公开(公告)号：US08791142B2

公开(公告)日：2014-07-29

申请号：US13203044

申请日：2010-03-02

Applicant: Anna Quattropani ,  Patrick Gerber ,  Jerome Dorbais

Inventor： Anna Quattropani ,  Patrick Gerber ,  Jerome Dorbais

IPC: A61K31/443 ,  C07D413/04

CPC classification number: C07D413/04 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/2063 ,  A61K9/4866 ,  A61K47/02 ,  C07D413/14

Abstract: The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.

Abstract translation: 本发明提供式（I）的恶二唑吡啶衍生物，其用作药物及其用于治疗多发性硬化症和其它疾病的用途。

公开(公告)号：US08247437B2

公开(公告)日：2012-08-21

申请号：US13155411

申请日：2011-06-08

Applicant: Dominique Swinnen ,  Agnes Bombrun ,  Jerome Gonzalez ,  Stefano Crosignani ,  Patrick Gerber ,  Catherine Jorand-Lebrun

Inventor： Dominique Swinnen ,  Agnes Bombrun ,  Jerome Gonzalez ,  Stefano Crosignani ,  Patrick Gerber ,  Catherine Jorand-Lebrun

IPC: C07D211/70 ,  C07D405/06 ,  A61K31/4418

CPC classification number: C07D211/46 ,  C07D211/58 ,  C07D213/74 ,  C07D215/46 ,  C07D239/42 ,  C07D241/20 ,  C07D285/08 ,  C07D295/185 ,  C07D401/12 ,  C07D487/08

Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Abstract translation: 本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化症 ，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。

公开(公告)号：US08053436B1

公开(公告)日：2011-11-08

申请号：US10110199

申请日：2000-10-18

Applicant: Serge Halazy ,  Dennis Church ,  Bruno Antonsson ,  Agnes Bombrun ,  Patrick Gerber ,  Jean-Claude Martinou

Inventor： Serge Halazy ,  Dennis Church ,  Bruno Antonsson ,  Agnes Bombrun ,  Patrick Gerber ,  Jean-Claude Martinou

IPC: A61K31/497 ,  C07D403/06 ,  C07D413/14

CPC classification number: C07D209/88 ,  C07D209/86

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07592477B2

公开(公告)日：2009-09-22

申请号：US10501344

申请日：2003-01-27

Applicant: Dominique Swinnen ,  Agnes Bombrun ,  Jerome Gonzalez ,  Patrick Gerber ,  Pierre-Andre Pittet

Inventor： Dominique Swinnen ,  Agnes Bombrun ,  Jerome Gonzalez ,  Patrick Gerber ,  Pierre-Andre Pittet

IPC: C07C229/00 ,  C07D271/06

CPC classification number: 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

Abstract: 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).

Abstract translation: 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）。

公开(公告)号：US20090029903A1

公开(公告)日：2009-01-29

申请号：US11547861

申请日：2005-03-29

Applicant: Dominique Swinnen ,  Catherine Jorand-Lebrun ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun

Inventor： Dominique Swinnen ,  Catherine Jorand-Lebrun ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun

IPC: A61K38/28 ,  C07C229/64 ,  A61K31/196 ,  C07D333/34 ,  A61K31/381

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20050043388A1

公开(公告)日：2005-02-24

申请号：US10493066

申请日：2002-10-24

Applicant: Agnes Bombrun ,  Patrick Gerber ,  Denis Church

Inventor： Agnes Bombrun ,  Patrick Gerber ,  Denis Church

IPC: A61K31/404 ,  A61K31/41 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/465 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P15/00 ,  A61P43/00 ,  C07D209/38 ,  C07D209/40 ,  C07D211/62 ,  C07D257/04 ,  C07D295/096 ,  C07D307/68 ,  C07D317/60 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  C07D513/04

CPC classification number: C07D257/04 ,  A61K31/404 ,  C07D209/38 ,  C07D209/40 ,  C07D211/62 ,  C07D295/096 ,  C07D307/68 ,  C07D317/60 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  C07D513/04

Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, 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 oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.(I).

Abstract translation: 本发明涉及式（I）的羟吲哚酰肼衍生物用于治疗和/或预防由胰岛素抵抗或高血糖介导的代谢紊乱的用途，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，本发明涉及式（I）的羟吲哚酰肼衍生物在特别是抑制PTP的活性，特别是PTP1B，TC-PTP，SHP和GLEPP-1的调节中的应用。 本发明还涉及新型羟吲哚酰肼衍生物及其制备方法（I）。

公开(公告)号：US08202865B2

公开(公告)日：2012-06-19

申请号：US12675235

申请日：2008-10-01

Applicant: Anna Quattropani ,  Cyril Montagne ,  Wolfgang Sauer ,  Stefano Crosignani ,  Agnes Bombrun ,  Mathilde Muzerelle ,  Jermone Dorbais ,  Delphine Marin ,  Jerome Gonzalez ,  Patrick Gerber

Inventor： Anna Quattropani ,  Cyril Montagne ,  Wolfgang Sauer ,  Stefano Crosignani ,  Agnes Bombrun ,  Mathilde Muzerelle ,  Jermone Dorbais ,  Delphine Marin ,  Jerome Gonzalez ,  Patrick Gerber

IPC: A61K31/5377 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4245 ,  C07D413/02 ,  C07D271/06

CPC classification number: C07D263/32 ,  C07D413/04 ,  C07D413/10

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07947851B2

公开(公告)日：2011-05-24

申请号：US11547861

申请日：2005-03-29

Applicant: Dominique Swinnen ,  Catherine Jorand-Lebrun ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun

Inventor： Dominique Swinnen ,  Catherine Jorand-Lebrun ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun

IPC: C07D333/34 ,  C07C65/03 ,  C07C211/44 ,  C07C233/65 ,  C07C311/15 ,  A61K31/165 ,  A61P3/10

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100168101A1

公开(公告)日：2010-07-01

申请号：US12645952

申请日：2009-12-23

Applicant: Agnes BOMBRUN ,  Patrick Gerber ,  Dennis Church

Inventor： Agnes BOMBRUN ,  Patrick Gerber ,  Dennis Church

IPC: A61K31/5377 ,  A61K31/404 ,  C07D209/40 ,  C07D413/12 ,  A61K31/4245 ,  C07D405/12 ,  A61K31/427 ,  C07D417/14 ,  C07D401/12 ,  A61K31/4439 ,  A61P3/10

CPC classification number: C07D257/04 ,  A61K31/404 ,  C07D209/38 ,  C07D209/40 ,  C07D211/62 ,  C07D295/096 ,  C07D307/68 ,  C07D317/60 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  C07D513/04

Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, 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 oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.

Abstract translation: 本发明涉及式（I）的羟吲哚酰肼衍生物用于治疗和/或预防由胰岛素抵抗或高血糖介导的代谢紊乱的用途，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，本发明涉及式（I）的羟吲哚酰肼衍生物在特别是抑制PTP的活性，特别是PTP1B，TC-PTP，SHP和GLEPP-1的调节中的应用。 本发明还涉及新型羟吲哚酰肼衍生物及其制备方法。

公开(公告)号：US07589232B2

公开(公告)日：2009-09-15

申请号：US10565538

申请日：2004-07-20

Applicant: Dominique Swinnen ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun ,  Catherine Jorand-Lebrun

Inventor： Dominique Swinnen ,  Patrick Gerber ,  Jerome Gonzalez ,  Agnes Bombrun ,  Catherine Jorand-Lebrun

IPC: C07C299/34 ,  A61K31/195

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。