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1. 发明授权

US5182273A Spirocyclic N, O derivatives of cyclotriphosphazenes and their use in therapy 失效
标题翻译：环磷酰胺的螺环N，O衍生物及其在治疗中的应用
公开(公告)号：US5182273A
公开(公告)日：1993-01-26
申请号：US780480
申请日：1991-10-22
申请人： Alain Duflos , Jean-Francois Patoiseau , Dennis Bigg , Robert Kiss
发明人： Alain Duflos , Jean-Francois Patoiseau , Dennis Bigg , Robert Kiss
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6593
CPC分类号： C07F9/65815
摘要： The present invention relates to compounds of the Formula I: ##STR1## wherein R is hydrogen, alkyl, cycloalkyl, phenyl, or alkylphenyl, and n is 2 through 4, the production thereof, pharmaceutical compositions thereof, and their use in antineoplastic therapy.
摘要翻译：本发明涉及式I化合物：其中R为氢，烷基，环烷基，苯基或烷基苯基，n为2至4，其制备，其药物组合物及其在抗肿瘤治疗中的用途。

2. 发明授权

US5254554A 3-hydroxy-substituted-1-phenyl-1,4-dihydro-4-oxopyridazines and derivatives, and use 失效
标题翻译： 3-羟基取代的-1-苯基-1,4-二氢-4-氧代哒嗪及其衍生物，并用于
公开(公告)号：US5254554A
公开(公告)日：1993-10-19
申请号：US886341
申请日：1992-05-20
申请人： Jean-Marie Autin , Dennis Bigg , Jean-Francois Patoiseau
发明人： Jean-Marie Autin , Dennis Bigg , Jean-Francois Patoiseau
IPC分类号： A61K31/50 , A61P1/00 , A61P11/00 , A61P25/20 , A61P29/00 , A61P37/08 , A61P43/00 , C07D237/16 , C07D401/12 , C07D237/22
CPC分类号： C07D237/16 , C07D401/12
摘要： The application discloses pharmacologically-active 3-hydroxy-1-phenyl-1,4-dihydro-4-oxopyridazine compounds, derivatives thereof, a method for the preparation thereof, pharmaceutical compositions thereof, and a method of treating anxiety and other physiological abnormalities therewith.
摘要翻译：本申请公开了药理活性的3-羟基-1-苯基-1,4-二氢-4-氧代哒嗪化合物，其衍生物，其制备方法，药物组合物，以及治疗焦虑症等生理异常的方法。

3. 发明授权

US5059599A Derivatives of 1-phenyl 1,4-dihydro 3-amino 4-oxo pyridazines, their preparation and their use in therapy 失效
标题翻译： 1-苯基1,4-二羟基3-氨基-4-氧代吡啶的衍生物及其制备及其在治疗中的应用
公开(公告)号：US5059599A
公开(公告)日：1991-10-22
申请号：US534180
申请日：1990-06-06
申请人： Gilbert Mouzin , Henri Cousse , Jean-Francois Patoiseau , Jean-Marie Autin , Dennis Bigg
发明人： Gilbert Mouzin , Henri Cousse , Jean-Francois Patoiseau , Jean-Marie Autin , Dennis Bigg
IPC分类号： C07D237/14 , A61K31/50 , A61K31/535 , A61P25/20 , C07D237/22 , C07D403/06
CPC分类号： C07D237/22
摘要： The present invention relates to derivatives of 1-phenyl 1,4-dihydro 3-amino 4-oxo pyridazines of the general formula I: ##STR1## and the production thereof. It also concerns pharmaceutical compositions comprising as active principle a compound of general formula I and use thereof for treatment of central nervous system disturbances, especially as an anxiolytic.
摘要翻译：本发明涉及通式Ⅰ的1-苯基1,4-二氢-3-氨基-4-氧代哒嗪衍生物及其制备。它还涉及包含作为活性成分的通式I化合物及其用于治疗中枢神经系统紊乱的药物组合物，特别是作为抗焦虑剂。

4. 发明授权

US5633255A 1,2-dihydro-2-oxo-3-aminoquinoxaline derivatives, their preparation and their therapeutic application 失效
标题翻译： 1,2-二氢-2-氧代-3-氨基喹喔啉衍生物，其制备及其治疗应用
公开(公告)号：US5633255A
公开(公告)日：1997-05-27
申请号：US411594
申请日：1995-04-06
申请人： Dennis Bigg , Jean-Francois Patoiseau , Jean-Marie Autin , Jean-Pierre Tarayre
发明人： Dennis Bigg , Jean-Francois Patoiseau , Jean-Marie Autin , Jean-Pierre Tarayre
IPC分类号： A61K31/495 , A61P11/00 , C07D241/44
CPC分类号： C07D241/44
摘要： 1,2-dihydro-2-oxo-3-amino-quinoxaline derivatives of general formula (I) in which R.sub.1 and R.sub.2 are independently hydrogen or a straight or branched C.sub.1 -C.sub.4 alkyl radical, R.sub.3 is a straight or branched C.sub.3 -C.sub.6 alkyl, alkenyl or hydroxy-alkyl grouping, their salts with pharmaceutically-acceptable acids, and a method for preparing them and their use in therapy are disclosed.
摘要翻译： PCT No.PCT / FR93 / 00991 Sec。 371日期：1995年4月6日 102（e）日期1995年4月6日PCT提交1993年10月7日PCT公布。公开号WO94 / 07870 日本1994年4月14日（I）通式（I）的1,2-二氢-2-氧代-3-氨基 - 喹喔啉衍生物，其中R 1和R 2独立地为氢或直链或支链C 1 -C 4 烷基，R3是直链或支链C 3 -C 6烷基，烯基或羟基 - 烷基，它们与药学上可接受的酸的盐，及其制备方法及其在治疗中的应用。

5. 发明申请

US20060135785A1 Alpha-phenyl acetanilide derivatives having an acat inhibiting activity and the therapeutic application thereof 审中-公开
标题翻译：具有抑制活性的α-苯基乙酰苯胺衍生物及其治疗应用
公开(公告)号：US20060135785A1
公开(公告)日：2006-06-22
申请号：US10531234
申请日：2003-10-15
申请人： Jean-Francois Patoiseau , Jean-Marie Autin , Andre Delhon , Didier Junquero
发明人： Jean-Francois Patoiseau , Jean-Marie Autin , Andre Delhon , Didier Junquero
IPC分类号： C07D257/02
CPC分类号： C07C317/44 , C07D257/04
摘要： The present invention relates to novel analide derivatives of formula I, enantiomers and stereoisomers thereof, and their pharmaceutically acceptable salts. The invention also relates to pharmaceutical compositions containing the compounds and methods of treating hypercholesterolemia and atherosclerosis therewith.
摘要翻译：本发明涉及式I的新型分离衍生物，其对映异构体和立体异构体及其药学上可接受的盐。本发明还涉及含有化合物的药物组合物和治疗高胆固醇血症和其动脉粥样硬化的方法。

6. 发明授权

US5591743A 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands 失效
标题翻译： 3,5-二氧代 - （2H，4H）-1,2,4-三嗪衍生物作为5HT1A配体
公开(公告)号：US5591743A
公开(公告)日：1997-01-07
申请号：US578522
申请日：1996-03-26
申请人： Jean-Francois Patoiseau , Francoise Couret , Christian Faure , Elisabeth Dupont-Passelaigue , Wouter Koek
发明人： Jean-Francois Patoiseau , Francoise Couret , Christian Faure , Elisabeth Dupont-Passelaigue , Wouter Koek
IPC分类号： C07D253/06 , A61K31/53 , A61P1/04 , A61P9/00 , A61P25/20 , C07D253/075 , C07D403/12 , C07D405/12 , A01N43/707
CPC分类号： C07D253/075 , C07D405/12
摘要： A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, n is 2 to 6, inclusive,A represents aryl piperazino II ##STR2## the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino ##STR3## in which R represents hydrogen or C.sub.1 -C.sub.3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT.sub.1A receptor agonist therewith.
摘要翻译： PCT No.PCT / FR94 / 00772 Sec。 371日期：1996年3月26日 102（e）1996年3月26日PCT 1994年6月27日PCT公布。第WO95 / 01965号公报日期：1995年1月19日A式Ⅰ的3,5-二氧代 - （2H，4H）-1,2,4-三嗪化合物其中：R1和R2相同或不同，表示氢或C1 C 1-6烷基，n为2至6，包括端值，A表示芳基哌嗪基II代表苯基，萘基，嘧啶基或吡啶基的Ar基团，未取代或被C 1 -C 3烷基，C 1 -C 3烷氧基，羟基，三氟甲基或卤素，或III苯并二恶烷基 - 甲基 - 氨基或吡啶并二恶烷基 - 甲基 - 氨基，其中R表示氢或C1-C3烷基，X表示氮或碳原子，其治疗上可接受的盐和对映体，药物其组合物，以及治疗需要5HT1A受体激动剂的疾病的方法。

7. 发明授权

US4714789A Halo-biphenyl tertiary alcohols useful in therapy in the treatment of atherosclerosis 失效
标题翻译：用于治疗动脉粥样硬化的卤代联苯三醇
公开(公告)号：US4714789A
公开(公告)日：1987-12-22
申请号：US884959
申请日：1986-07-14
申请人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Jean-Francois Patoiseau
发明人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Jean-Francois Patoiseau
IPC分类号： C07C29/40 , A61K31/045 , A61P3/04 , A61P3/06 , A61P9/10 , C07C27/00 , C07C33/46 , C07C67/00 , C07C33/34
CPC分类号： C07C33/46
摘要： The invention concerns halo-biphenyl tertiary alcohols of the general formula: ##STR1## in which: X is chlorine or bromine in ortho or meta position.R and R.sub.1, which may be identical or different, represent an alkyl group of low molecular weight having from 1 to 4 carbon atoms, inclusive.These new derivatives are useful as medicaments, particularly in the treatment of atherosclerosis and obesity.
摘要翻译：本发明涉及以下通式的卤代 - 联苯叔醇：其中：X是邻位或间位的氯或溴。 R和R 1可以相同或不同，表示具有1-4个碳原子的低分子量烷基。这些新衍生物可用作药物，特别是用于治疗动脉粥样硬化和肥胖症。

8. 发明授权

US06303603B1 3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors 有权
标题翻译： 3-羟基-2（H）-1,2,4-三嗪衍生物作为5个HT1A受体的配体
公开(公告)号：US06303603B1
公开(公告)日：2001-10-16
申请号：US09529728
申请日：2000-04-14
申请人： Jean-Francois Patoiseau , Elisabeth Dupont-Passelaigue , Wouter Koek
发明人： Jean-Francois Patoiseau , Elisabeth Dupont-Passelaigue , Wouter Koek
IPC分类号： A61K3153
CPC分类号： C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R1 represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched 1-C4 alkyl group; a C1-C4phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. R2 represents: hydrogen; a linear or branched C1-C4 alkyl radical; a C1-C4 phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR3 substituted. R3 represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R4 represents hydrogen or a C1-C3 alkyl group and n can be whole numbers ranging between 3 and 5.
摘要翻译：本发明涉及通式（I）的新的3-氧代 - （2H）-1,2,4-三嗪衍生物，其中当R1是任意取代的氮原子时，R 1表示：氢; 直链或支链的1-C4烷基; C1-C4苯基烷基，苯环任选被一个或多个基团取代，例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基。 R2表示：氢; 直链或支链C 1 -C 4烷基; C 1 -C 4苯基或苯基烷基，苯环任选被一个或几个基团例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基取代。 A表示氧原子或任选被NR 3取代的氮原子。 R3表示氢或甲基。 B表示其中Ar本身表示芳族结构的基团，例如苯基，吡啶基或嘧啶基，任选被一个或多个基团例如C 1 -C 3烷基，C 1 -C 3烷氧基，羟基，三氟甲基或卤素取代， n可以是3到5之间的整数; （IIb）其中Ar如式（IIa）中所定义，m可以是1和2之间的整数; （IIc）其中R4表示氢或C1-C3烷基，n可以是3至5的整数。

9. 发明申请

US20080167313A1 1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy 有权
公开(公告)号：US20080167313A1
公开(公告)日：2008-07-10
申请号：US11885630
申请日：2006-03-02
申请人： Elisabeth Dupont-Passelaigue , Isabelle Leroy , Jean-Francois Patoiseau , Didier Junquero , Yves Rival , Andre Delhon
发明人： Elisabeth Dupont-Passelaigue , Isabelle Leroy , Jean-Francois Patoiseau , Didier Junquero , Yves Rival , Andre Delhon
IPC分类号： A61K31/53 , C07D253/06 , A61P3/06 , A61P3/04 , A61P3/10 , A61P17/00
CPC分类号： C07D253/075
摘要： The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl, C5-C6 cycloalkyl, nitrile, C1-C4 alkoxycarbonylvinyl, hydroxycarbonylvinyl, C1-C4 alkoxycarbonyl, carboxylate, benzyloxy or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); YR3 represents oxygen or NR3 for which R3 represents hydrogen, a linear or branched C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); Z represents an oxygen atom or a carbon atom capable of being bound to the ortho, meta or para positions of the phenyl group of formula I; n can be 0 to 5 when Z=C or 2 to 4 when Z=O; X represents oxygen or sulphur; R4, R5, R6, R7 and R8 represent hydrogen or fluorine; R9, R10 and R11 represent hydrogen or a linear or branched C1-C5 alkyl group as well as the pharmaceutically acceptable base addition salts, and the various enantiomers of compounds having asymmetric carbons, and their mixtures in all proportions including in particular the racemic mixtures.

10. 发明授权

US5760087A Glycylanilide derivatives, their preparation and their application in therapy 失效
标题翻译：甘氨酰苯胺衍生物，其制备及其在治疗中的应用
公开(公告)号：US5760087A
公开(公告)日：1998-06-02
申请号：US875191
申请日：1997-07-17
申请人： Jean-Francois Patoiseau , Jean-Marie Autin , Andre Delhon , Philippe Oms
发明人： Jean-Francois Patoiseau , Jean-Marie Autin , Andre Delhon , Philippe Oms
IPC分类号： A61K31/165 , A61P3/06 , A61P9/10 , A61P43/00 , C07C231/02 , C07C237/22 , C07C323/60 , A01N37/18
CPC分类号： C07C237/22 , C07C323/60
摘要： The invention relates to new derivatives of glycylanilides having general formula (I), wherein, particularly, R.sub.1, R.sub.3, R.sub.4, R.sub.8, R.sub.9 represent CH.sub.3 ; R.sub.2, R.sub.5, R.sub.6, R.sub.7 represent H; R.sub.10 represents C.sub.12 H.sub.25 and A is a sulfur atom. It also relates to the preparation process and the pharmaceutical compositions comprising as active principle at least one of said compounds, as well as the utilization of said derivatives for the fabrication of drugs intended to the treatment of hypercholesterolemy or atherosclerosis. ##STR1##
摘要翻译： PCT No.PCT / FR96 / 00081 Sec。 371日期1997年7月17日 102（e）日期1997年7月17日PCT 1996年1月18日PCT PCT。第WO96 / 22279号公报日期：1996年7月25日本发明涉及具有通式（I）的脯氨酰苯胺的新衍生物，其中，特别地，R 1，R 3，R 4，R 8，R 9表示CH 3; R2，R5，R6，R7表示H; R 10表示C12H25，A为硫原子。它还涉及制备方法和药物组合物，其包含作为至少一种所述化合物的活性成分，以及所述衍生物用于制备旨在治疗高胆固醇血症或动脉粥样硬化的药物的用途。（一）

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