blood platelet aggregation.
摘要翻译：本发明涉及具有下式的衍生物：其中R 1是氢或具有1-6个碳原子的烷基; X为（CHR2）m，其中m为2至15的整数，或（CHR2）nR3，其中n为1至15的整数，R2为氢或羟基，酰氧基或具有1-6碳的烷基当存在几个基团（CHR 2）时，各个符号R 2可以在每个基团（CHR 2）中具有不同的含义，R 3是三氯甲基，乙酰基，羧基或烷氧基羰基，或苯基，苯氧基，苯甲酰基，噻吩基或吡啶基任选被至少一个卤素原子取代的羟基，硝基，氨基，氰基，羧基，烷氧基羰基，具有1-6个碳原子的烷基，具有1-6个碳原子的烷氧基或亚甲二氧基，式（I）的衍生物。

28. 发明授权

US09120819B2 FGF-receptor agonist dimeric compounds 有权
标题翻译： FGF受体激动剂二聚化合物
公开(公告)号：US09120819B2
公开(公告)日：2015-09-01
申请号：US12171373
申请日：2008-07-11
申请人： Francoise Bono , Nathalie Guillo , Jean-Pierre Maffrand , Pierre Fons , Jacob-Alsboek Olsen , Gilles Anne-Archard
发明人： Francoise Bono , Nathalie Guillo , Jean-Pierre Maffrand , Pierre Fons , Jacob-Alsboek Olsen , Gilles Anne-Archard
IPC分类号： C07D519/00 , C07D209/02 , A61K31/435 , C07D221/02 , A61K47/48
CPC分类号： C07D519/00 , A61K31/435 , A61K47/55 , C07D209/02 , C07D221/02
摘要： FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 are disclosed in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group, wherein the monomer unit is of the general formula I.
摘要翻译：公开了对应于通式M1-L-M2的FGF受体激动剂化合物，其中M1和M2可以相同或不同，各自独立地表示单体单元M，L表示连接基团，其中单体单元具有通式I。

29. 发明授权

US4529596A Thieno [3,2-c] pyridine derivatives and their therapeutic application 失效
标题翻译：噻吩并[3,2-c]吡啶衍生物及其治疗应用
公开(公告)号：US4529596A
公开(公告)日：1985-07-16
申请号：US510582
申请日：1983-07-05
申请人： Daniel Aubert , Claude Ferrand , Jean-Pierre Maffrand
发明人： Daniel Aubert , Claude Ferrand , Jean-Pierre Maffrand
IPC分类号： A61K31/435 , A61P7/02 , C07D495/04
CPC分类号： C07D495/04
摘要： This invention relates to new thieno [3,2-c] pyridine derivatives having the formula: ##STR1## in which: Y represents the OH group or an OR group in which R is a straight or branched lower alkyl radical, or Y represents a group ##STR2## in which R.sub.1 and R.sub.2 are each independently of each other, hydrogen or a straight or branched lower alkyl group; or R.sub.1 and R.sub.2 form together and with the nitrogen atom to which they are attached a heterocycle which may include a second heteroatom such as oxygen or nitrogen, wherein the latter may be substituted by a lower alkyl or benzyl radical which may be substituted; and X represents hydrogen, a halogen or a lower alkyl radical; and their addition salts with pharmaceutically acceptable mineral or organic acids if Y represents the group OR or ##STR3## or with mineral bases if Y represents OH, as well as the two enantiomers or their mixture.The invention also relates to the preparation process of new thieno [3,2-c] pyridine derivatives and to their therapeutic application as blood-platelet aggregation inhibiting agents and antithrombotics.
摘要翻译：本发明涉及具有下式的新的噻吩并[3,2-c]吡啶衍生物：其中：Y表示OH基或OR基，其中R是直链或支链低级烷基，或 Y表示其中R 1和R 2各自独立地为氢或直链或支链低级烷基的基团或者R 1和R 2与它们所连接的氮原子一起形成杂环，其可以包括第二杂原子如氧或氮，其中后者可以被可被取代的低级烷基或苄基取代; X表示氢，卤素或低级烷基; 如果Y代表基团OR或或者与Y表示OH的矿物碱，以及它们的两种对映异构体或它们的混合物，则它们与药学上可接受的矿物或有机酸的加成盐。本发明还涉及新的噻吩并[3,2-c]吡啶衍生物的制备方法及其作为血小板聚集抑制剂和抗血栓形成剂的治疗应用。

30. 发明授权

US4515951A Preparation of 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one compounds 失效
标题翻译： 5,6,7,7a-四氢-4H-噻吩并[3,2-c]吡啶-2-酮化合物的制备
公开(公告)号：US4515951A
公开(公告)日：1985-05-07
申请号：US635461
申请日：1984-07-25
申请人： Robert Boigegrain , Jean-Pierre Maffrand , Norio Suzuki , Kynichi Matsubayachi , Shinichiro Ashida
发明人： Robert Boigegrain , Jean-Pierre Maffrand , Norio Suzuki , Kynichi Matsubayachi , Shinichiro Ashida
IPC分类号： C07D495/00 , A61K31/381 , A61K31/435 , A61P7/02 , C07D495/04 , C07F5/02 , C07F7/10
CPC分类号： C07D495/04 , C07F5/025 , C07F7/10
摘要： The present invention provides derivatives of 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridin-2-one of the general formula: ##STR1## in which R is a hydrogen atom or a phenyl radical, which is optionally substituted by at least one halogen atom or lower alkyl radical, lower alkoxy radical, nitro group, carboxyl group, alkoxycarbonyl radical or cyano group, R' is a hydrogen atom or a lower alkyl radical and n is 0, 1, 2, 3, or 4; and the addition salts thereof with pharmaceutically acceptable mineral or organic acids.The present invention also provides a process for the preparation of these compounds, as well as pharmaceutical compositions containing them.
摘要翻译：本发明提供了通式如下的5,6,7,7a-四氢-4H-噻吩并[3,2-c]吡啶-2-酮的衍生物：其中R是氢原子或苯基，其任选被至少一个卤素原子或低级烷基取代，低级烷氧基，硝基，羧基，烷氧基羰基或氰基，R'是氢原子或低级烷基，n是0 ，1，2，3或4; 和其与药学上可接受的矿物或有机酸的加成盐。本发明还提供了制备这些化合物的方法以及含有它们的药物组合物。

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