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1. 发明授权

US07842806B2 Pyridopyrimidone derivatives, preparation thereof, therapeutic use thereof 失效
标题翻译：吡啶并嘧啶衍生物，其制备方法，治疗用途
公开(公告)号：US07842806B2
公开(公告)日：2010-11-30
申请号：US12166431
申请日：2008-07-02
申请人： Pierre Perreaut , Samir Jegham , Bernard Bourrie , Pierre Casellas , Jean-Robert Labrosse , Florence Durand
发明人： Pierre Perreaut , Samir Jegham , Bernard Bourrie , Pierre Casellas , Jean-Robert Labrosse , Florence Durand
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.
摘要翻译：本公开涉及吡啶并[2,3-d]嘧啶酮化合物，其制备方法及其治疗用途，其中所述化合物为通式（I）：以碱的形式或加成盐与其为药学上可接受的，为水合物或溶剂化物形式，也为对映异构体，非对映异构体及其混合物的形式。本公开还涉及制备所述化合物的方法，含有通式（I）化合物的药物组合物以及所述化合物和组合物的治疗用途。

2. 发明授权

US07767681B2 2-Carbamide-4-phenylthiazole derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译： 2-羧酰胺-4-苯基噻唑衍生物，其制备及其治疗用途
公开(公告)号：US07767681B2
公开(公告)日：2010-08-03
申请号：US11649316
申请日：2007-01-03
申请人： Pierre Casellas , Daniel Floutard , Pierre Fraisse , Samir Jegham
发明人： Pierre Casellas , Daniel Floutard , Pierre Fraisse , Samir Jegham
IPC分类号： A61K31/497 , C07D413/14
CPC分类号： C07D417/12 , C07D277/40 , C07D277/46
摘要： The disclosure concerns 2-carbamide-4-phenylthiazole derivatives of general formula (I). The disclosure also concerns pharmaceutical compositions containing a compound of general formula (I) and to processes for preparing and methods of using compounds of general formula (I).
摘要翻译：本公开涉及通式（I）的2-氨基-4-苯基噻唑衍生物。本公开还涉及含有通式（I）化合物的药物组合物及其制备方法和使用通式（I）的化合物的方法。

3. 发明申请

US20100099694A1 2-ANILINO-4-HETEROARYL PYRIMIDINE DERIVATIVES, AND PREPARATION THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS, AND IN PARTICULAR IKK INHIBITORS 审中-公开
标题翻译： 2-苯胺-4-异喹啉衍生物及其作为药物，药物组合物和特定IKK抑制剂的制剂
公开(公告)号：US20100099694A1
公开(公告)日：2010-04-22
申请号：US12496107
申请日：2009-07-01
申请人： Didier BABIN , Monsif BOUABOULA , Pierre CASELLAS , Serge MIGNANI , Jean-Flaubert NGUEFACK , Jean WAGNON
发明人： Didier BABIN , Monsif BOUABOULA , Pierre CASELLAS , Serge MIGNANI , Jean-Flaubert NGUEFACK , Jean WAGNON
IPC分类号： A61K31/506 , C07D401/14 , C12N9/99 , A61P29/00 , A61P3/10 , A61P35/00
CPC分类号： C07D401/14
摘要： The disclosure relates to a compound of formula (I): wherein R, R2, R3, R4, R5, z, D and W are as defined in the specification, to compositions containing them, to processes for preparing them, and to their use in the treatment or prevention of conditions capable of being modulated by the inhibition of the activity of protein kinases.
摘要翻译：本公开涉及式（I）化合物：其中R，R 2，R 3，R 4，R 5，Z，D和W如说明书中所定义，含有它们的组合物，其制备方法及其用途在治疗或预防能够通过抑制蛋白激酶活性调节的条件下进行。

4. 发明申请

US20090233923A1 PYRIDO-PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权
标题翻译：吡啶二吡啶衍生物，其制备方法及其治疗方法
公开(公告)号：US20090233923A1
公开(公告)日：2009-09-17
申请号：US12415256
申请日：2009-03-31
申请人： Bernard Bourrie , Pierre Casellas , Samir Jegham , Pierre Perreaut
发明人： Bernard Bourrie , Pierre Casellas , Samir Jegham , Pierre Perreaut
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04
摘要： The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
摘要翻译：本公开涉及通式（I）的吡啶并[2,3-d]嘧啶衍生物及其制备方法及其治疗应用：及其酸加成盐，水合物和溶剂化物，以及对映异构体，非对映异构体和混合物的形式其中。本公开还涉及制备所述衍生物的方法，含有通式（I）的化合物的药物组合物及其治疗用途。

5. 发明申请

US20090156574A1 2-ACYLAMINO-4-PHENYLTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF 失效
标题翻译： 2-氨基亚氨基-4-苯基噻唑衍生物，其制备方法及其应用
公开(公告)号：US20090156574A1
公开(公告)日：2009-06-18
申请号：US12360568
申请日：2009-01-27
申请人： Pierre CARAYON , Pierre CASELLAS , Daniel FLOUTARD , Pierre FRAISSE , Samir JEGHAM , Bernard LABEEUW
发明人： Pierre CARAYON , Pierre CASELLAS , Daniel FLOUTARD , Pierre FRAISSE , Samir JEGHAM , Bernard LABEEUW
IPC分类号： C07D411/02 , C07D277/38 , A61K31/497 , A61K31/427 , A61K31/535 , A61P3/00 , A61P9/00 , A61P31/12 , A61K31/4545 , A61K31/445 , A61K31/425
CPC分类号： C07D401/04 , C07D277/46 , C07D405/12 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/08
摘要： The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.
摘要翻译：本发明涉及通式（I）的2-酰基氨基-4-苯基噻唑衍生物：其药学上可接受的酸加成盐，该衍生物的水合物或溶剂合物或其药学上可接受的酸加成盐，其中间体，其制备方法，及其治疗应用。

6. 发明授权

US07456193B2 Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics 失效
标题翻译：吡啶并吲哚酮衍生物在3位被杂环基取代，其制备及其在治疗中的应用
公开(公告)号：US07456193B2
公开(公告)日：2008-11-25
申请号：US11109121
申请日：2005-04-19
申请人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux
发明人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux
IPC分类号： A61K31/437 , C07D487/04 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group of general formula (I): in which: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a thienyl mono- or polysubstituted by a methyl group; or a monocyclic or bicyclic heterocyclic radical chosen from: a pyridyl, an N-oxidopyridinio, a pyrazolyl, an (N-phenyl)pyrazolyl, an (N-halophenyl)pyrazolyl, a furyl, an indolyl, an (N-benzyl)indolyl, an (N-halobenzyl)indolyl, a benzothienyl or a benzofuryl, the said radicals being unsubstituted or substituted one or more times by a halogen atom or a methyl or methoxy group; R4 and R5 are identical or different and each independently represent a hydrogen or halogen atom or a hydroxyl, hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, C1-C4)alkoxy, (C1-C4)alkoxycarbonyl or cyano group. Preparation process and application in therapeutics.
摘要翻译：本发明涉及通式（I）的杂环基在3-位上取代的吡啶并吲哚酮衍生物：其中：R 1表示氢原子或（C 1〜（C 1 -C 4）烷基; R 2表示氢原子或（C 1 -C 4 -C 4）烷基; R 3表示被甲基单取代或多取代的噻吩基; 或选自以下的单环或双环杂环基：吡啶基，N-氧化吡啶基，吡唑基，（N-苯基）吡唑基，（N-卤代苯基）吡唑基，呋喃基，吲哚基，（N-苄基）吲哚基，（N-卤代苄基）吲哚基，苯并噻吩基或苯并呋喃基，所述基团是未取代的或被卤素原子或甲基或甲氧基取代一次或多次; R 4和R 5相同或不同，并且各自独立地表示氢或卤素原子或羟基，羟甲基，（C 1 -C 3 - （C 1 -C 4）烷基，三氟甲基，C 1 -C 4烷氧基，（C 1 -C 4 - 4）烷氧基羰基或氰基。制剂工艺及其在治疗中的应用

7. 发明申请

US20070259847A1 2-Amido-4-phenylthiazole Derivatives, The Preparation And The Therapeutic Use Thereof 失效
标题翻译： 2-酰氨基-4-苯基噻唑衍生物，其制备及其治疗用途
公开(公告)号：US20070259847A1
公开(公告)日：2007-11-08
申请号：US11736770
申请日：2007-04-18
申请人： Pierre CASELLAS , Daniel FLOUTARD , Pierre FRAISSE , Samir JEGHAM
发明人： Pierre CASELLAS , Daniel FLOUTARD , Pierre FRAISSE , Samir JEGHAM
IPC分类号： A61K31/454 , A61K31/427 , C07D417/02
CPC分类号： C07D417/12 , C07D417/14
摘要： The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below: in which R1, R2, R3, Y, m, n, and p are as defined in the disclosure; as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic use thereof.
摘要翻译：本公开涉及以下通式（I）的2-氨基-4-苯基噻唑衍生物：其中R 1，R 2，R 3， >，Y，m，n和p如本公开中所定义; 以及它们的异构体，盐和溶剂合物，含有它们的药物组合物及其治疗用途。

8. 发明申请

US20050272760A1 Use of pyridoindolone derivatives for the preparation of medicinal products 有权
标题翻译：吡啶并吲哚酮衍生物用于制备药用产品
公开(公告)号：US20050272760A1
公开(公告)日：2005-12-08
申请号：US11204275
申请日：2005-08-15
申请人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq
发明人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq
IPC分类号： A61K45/00 , A61K31/437 , A61K31/519 , A61K45/06 , A61P35/00 , A61P43/00 , C07D471/04 , A61K31/4745
CPC分类号： A61K31/437 , A61K31/435 , A61K45/06 , A61K2300/00
摘要： The invention relates to a novel use of compounds of formula: for the preparation of medicinal products that are useful as anticancer agents.
摘要翻译：本发明涉及式的化合物的新用途：用于制备可用作抗癌剂的药用产品。

9. 发明授权

US06689797B2 Tetrahydropyridines, preparation method and pharmaceutical compositions containing same 失效
标题翻译：四氢吡啶类，制备方法和含有它们的药物组合物
公开(公告)号：US06689797B2
公开(公告)日：2004-02-10
申请号：US10169528
申请日：2002-10-15
申请人： Marco Baroni , Bernard Bourrie , Rosanna Cardamone , Pierre Casellas
发明人： Marco Baroni , Bernard Bourrie , Rosanna Cardamone , Pierre Casellas
IPC分类号： A61K3144
CPC分类号： C07D405/06 , C07D409/06
摘要： The present invention relates to compounds of formula (I): in which R1 represents a hydrogen or halogen atom, or a group CF3; R2 and R3 represent, independently, a hydrogen atom or a methyl group; n and n′ each represent, independently, 0 or 1; * represents the positions of attachment; A represents N or CH; X represents a sulfur or oxygen atom; R4 and R5 represent, independently, a hydrogen atom or a (C1-C6) alkyl group; and also their salts or solvates, to a method for the preparation thereof and to the pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物：其中R 1表示氢或卤素原子或基团CF 3; R 2和R 3独立地表示氢原子或甲基; n和n'各自独立地表示， 0或1; *表示连接位置; A表示N或CH; X表示硫或氧原子; R4和R5独立地表示氢原子或（C1-C6）烷基;以及它们的盐或溶剂合物，其制备方法和含有它们的药物组合物。

10. 发明授权

US5925768A 3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity 失效
标题翻译：具有大麻素受体亲和力的3-吡唑酰胺衍生物
公开(公告)号：US5925768A
公开(公告)日：1999-07-20
申请号：US77767
申请日：1998-06-03
申请人： Francis Barth , Pierre Casellas , Joseph Millan , Didier Oustric , Murielle Rinaldi , Martine Sarran
发明人： Francis Barth , Pierre Casellas , Joseph Millan , Didier Oustric , Murielle Rinaldi , Martine Sarran
IPC分类号： A61K31/00 , A61K31/415 , A61P37/00 , A61P37/02 , A61P43/00 , C07D231/14
CPC分类号： C07D231/14
摘要： The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.sub.1 -C.sub.4)alkyl or a trifluoromethyl;or else R.sub.4 is hydrogen and R.sub.5 and w.sub.6 together constitute an ethylene or trimethylene radical; andR.sub.6 is hydrogen, a (C.sub.1 -C.sub.4)alkyl, a fluorine, a hydroxyl, a (C.sub.1 -C.sub.5)alkoxy, a (C.sub.1 -C.sub.5)alkylthio, a hydroxy(C.sub.1 -C.sub.5)alkoxy, a cyano, a (C.sub.1 -C.sub.5)alkylsulfinyl or a (C.sub.1 -C.sub.5)alkylsulfonyl with the proviso that when the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5 and/or g.sub.6 are a (C.sub.1 -C.sub.4)alkyl R.sub.6 is only hydrogen;to a process for their preparation and to the pharmaceutical compositions in which they are present.These compounds have a good affinity for the peripheral cannabinoid receptors.
摘要翻译： PCT No.PCT / FR96 / 01953 Sec。 371日期1998年6月3日第 102（e）1998年6月3日PCT PCT 1996年12月6日PCT公布。公开号WO97 / 21682 日期：1997年6月19日本发明涉及下式的化合物，其中：X 1为基团-NR 1 R 2或基团-OR 2; g2，g3，g4，g5，g6和w2，w3，w4，w5，w6相同或不同，各自独立地为氢，卤素原子，（C1-C4）烷基，（C1-C4）烷氧基，三氟甲基，硝基或（C 1 -C 4）烷硫基，条件是至少一个取代基g2，g3，g4，g5，g6和至少一个取代基w2，w3，w4，w5，w6是其他比氢; R1是氢或（C1-C4）烷基; R 2是未被取代或被选自卤素原子，（C 1 -C 4）烷基和（C 1 -C 4）烷氧基的取代基单取代或多取代的非芳族（C 3 -C 15）碳环基团; R3是氢或基团-CH2R6; 和R 4和R 5各自独立地为氢，（C 1 -C 4）烷基或三氟甲基; 或者R4是氢，R5和w6一起构成乙烯或三亚甲基; （C 1 -C 5）烷氧基，（C 1 -C 5）烷硫基，羟基（C 1 -C 5）烷氧基，氰基，（C 1 -C 5）烷氧基， -C 5）烷基亚磺酰基或（C 1 -C 5）烷基磺酰基，条件是当取代基g2，g3，g4，g5和/或g6为（C1-C4）烷基时，R6仅为氢; 涉及其制备方法及其存在的药物组合物。这些化合物对外周大麻素受体具有良好的亲和力。

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