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11. 发明授权

US5679693A 1-azoniabicyclo�2.2.1!heptanes, method of preparing them and pharmaceutical compositions in which they are present 失效
标题翻译： 1-氮杂双环[2.2.1]庚烷，其制备方法和其中存在的药物组合物
公开(公告)号：US5679693A
公开(公告)日：1997-10-21
申请号：US685489
申请日：1996-07-24
申请人： Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
发明人： Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
IPC分类号： C07D453/02 , C07D487/08 , A61K31/44
CPC分类号： C07D487/08 , C07D453/02
摘要： The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tricyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl;. Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-AZONIABICYCLO�2.2.1!HEPTANE optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.
摘要翻译：本发明涉及式（I）的四元碱性酰胺，其中Ar是任选取代的单，二或三环芳族或杂芳族基团; T是直接键，羟基亚甲基，烷氧基是C1-C4的烷氧基亚甲基或C1-C5-亚烷基; Ar'是未取代的或单取代或多取代的苯基，噻吩基，苯并噻吩基，萘基或吲哚基; R是氢或C 1 -C 4烷基或C 1 -C 4 - ω-烷氧基（C 2 -C 4）烷基或C 2 -C 4 - ω-烷酰氧基（C 1 -C 4）烷基。 Q是氢; 或者Q和R一起形成1,2-亚乙基，1,3-亚丙基或1,4-亚丁基; Am（+）是其中X1，X2和X3与它们所键合的氮原子一起形成任选被苯基或苄基取代的1-亚烷基亚氨基C [2.2.1]庚烷的基团并且A（ - ）是药学上可接受的阴离子。这些化合物可用于制备用于治疗涉及速激肽系统的病理状况的药物。

12. 发明授权

US5583134A 1-azoniabicyclo[2.2.2] octanes and pharmaceutical compositions in which they are present 失效
标题翻译： 1-氮杂双环[2.2.2]辛烷及其存在的药物组合物
公开(公告)号：US5583134A
公开(公告)日：1996-12-10
申请号：US239417
申请日：1994-05-06
申请人： Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
发明人： Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
IPC分类号： C07D453/02 , C07D487/08 , C07D401/12 , A61K31/445
CPC分类号： C07D487/08 , C07D453/02
摘要： The present invention relates to quaternary basic amides of the formula: ##STR1## These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachkinin system.
摘要翻译：本发明涉及下式的四级碱性酰胺：（I）这些化合物可用于制备用于治疗涉及速激肽系统的病理状况的药物。

13. 发明申请

US20110183960A1 THIOPHENE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 有权
标题翻译：噻吩-2-羧酰胺衍生物，其制备方法及其治疗用途
公开(公告)号：US20110183960A1
公开(公告)日：2011-07-28
申请号：US13057043
申请日：2009-07-30
申请人： Francis Barth , Jean-Philippe Ducoux , Patrick Gueule , Murielle Rinaldi-carmona , Arnaud Rouquette
发明人： Francis Barth , Jean-Philippe Ducoux , Patrick Gueule , Murielle Rinaldi-carmona , Arnaud Rouquette
IPC分类号： A61K31/4535 , C07D409/06 , C07D409/14 , A61K31/4545 , A61K31/454 , A61K31/397 , A61P25/00 , A61P25/30 , A61P25/28 , A61P3/00 , A61P3/04 , A61P3/10 , A61P3/06 , A61P29/00 , A61P1/00 , A61P1/04 , A61P1/12 , A61P1/16 , A61P25/16
CPC分类号： C07D409/06 , C07D409/14
摘要： The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n′—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).
摘要翻译：本发明的主题是对应于式（I）的化合物，其中：R 1和R 2与它们所连接的氮原子一起构成含有4至7个原子的饱和杂环基团，其优选被取代; 两个取代基R 3和R 6中的一个是Y-A-R 9基团; Y是氧原子或-S（O）n'-或-OSO 2基团; A是未取代的（C 1 -C 4）亚烷基; R9是-OR19，-CH3，-NR19R20，-CONR19R20，-NR15COR19，-S（O）nR21或-NR13SO2R21基团; -R10是氢原子或（C1-C4）烷基。本发明还涉及式（I）化合物的制备方法和治疗用途。

14. 发明申请

US20080039510A1 (1,5-DIPHENYL-1H-PYRAZOL-3-YL)OXADIAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS 失效
标题翻译：（1,5-二苯基-1H-吡唑-3-基）亚唑衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US20080039510A1
公开(公告)日：2008-02-14
申请号：US11835670
申请日：2007-08-08
申请人： Francis BARTH , Christian CONGY , Patrick GUEULE , Murielle RINALDI-CARMONA , Didier VAN BROECK
发明人： Francis BARTH , Christian CONGY , Patrick GUEULE , Murielle RINALDI-CARMONA , Didier VAN BROECK
IPC分类号： A61K31/42 , A61K31/415 , A61P1/00 , A61P25/00 , C07D231/10 , C07D271/06 , C07D271/10
CPC分类号： C07D413/04
摘要： The invention relates to compounds having formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to a method of preparing said compounds and to the application thereof in therapeutics.
摘要翻译：本发明涉及具有式（I）的化合物：其中R1，R2，R3和R4如本文所定义。本发明还涉及制备所述化合物的方法及其在治疗中的应用。

15. 发明授权

US06951940B2 Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them 失效
标题翻译：哌啶衍生物，其获得方法和含有它们的药物组合物
公开(公告)号：US06951940B2
公开(公告)日：2005-10-04
申请号：US10663124
申请日：2003-09-16
申请人： Jean-Philippe Ducoux , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto
发明人： Jean-Philippe Ducoux , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto
IPC分类号： A61K31/45 , A61K31/4545 , A61P1/00 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/00 , A61P11/08 , A61P13/00 , A61P13/02 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/22 , A61P25/24 , A61P29/00 , A61P37/00 , A61P43/00 , C07D211/00 , C07D211/26 , C07D211/30 , C07D211/34 , C07D267/00 , C07D295/03 , C07D413/06 , C07D401/06 , A61K31/496 , C07D401/14
CPC分类号： C07D211/34 , C07D211/26
摘要： The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.
摘要翻译：本发明涉及下列化合物：以及其与无机或有机酸的盐，其溶剂合物和/或其水合物，其对人NK1 / / SUB具有强亲和力和高选择性物质P的受体。本发明还涉及制备它们的方法，用于制备可用于制备的式（VII）的中间体化合物，含有它们的药物组合物及其保险丝，用于制备用于治疗涉及物质P和人NK 1受体的任何病理学。

16. 发明授权

US06291672B1 Human NK3 receptor-selective antagonist compounds, method for obtaining them and pharmaceutical compositions containing them 失效
标题翻译：人NK3受体选择性拮抗剂化合物，其获得方法和含有它们的药物组合物
公开(公告)号：US06291672B1
公开(公告)日：2001-09-18
申请号：US09437203
申请日：1999-11-09
申请人： Daniel Bichon , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
发明人： Daniel Bichon , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/32 , C07D211/58 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： Compounds of the formula are useful as human NK3 receptor antagonists.
摘要翻译：该化合物可用作人NK3受体拮抗剂

17. 发明授权

US06242637B1 Substituted heterocylic compounds, method of preparing them and pharmaceutical compositions in which they are present 失效
标题翻译：取代的杂环化合物，其制备方法和其中存在的药物组合物
公开(公告)号：US06242637B1
公开(公告)日：2001-06-05
申请号：US09175331
申请日：1998-10-20
申请人： Xavier Emonds-Alt , Isabelle Grossriether , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
发明人： Xavier Emonds-Alt , Isabelle Grossriether , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
IPC分类号： C07C6976
CPC分类号： C07D453/02 , C07C215/28 , C07C215/30 , C07C219/22 , C07C233/18 , C07C255/36 , C07C255/42 , C07C255/43 , C07C271/22 , C07D263/38 , C07D265/32 , C07D309/12 , C07D401/06 , C07D413/06 , C07D413/14 , C07D417/14 , Y02P20/55
摘要： The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.
摘要翻译：本发明涉及下列化合物：A是选自：A1）-O-CO-A2）-CH2-O-CO-A3）-O-CH2-CO-A4）-O-CH2- CH2-A5）-N（R1）-CO-A6）-N（R1）-CO-CO-A7）-N（R1）-CH2-CH2-A8）-O-CH2-其中：R1是氢或（C 1 -C 4） - 烷基; 而Am是含氮杂环。

18. 发明授权

US6124316A Compounds which are specific antagonists of the human NK3 receptor and their use as medicinal products and diagnostic tools 失效
标题翻译：作为人NK3受体的特异性拮抗剂的化合物及其作为药物和诊断工具的用途
公开(公告)号：US6124316A
公开(公告)日：2000-09-26
申请号：US306825
申请日：1999-05-07
申请人： Daniel Bichon , Patrick Gueule , Didier Van Broeck , Xavier Emonds-Alt , Vincenzo Proietto
发明人： Daniel Bichon , Patrick Gueule , Didier Van Broeck , Xavier Emonds-Alt , Vincenzo Proietto
IPC分类号： C07D491/107 , A61K31/00 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/452 , A61K31/4523 , A61P1/00 , A61P9/00 , A61P9/12 , A61P11/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P29/00 , A61P43/00 , C07D211/22 , C07D211/52 , C07D211/56 , C07D211/58 , C07D211/64 , C07D211/70 , C07D401/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D401/04 , C07D211/52 , C07D211/58 , C07D211/70 , C07D401/12 , C07D401/14
摘要： A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.12 group; or R.sub.2 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring;or Ar and R.sub.2, together with the carbon atom to which they are attached, constitute a group of formula: ##STR2## which is NK.sub.3 antagonists.
摘要翻译：下式化合物：其中：Ar表示吡啶-2-基或未被取代或被卤素，甲基或（C 1 -C 4）烷氧基取代的苯基; R1表示甲基; R11表示氢; 或R 1和R 11一起表示 - （CH 2）3 - 基; R2表示羟基; （C1-C7）烷氧基; （C 1 -C 7）酰氧基; 氰基; -NR6R7基团; -NR3COR4基团; -NR3COOR8基团; 一个-NR 3 SO 2 R 9基团; -NR3CONR10R12基团; （C1-C7）酰基; （C1-C7）烷氧基羰基; 一个-CONR10R12组; -CH 2 OH基团; （C1-C7）烷氧基甲基; （C1-C7）酰氧基甲基; （C1-C7）烷基氨基羰氧基甲基; 一个-CH2NR13R14组; 一个-CH2NR3COR4基团; 一个-CH2NR3COOR8基团; 一个-CH2NR3SO2R9组; 一个-CH2NR3CONR10R12组; 或R2构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; 或Ar和R2与它们所连接的碳原子一起构成下式的基团：其是NK3拮抗剂。

19. 发明授权

US5965580A Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them 失效
标题翻译：哌啶衍生物，其获得方法和含有它们的药物组合物
公开(公告)号：US5965580A
公开(公告)日：1999-10-12
申请号：US35823
申请日：1998-03-06
申请人： Nathalie Chabert , Jean-Philippe Ducoux , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
发明人： Nathalie Chabert , Jean-Philippe Ducoux , Xavier Emonds-Alt , Patrick Gueule , Vincenzo Proietto , Didier Van Broeck
IPC分类号： C07D211/14 , A61K31/445 , A61K31/4468 , A61K31/451 , A61P1/00 , A61P1/08 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D211/44 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/76 , C07D413/04 , C07D417/04 , C07D211/72 , C07D211/84 , C07D213/81
CPC分类号： C07D417/04 , C07D211/22 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/76
摘要： Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.
摘要翻译：哌啶衍生物，其用于获得它们的方法和含有它们的药物组合物，其用作神经激肽受体拮抗剂，特别可用于治疗所有物质P-和神经激肽依赖性病理学。

20. 发明授权

US5741910A Compounds which are selective antagonists of the human NK.sub.3 receptor and their use as medicinal products and diagnostic tools 失效
标题翻译：作为人NK3受体的选择性拮抗剂的化合物及其作为药物产品和诊断工具的用途
公开(公告)号：US5741910A
公开(公告)日：1998-04-21
申请号：US607976
申请日：1996-02-29
申请人： Daniel Bichon , Patrick Gueule , Didier Van Broeck , Xavier Emonds-Alt , Vincenzo Proietto
发明人： Daniel Bichon , Patrick Gueule , Didier Van Broeck , Xavier Emonds-Alt , Vincenzo Proietto
IPC分类号： C07D491/107 , A61K31/00 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/452 , A61K31/4523 , A61P1/00 , A61P9/00 , A61P9/12 , A61P11/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P29/00 , A61P43/00 , C07D211/22 , C07D211/52 , C07D211/56 , C07D211/58 , C07D211/64 , C07D211/70 , C07D401/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D211/34
CPC分类号： C07D401/04 , C07D211/52 , C07D211/58 , C07D211/70 , C07D401/12 , C07D401/14
摘要： A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy; R.sub.1 represents a methyl group; R.sub.11 represents hydrogen; or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group; R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.12 group; or R.sub.2 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; or Ar and R.sub.2, together with the carbon atom to which they are attached, constitute a group of formula: ##STR2## as NK.sub.3 antagonists.
摘要翻译：下式的化合物：其中：Ar表示吡啶-2-基或未被取代或被卤素，甲基或（C 1 -C 4）烷氧基取代的苯基; R1表示甲基; R11表示氢; 或R 1和R 11一起表示 - （CH 2）3 - 基; R2表示羟基; （C1-C7）烷氧基; （C1-C7）酰氧基; 氰基; -NR6R7基团; -NR3COR4基团; -NR3COOR8基团; 一个-NR 3 SO 2 R 9基团; -NR3CONR10R12基团; （C1-C7）酰基; （C1-C7）烷氧基羰基; 一个-CONR10R12组; -CH 2 OH基团; （C1-C7）烷氧基甲基; （C1-C7）酰氧基甲基; （C1-C7）烷基氨基羰氧基甲基; 一个-CH2NR13R14组; 一个-CH2NR3COR4基团; 一个-CH2NR3COOR8基团; 一个-CH2NR3SO2R9组; 一个-CH2NR3CONR10R12组; 或R2构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; 或Ar和R 2与它们所连接的碳原子一起构成作为NK3拮抗剂的下式的基团。

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