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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US08410110B2 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：US08410110B2
公开(公告)日：2013-04-02
申请号：US13225760
申请日：2011-09-06
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
CPC分类号： C07D209/88 , C07D209/86
摘要： Piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:
摘要翻译：用作药物活性化合物的哌嗪化合物和可用于治疗与凋亡相关的疾病的药物制剂中的哌嗪化合物，包括神经变性疾病，与多聚谷氨酰胺束相关的疾病，癫痫，缺血，不育症，心血管疾病，肾脏缺氧，肝炎和AIDS，其中哌嗪化合物由式（I）表示，术语R 0，R 1，R 2，R 3，k，l，m，n和X定义如下：

6. 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。

7. 发明授权

US08012995B1 Pharmaceutically active sulfonamide derivatives 失效
标题翻译：药物活性磺酰胺衍生物
公开(公告)号：US08012995B1
公开(公告)日：2011-09-06
申请号：US10070954
申请日：2000-09-28
申请人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean Pierre Gotteland , Marco Biamonte
发明人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean Pierre Gotteland , Marco Biamonte
IPC分类号： A61P25/00 , A61P9/00 , A61K31/4436 , A61K31/4439 , A61K31/44 , C07D417/14 , C07D417/12 , C07D409/14 , C07D409/12 , C07D213/74
CPC分类号： C07D409/12 , C07D333/34 , C07D409/14 , C07D413/12 , C07D471/04 , C07D471/10 , C07D487/08 , C07D495/04
摘要： The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6 membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
摘要翻译：本发明涉及式（I0）的磺酰胺衍生物，特别用作药物活性化合物，以及含有这种磺酰胺衍生物的药物制剂。所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别有效和选择性抑制剂本发明还涉及新型磺酰胺衍生物及其制备方法，本发明式（I）化合物作为合适的药剂是其中Ar 1和Ar 2独立地为每个其它取代或未取代的芳基或杂芳基，X是O或S，优选O; R 1是氢或C 1 -C 6烷基，或者R 1与Ar 1; n形成取代或未取代的5-6元饱和或不饱和环是0至5的整数，优选1-3和最优选1;式（I）中的Y是未取代的或取代的4-1 含有至少一个氮原子的2-元饱和环状或双环烷基，由此一个氮原子，由此所述环中的一个氮原子与式（I）的磺酰基形成键，从而提供磺酰胺。

8. 发明授权

US08008341B2 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：US08008341B2
公开(公告)日：2011-08-30
申请号：US12142296
申请日：2008-06-19
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： A61P25/00 , A61P37/00 , A61K31/4468 , C07D211/96
CPC分类号： C07D211/96
摘要： The present invention relates to benzsulfonamide derivatives of formula I and methods of use thereof. The benzsulfonamide derivatives of the present invention are efficient modulators of the JNK pathway. In particular the benzsulfonamide derivatives of the present invention are selective inhibitors of JNK 2 and 3.
摘要翻译：本发明涉及式I的苯磺酰胺衍生物及其使用方法。本发明的苯磺酰胺衍生物是JNK途径的有效调节剂。特别地，本发明的苯磺酰胺衍生物是JNK 2和3的选择性抑制剂。

9. 发明授权

US07544700B2 Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases 失效
标题翻译：携带亲脂性和可离子化部分的药学活性磺酰胺衍生物作为蛋白质JunKinases的抑制剂
公开(公告)号：US07544700B2
公开(公告)日：2009-06-09
申请号：US10381665
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： A61P25/00 , A61P25/16 , A61K31/4535 , A61K31/55 , A61K31/4025 , C07D333/34 , C07D409/12 , C07D409/14 , C07D413/14
CPC分类号： C07D409/12 , C07D333/34 , C07D409/14 , C07D413/14
摘要： The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
摘要翻译：本发明涉及具有亲油部分并且基本上可溶的磺酰胺衍生物。所述化合物特别用作药物活性化合物。本发明还涉及含有这种磺酰胺衍生物的药物制剂。所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效和选择性抑制剂。本发明还涉及新型磺酰胺衍生物及其制备方法。根据本发明的式（I）化合物是合适的药物，其中Ar 1和Ar 2彼此独立地为取代或未取代的芳基或杂芳基，X为O或S，优选为O; R1是氢或C1-C6-烷基，或R1与Ar1形成取代或未取代的5-6元饱和或不饱和环; n为0至5的整数，优选1-3至最优选1; 式（I）中的Y是未被取代的或取代的4-12元饱和的环状或双环烷基，其被至少一个亲电链连接的可离子化部分取代，并且含有至少一个氮原子，其中一个所述环内的氮原子与式（I）的磺酰基形成键，从而提供磺酰胺。

10. 发明授权

US07470686B2 Method of inhibiting the expression and/or the activity of JNK 有权
标题翻译：抑制JNK表达和/或活性的方法
公开(公告)号：US07470686B2
公开(公告)日：2008-12-30
申请号：US11779585
申请日：2007-07-18
申请人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
发明人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
IPC分类号： A61K31/506 , C07D417/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/64 , C07D417/06 , C07D417/14
摘要： The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.
摘要翻译：本发明涉及特别用作药物活性化合物的苯并唑衍生物以及含有这种苯并唑衍生物的药物制剂。所述的苯并唑衍生物是JNK途径的有效调节剂，它们特别是JNK2和/或3的有效和选择性抑制剂。本发明还涉及新的苯并唑衍生物及其制备方法。 X为O，S或NRO，其中R 0为H或未经取代或取代的C 1 -C 6烷基; G是未经证实或取代的嘧啶基。

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