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1. 发明申请

US20080167318A1 Pharmaceutically active pyrrolidine derivatives 审中-公开
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US20080167318A1
公开(公告)日：2008-07-10
申请号：US11783341
申请日：2007-04-09
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
IPC分类号： A61K31/497 , A61K31/40 , A61K31/403 , A61P15/06 , C07D209/56 , C07D455/02 , C07D403/02 , C07D207/02 , A61P15/02 , A61K31/47
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2—, —SO2NH—, —CH2—, B is either a group —C═O)—NR8R9 or represents a heterocyclic residue having the formula wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式I的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式I的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法。其中X选自CR 6，S 6，S 6，N 6，R 6，O 6， > 7 ; A选自 - （CO） - ， - （CO）-O-，-C（-NH） - ， - （CO）-NH-， - （CS）-NH， 2 - ， - SO 2 NH - ， - CH 2 - ， - B是基团-CO）-NR 8 - 或者表示具有下式的杂环残基：其中Q是NR 10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

2. 发明授权

US07211601B2 Pharmaceutically active pyrrolidine derivatives 有权
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US07211601B2
公开(公告)日：2007-05-01
申请号：US10239912
申请日：2001-03-20
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
IPC分类号： A61K31/40 , C07D207/10 , C07D207/14
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22-, —SO2NH—, —CH2-, B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式（I）的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法，其中X选自CR 6 R 7，NOR 6，NNR 6 R 7; A选自 - （CO） - ， - （CO）-O - ， - C（-NH） - ， - （CO）-NH-， - （CS）-NH，-SO 2 2-， SO 2 NH - ， - CH 2 - ，B为基团 - （CO）-NR 8 R 9，或表示具有式（a）的杂环残基，其中Q为NR10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

3. 发明授权

US07018988B2 Pharmaceutically active pyrrolidine derivatives as Bax inhibitors 失效
标题翻译：作为Bax抑制剂的药物活性吡咯烷衍生物
公开(公告)号：US07018988B2
公开(公告)日：2006-03-28
申请号：US10240000
申请日：2001-03-20
申请人： Serge Halazy , Anna Quattropani , Agnes Bombrun , Mattias Schwarz , Russel Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Agnes Bombrun , Mattias Schwarz , Russel Thomas , Anthony Baxter
IPC分类号： A01N57/00 , A61K31/675
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CR R , NOR , NNR R ; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2—, —SO2NH—; —CH2—; B is either a group —(C═O)—NR R or represents a heterocyclic residue having the formula (II) wherein Q is NR , O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式（I）的新的取代的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式（I）的吡咯烷衍生物可用于治疗和/或预防神经退行性疾病，与多组胺胺束相关的疾病，癫痫，缺血，不育症，心血管疾病，肾脏缺氧，肝炎和艾滋病。所述吡咯烷衍生物显示相对于细胞死亡激动剂Bax和/或导致Bax的活化途径的调节和最显着的下调至抑制活性，因此可以阻止细胞色素（c）的释放。本发明还涉及新的药学活性取代的吡咯烷衍生物及其制备方法，其中X选自O，S，CR 6 R 7，NOR 6，NNR <6> R 7; A选自 - （CO） - ， - （CO）-O - ， - C（-NH） - ， - （CO）-NH-， - （CS）-NH，-SO 2 - SO2NH-; -CH 2 - ; B是基团 - （C-O）-NR 8 R 9，或表示具有式（II）的杂环残基，其中Q是NR 10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

4. 发明授权

US06770656B2 Amine derivatives for the treatment of apoptosis 失效
标题翻译：胺衍生物用于治疗凋亡
公开(公告)号：US06770656B2
公开(公告)日：2004-08-03
申请号：US10182745
申请日：2002-12-26
申请人： Serge Halazy , Matthias Schwarz , Bruno Antonsson , Agnes Bombrun , Jean-Claude Martinou , Dennis Church
发明人： Serge Halazy , Matthias Schwarz , Bruno Antonsson , Agnes Bombrun , Jean-Claude Martinou , Dennis Church
IPC分类号： C07D21304
CPC分类号： C07D217/26 , C07B2200/07 , C07C237/22 , C07C2601/14 , C07D207/16 , C07D211/60 , C07D277/06
摘要： The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.
摘要翻译：本发明涉及特别用作药物活性化合物的取代胺衍生物，以及含有式（I）胺衍生物的药物制剂。所述取代的胺衍生物是Bax功能和/或活化的有效调节剂，特别是抑制剂。本发明还涉及新型取代的胺衍生物及其制备方法。

5. 发明授权

US07417058B2 Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases 失效
标题翻译：药物活性苯并磺酰胺衍生物作为蛋白质垃圾酶的抑制剂
公开(公告)号：US07417058B2
公开(公告)日：2008-08-26
申请号：US10381197
申请日：2001-09-27
申请人： Serge Halazy , Dennis Church , Stephen J. Arkinstall , Marco Biamonte , Montserrat Camps , Jean-Pierre Gotteland , Thomas Rueckle
发明人： Serge Halazy , Dennis Church , Stephen J. Arkinstall , Marco Biamonte , Montserrat Camps , Jean-Pierre Gotteland , Thomas Rueckle
IPC分类号： A61K31/445 , A61P25/00 , A61P37/00 , C07D211/96
CPC分类号： C07D211/96
摘要： The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.
摘要翻译：本发明涉及式I的苯并磺酰胺衍生物，其特别用作药物活性化合物，以及含有该苯磺酰胺衍生物的药物制剂。所述苯磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效和选择性的抑制剂。本发明还涉及新型苯磺酰脲衍生物及其制备方法（一世）。根据本发明的式I化合物是合适的制药剂，其中Ar 1是取代或未取代的芳基或杂芳基。 X是O或S，优选O.R1是氢或C1-C6-烷基，优选H.R2是氢，-COOR3，-CONR3R3'，OH，被OH基取代的C1-C4烷基，肼基羰基，硫酸酯，磺酸酯，胺或铵盐; n为0或1，优选为1。

6. 发明授权

US06589953B2 Indole derivatives as 5-HT1B and 5-HT1D agonists 失效
公开(公告)号：US06589953B2
公开(公告)日：2003-07-08
申请号：US09903469
申请日：2001-07-11
申请人： Michel Perez , Serge Halazy
发明人： Michel Perez , Serge Halazy
IPC分类号： C07D40312
CPC分类号： C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention concerns novel indole piperazine derivatives of formula (I). It also concerns a method for preparing said compounds and their use as therapeutically active substances, in particular for treating or preventing diseases related to the disfunction of 5-HT1-like receptors.

7. 发明授权

US5789412A Piperazides derived from arylpiperazine, processes for their preparation, their use as medicaments and pharmaceutical compositions comprising them 失效
标题翻译：衍生自芳基哌嗪的哌嗪，其制备方法，它们作为药物的用途和包含它们的药物组合物
公开(公告)号：US5789412A
公开(公告)日：1998-08-04
申请号：US776057
申请日：1997-01-20
申请人： Serge Halazy , Catherine Jorand , Peter Pauwels
发明人： Serge Halazy , Catherine Jorand , Peter Pauwels
IPC分类号： C07D295/16 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/495 , A61P25/00 , C07D213/38 , C07D275/02 , C07D277/20 , C07D277/32 , C07D295/185 , C07D295/205 , C07D295/215 , C07D317/66 , C07D319/18 , C07D401/14 , C07D403/12
CPC分类号： C07D295/185 , C07D295/205 , C07D295/215 , C07D317/66 , C07D319/18
摘要： Novel 5HT receptor antagonists of general formula (I) ##STR1## in which Ar.sub.1 and Ar.sub.2 are aromatic residues, X is O, NH, CH.sub.2 O, or CH.sub.2 NH, and R.sub.1 is hydrogen or linear or branched alkyl comprising 1-6 carbon atoms, as well as their salts, hydrates, solvates, and physiologically-acceptable bioprecursors for their therapeutic use, their geometric and optical isomers, and their mixtures in all proportions and in racemic form, methods for the preparation of these novel antagonists, and their use in the treatment of a living animal and pharmaceutical compositions comprising them.
摘要翻译： PCT No.PCT / FR95 / 00975 Sec。 371日期1997年1月20日 102（e）日期1997年1月20日PCT提交1995年7月20日PCT公布。出版物WO96 / 02525 日期1996年2月1日通式（I）的新型5HT受体拮抗剂其中Ar1和Ar2为芳族残基，X为O，NH，CH2O或CH2NH，R1为氢或直链或支链烷基包括1-6个碳原子，以及它们的盐，水合物，溶剂化物和生理上可接受的生物前体，用于其治疗用途，它们的几何和旋光异构体及其各种比例和外消旋形式的混合物，制备这些物质的方法新型拮抗剂及其在治疗活体动物中的应用和包含它们的药物组合物。

8. 发明授权

US5641779A Selective ligands of 5-HT.sub.1D -5-HT.sub.1B receptors derived from indolepiperazine which are useful medicaments 失效
标题翻译：可用作药物的来自吲哚哌嗪的5-HT1D-5-HT1B受体的选择性配体
公开(公告)号：US5641779A
公开(公告)日：1997-06-24
申请号：US464734
申请日：1995-06-29
申请人： Serge Halazy , Michel Perez , Michael Briley
发明人： Serge Halazy , Michel Perez , Michael Briley
IPC分类号： A61K31/495 , A61K31/496 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/16 , C07D409/12 , C07D241/36
CPC分类号： C07D209/16 , C07D409/12
摘要： The present invention relates to compounds having the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a linear or branched alkyl radical or a phenyl, benzyl, cycloalkyl, polycycloalkyl, dibenzocycloalkyl, dibenzooxepine, dibenzoazepine, dibenzothiepine, benzopyrrolocycloalkyl, benzothienocycloalkyl or naphthyl radical, optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, aryl acyl, alkoxy and alkyl thio radicals.Z is C.dbd.O, SO.sub.2 or (CH.sub.2).sub.n in which n is between 1 and 5.R.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a phenyl, benzyl, cycloalkyl, pyrrole, furan, pyridinyl or thiophenyl radical, optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, aryl, acyl, alkoxy and alkylthio radicals.R'.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a phenyl radical.R.sub.3 is a hydrogen atom, a linear or branched alkyl radical or a benzyl or phenethyl radical.R.sub.4 is a hydrogen, chlorine, fluorine or bromine atom or a linear or branched alkyl radical.R.sub.5 is a hydrogen atom, a linear or branched alkyl radical or a benzyl or phenethyl radical.R.sub.6 is a hydrogen atom, a linear or branched alkyl radical, an acyl (COR.sub.7), acyloxy (CO.sub.2 R.sub.7) or acylamino (CONHR.sub.7) radical in which R.sub.7 represents a linear or branched alkyl radical, or a variously substituted phenyl radical.
摘要翻译： PCT No.PCT / FR93 / 01317 Sec。 371日期：1995年6月29日 102（e）日期1995年6月29日PCT 1993年12月29日PCT PCT。第WO94 / 15916号公报日本时间1994年7月21日本发明涉及具有下式的化合物：其中R 1为氢原子，直链或支链烷基或苯基，苄基，环烷基，多环烷基，二苯并环烷基，二苯并氧杂，二苯并吖庚因，二苯并噻ine，苯并吡咯环烷基，苯并噻吩基环烷基或萘基，任选被一个或多个选自卤素原子和烷基，芳基酰基，烷氧基和烷基硫基的取代基取代。 Z是C = O，SO 2或（CH 2）n，其中n在1和5之间。R2是氢原子，直链或支链烷基或苯基，苄基，环烷基，吡咯，呋喃，吡啶基或硫代苯基，任选地被一个或多个选自卤素原子和烷基，芳基，酰基，烷氧基和烷硫基的取代基取代。 R'2是氢原子，直链或支链烷基或苯基。 R3是氢原子，直链或支链烷基或苄基或苯乙基。 R4是氢，氯，氟或溴原子或直链或支链烷基。 R5是氢原子，直链或支链烷基或苄基或苯乙基。 R6是氢原子，直链或支链烷基，酰基（COR7），酰氧基（CO2R7）或酰基氨基（CONHR7）基团，其中R7表示直链或支链烷基或各种取代的苯基。

9. 发明授权

US5494912A 9-purinyl phosphonic acid derivitives for treating gout 失效
标题翻译：用于治疗痛风的9-嘌呤基膦酸衍生物
公开(公告)号：US5494912A
公开(公告)日：1996-02-27
申请号：US467497
申请日：1995-06-06
申请人： Serge Halazy , Charles Danzin
发明人： Serge Halazy , Charles Danzin
IPC分类号： A61K31/675 , A61K31/52
CPC分类号： A61K31/675
摘要： This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immunosuppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.
摘要翻译：本发明涉及新型的嘌呤核苷磷酸化酶抑制剂，其制备方法和中间体及其作为免疫抑制剂，抗淋巴瘤，抗白血病，抗病毒和抗原虫药的用途。

10. 发明授权

US08053436B1 9-(piperazinylalkyl) carbazoles as bax-modulators 失效
标题翻译： 9-（哌嗪基烷基）咔唑作为bax调节剂
公开(公告)号：US08053436B1
公开(公告)日：2011-11-08
申请号：US10110199
申请日：2000-10-18
申请人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
发明人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
IPC分类号： A61K31/497 , C07D403/06 , C07D413/14
CPC分类号： C07D209/88 , C07D209/86
摘要： The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.
摘要翻译：本发明涉及特别用作药物活性化合物的式（I）咔唑的哌嗪衍生物，以及含有咔唑类哌嗪衍生物的药物制剂。所述咔唑的哌嗪衍生物是Bax功能和/或活化的有效调节剂，特别是有效的抑制剂。本发明还涉及咔唑的新型哌嗪衍生物及其制备方法。

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