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1. 发明申请

US20130116289A1 5-(BIPHENYL-4-YL)-3-PHENYL-1,2,4-OXADIAZOLYL DERIVATIVES AS LIGANDS ON THE SPHINGOSINE 1-PHOSPHATE(SIP)RECEPTORS 有权
标题翻译： 5-（联苯-4-基）-3-苯基-1,2,4-氧杂二唑衍生物作为配位体1-磷酸酯（SIP）受体的配体
公开(公告)号：US20130116289A1
公开(公告)日：2013-05-09
申请号：US13809013
申请日：2011-07-06
申请人： Agnes Bombrun , Anna Quattropani , Jerome Gonzalez , Jerome Dorbais , Chris Knight , Charles Baker-Glenn
发明人： Agnes Bombrun , Anna Quattropani , Jerome Gonzalez , Jerome Dorbais , Chris Knight , Charles Baker-Glenn
IPC分类号： A61K31/4245 , C07D271/12 , A61K31/70
CPC分类号： C07D271/06 , A61K31/4245
摘要： The present invention provides compounds of Formula (I), as selective S1P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases.
摘要翻译：本发明提供作为选择性S1P1抑制剂的式（I）化合物及其用于治疗多发性硬化症和其它疾病的用途。

2. 发明授权

US09029405B2 5-(biphenyl-4-yl)-3-phenyl-1,2,4-oxadiazolyl derivatives as ligands on the sphingosine 1-phosphate(SIP)receptors 有权
标题翻译： 5-（联苯-4-基）-3-苯基-1,2,4-恶二唑基衍生物作为鞘氨醇1-磷酸（SIP）受体上的配体
公开(公告)号：US09029405B2
公开(公告)日：2015-05-12
申请号：US13809013
申请日：2011-07-06
申请人： Agnes Bombrun , Anna Quattropani , Jerome Gonzalez , Jerome Dorbais , Chris Knight , Charles Baker-Glenn
发明人： Agnes Bombrun , Anna Quattropani , Jerome Gonzalez , Jerome Dorbais , Chris Knight , Charles Baker-Glenn
IPC分类号： A61K31/4245 , C07D271/06
CPC分类号： C07D271/06 , A61K31/4245
摘要： The present invention provides compounds of Formula (I), as selective S1P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases.
摘要翻译：本发明提供作为选择性S1P1抑制剂的式（I）化合物及其用于治疗多发性硬化症和其它疾病的用途。

3. 发明申请

US20100240658A1 Oxadiazole Derivatives 有权
标题翻译：恶二唑衍生物
公开(公告)号：US20100240658A1
公开(公告)日：2010-09-23
申请号：US12675235
申请日：2008-10-01
申请人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jerome Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
发明人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jerome Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
IPC分类号： A61K31/5377 , C07D271/06 , C07D413/02 , A61K31/4245 , A61K31/4439 , A61K31/454
CPC分类号： C07D263/32 , C07D413/04 , C07D413/10
摘要： The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S 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，W，Q和S具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

4. 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。

5. 发明授权

US08202865B2 Oxadiazole derivatives 有权
标题翻译：恶二唑衍生物
公开(公告)号：US08202865B2
公开(公告)日：2012-06-19
申请号：US12675235
申请日：2008-10-01
申请人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jermone Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
发明人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jermone Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/4439 , A61K31/4245 , C07D413/02 , C07D271/06
CPC分类号： C07D263/32 , C07D413/04 , C07D413/10
摘要： The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S 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，W，Q和S具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

6. 发明授权

US08404676B2 Oxadiazole diaryl compounds 有权
标题翻译：恶二唑二芳基化合物
公开(公告)号：US08404676B2
公开(公告)日：2013-03-26
申请号：US12675254
申请日：2008-10-01
申请人： Cyril Montagne , Anna Quattropani , Wolfgang Sauer , Agnes Bombrun
发明人： Cyril Montagne , Anna Quattropani , Wolfgang Sauer , Agnes Bombrun
IPC分类号： A61K31/55 , A61K31/454 , A61K31/5377 , A61K31/4245 , A61K31/4439 , A61K31/4545 , C07D401/10 , C07D413/10 , C07D271/06 , C07D413/14 , A61P19/02 , A61P3/10 , A61P17/06 , A61P27/02 , A61P11/06 , A61P9/10 , A61P7/06 , A61P31/00 , A61P35/00 , A61P43/00
CPC分类号： C07D413/10 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D271/06 , C07D271/07 , C07D413/14
摘要： The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, 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，Rc和W具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

7. 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。

8. 发明申请

US20100305104A1 Oxadiazole Diaryl Compounds 有权
标题翻译：恶二唑二芳基化合物
公开(公告)号：US20100305104A1
公开(公告)日：2010-12-02
申请号：US12675254
申请日：2008-10-01
申请人： Cyril Montagne , Anna Quattropani , Wolfgang Sauer , Agnes Bombrun
发明人： Cyril Montagne , Anna Quattropani , Wolfgang Sauer , Agnes Bombrun
IPC分类号： A61K31/55 , C07D401/10 , A61K31/454 , C07D413/10 , A61K31/5377 , C07D271/06 , A61K31/4245 , A61K31/4439 , C07D413/14 , A61K31/4545 , A61P19/02 , A61P3/10 , A61P17/06 , A61P27/02 , A61P11/06 , A61P7/02 , A61P9/10 , A61P7/06 , A61P31/00 , A61P35/00 , A61P43/00
CPC分类号： C07D413/10 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D271/06 , C07D271/07 , C07D413/14
摘要： The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, 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，Rc和W具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

9. 发明申请

US20090018169A1 Sulfonamide Derivatives for the Treatment of Bacterial Infections 审中-公开
标题翻译：用于治疗细菌感染的磺酰胺衍生物
公开(公告)号：US20090018169A1
公开(公告)日：2009-01-15
申请号：US12278831
申请日：2007-02-09
申请人： Jerome Gonzalez , Dominique Swinnen , Agnes Bombrun , Rob Hooft Van Huijsduijnen , Timothy Wells
发明人： Jerome Gonzalez , Dominique Swinnen , Agnes Bombrun , Rob Hooft Van Huijsduijnen , Timothy Wells
IPC分类号： A61K31/381 , C07D409/12 , A61K31/4436 , A61P31/04 , C07D333/04
CPC分类号： A61K31/381 , A61K31/4436
摘要： This present invention is related to sulfonamide derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of bacterial infections such as tuberculosis.
摘要翻译：本发明涉及式（I）的磺酰胺衍生物，其药物组合物，其制备方法及其用于治疗和/或预防细菌感染如结核病的用途。

10. 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。

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