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1. 发明授权

US06331549B1 1-aminoethylquinoline derivatives for treating urinary incontinence 失效
标题翻译：用于治疗尿失禁的1-氨基乙基喹啉衍生物
公开(公告)号：US06331549B1
公开(公告)日：2001-12-18
申请号：US09831442
申请日：2001-05-09
申请人： Christophe Philippo , Patrick Mougenot , Gérard Defosse , Alain Braun , Philippe Bovy
发明人： Christophe Philippo , Patrick Mougenot , Gérard Defosse , Alain Braun , Philippe Bovy
IPC分类号： C07D21514
CPC分类号： C07D215/14 , C07D215/18 , C07D219/02
摘要： The invention relates to 1-aminoethylquinoline derivatives, to pharmaceutical compositions containing them, to therapeutic methods of using them and to processes for preparing them.
摘要翻译：本发明涉及1-氨基乙基喹啉衍生物，含有它们的药物组合物，其使用方法及其制备方法。

2. 发明授权

US06200991B1 Imidazole derivatives, preparation and therapeutic application thereof 失效
标题翻译：咪唑衍生物，其制备和治疗应用
公开(公告)号：US06200991B1
公开(公告)日：2001-03-13
申请号：US09554138
申请日：2000-06-19
申请人： Gilles Courtemanche , Gérard DeFosse , Olivier Crespin , Philippe Bovy
发明人： Gilles Courtemanche , Gérard DeFosse , Olivier Crespin , Philippe Bovy
IPC分类号： A61K31454
CPC分类号： C07D451/02 , C07D401/12 , C07D401/14
摘要： A compound of formula (I) the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M3 muscarinic and/or S—HT4 serotoninergic receptors.
摘要翻译：式（I）化合物制备式（I）化合物的方法，其药物组合物和治疗与M3毒蕈碱和/或S-HT4血清素能受体相关的疾病的方法。

3. 发明授权

US6063810A 2-aminoethyl-benzofuran derivatives, preparation thereof and therapeutical use thereof 失效
标题翻译： 2-氨基乙基 - 苯并呋喃衍生物，其制备及其治疗用途
公开(公告)号：US6063810A
公开(公告)日：2000-05-16
申请号：US125947
申请日：1998-08-31
申请人： Christophe Philippo , Gilles Courtemanche , Eykmar Fett , Marie Claire Orts , Philippe Bovy , Stephen Eric O'Connor , Anne Marie Galzin
发明人： Christophe Philippo , Gilles Courtemanche , Eykmar Fett , Marie Claire Orts , Philippe Bovy , Stephen Eric O'Connor , Anne Marie Galzin
IPC分类号： A61K31/00 , A61K31/34 , A61K31/343 , A61K31/395 , A61K31/397 , A61K31/443 , A61K31/445 , A61K31/4453 , A61P1/00 , A61P9/00 , A61P9/14 , A61P11/00 , A61P11/02 , A61P25/06 , C07D307/79 , C07D307/85 , C07D307/91 , C07D405/06
CPC分类号： C07D307/79
摘要： Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.4 taken together form a C.sub.2-6 cycloalkyl or C.sub.3-6 cycloalkenyl ring, e.g., piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures;, as well as pharmaceutically acceptable acid addition salts thereof. The compounds may be used in therapy.
摘要翻译： PCT No.PCT / FR97 / 00383 Sec。 371日期1998年8月31日 102（e）日期1998年8月31日PCT 1997年3月5日PCT公布。公开号WO97 / 32870 日期：1997年9月12日，式（I）的化合物，其中A为氢原子或羟基; B是氢原子或C 1-8烷基，C 1-8烯基，C 1-8氟烷基或C 1-8全氟烷基; R 1，R 2和R 5各自相同或不同，为氢原子，卤素如氯，溴或氟，C 1-8烷基，C 1-8烯基，C 3-8环烷基，C 3-8环烯基，C 6，C 10或C 14芳基，C 1-6烷氧基羰基，C 1-6羟基烷基，C 1-6烷氧基烷基，C 1-6烷氧基，C 1-8氟代烷基或C 1-8全氟烷基，或者R 1和R 2一起形成C 3-8 环烷基，C3-8环烯基或C6，C10或C14芳基环，其中R1和R2均为氢的化合物; R 3和R 4各自相同或不同，为氢原子或C 1-8烷基，C 1-8烯基，C 3-8环烷基或C 3-8环烯基，或者R 3和R 4一起形成C2- 6环烷基或C 3-6环烯基环，例如哌啶基，氮杂环丁烷基或吡咯烷基; 以对映异构体，非对映异构体或其混合物的形式，包括外消旋混合物，以及其药学上可接受的酸加成盐。该化合物可用于治疗。

4. 发明授权

US07659298B2 Pyrazole derivatives and use thereof as orexin receptor antagonists 有权
标题翻译：吡唑衍生物及其作为食欲素受体拮抗剂的用途
公开(公告)号：US07659298B2
公开(公告)日：2010-02-09
申请号：US11425583
申请日：2006-06-21
申请人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
发明人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
IPC分类号： A61K31/4155 , A61K31/44 , C07D231/10 , C07D401/14
CPC分类号： C07D409/04 , C07D231/16 , C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
摘要翻译：本发明涉及食欲素受体拮抗剂通式（I）化合物及其异构体，盐和溶剂合物，其含有它们的药物组合物及其治疗应用。

5. 发明申请

US20110059964A1 PYRAZOLE DERIVATIVES AND USE THEREOF AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡唑衍生物及其作为OREXIN受体拮抗剂的用途
公开(公告)号：US20110059964A1
公开(公告)日：2011-03-10
申请号：US12699231
申请日：2010-02-03
申请人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
发明人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
IPC分类号： A61K31/415 , C07D401/12 , C07D231/16 , C07D471/04 , C07D405/12 , C07D413/12 , C07D403/12 , C07D401/14 , C07D413/14 , A61K31/4709 , A61K31/4375 , A61K31/423 , A61K31/428 , A61K31/498 , A61K31/5377 , C07D401/04 , C07D413/06 , C07D409/04 , C07F9/54 , A61P3/04 , A61P3/10 , A61P25/00 , A61P25/24 , A61P25/22 , A61P15/00 , A61P29/00 , A61P11/00 , A61P9/00
CPC分类号： C07D409/04 , C07D231/16 , C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
摘要翻译：本发明涉及食欲素受体拮抗剂通式（I）化合物及其异构体，盐和溶剂合物，其含有它们的药物组合物及其治疗应用。

6. 发明申请

US20080161310A1 FLUOROPYRROLIDINES HAVING DIPEPTIDYL PEPTIDASE ENZYME INHIBITORY ACTIVITY 失效
标题翻译：具有脯氨酸肽酶抑制活性的氟罗哌啶
公开(公告)号：US20080161310A1
公开(公告)日：2008-07-03
申请号：US12042595
申请日：2008-03-05
申请人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
IPC分类号： A61K31/53 , C07D239/24 , C07D471/04 , C07D401/04 , C07D251/02 , A61P3/10 , A61K31/506 , A61K31/519 , A61K31/501
CPC分类号： C07D451/04 , C07D207/16 , C07D211/58 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/14
摘要： The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
摘要翻译：本发明涉及含有氟原子的新的具有通式（I）的DPP-IV酶抑制剂。

7. 发明授权

US07348327B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07348327B2
公开(公告)日：2008-03-25
申请号：US10507005
申请日：2003-03-04
申请人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
IPC分类号： C07D401/04 , C07D403/04 , C07D211/06 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501
CPC分类号： C07D451/04 , C07D207/16 , C07D211/58 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/14
摘要： The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
摘要翻译：本发明涉及含有氟原子的新的具有通式（I）的DPP-IV酶抑制剂。

8. 发明授权

US07655663B2 Fluoropyrrolidines having dipeptidyl peptidase enzyme inhibitory activity 失效
标题翻译：具有二肽基肽酶抑制活性的氟代吡咯烷
公开(公告)号：US07655663B2
公开(公告)日：2010-02-02
申请号：US12042595
申请日：2008-03-05
申请人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
IPC分类号： A61K31/497 , A61K31/501 , A61K31/506 , C07D239/02 , C07D241/02
CPC分类号： C07D451/04 , C07D207/16 , C07D211/58 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/14
摘要： The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
摘要翻译：本发明涉及含有氟原子的新的具有通式（I）的DPP-IV酶抑制剂。

9. 发明申请

US20060276487A1 New compounds useful for DPP-IV enzyme inhibition 失效
标题翻译：用于DPP-IV酶抑制的新化合物
公开(公告)号：US20060276487A1
公开(公告)日：2006-12-07
申请号：US11364154
申请日：2006-02-28
申请人： Peter Aranyi , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Zoltan Kapui , Edit Susan , Tibor Szabo , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Zoltan Kapui , Edit Susan , Tibor Szabo , Katalin Urban-Szabo , Marton Varga
IPC分类号： A61K31/506 , A61K31/4745 , A61K31/4709 , A61K31/4439 , A61K31/401 , C07D403/02 , C07D471/02
CPC分类号： C04B35/632 , C07D207/16 , C07D213/74 , C07D215/38 , C07D221/22 , C07D231/38 , C07D241/20 , C07D253/06 , C07D261/14 , C07D277/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07D471/04
摘要： The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).
摘要翻译：本发明涉及具有二肽基肽酶IV酶抑制活性的通式（I）的新化合物，其药物组合物，使用所述化合物的方法，其制备方法和通式（II），（IV）的中间体），（V），（VII），（VIII）和（IX）。

10. 发明申请

US20050176731A1 Oxophenyl-cyclohexyl-propanolamine derivatives, production and use therof in therapeutics 失效
标题翻译：氧代苯基 - 环己基 - 丙醇胺衍生物，生产和使用治疗学
公开(公告)号：US20050176731A1
公开(公告)日：2005-08-11
申请号：US10515093
申请日：2003-05-26
申请人： Philippe Bovy , Roberto Cecchi , Tiziano Croci , Olivier Venier
发明人： Philippe Bovy , Roberto Cecchi , Tiziano Croci , Olivier Venier
IPC分类号： C07D295/18 , A61K31/40 , A61K31/4035 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/472 , A61K31/495 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P13/02 , A61P13/10 , A61P15/00 , A61P15/04 , A61P15/06 , A61P17/02 , A61P25/18 , A61P25/24 , A61P27/06 , A61P29/00 , A61P43/00 , C07D207/16 , C07D209/44 , C07D211/16 , C07D211/22 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/64 , C07D217/02 , C07D221/20 , C07D295/192 , C07D471/10 , A61K31/4747
CPC分类号： C07D221/20 , C07D207/16 , C07D209/44 , C07D211/16 , C07D211/22 , C07D211/58 , C07D211/62 , C07D295/192
摘要： The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1表示H，（C 1 -C 4）烷基，-CO（C 1 -C 4）烷基，（C 1 -C 4）烷基苯基或 - CO-苯基，所述苯基任选被取代，R 2表示H，卤素原子，-S（O）z R 3 R 3，，-NHSO 2 R 3，-NHSO 2 - 苯基或-NHSO 2 - （C 1 -C 4）烷基苯基，其中z等于0,1或2，并且其中R 3表示（C 1 -C 4）烷基，所述苯基任选被取代; A选自其中n等于0,1或2，R 4和R 5代表H，（C 1 -C 4）烷基，羟基，氰基，苯基，苄基，哌啶基，-CONH 2，-CO-苯基，-COOR 3，-CH（苯基）（OH）和-C（苯基）2 （OH）基团，或R 4和R 5一起形成任选取代的6元芳环，R 6表示 H，（C 1 -C 4）烷基，苯基或苄基，B表示任选与苯基或任选取代的稠合的5或6元含氮杂环或稠环; 它们的加成盐; 其制备方法及其治疗应用。

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