专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US08399448B2 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis 有权
标题翻译： 6-氨基 - 嘧啶-4-甲酰胺衍生物和与鞘氨醇1-磷酸（S1P）受体结合以治疗多发性硬化症的相关化合物
公开(公告)号：US08399448B2
公开(公告)日：2013-03-19
申请号：US12671996
申请日：2008-07-29
申请人： Agnes Bombrun , Matthias Schwarz , Stefano Crosignani , David Covini , Delphine Marin
发明人： Agnes Bombrun , Matthias Schwarz , Stefano Crosignani , David Covini , Delphine Marin
IPC分类号： A61K31/33 , A61K31/497 , A61K31/535 , C07D239/24 , C07D401/12 , C07D403/12 , C07D413/12
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful, for example, in the treatment of autoimmune disorders, such as multiple sclerosis.
摘要翻译：本发明涉及式（I）的化合物：其中X，W，Q，R，R 1和R 2具有权利要求1中给出的含义。该化合物可用于例如治疗自身免疫性疾病如多发性硬化。

12. 发明申请

US20100210619A1 6-Amino-Pyrimidine-4-Carboxamide Derivatives and Related Compounds Which Bind to the Sphingosine 1-Phosphate (S1P) Receptor for the Treatment of Multiple Sclerosis 有权
标题翻译： 6-氨基 - 嘧啶-4-羧酰胺衍生物及其与1-磷酸鞘氨醇受体（S1P）接合治疗多发性硬化症的相关化合物
公开(公告)号：US20100210619A1
公开(公告)日：2010-08-19
申请号：US12671996
申请日：2008-07-29
申请人： Agnes Bombrun , Matthias Schwarz , Stefano Crosignani , David Covini , Delphine Marin
发明人： Agnes Bombrun , Matthias Schwarz , Stefano Crosignani , David Covini , Delphine Marin
IPC分类号： A61K31/397 , C07D239/42 , A61K31/505 , C07D403/12 , A61K31/496 , C07D413/12 , A61K31/5377 , A61P3/10 , A61P19/02 , A61P17/06 , A61P11/06 , A61P1/00
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 15. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
摘要翻译：本发明涉及式（I）的化合物：其中X，W，Q，R，R 1和R 2具有权利要求15中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

13. 发明授权

US08202856B2 Triazole oxadiazoles derivatives 有权
标题翻译：三唑恶二唑衍生物
公开(公告)号：US08202856B2
公开(公告)日：2012-06-19
申请号：US12809816
申请日：2008-12-17
申请人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin , Agnes Bombrun , Wesley Blackaby , Charles Baker-Glenn , Chris Knight , Craig Rouse
发明人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin , Agnes Bombrun , Wesley Blackaby , Charles Baker-Glenn , Chris Knight , Craig Rouse
IPC分类号： A61K31/397 , A61K31/4545 , A61K31/444 , A61K31/5377 , A61K31/4245 , A61K31/4439 , A61K31/4725 , A61K31/497 , C07D413/04 , C07D413/14 , C07D401/14 , A61P19/02 , A61P3/10 , A61P9/10 , A61P29/00 , A61P1/04 , A61P17/06 , A61P11/06
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula I: wherein R1, R2,Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
摘要翻译：本发明涉及式I化合物：其中R1，R2，Ra，Rb，X具有权利要求1中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

14. 发明申请

US20070105913A1 Alkynyl aryl carboxamides 失效
标题翻译：炔基芳基甲酰胺
公开(公告)号：US20070105913A1
公开(公告)日：2007-05-10
申请号：US10565538
申请日：2004-07-20
申请人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
IPC分类号： A61K31/44 , A61K31/40 , A61K31/24 , A61K31/195 , A61K31/16
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译：本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症 - 高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。（I'）A是C 2 -C 15炔基，C 2 -C 6 - 炔基芳基 C 2 -C 6 - 炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是芳基，其可任选地被3-8元环烷基稠合。 R 1和R 2彼此独立地选自氢或（C 1 -C 6 - / SUB）烷基。 R 4和R 5各自彼此独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 3烷基羧基，C 2 -C 3链烯基羧基，C 2 -C 3烷基羧基，C 1 -C 3烷基羧基，亚磺酰基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，由此R 4中的至少一个或者R 5不是氢或C 1 -C 6烷基。

15. 发明授权

US07592477B2 Substituted methylene amide derivatives as modulators of protein tyrosine phosphatases (PTPs) 失效
标题翻译：取代的亚甲基酰胺衍生物作为蛋白酪氨酸磷酸酶（PTP）的调节剂
公开(公告)号：US07592477B2
公开(公告)日：2009-09-22
申请号：US10501344
申请日：2003-01-27
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Patrick Gerber , Pierre-Andre Pittet
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Patrick Gerber , Pierre-Andre Pittet
IPC分类号： C07C229/00 , C07D271/06
CPC分类号： C07D213/40 , C07C2601/14 , C07D211/26 , C07D211/58 , C07D211/96 , C07D271/06 , C07D277/28 , C07D285/06 , C07D307/79 , C07D307/91 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D401/04
摘要： The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).
摘要翻译：本发明涉及式（I）的取代的亚甲基酰胺衍生物及其用于治疗和/或预防由胰岛素抵抗或疟疾引起的代谢紊乱，包括I型和/或II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，肥胖症，多囊卵巢综合征（PCOS）。特别地，本发明涉及使用式（I）的取代的亚甲基酰胺衍生物来调节，特别是抑制PTP的活性。本发明还涉及治疗II型糖尿病，肥胖症和调节哺乳动物食欲的方法。本发明还涉及新型取代的亚甲基酰胺衍生物及其制备方法。式（I）。

16. 发明申请

US20090029903A1 1,1'-(1,2-Ethynediyl)Bis-Benzene Derivatives As Ptp 1-B Inhibitors 有权
标题翻译： 1,1'-（1,2-乙炔二基）双苯衍生物作为Ptp 1-B抑制剂
公开(公告)号：US20090029903A1
公开(公告)日：2009-01-29
申请号：US11547861
申请日：2005-03-29
申请人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
发明人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
IPC分类号： A61K38/28 , C07C229/64 , A61K31/196 , C07D333/34 , A61K31/381
CPC分类号： C07D319/08 , A61K38/28 , C07C33/28 , C07C51/31 , C07C63/66 , C07C65/28 , C07C67/343 , C07C69/76 , C07C211/29 , C07C217/58 , C07C229/38 , C07C229/60 , C07C229/64 , C07C233/31 , C07C233/81 , C07C233/87 , C07C235/46 , C07C235/84 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/42 , C07C311/04 , C07C311/13 , C07C311/19 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D333/34
摘要： The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
摘要翻译：本发明涉及式（I）的羧酸及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及式（I）的羧酸的用途，特别是抑制PTP的活性。

17. 发明申请

US20050124656A1 Substituted methylene amide derivatives as modulators of protein tyrosine phosphatases(ptps) 失效
标题翻译：取代的亚甲基酰胺衍生物作为蛋白酪氨酸磷酸酶（ptps）的调节剂
公开(公告)号：US20050124656A1
公开(公告)日：2005-06-09
申请号：US10501344
申请日：2003-01-27
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Patrick Gerber , Pierre-Andre Pittet
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Patrick Gerber , Pierre-Andre Pittet
IPC分类号： A61K20060101 , A61K31/16 , A61K31/198 , A61K31/275 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4436 , A61K31/445 , A61K31/498 , A61K31/5377 , A61K45/00 , A61P20060101 , A61P3/04 , A61P3/06 , A61P3/10 , A61P15/00 , A61P43/00 , C07B61/00 , C07C20060101 , C07C51/09 , C07C233/13 , C07C233/18 , C07C233/31 , C07C233/36 , C07C233/47 , C07C233/56 , C07C237/42 , C07C237/44 , C07C255/60 , C07C317/32 , C07D20060101 , C07D211/26 , C07D211/58 , C07D211/92 , C07D211/96 , C07D213/40 , C07D271/06 , C07D277/20 , C07D277/28 , C07D277/38 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/91 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/70 , C07D401/04 , C07D401/06 , C07D409/12 , A61K31/7008 , A61K31/20 , A61K31/277
CPC分类号： C07D213/40 , C07C2601/14 , C07D211/26 , C07D211/58 , C07D211/96 , C07D271/06 , C07D277/28 , C07D285/06 , C07D307/79 , C07D307/91 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D401/04
摘要： The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).
摘要翻译：本发明涉及式（I）的取代的亚甲基酰胺衍生物及其用于治疗和/或预防由胰岛素抵抗或疟疾引起的代谢紊乱，包括I型和/或II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，肥胖症，多囊卵巢综合征（PCOS）。特别地，本发明涉及使用式（I）的取代的亚甲基酰胺衍生物来调节，特别是抑制PTP的活性。本发明还涉及治疗II型糖尿病，肥胖症和调节哺乳动物食欲的方法。本发明还涉及新型取代的亚甲基酰胺衍生物及其制备方法。式（I）。

18. 发明授权

US07947851B2 1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP 1-B inhibitors 有权
标题翻译： 1,1'-（1,2-乙炔二基）双苯衍生物作为PTP 1-B抑制剂
公开(公告)号：US07947851B2
公开(公告)日：2011-05-24
申请号：US11547861
申请日：2005-03-29
申请人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
发明人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
IPC分类号： C07D333/34 , C07C65/03 , C07C211/44 , C07C233/65 , C07C311/15 , A61K31/165 , A61P3/10
CPC分类号： C07D319/08 , A61K38/28 , C07C33/28 , C07C51/31 , C07C63/66 , C07C65/28 , C07C67/343 , C07C69/76 , C07C211/29 , C07C217/58 , C07C229/38 , C07C229/60 , C07C229/64 , C07C233/31 , C07C233/81 , C07C233/87 , C07C235/46 , C07C235/84 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/42 , C07C311/04 , C07C311/13 , C07C311/19 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D333/34
摘要： The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
摘要翻译：本发明涉及式（I）的羧酸及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及式（I）的羧酸的用途，特别是抑制PTP的活性。

19. 发明授权

US07589232B2 Alkynyl aryl carboxamides 失效
标题翻译：炔基芳基甲酰胺
公开(公告)号：US07589232B2
公开(公告)日：2009-09-15
申请号：US10565538
申请日：2004-07-20
申请人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
IPC分类号： C07C299/34 , A61K31/195
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译：本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症 - 高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。（I'）A是C 2 -C 15炔基，C 2 -C 6炔基芳基，C 2 -C 6炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是可以任选被3-8元环烷基稠合的芳基。 R 1和R 2彼此独立地选自氢或（C 1 -C 6）烷基。 R 4和R 5各自独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 3烷基羧基，C 2 -C 3烯基羧基，C 2 -C 3炔基羧基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，或者R 5不是氢或C 1 -C 6烷基。

20. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式