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1. 发明授权

US5025013A Benzopyran derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：苯并吡喃衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5025013A
公开(公告)日：1991-06-18
申请号：US465330
申请日：1990-01-16
申请人： Michel Barreau , Jean-Claude Hardy , Jean-Paul Martin , Christian Renault
发明人： Michel Barreau , Jean-Claude Hardy , Jean-Paul Martin , Christian Renault
IPC分类号： A61K31/35 , A61K31/352 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/47 , A61K31/495 , A61P9/06 , C07D311/58 , C07D311/70 , C07D405/06 , C07D405/12 , C07D405/14
CPC分类号： C07D405/06 , C07D311/58 , C07D405/12 , C07D405/14
摘要： New benzopyran derivatives of general formula (I) in which:R.sub.1 represents a hydrogen or halogen atom or a hydroxy, alkyloxy, nitro, amino, alkylsulphonamido or acylamino radical,R represents(1) radical ##STR1## R.sub.2 and R.sub.3, which may be identical or different, being H, halogen, OH, alkyl, alkyloxy, NH.sub.2, alkylsulphonamido or NO.sub.2, or(2) a radical ##STR2## n being 0 or 1, R.sub.4 being H, alkyl or optionally substituted phenyl and Q is acyl, alkylsulphonyl or ##STR3## Y being --CO-- or --SO.sub.2 -- and Z being a single bond, --CH.sub.2 -- or --NH--, or(3) a radical ##STR4## n being 0 or 1, m being 0 or 2, X being C or N (if n=0), W being a bond or --NH-- and AR being pyridyl, indolyl, quinolyl, 2-alkylquinolyl or phenyl optionally substituted with R.sub.2 and R.sub.3, provided that n=0 when X equals N, or(4) a radical of general formula: ##STR5## R.sub.7 being H or alkyl, or alternatively (5) a radical ##STR6## R' and R" are identical and represent hydrogen atoms or alkyl radicals, their isomeric forms and the mixtures thereof, and their addition salts with acids.These new products are useful as anti-arrhythmic and antifibrillating agents. ##STR7##
摘要翻译：新的通式（I）的苯并吡喃衍生物，其中：R 1表示氢或卤素原子或羟基，烷氧基，硝基，氨基，烷基磺酰胺基或酰基氨基，R表示（1）基团R 2和R 3，其可以是相同或不同的是H，卤素，OH，烷基，烷氧基，NH 2，烷基磺酰胺基或NO 2，或（2）基团n为0或1，R 4为H，烷基或任选取代的苯基，Q为酰基，烷基磺酰基或Y为-CO-或-SO 2 - ，Z为单键，-CH 2 - 或-NH-，或（3）基团n为0或1，m为0或2， X是C或N（如果n = 0），W是键或-NH-，并且AR是吡啶基，吲哚基，喹啉基，2-烷基喹啉基或任选被R 2和R 3取代的苯基，条件是当X等于N时，n = ，或（4）通式如下的基团：R7是H或烷基，或者（5）基团R'和R“相同并代表氢原子或烷基，它们的异构形式和其混合物， d它们与酸的加成盐。这些新产品可用作抗心律不齐和抗纤颤剂。（一）

2. 发明授权

US4994470A Benzopyran derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并吡喃衍生物和含有它们的药物组合物
公开(公告)号：US4994470A
公开(公告)日：1991-02-19
申请号：US465448
申请日：1990-01-16
申请人： Michel Barreau , Jean-Claude Hardy , Christian Renault
发明人： Michel Barreau , Jean-Claude Hardy , Christian Renault
IPC分类号： A61K31/443 , A61K31/445 , A61P9/06 , C07D405/06 , C07D405/14
CPC分类号： C07D405/06
摘要： New benzopyran derivatives of general formula (I) in which:R.sub.1 denotes a hydrogen or halogen atom or a hydroxy, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, or acylamino radical,R denotes a radical of general formula: ##STR1## in which A denotes a single bond or a methylene radical and R.sub.2 and R.sub.3 which may be identical or different, denote a hydrogen or halogen atom or a hydroxy, alkyl, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano radical, or form together, when they are adjacent, a methylenedioxy or ethylenedioxy radical, or alternatively R denotes a 2-oxo-2H-benzimidazolyl radical,and R' and R" are identical and denote hydrogen atoms or alkyl radicals, their isomeric forms and their preparation.These new products are useful as antiarrhythmic and antifibrillating agents. ##STR2##
摘要翻译：新的通式（I）的苯并吡喃衍生物，其中：R1表示氢或卤素原子或羟基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基或酰基氨基，R表示通式的基团： IMAGE>其中A表示单键或亚甲基，R 2和R 3可以相同或不同，表示氢或卤素原子或羟基，烷基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基，酰基氨基，氨磺酰基或氰基，或者当它们相邻时一起形成亚甲二氧基或亚乙二氧基，或者R表示2-氧代-2H-苯并咪唑基，R'和R“相同且表示氢原子或烷基，它们的异构形式及其制备方法。这些新产品可用作抗心律不齐和抗纤颤剂。（一）

3. 发明授权

US6057454A 1-oxo-1H-inden-2-yl-1H-imidazole-2-carboxylic acid intermediates 失效
标题翻译： 1-氧代-1H-茚-2-基-1H-咪唑-2-羧酸中间体
公开(公告)号：US6057454A
公开(公告)日：2000-05-02
申请号：US205689
申请日：1998-12-04
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/14 , A61P3/00 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00 , C07D233/90 , C07D487/04 , C07F9/6506 , C07F9/6561 , C07D401/10 , C07D413/10 , C07D403/10
CPC分类号： C07D487/04 , C07D233/90 , C07F9/65066 , C07F9/6561
摘要： A compound of formula (II): ##STR1## in which R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (II) can be used to prepare compounds of formula (I): ##STR2## in which R and R.sub.1 have the same meanings as above. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, also known as the quisqualate receptor. The compounds of formula (I) are also non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
摘要翻译：式（II）的化合物：其中R是氢原子或羧基，烷氧基羰基，-CO-NR4R5，-PO3H2或-CH2OH基团，R1是-alk-NH2，-alk-NH-CO-R3 ，-alk-COOR 4，-alk-CO-NR 5 R 6或-CO-NH-R 7基团。式（II）化合物可用于制备式（I）的化合物：其中R和R 1具有与上述相同的含义。式（I）化合物具有有价值的药理学性质，并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的拮抗剂，也称为quisqualate受体。式（I）化合物也是N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，更具体地是NMDA受体甘氨酸调节位点的配体。

4. 发明授权

US5902803A 5H,10H-imidazo�1,2-a!indeno�1,2-e!pyrazin-4-one derivatives, preparation thereof, and drugs containing said derivatives 失效
标题翻译： 5H，10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物，其制备方法和含有所述衍生物的药物
公开(公告)号：US5902803A
公开(公告)日：1999-05-11
申请号：US930967
申请日：1997-10-03
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/14 , A61P3/00 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00 , C07D233/90 , C07D487/04 , C07F9/6506 , C07F9/6561
CPC分类号： C07D487/04 , C07D233/90 , C07F9/65066 , C07F9/6561
摘要： Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartame (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
摘要翻译： PCT No.PCT / FR96 / 00496 Sec。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年4月2日PCT PCT。出版物WO96 / 31511 PCT 日期：10月10日，式（I）的化合物，其中R为氢原子或羧基，烷氧基羰基，-CO-NR4R5，-PO3H2或-CH2OH基，R1为-alk-NH2，-alk-NH- CO-R3，-alk-COOR4，-alk-CO-NR5R6或-CO-NH-R7基团。式（I）化合物具有有价值的药理学性质，也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的拮抗剂。此外，式（I）化合物是N-甲基-D-阿斯巴甜（NMDA）受体的非竞争性拮抗剂，更具体地是NMDA受体甘氨酸调节剂位点的配体。

5. 发明授权

US4970213A Benzo(1,8)naphthyridine derivatives as intermediates 失效
标题翻译：苯并（1,8）萘啶衍生物作为中间体
公开(公告)号：US4970213A
公开(公告)日：1990-11-13
申请号：US465329
申请日：1990-01-16
申请人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
发明人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
IPC分类号： A61K31/435 , A61P31/04 , C07D471/04
CPC分类号： C07D471/04
摘要： New benzo[b][1,8]naphthyridine derivatives of general formula (I) in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy, alkylamino or protected alkylamino radical, Hal is F, Cl or Br if R' is hydrogen, or Hal and R' are F, and Alk is an alkyl radical, and their preparation.These new products can be used as intermediates for the preparation of biologically active products. ##STR1##
摘要翻译：其中R为氢原子或烷基，氟代烷基，环烷基（3至6 C），烷氧基，烷基氨基或保护的烷基氨基的通式（I）的新苯并[b] [1,8]萘啶衍生物，Hal为F ，如果R'为氢，Cl或Br，或Hal和R'为F，Alk为烷基，及其制备。这些新产品可用作制备生物活性产品的中间体。（一）

6. 发明授权

US4021554A 1,4-Oxathiino[2,3-c]pyrrole derivatives 失效
标题翻译： 1,4-oxathiino {8,2,3- C {9吡咯衍生物
公开(公告)号：US4021554A
公开(公告)日：1977-05-03
申请号：US628927
申请日：1975-11-05
申请人： Claude Cotrel , Claude Jeanmart , Michel Barreau
发明人： Claude Cotrel , Claude Jeanmart , Michel Barreau
IPC分类号： C07D515/04 , A61K31/40 , A61K31/435 , A61K31/495 , A61K31/496 , A61K31/50 , A61P25/08 , A61P25/20 , C07D215/38 , C07D241/04 , C07D327/00 , C07D497/04 , C07D519/00 , C07D411/14
CPC分类号： C07D215/38 , C07D497/04
摘要： 1,4-Oxathiino[2,3-c]pyrrole derivatives of the formula: ##STR1## wherein A represents a phenyl, 2-pyridyl, 3-pyridazinyl, 2-quinolyl or naphthyridinyl radical, or a said radical substituted by one or two atoms or radicals selected from halogen, alkyl of 1 through 4 carbon atoms, alkoxy of 1 through 4 carbon atoms and nitro, and R represents alkyl of 1 through 4 carbon atoms, cycloalkyl of 3 through 6 carbon atoms, alkenyl of 2 through 4 carbon atoms or alkynyl of 2 through 4 carbon atoms, possess pharmacological properties, and are especially useful as tranquillizers, anti-convulsant agents, decontracturants, and agents to produce hypnosis.
摘要翻译：其中A代表苯基，2-吡啶基，3-哒嗪基，2-喹啉基或萘啶基，或被一个或多个取代基取代的所述基团取代的下式的1,4-氧硫杂环丁烷并[2,3-c] 选自卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基和硝基的两个原子或基团，R表示1至4个碳原子的烷基，3至6个碳原子的环烷基，2至4的烯基具有2至4个碳原子的碳原子或炔基具有药理学性质，并且特别可用作镇静剂，抗惊厥剂，脱保护剂和产生催眠剂的试剂。

7. 发明授权

US5789406A Indeno�1,2-E!pyrazine-4-ones, their preparation and the medicaments containing them 失效
标题翻译：茚并[1,2-E]吡嗪-4-酮，它们的制备方法和含有它们的药物
公开(公告)号：US5789406A
公开(公告)日：1998-08-04
申请号：US714163
申请日：1996-09-27
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/08 , A61P1/16 , A61P3/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P37/04 , A61P39/02 , C07D405/04 , C07D409/04 , C07D487/04 , C07D487/14 , C07D491/147 , C07D495/14 , C02D487/04
CPC分类号： C07D487/04
摘要： The compounds of formula (I) ##STR1## wherein R, R.sub.1 and R.sub.2 are defined in the disclosure, and salts thereof. The compounds of formula (I) are non-competitive N-methyl-D-asparate (NMDA) receptor antagonists, particularly NMDA receptor glycine modulation site ligands, and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor is also known as the quisqualate receptor.
摘要翻译： PCT No.PCT / FR95 / 00357 Sec。 371日期1996年9月27日第 102（e）1996年9月27日PCT 1995年3月23日PCT公布。公开号WO95 / 26349 日期1995年10月5日本公开内容中定义R 1，R 2和R 2的式（I）化合物（Ⅰ）及其盐。式（I）化合物是非竞争性的N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体，是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，该受体也称为quisqualate受体。

8. 发明授权

US5777114A Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones, preparation thereof and drugs containing same 失效
标题翻译：螺[杂环咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-酮，其制备方法和含有它们的药物
公开(公告)号：US5777114A
公开(公告)日：1998-07-07
申请号：US836410
申请日：1997-06-30
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
IPC分类号： C07D487/04 , A61K31/495 , A61P9/02 , A61P9/08 , A61P9/10 , A61P9/14 , A61P11/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07D471/20 , C07D487/20 , C07D471/235 , C07D487/241
CPC分类号： C07D471/20 , C07D487/20
摘要： Compounds of formula (I): ##STR1## wherein R.sub.3 and R.sub.4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl, --CHO, --COOR.sub.11, --CO--alk--COOR.sub.6, --CO--alk--NR.sub.6 R.sub.12, --CO--alk--CONR.sub.6 R.sub.8, --CO--COOR.sub.6, --CO--CH.sub.2 --O--CH.sub.2 --COOR.sub.6, --CO--CH.sub.2 --S--CH.sub.2 --COOR.sub.6, --CO--CH.dbd.CH--COOR.sub.6, CO--alk, --CO--Ar", --CO--alk--Ar", --CO--NH--Ar", --CO--NH--alk--Ar", --CO--Het, --CO--alk--Het, --CO--NH--Het, --CO--NH--alk--Het, --CO--NH.sub.2, --CO--NH--alk, --CO--N(alk)alk', --CS--NH.sub.2, --CS--NH--alk, --CS--NH--Ar", --CS--NH--Het, --alk--Het, --alk--NR.sub.6 R.sub.8, --alk--COOR.sub.6, --alk--CO--NR.sub.6 R.sub.8, --alk--Ar", --SO.sub.2 --alk or --SO.sub.2 --Ar radical, or a --CO-cycloalkyl radical where the cycloalkyl is optionally 2-substituted by a carboxyl radical; or (b) a 2-pyrrolidin-5-one ring. The compounds of formula (I) have useful pharmacological properties and are .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.
摘要翻译： PCT No.PCT / FR95 / 01430 Sec。 371日期：1997年6月30日 102（e）日期1997年6月30日PCT 1995年10月30日PCT PCT。 WO96 / 14318 PCT公开号日期：1996年5月17日式（I）化合物：其中R 3和R 4与它们所连接的碳原子一起形成（a）2-或3-吡咯烷环，或4-哌啶环或2-氮杂环庚烷环，所述环任选在氮原子上被烷基，-CHO，-COOR11，-CO-烷基-COOR6，-CO-alk-NR6R12，-CO- CONR6R8，-CO-COOR6，-CO-CH2-O-CH2-COOR6，-CO-CH2-S-CH2-COOR6，-CO-CH = CH-COOR6，-CO-烷基，-CO-Ar“ CO-NH-Ar“，-CO-NH-alk-Ar”，-CO-Het，-CO-alk-Het，-CO-NH-Het，-CO- NH-alk-Het，-CO-NH2，-CO-NH-alk，-CO-N（alk）alk'，-CS-NH2，-CS-NH-alk，-CS-NH-Ar“ CS-NH-Het，-alk-Het，-alk-NR6R8，-alk-COOR6，-alk-CO-NR6R8，-alk-Ar“，-SO2-alk或-SO2-Ar基，或-CO - 环烷基，其中环烷基任选被羧基任意地2-取代; 或（b）2-吡咯烷-5-酮环。式（I）化合物具有有用的药理学性质，并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，所述受体也称为quisqualate受体。此外，式（I）化合物是非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体。

9. 发明授权

US5225207A Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：衍生自铂的复合物，其制备物和含有它们的药物组合物
公开(公告)号：US5225207A
公开(公告)日：1993-07-06
申请号：US775410
申请日：1991-10-15
申请人： Michel Barreau , Jean-Claude Chottard , Jean-Bernard Le Peco , Patrick Mailliet
发明人： Michel Barreau , Jean-Claude Chottard , Jean-Bernard Le Peco , Patrick Mailliet
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： New complexes of general formula (I) in whichR.sub.1 and R.sub.2 together form a saturated or unsaturated polycyclic carbocyclic radical containing 7 to 12 carbon atoms, or a saturated or partially saturated mono-, bi- or tricyclic heterocyclic radical containing 5 to 11 chain members and a hetero-atom chosen from oxygen, sulphur or nitrogen, which latter atom can optionally be substituted by an alkoxycarbonyl radical, and,X.sub.1 and X.sub.2 represent chlorine atoms or together formeither a radical of structure: ##STR1## in which n is 0 to 2 and R.sub.6 and R.sub.7, which are identical or different, are hydrogen atoms or, when n=1, can be alkyl radicals or form, together with the carbon atom to which they are attached, a cyclobutyl radical,or a radical of structure: ##STR2## in which n, R.sub.6 and R.sub.7 are defined as above, or their salts where such exist, and their hydrates, their preparation and the pharmaceutical compositions which contain them. ##STR3##
摘要翻译：通式（I）的新络合物，其中R 1和R 2一起形成含有7至12个碳原子的饱和或不饱和多环碳环基团，或含有5至11个链成员的饱和或部分饱和的单，双或三环杂环基团和选自氧，硫或氮的杂原子，其后一个原子可任选被烷氧基羰基取代，并且，X 1和X 2表示氯原子或一起形成结构式如下的基团：其中 n为0〜2，R6和R7为相同或不同的氢原子，n = 1时，可以为烷基，也可以与它们所连接的碳原子一起形成环丁基或结构基团：其中n，R6和R7如上所定义，或其盐，如此存在，以及它们的水合物，它们的制备和含有它们的药物组合物。（一）

10. 发明授权

US4769366A Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them 失效
标题翻译：具有抗精神病活性的新型1,3-二取代吡咯并[1,2-a]吖庚因衍生物和含有它们的药物组合物
公开(公告)号：US4769366A
公开(公告)日：1988-09-06
申请号：US839101
申请日：1986-03-13
申请人： Michel Barreau , Marie-Therese Comte , Daniel Farge , Jean-Luc Malleron , Gerard Ponsinet , Gerard Roussel
发明人： Michel Barreau , Marie-Therese Comte , Daniel Farge , Jean-Luc Malleron , Gerard Ponsinet , Gerard Roussel
IPC分类号： A61K31/55 , A61P25/18 , C07D487/04 , A61K31/395 , C07D223/00
CPC分类号： C07D487/04
摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C,or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain,and the pharmaceutically acceptable salts thereof,are useful as antipsychotics.
摘要翻译：吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基，和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2至18个C的烷基羰氧基烷基，所述烷基除了另外说明的含有1至4个C的直链或支链以外，其盐可用作抗精神病药。

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