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11. 发明授权

US5849780A 1-benzenesulfonyl-1-1,3-dihydroindol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present 失效
标题翻译： 1-苯磺酰基-1,1,3-二氢吲哚-2-酮衍生物及其制备方法及其存在的药物组合物
公开(公告)号：US5849780A
公开(公告)日：1998-12-15
申请号：US323921
申请日：1994-10-17
申请人： Alain Di Malta , Loic Foulon , Georges Garcia , Dino Nisato , Richard Roux , Claudine Serradeil-Legal , Gerard Valette , Jean Wagnon
发明人： Alain Di Malta , Loic Foulon , Georges Garcia , Dino Nisato , Richard Roux , Claudine Serradeil-Legal , Gerard Valette , Jean Wagnon
IPC分类号： C07D209/34 , C07D209/92 , C07D209/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D471/10 , C07D491/10 , A61K31/40 , A61K31/44
CPC分类号： C07D209/34 , C07D209/92 , C07D209/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D471/10 , C07D491/10
摘要： The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.
摘要翻译：本发明涉及式（I）的1-苯磺酰基-1,3-二氢吲哚-2-酮衍生物及其盐，在适当情况下为它们的制备及其存在于其中的药物组合物。这些化合物对血管加压素和/或卵母细胞受体具有亲和力。

12. 发明授权

US5728723A 1-benzenesulfonyl-1,3-dihydro-indol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present 失效
标题翻译： 1-苯磺酰基-1,3-二氢 - 吲哚-2-酮衍生物，其制备方法及其存在的药物组合物
公开(公告)号：US5728723A
公开(公告)日：1998-03-17
申请号：US478738
申请日：1995-06-07
申请人： Alain Di Malta , Loic Foulon , Georges Garcia , Dino Nisato , Richard Roux , Claudine Serradeil-Legal , Gerard Valette , Jean Wagnon
发明人： Alain Di Malta , Loic Foulon , Georges Garcia , Dino Nisato , Richard Roux , Claudine Serradeil-Legal , Gerard Valette , Jean Wagnon
IPC分类号： C07D209/34 , C07D209/92 , C07D209/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D471/10 , C07D491/10 , A61K31/405 , C07D209/04
CPC分类号： C07D209/34 , C07D209/92 , C07D209/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D471/10 , C07D491/10
摘要： The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.
摘要翻译：本发明涉及式（I）的1-苯磺酰基-1,3-二氢吲哚-2-酮衍生物及其盐，在适当情况下为它们的制备及其存在于其中的药物组合物。这些化合物对血管加压素和/或卵母细胞受体具有亲和力。

13. 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。

14. 发明授权

US4978759A Process for the stereospecific synthesis of optically pure 4-amino-3-hydroxycarboxylic acid derivatives 失效
标题翻译：光学纯的4-氨基-3-羟基羧酸衍生物的立体有择合成方法
公开(公告)号：US4978759A
公开(公告)日：1990-12-18
申请号：US881191
申请日：1986-07-02
申请人： Patrick Jouin , Dino Nisato , Bertrand Castro
发明人： Patrick Jouin , Dino Nisato , Bertrand Castro
IPC分类号： C07B53/00 , C07B31/00 , C07C67/00 , C07C227/32 , C07C229/22 , C07C229/24 , C07C229/26 , C07C229/28 , C07C229/30 , C07C229/34 , C07C239/00 , C07C269/00 , C07C313/00 , C07C323/25 , C07D207/26 , C07D207/263 , C07D207/273 , C07D207/40 , C07D207/404 , C07D209/20 , C07D319/06
CPC分类号： C07D207/27 , C07C227/32 , C07D207/408 , C07D209/20 , C07D319/06 , Y02P20/55 , Y10S530/86
摘要： The process described makes it possible to obtain optically pure 4-amino-3-hydroxycarboxylic acids by means of a series of stereoselective steps. The starting material is an alpha-amino acid in the L or D configuration, with which Meldrum's acid is reacted. The resulting pyrrolone derivative is reduced prior to opening of the pyrrolidine ring. The invention also relates to the new products obtained by the said process and to the pyrrolone derivatives obtained as intermediates.
摘要翻译：所述方法使得可以通过一系列立体选择性步骤获得光学纯的4-氨基-3-羟基羧酸。起始材料是L或D构型的α-氨基酸，Meldrum的酸与其反应。所得的吡咯烷酮衍生物在吡咯烷环的打开之前还原。本发明还涉及通过所述方法获得的新产品和作为中间体获得的吡咯烷酮衍生物。

15. 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。

16. 发明授权

US4735947A Methyllevallorphanium salts having peripheral opiate antagonistic activity 失效
标题翻译：具有外周鸦片拮抗活性的甲基高铝盐
公开(公告)号：US4735947A
公开(公告)日：1988-04-05
申请号：US825798
申请日：1986-02-04
申请人： Alberto Bianchetti , Dino Nisato , Luciano Manara , Roberto Sacilotto
发明人： Alberto Bianchetti , Dino Nisato , Luciano Manara , Roberto Sacilotto
IPC分类号： A61K31/47 , A61P25/30 , C07D221/28 , A61K31/485
CPC分类号： C07D221/28
摘要： Methyllevallorphanium salts having peripheral antagonistic activity of formula ##STR1## wherein Y.sup.n(-) represents the anion a pharmaceutically acceptable acid other than halogen and n represents the number of negative charges of said anion; a process for their preparation by exchange of the halogen ion with the Y.sup.n(-) anion; and pharmaceutical compositions containing them as active ingredients.
摘要翻译：具有式的具有周期性拮抗活性的甲基高铝盐其中Yn（ - ）表示阴离子是除卤素以外的药学上可接受的酸，n表示所述阴离子的负电荷数; 通过交换卤素离子与Yn（ - ）阴离子制备它们的方法; 和含有它们作为活性成分的药物组合物。

17. 发明授权

US4514408A N-substituted nicotinamide 1-oxide as histamine H.sub.2 receptor blockers 失效
标题翻译： N-取代烟酰胺1-氧化物作为组胺H2受体阻断剂
公开(公告)号：US4514408A
公开(公告)日：1985-04-30
申请号：US522749
申请日：1983-08-12
申请人： Dino Nisato , Sergio Boveri
发明人： Dino Nisato , Sergio Boveri
IPC分类号： C07D211/22 , C07D211/46 , C07D213/64 , C07D213/81 , C07D213/82 , C07D213/89 , C07D295/096 , C07D401/12 , A61K31/455
CPC分类号： C07D213/64 , C07D211/22 , C07D211/46 , C07D213/81 , C07D213/82 , C07D213/89 , C07D295/096 , C07D401/12
摘要： N-substituted nicotinamide 1-oxide having histamine H.sub.2 receptor blocking activity of formula ##STR1## wherein X is a nitrogen atom or a CH group and Am represents a mono- or disubstituted amino group, a pyrrolidino, morpholino, thiomorpholino, hexamethyleneimino group, or an optionally substituted piperidino or piperazino group; their salts; a process for their preparation; and pharmaceutical compositions containing them as active ingredients.
摘要翻译：具有式的组胺H2受体阻断活性的N-取代烟酰胺1-氧化物，其中X是氮原子或CH基团，并且Am表示一或二取代的氨基，吡咯烷子基，吗啉代，硫代吗啉代，六亚甲基亚氨基或任选取代的哌啶子基或哌嗪基; 他们的盐其准备过程; 和含有它们作为活性成分的药物组合物。

18. 发明授权

US5578633A N-sulfonylindoline derivatives, their preparation and the pharmaceutical compositions in which they are present 失效
公开(公告)号：US5578633A
公开(公告)日：1996-11-26
申请号：US458614
申请日：1995-06-02
申请人： Jean Wagnon , Paul de Cointet , Dino Nisato , Claude Plouzane , Claudine Serradeil-Legal , Bernard Tonnerre
发明人： Jean Wagnon , Paul de Cointet , Dino Nisato , Claude Plouzane , Claudine Serradeil-Legal , Bernard Tonnerre
IPC分类号： C07C311/08 , C07C311/13 , C07C311/21 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/06 , C07D417/06 , A61K31/40 , C07D209/04
CPC分类号： C07D401/06 , C07C311/08 , C07C311/13 , C07C311/21 , C07D209/42 , C07D401/12 , C07D403/06 , C07D417/06
摘要： The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.

19. 发明授权

US5397801A N-sulfonylindoline derivatives, their preparation and the pharmaceutical compositions in which they are present 失效
标题翻译： N-磺酰基二氢吲哚衍生物，其制备方法及其存在的药物组合物
公开(公告)号：US5397801A
公开(公告)日：1995-03-14
申请号：US240360
申请日：1994-05-10
申请人： Jean Wagnon , Paul de Cointet , Dino Nisato , Claude Plouzane , Claudine Serradeil-Legal , Bernard Tonnerre
发明人： Jean Wagnon , Paul de Cointet , Dino Nisato , Claude Plouzane , Claudine Serradeil-Legal , Bernard Tonnerre
IPC分类号： C07C311/08 , C07C311/13 , C07C311/21 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/06 , C07D417/06 , A61K31/40 , C07D209/10 , C07D413/06
CPC分类号： C07D401/06 , C07C311/08 , C07C311/13 , C07C311/21 , C07D209/42 , C07D401/12 , C07D403/06 , C07D417/06
摘要： The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.
摘要翻译：本发明涉及式（I）和（I）的制备方法的N-磺酰基衍生物及其制备的药物组合物。式（I）和（I）的化合物对加压素和卵母细胞受体具有亲和力。

20. 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。

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