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1. 发明授权

US5444056A Aminoalkoxyphenyl derivatives, process for their preparation and compositions containing them 失效
标题翻译：氨基烷氧基苯基衍生物，其制备方法和含有它们的组合物
公开(公告)号：US5444056A
公开(公告)日：1995-08-22
申请号：US476342
申请日：1990-02-07
申请人： Jean Gubin , Pierre Chatelain , Henri Inion , Gilbert Rosseels
发明人： Jean Gubin , Pierre Chatelain , Henri Inion , Gilbert Rosseels
IPC分类号： A61K31/13 , A61K31/255 , A61K31/34 , A61K31/343 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P9/00 , A61P25/02 , A61P27/02 , A61P27/06 , C07C317/22 , C07D207/325 , C07D209/30 , C07D213/70 , C07D295/08 , C07D295/092 , C07D307/82 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D221/02 , A61K31/33
CPC分类号： C07D295/088 , C07C317/22 , C07D209/30 , C07D307/82 , C07D471/04 , C07C2101/14
摘要： An aminoalkoxyphenyl derivative of general formula:Cy--B--Ph--O--A--Am (1)as well as a pharmaceutically acceptable salt thereof in whichB represents a --S--, --SO-- or --SO.sub.2 -- group,Ph represents an optionally substituted phenyl radical,A denotes a straight or branched alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxy propylene radical in which the hydroxy is optionally substituted by a C.sub.1 -C.sub.4 alkyl radical.Am represents a group: ##STR1## and Cy is a cyclic group, provided that when Cy represents either a benzo[b]furyl group substituted at position 4 by a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or a benzo[b]thienyl group substituted at position 4 by a halogen atom or by a C.sub.1 -C.sub.4 alkyl group and when B represents a --SO.sub.2 -- group, R.sub.3 represents a --Alk--Ar radical.
摘要翻译：通式为Cy-B-Ph-OA-Am（1）的氨基烷氧基苯基衍生物及其药学上可接受的盐，其中B表示-S-，-SO-或-SO2-基，Ph表示任选取代的苯基，A表示具有2至5个碳原子的直链或支链亚烷基或2-羟基丙烯基，其中羟基任选被C 1 -C 4烷基取代。 Am表示一组：（F）或（G）或（H），Cy是环状基团，条件是当Cy表示在4位被取代的苯并[b]呋喃基时，卤素原子或C1-C4烷基，或在4位被卤素原子或C1-C4烷基取代的苯并[b]噻吩基，当B表示-SO 2 - 基时，R 3表示-Alk -Ar根本

2. 发明授权

US5223510A Alkylaminoalkyl derivatives of benzofuran, benzothiophene, indole and indolizine, process for their preparation and compositions containing them 失效
标题翻译：苯并呋喃，苯并苯，吲哚和吲哚的烷基胺衍生物及其制备及其组合物的制备方法
公开(公告)号：US5223510A
公开(公告)日：1993-06-29
申请号：US736580
申请日：1991-07-26
申请人： Jean Gubin , Pierre Chatelain , Jean Lucchetti , Gilbert Rosseels , Henri Inion
发明人： Jean Gubin , Pierre Chatelain , Jean Lucchetti , Gilbert Rosseels , Henri Inion
IPC分类号： A61K31/34 , A61K9/48 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/435 , A61K31/437 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D209/00 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/44 , C07D221/00 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/58 , C07D409/06 , C07D417/12 , C07D471/04
CPC分类号： C07D409/06 , C07D209/12 , C07D307/80 , C07D307/81 , C07D333/56 , C07D471/04
摘要： The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: ##STR1## in which: Het represents one of the groups: ##STR2## in which T,T' and T"represent particularly a group: ##STR3## R and R.sub.a, identical or different, represent X represent --O-- or --S--Y represents a radical ##STR4## These compounds are useful as medecines particularly for the treatment of pathological syndroms of the cardio-vascular system.
摘要翻译：本发明的主题是以下通式的苯并呋喃，苯并噻吩，吲哚或中氮茚化合物：其中：Het代表下列组之一：其中T，T'和T' “代表特别是一组：R和R a相同或不同，表示X表示-O-或-S-Y表示基团这些化合物可用作特别用于治疗心脏病理综合征的药物血管系统。

3. 发明授权

US5182291A Pyrozala-pyridyl aminoabkoxyphenol compounds 失效
标题翻译：吡罗扎 - 吡啶基氨基氨基苯酚化合物
公开(公告)号：US5182291A
公开(公告)日：1993-01-26
申请号：US716252
申请日：1991-06-17
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： C07D209/30 , C07D213/70 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
CPC分类号： C07D213/70 , C07C309/00 , C07C317/00 , C07D209/30 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
摘要： Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radical orR.sub.3 and R.sub.4 when taken together, denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by --O--, ##STR2## R.sub.6 denoting hydrogen or a lower alkyl or pheny radical, Cy represents a cyclic group with the proviso that when Cy represents a benzo[b]furyl or benzo[b]thienyl group and B represents a --SO.sub.2 -- group, R.sub.3 represents a radical --Alk--R.sub.5, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.
摘要翻译：用于治疗下列心血管系统的某些病理学综合征的氨基烷氧基苯基衍生物：其中：B表示-S-，-SO-或-SO 2 - 基团，R 1和R 2各自相同或不同，表示氢，甲基或乙基或卤素，A表示具有2至5个碳原子的直链或支链亚烷基或2-羟基亚丙基，其中羟基任选被低级烷基取代，R 3 表示烷基或式Al-R 5的基团，其中Alk表示单键或具有1至5个碳原子的直链或支链亚烷基，R5表示吡啶基，苯基，2,3-亚甲二氧基苯基或3,4-亚甲二氧基苯基或被一个或多个选自卤素原子，低级烷基或低级烷氧基的取代基取代的苯基，R4表示氢或烷基或R3和R4，当一起表示具有3至6个碳原子并且任选被苯基取代或任选地被-O - ， - 表示氢或低级烷基或苯基的-C 1-6的亚烷基或亚烯基，Cy表示环状基团，条件是当Cy表示苯并[b]呋喃基或苯并[b]噻吩基，B表示-SO 2 - 基时，R 3表示基团-Alk-R 5，以及其N-氧化物衍生物及其药学上可接受的盐。

4. 发明授权

US4957925A Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same 失效
标题翻译：氨基烷氧基苯基衍生物，制备方法和含有它们的组合物
公开(公告)号：US4957925A
公开(公告)日：1990-09-18
申请号：US82554
申请日：1987-08-07
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： An aminoalkoxyphenyl compound of formula ##STR1## as well as a pharmaceutically acceptable salt of this compound.
摘要翻译：式IMAMA的氨基烷氧基苯基化合物以及该化合物的药学上可接受的盐。

5. 发明授权

US5017579A Use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure 失效
标题翻译：氨基烷氧基苯基衍生物用于减少和/或控制过度眼压的用途
公开(公告)号：US5017579A
公开(公告)日：1991-05-21
申请号：US306498
申请日：1989-02-06
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat , Gerard Le Fur
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat , Gerard Le Fur
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： The present invention is directed to the use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure and compositions suitable for this case.

6. 发明授权

US5039700A Benzofuranyl aminoalkoxyphenyl compounds 失效
标题翻译：苯并呋喃基氨基烷氧基苯基化合物
公开(公告)号：US5039700A
公开(公告)日：1991-08-13
申请号：US495134
申请日：1990-03-19
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5 in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radicalCy represents a benzo[b]furyl, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.

7. 发明授权

US5215988A Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same 失效
标题翻译：氨基烷氧基苯基衍生物，制备方法和含有它们的组合物
公开(公告)号：US5215988A
公开(公告)日：1993-06-01
申请号：US745268
申请日：1991-08-14
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： C07D209/30 , C07D213/70 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
CPC分类号： C07D213/70 , C07C309/00 , C07C317/00 , C07D209/30 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
摘要： The present invention relates to aminoalkoxyphenyl compounds of formula: ##STR1## in which: B is selected from --S--, --SO-- and --SO.sub.2 --,R.sub.1 and R.sub.2, which are identical or different, are selected from hydrogen, methyl, ethyl and halogen,A is selected from a straight- or branched-alkylene radical having from 2 to 5 carbon atoms, a 2-hydroxypropylene radical, and a 2-(lower alkoxy) propylene radical,R.sub.3 is selected from C.sub.1 -C.sub.8 alkyl and a radical of formula:--Alk--Ar in which Alk is selected from a single bond and a linear- or branched-alkylene radical having from 1 to 5 carbon atoms; and Ar is selected from pyridyl, phenyl, 2-3-methyleneoxyphenyl, 3,4-methylenedioxyphenyl and phenyl substituted with one or more substituents, which may be identical or different, selected from halogen atoms, C.sub.1 -C.sub.8 alkyl groups and C.sub.1 -C.sub.8 alkoxy groups,R.sub.4 is selected from hydrogen and C.sub.1 -C.sub.8 alkyl, orR.sub.3 and R.sub.4, when taken together, denote a 1,4-tetra-methylene, 1,5-pentamethylene, 3-oxa-1,5-pentamethylene, 3-aza-1,5-pentamethylene, 3-methylaza-1,5-pentamethylene, 3-phenylaza-1,5-pentamethylene or --CH.dbd.CH--N.dbd.CH-- radical,R is selected from hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6, cycloalkyl, benzyl, phenyl optionally substituted with one or more substituents, which may be identical or different, selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy as well as a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及下式的氨基烷氧基苯基化合物：其中：B选自-S-，-SO-和-SO 2 - ，R 1和R 2相同或不同，选自氢，甲基，乙基和卤素，A选自具有2至5个碳原子的直链或支链亚烷基，2-羟基亚丙基和2-（低级烷氧基）丙烯基，R 3选自C 1 -C 8烷基和其中Alk选自单键和具有1至5个碳原子的直链或支链亚烷基的式：-Alk-Ar的基团; 并且Ar选自吡啶基，苯基，2-3亚甲基氧基苯基，3,4-亚甲二氧基苯基和被一个或多个可以相同或不同的取代基取代的苯基，其可以选自卤素原子，C 1 -C 8烷基和C 1 -C 8 烷氧基，R 4选自氢和C 1 -C 8烷基，或者R 3和R 4一起表示1,4-四亚甲基，1,5-亚戊基，3-氧杂-1,5-五亚甲基，3 1-氮杂-1,5-五亚甲基，3-甲基-1,5-五亚甲基，3-苯基氮杂-1,5-五亚甲基或-CH = CH-N = CH-基，R选自氢，C 1 -C 8烷基 C 3 -C 6，环烷基，苄基，任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的苯基以及其药学上可接受的盐。

8. 发明授权

US4994474A Alkyl- or aryl-aminoalkoxy-benzene-sulfonyl indoles 失效
标题翻译：烷基或芳基 - 氨基烷氧基 - 苯磺酰基吲哚
公开(公告)号：US4994474A
公开(公告)日：1991-02-19
申请号：US306499
申请日：1989-02-06
申请人： Jean Gubin , Pierre Chatelain , Henri Inion
发明人： Jean Gubin , Pierre Chatelain , Henri Inion
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： The present invention relates to aminoalkoxyphenyl derivatives of formula: ##STR1## and its N-oxide and pharmaceutically acceptable salts, in which: B represents a--S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radial or a halogen atom,A denotes a straight-or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radial in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkkyl radical or a radical of formula:--Alk--Ar in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and Ar denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl group or lower alkoxy groups,R.sub.11 denotes hydrogen or a lower alkyl, phenyl, diphenylmethyl, benzyl or halogenobenzyl radical,R.sub.4 denotes hydrogen or an alkyl radical, or R.sub.3 and R.sub.4 when taken together denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by ##STR2## R represent hydrogen, an alkyl radical, a cycloalkyl radical, a benzyl radical or a phenyl radical optionally substituted with one or more substituents, which may be identical or different, selected from halogen atoms and from lower alkyl, lower alkoxy or nitro groups, are described. The compounds of the invention possess exceptional pharmacological properties, especially calcium transport inhibitory properties, as well as bradycardic, hypotensive and antiadrenergic properties.

9. 发明授权

US4103012A Indolizine derivatives, pharmaceutical compositions and methods containing same 失效
标题翻译：中氮茚衍生物，药物组合物和含有它们的方法
公开(公告)号：US4103012A
公开(公告)日：1978-07-25
申请号：US769332
申请日：1977-02-16
申请人： Jean Gubin , Gilbert Rosseels
发明人： Jean Gubin , Gilbert Rosseels
IPC分类号： A61K31/435 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07D213/20 , C07D471/04 , A61K31/44 , C07D221/22
CPC分类号： C07D471/04 , C07D213/20
摘要： Novel indolizine derivatives of the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R represents a branched- or straight-chain alkyl radical having from 1 to 5 carbon atoms, a phenyl radical, a mono-fluoro-, mono-chloro- or mono-bromo-phenyl, a di-fluoro-, di-chloro- or di-bromo-phenyl radical, a methoxy-phenyl radical or a methyl-phenyl radical optionally substituted on the aromatic moiety by an atom of fluorine, chlorine or bromine and R.sub.1 and R.sub.2, which are different, represent a hydrogen atom or a group of the formula: ##STR2## wherein R.sub.3 and R.sub.4 which are identical, each represent a hydrogen atom or a methyl radical, Am represents a dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino, morpholino, piperidino, pyrrolidino or 4-methyl-piperazino group and n is an integer in the range of from 2 to 6 inclusive.They are effective for treating certain pathological or otherwise abnormal conditions of the heart and more particularly sinus tachycardia. Certain of them are also useful in the treatment of angina pectoris and cardiac arrhythmia.
摘要翻译：新的具有下式的中氮茚衍生物：其中R表示具有1至5个碳原子的支链或直链烷基，苯基，单氟，单氯 - 或 - 溴 - 苯基，二 - 氟 - ，二氯 - 或二 - 溴 - 苯基，甲氧基 - 苯基或甲基 - 苯基，其任选在芳族部分上被氟原子取代，氯或溴以及不同的R 1和R 2表示氢原子或下式的基团：其中R 3和R 4 + L相同，各自表示氢原子或甲基，Am表示二甲基氨基，二乙基氨基，二正丙基氨基，二正丁基氨基，吗啉代，哌啶子基，吡咯烷子基或4-甲基哌嗪基，n为2-6以下的整数。

10. 发明授权

US5401855A 4-hydroxyphenylthio derivatives, their preparation and their use for the preparation of aminoalkoxyphenylsulphonyl derivatives 失效
标题翻译： 4-羟基苯硫基衍生物，它们的制备及其在制备氨基烷氧基苯磺酰基衍生物中的应用
公开(公告)号：US5401855A
公开(公告)日：1995-03-28
申请号：US80171
申请日：1993-06-23
申请人： Jean Gubin , Henri Inion
发明人： Jean Gubin , Henri Inion
IPC分类号： C07D209/30 , C07D307/82 , C07D333/62 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D209/30
摘要： The subject of the invention is 4-hydroxyphenylthio derivatives of general formula: ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, each represent hydrogen, a methyl or ethyl radical or a halogen atom,R represents a (C.sub.1 -C.sub.6) alkyl, (C.sub.3 -C.sub.6) cycloalkyl or phenyl radical,R.sub.3 represents hydrogen or a halogen atom, X represents --O--, --S-- or --NR.sub.4 -- in which R.sub.4 represents hydrogen or a (C.sub.1 -C.sub.4) alkyl group, useful as synthetic intermediates, especially for the preparation of aminoalkoxyphenylsulphonyl derivatives which are pharmaceutically active compounds.
摘要翻译：本发明的主题是以下通式的4-羟基苯硫基衍生物：其中：R 1和R 2相同或不同，各自表示氢，甲基或乙基或卤素原子，R表示（C1 -C 6）烷基，（C 3 -C 6）环烷基或苯基，R 3表示氢或卤素原子，X表示-O - ， - S-或-NR 4 - ，其中R 4表示氢或（C 1 -C 4）烷基可用作合成中间体，特别是用于制备作为药物活性化合物的氨基烷氧基苯基磺酰基衍生物。

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