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1. 发明申请

US20120245170A1 PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT 有权
标题翻译：吡唑并吡啶衍生物作为抗原剂
公开(公告)号：US20120245170A1
公开(公告)日：2012-09-27
申请号：US13500757
申请日：2010-10-13
申请人： Karim Bedjeguelal , Rémi Rabot , El Bachir Kaloun , Patrice Mayer , Arnaud Marchand , Nicolas Rahier , Philippe Schambel , Hugues Bienayme
发明人： Karim Bedjeguelal , Rémi Rabot , El Bachir Kaloun , Patrice Mayer , Arnaud Marchand , Nicolas Rahier , Philippe Schambel , Hugues Bienayme
IPC分类号： A61K31/437 , A61K31/5377 , A61P35/00 , A61K31/444 , A61K31/4545 , C07D487/04 , C07D471/04 , A61K31/496
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.
摘要翻译：本发明涉及以下通式（I）：（式I）及其药学上可接受的盐，其制备方法及其用途，特别是抗癌剂的化合物。

2. 发明授权

US5637779A Process for the preparation of vitamin A and new intermediates 失效
标题翻译：制备维生素A和新中间体的方法
公开(公告)号：US5637779A
公开(公告)日：1997-06-10
申请号：US383209
申请日：1995-02-03
申请人： Jean-Erick Ancel , Hugues Bienayme
发明人： Jean-Erick Ancel , Hugues Bienayme
IPC分类号： B01J27/122 , B01J31/30 , C07B61/00 , C07C35/18 , C07C43/178 , C07C43/303 , C07C403/08 , C07C403/10 , C07C403/14 , C07D317/20 , C07D319/06
CPC分类号： C07C403/14 , C07C403/10 , C07C403/12 , C07B2200/09 , C07C2101/16
摘要： A process for the preparation of vitamin A which comprises condensing ethynyl-.beta.-ionol with the acetal of a C.sub.5 allylic halide in the presence of a catalytic amount of a copper-based catalyst and a base; hydrogenating the condensed compound; eliminating the hydroxyl functional group to obtain retinal; and correcting the retinal obtained.
摘要翻译：一种制备维生素A的方法，其包括在催化量的铜基催化剂和碱的存在下将乙炔基-β-醇与C5烯丙基卤的缩醛缩合; 氢化缩合化合物; 消除羟基官能团以获得视网膜; 并校正获得的视网膜。

3. 发明申请

US20100063102A1 TREATMENT OF FAECAL INCONTINENCE 审中-公开
标题翻译：治疗无效性
公开(公告)号：US20100063102A1
公开(公告)日：2010-03-11
申请号：US12448731
申请日：2008-01-28
申请人： Jacques Ferte , Hugues Bienayme , Francisco Carlos Perez Martinez
发明人： Jacques Ferte , Hugues Bienayme , Francisco Carlos Perez Martinez
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： A61K31/4439
摘要： Use of a compound corresponding to formula (I) in which R represents hydrogen or a group chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene, cycloalkylidyne and —CONH2 groups, and the —COR′ and —COOR′ groups, in which R′ is chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene and cycloalkylidyne groups, it being possible for said groups R and/or R′ to be substituted and/or interrupted with -0-, —COO—, —OCO—, —NHCO— or —CONH— functions, or a pharmaceutically acceptable salt of said compound, for obtaining a medicament for use in the treatment of faecal incontinence.
摘要翻译：使用对应于式（I）的化合物，其中R表示氢或选自烷基，亚烷基，亚烷基，环烷基，亚环烷基，环亚烷基和-CONH 2基团的基团，以及-COR'和-COOR'基团，其中R “选自烷基，亚烷基，亚烷基，环烷基，亚环烷基和环烷基炔基，所述基团R和/或R'可以被-O-，-COO-，-OCO-， - NHCO-或-CONH-官能团，或所述化合物的药学上可接受的盐，以获得用于治疗大便失禁的药物。

4. 发明授权

US5563297A Intermediates for the preparation of vitamin A and carotenoids and process for their preparation 失效
标题翻译：用于制备维生素A和类胡萝卜素的中间体及其制备方法
公开(公告)号：US5563297A
公开(公告)日：1996-10-08
申请号：US320150
申请日：1994-10-07
申请人： Hugues Bienayme
发明人： Hugues Bienayme
IPC分类号： B01J31/24 , C07B61/00 , C07C45/54 , C07C45/65 , C07C45/67 , C07C47/20 , C07C47/21 , C07C47/228 , C07C47/232 , C07C49/203 , C07C49/213 , C07C49/217 , C07C49/683 , C07C49/796 , C07C69/96 , C07C403/00 , C07C403/14
CPC分类号： C07C403/14 , C07C403/02 , C07C403/12 , C07C45/54 , C07C45/67 , C07C47/20 , C07C47/21 , C07C47/232 , C07C49/217 , C07C49/683 , C07C49/796 , C07C69/96 , C07B2200/09 , C07C2101/16
摘要： The present invention relates to novel intermediates for the preparation of vitamin A and carotenoids, corresponding to the following formula (I): ##STR1## in which X is a carbon atom; n is equal to 1 or 2; R.sub.1, R.sub.2 and R.sub.3, which may be identical or different, each independently represent hydrogen, alkyl containing 1 to 4 carbon atoms, alkenyl containing 2 to 11 carbon atoms or aryl, each alkyl and alkenyl may be linear, branched or cyclic, or R.sub.1 and R.sub.2 can together with the carbon atom to which they are attached form a cycloaliphatic compound which is optionally substituted; and R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8, which may be identical or different, each independently represent hydrogen, alkyl containing 1 to 4 carbon atoms or alkenyl containing 2 to 10 carbon atoms, each alkyl or alkenyl being linear, or if containing sufficient numbers of carbon atoms, may also be branched or cyclic, or an aryl containing 6 to 10 carbon atoms, or any two of R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 may together form, along with the carbon atom(s) to which they are attached, a cycloalkylidene group containing 3 to 10 carbon atoms, as well as the process for their preparation and their use.
摘要翻译：本发明涉及用于制备维生素A和类胡萝卜素的新型中间体，其对应于下式（I）：其中X为碳原子的式（I） n等于1或2; R 1，R 2和R 3可以相同或不同，各自独立地表示氢，含有1至4个碳原子的烷基，含有2至11个碳原子的烯基或芳基，每个烷基和烯基可以是直链，支链或环状的，或者R1 并且R 2可以与它们所连接的碳原子一起形成任选被取代的脂环族化合物; 和可以相同或不同的R 4，R 5，R 6，R 7和R 8各自独立地表示氢，含有1至4个碳原子的烷基或含2至10个碳原子的链烯基，每个烷基或烯基是直链的，或者如果含有足够的碳原子数也可以是支链或环状的，或含有6至10个碳原子的芳基，或者R 4，R 5，R 6，R 7和R 8中的任何两个可以一起与它们的碳原子一起形成，，含有3至10个碳原子的亚环烷基，以及其制备方法及其用途。

5. 发明申请

US20090036496A1 Treatment of Stress Urinary Incontinence and Mixed Urinary Incontinence 审中-公开
标题翻译：治疗压力性尿失禁和混合性尿失禁
公开(公告)号：US20090036496A1
公开(公告)日：2009-02-05
申请号：US12083233
申请日：2006-08-28
申请人： Hugues Bienayme , Jacques Ferte
发明人： Hugues Bienayme , Jacques Ferte
IPC分类号： A61K31/4439 , A61P13/10
CPC分类号： A61K31/4439
摘要： Use of a compound corresponding to formula (I): in which R represents hydrogen or a group chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene, cycloalkylidyne and —CONH2 groups, and —COR′ and —COOR′ groups, where R′ is chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene and cycloalkylidyne groups, it being possible for said groups R and/or R′ to be substituted and/or interrupted with —O—, —COO—, —OCO—, —NHCO— or —CONH— functions, or a pharmaceutically acceptable salt of said compound, for obtaining a medicinal product for use in the treatment of stress urinary incontinence and of mixed urinary incontinence.
摘要翻译：使用对应于式（I）的化合物：其中R表示氢或选自烷基，亚烷基，亚烷基，环烷基，亚环烷基，环亚烷基和-CONH 2基团的基团，以及-COR'和-COOR'基团，其中R' 选自烷基，亚烷基，亚烷基，环烷基，亚环烷基和环烷基炔基，所述基团R和/或R'可以被-O - ， - COO - ， - OCO - ， - NHCO取代和/ - 或-CONH-官能团，或所述化合物的药学上可接受的盐，用于获得用于治疗压力性尿失禁和混合性尿失禁的药物。

6. 发明申请

US20080293774A1 Treatment of the Symptoms of Bladder Irritation 审中-公开
标题翻译：治疗膀胱刺激症状
公开(公告)号：US20080293774A1
公开(公告)日：2008-11-27
申请号：US12083246
申请日：2006-08-28
申请人： Hugues Bienayme , Jacques Ferte
发明人： Hugues Bienayme , Jacques Ferte
IPC分类号： A61K31/444 , A61P13/10
CPC分类号： A61K31/4439
摘要： Use of a compound corresponding to formula (I), for obtaining a medicinal product for use in the treatment of the symptoms of bladder irritation.
摘要翻译：使用相应于式（I）的化合物，获得用于治疗膀胱刺激症状的药用产品。

7. 发明授权

US5663459A Intermediates for the preparation of vitamin A and carotenoids and process for their preparation 失效
标题翻译：用于制备维生素A和类胡萝卜素的中间体及其制备方法
公开(公告)号：US5663459A
公开(公告)日：1997-09-02
申请号：US473226
申请日：1995-06-07
申请人： Hugues Bienayme , Pierre Meilland
发明人： Hugues Bienayme , Pierre Meilland
IPC分类号： C07C33/14 , C07C49/21 , C07C403/00 , C07C403/06 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/14 , C07C403/16 , C07C403/20
CPC分类号： C07C403/14 , C07C403/02 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/16 , C07C403/20 , C07B2200/09 , C07C2101/16
摘要： The present invention relates to novel intermediates for the preparation of vitamin A and carotenoids corresponding to the formula (II): ##STR1## in which A represents a hydrogen or an alkyl, alkenyl or alkoxy group containing 1 to 4 carbon atoms, and X represents a carbon atom, and to a process for their preparation and their use, and further relates to compounds for preparing intermediates of formula (II) corresponding to the formula (III): ##STR2## in which R represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkylcarbonyl, alkenylcarbonyl, alkoxyalkyl or alkoxyalkenyl group in which the alkyl groups have 1 to 10 carbon atoms and the alkenyl groups have 2 to 10 carbon atoms, each of said groups being linear or branched and each being substituted or unsubstituted.
摘要翻译：本发明涉及用于制备对应于式（II）的维生素A和类胡萝卜素的新型中间体：其中A表示氢或含有1至4个碳原子的烷基，烯基或烷氧基，并且X表示碳原子，并涉及其制备方法及其应用，还涉及制备对应于式（III）的式（II）的中间体的化合物：其中R表示氢原子，碳原子数1〜10的烷基，碳原子数2〜10的烯基，烷基，碳原子数1〜10的烷基羰基，链烯基羰基，烷氧基烷基或烷氧基烯基，烯基具有2〜 10个碳原子，所述基团各自为直链或支链的，各自为取代或未取代的。

8. 发明授权

US08889711B2 Pyrazolopyridine derivatives as anticancer agent 有权
标题翻译：吡唑并吡啶衍生物作为抗癌剂
公开(公告)号：US08889711B2
公开(公告)日：2014-11-18
申请号：US13500757
申请日：2010-10-13
申请人： Karim Bedjeguelal , Rémi Rabot , El Bachir Kaloun , Patrice Mayer , Arnaud Marchand , Nicolas Rahier , Philippe Schambel , Hugues Bienayme
发明人： Karim Bedjeguelal , Rémi Rabot , El Bachir Kaloun , Patrice Mayer , Arnaud Marchand , Nicolas Rahier , Philippe Schambel , Hugues Bienayme
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , A61K31/44
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.
摘要翻译：本发明涉及以下通式（I）：（式I）及其药学上可接受的盐，其制备方法及其用途，特别是抗癌剂的化合物。

9. 发明授权

US08426437B2 Pyrroloquinoline derivatives and their use as protein kinases inhibitors 有权
标题翻译：吡咯并喹啉衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：US08426437B2
公开(公告)日：2013-04-23
申请号：US11988142
申请日：2006-06-30
申请人： Hugues Bienayme , Antoine Dumoulin , Serge Grisoni , Bachir Kaloun El , Stephane Poigny , Remi Rabot , Rachid Rahali , Eric Tam , Pascaline Klein , Karim Bedjeguelal , Houcine Rahali
发明人： Hugues Bienayme , Antoine Dumoulin , Serge Grisoni , Bachir Kaloun El , Stephane Poigny , Remi Rabot , Rachid Rahali , Eric Tam , Pascaline Klein , Karim Bedjeguelal , Houcine Rahali
IPC分类号： A61K31/437 , C07D487/04 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.
摘要翻译：本发明涉及式I的蛋白激酶抑制剂：其可用于治疗各种疾病，特别是癌症，中枢神经系统的炎症或病症。它还涉及含有根据本发明的化合物及其在治疗中的用途的药物组合物。

10. 发明申请

US20090048304A1 Crystal Form of Besipirdine Chlorhydrate, Process Preparation and Use Thereof 审中-公开
标题翻译：贝西地平氯化钙的晶体形式，工艺制备及其用途
公开(公告)号：US20090048304A1
公开(公告)日：2009-02-19
申请号：US12223602
申请日：2007-02-20
申请人： Hugues Bienayme , Jacques Ferte
发明人： Hugues Bienayme , Jacques Ferte
IPC分类号： C07D401/12 , A61K31/4439 , A61P13/10
CPC分类号： C07D401/12
摘要： Crystal form of besipirdine chlorhydrate (Form I) corresponding to the Formula (A) below: the aforementioned form being characterized at least by one of the following physico-chemical properties: a) In FTIR, it displays at least the following absorption bands of the infrared spectrum: 778, 1198, 1121, but not the following absorption bands of the infrared spectrum: 3395, 1583, 732, the aforementioned bands being expressed in cm−1 at ±5 cm−1; b) In PXRD, it shows at least the following reflections, which are the most intense ones but whose intensity hereafter is given for information only: Formula (II) c) In DSC, it displays at least an endothermic peak at 187.3±2.0° C. using 5° C./min scanning conditions, and a fusion enthalpy ΔH of 130.4±2.0 J/g. The invention also relates to the processes used for the preparation of form I as well as its applications in urology.
摘要翻译：对应于下式（A）的水合形式的苦参碱水合物（形式I）：上述形式的特征在于至少具有下列物理化学性质之一：a）在FTIR中，它显示至少以下吸收带红外光谱：778,1198,1121，但不是红外光谱的以下吸收带：3395,1583,732，上述条带以±5cm -1的cm-1表示; b）在PXRD中，至少显示以下反射，其最强烈的反射强度，但其强度仅供参考：式（II）c）在DSC中，至少显示187.3±2.0°的吸热峰 C.使用5℃/ min扫描条件，熔融焓DeltaH为130.4±2.0J / g。本发明还涉及用于制备形式I的方法及其在泌尿学中的应用。

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