公开(公告)号：WO2011058149A1

公开(公告)日：2011-05-19

申请号：PCT/EP2010/067412

申请日：2010-11-12

Applicant: MERCK SERONO S.A. ,  GAILLARD, Pascale ,  JEANCLAUDE-ETTER, Isabelle ,  POMEL, Vincent ,  SEBILLE, Eric ,  JEYAPRAKASHNARAYANAN, Seenisamy ,  MUZERELLE, Mathilde

Inventor： GAILLARD, Pascale ,  JEANCLAUDE-ETTER, Isabelle ,  POMEL, Vincent ,  SEBILLE, Eric ,  JEYAPRAKASHNARAYANAN, Seenisamy ,  MUZERELLE, Mathilde

IPC: C07D495/04 ,  C07D495/14 ,  A61K31/56 ,  A61P37/00

CPC classification number: C07D495/04 ,  C07D495/14

Abstract: This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.

Abstract translation: 本发明涉及作为用于治疗自身免疫性疾病，炎症性疾病，多发性硬化和其它疾病如癌症的Pi3k抑制剂的式（I *）化合物。

公开(公告)号：WO2008101979A1

公开(公告)日：2008-08-28

申请号：PCT/EP2008/052102

申请日：2008-02-21

Applicant: LABORATOIRES SERONO SA ,  GAILLARD, Pascale ,  POMEL, Vincent ,  JEANCLAUDE-ETTER, Isabelle ,  DORBAIS, Jérôme ,  KLICIC, Jasna ,  MONTAGNE, Cyril

Inventor： GAILLARD, Pascale ,  POMEL, Vincent ,  JEANCLAUDE-ETTER, Isabelle ,  DORBAIS, Jérôme ,  KLICIC, Jasna ,  MONTAGNE, Cyril

IPC: C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/14 ,  C07D451/02 ,  A61K31/498 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D451/02

Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Abstract translation: 本发明涉及式（I）的喹喔啉化合物，特别是用于治疗自身免疫性疾病和/或炎性疾病，心血管疾病，神经变性疾病，细菌或病毒感染，肾脏疾病，血小板聚集，癌症，移植，移植排斥 或肺部受伤。

公开(公告)号：WO2006053882A3

公开(公告)日：2006-09-08

申请号：PCT/EP2005056020

申请日：2005-11-16

Applicant: ARES TRADING SA ,  ESPOSITO PIERANDREA ,  CHICCO DANIELA ,  DONATI LUCA ,  LEONARDI ANDREA ,  BERTERO STEFANIA ,  GOTTELAND JEAN-PIERRE ,  GAILLARD PASCALE ,  JEANCLAUDE-ETTER ISABELLE ,  GRANDOLINI SIMONE ,  MAIO MARIO

Inventor： ESPOSITO PIERANDREA ,  CHICCO DANIELA ,  DONATI LUCA ,  LEONARDI ANDREA ,  BERTERO STEFANIA ,  GOTTELAND JEAN-PIERRE ,  GAILLARD PASCALE ,  JEANCLAUDE-ETTER ISABELLE ,  GRANDOLINI SIMONE ,  MAIO MARIO

IPC: A61K47/10 ,  A61K31/428 ,  A61K31/506 ,  A61K47/14 ,  A61K47/26

CPC classification number: A61K31/506 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/1617 ,  A61K31/428 ,  A61K47/10 ,  A61K47/14 ,  A61K47/26

Abstract: The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.

Abstract translation: 本发明涉及含有苯并噻唑衍生物的聚乙二醇甘油酯药物制剂。 特别地，本发明涉及苯并噻唑硬脂酰聚乙二醇化学药物制剂，其制备方法和用途。

公开(公告)号：WO2012155199A1

公开(公告)日：2012-11-22

申请号：PCT/AU2012/000538

申请日：2012-05-16

Applicant: BIONOMICS LIMITED ,  MERCK PATENT GMBH ,  HARVEY, Andrew ,  BOMBRUN, Agnes ,  COOKE, Rachel ,  JEANCLAUDE-ETTER, Isabelle ,  KUCHEL, Nathan ,  MOLETTE, Jerome ,  MOULD, Jorgen ,  PAUL, Dharam ,  SINGH, Rajinder ,  DONINI, Cristina ,  COLOVRAY, Veronique

Inventor： HARVEY, Andrew ,  BOMBRUN, Agnes ,  COOKE, Rachel ,  JEANCLAUDE-ETTER, Isabelle ,  KUCHEL, Nathan ,  MOLETTE, Jerome ,  MOULD, Jorgen ,  PAUL, Dharam ,  SINGH, Rajinder ,  DONINI, Cristina ,  COLOVRAY, Veronique

IPC: C07D213/16 ,  A61K31/50 ,  C07D213/89 ,  A61K31/165 ,  A61K31/505 ,  C07D231/12 ,  A61K31/351 ,  A61P37/06 ,  C07D233/56 ,  A61K31/415 ,  C07C233/06 ,  C07D237/08 ,  A61K31/4164 ,  C07D209/52 ,  C07D239/24 ,  A61K31/44 ,  C07D211/16 ,  C07D241/12 ,  A61K31/4402 ,  C07D211/26 ,  C07D309/14 ,  A61K31/4427 ,  C07D211/38 ,  C07D401/12 ,  A61K31/4436 ,  C07D213/61 ,  C07D405/12 ,  A61K31/445 ,  C07D213/64 ,  C07D411/12 ,  A61K31/454 ,  C07D213/70 ,  C07D413/12 ,  A61K31/4965

CPC classification number: C07D213/40 ,  C07C217/90 ,  C07D209/52 ,  C07D211/16 ,  C07D211/26 ,  C07D211/38 ,  C07D213/16 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D237/08 ,  C07D239/24 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D309/14 ,  C07D401/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D451/04

Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

Abstract translation: 本发明涉及可用于调节细胞中钾通道活性的化合物，特别是在T细胞中发现的Kv1.3通道的活性。 本发明还涉及这些化合物在治疗或预防自身免疫性和炎性疾病，包括多发性硬化症中的用途，含有这些化合物的药物组合物及其制备方法。

公开(公告)号：WO2006053882A2

公开(公告)日：2006-05-26

申请号：PCT/EP2005/056020

申请日：2005-11-16

Applicant: ARES TRADING S.A. ,  ESPOSITO, Pierandrea ,  CHICCO, Daniela ,  DONATI, Luca ,  LEONARDI, Andrea ,  BERTERO, Stefania ,  GOTTELAND, Jean-Pierre ,  GAILLARD, Pascale ,  JEANCLAUDE-ETTER, Isabelle ,  GRANDOLINI, Simone ,  MAIO, Mario

Inventor： ESPOSITO, Pierandrea ,  CHICCO, Daniela ,  DONATI, Luca ,  LEONARDI, Andrea ,  BERTERO, Stefania ,  GOTTELAND, Jean-Pierre ,  GAILLARD, Pascale ,  JEANCLAUDE-ETTER, Isabelle ,  GRANDOLINI, Simone ,  MAIO, Mario

CPC classification number: A61K31/506 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/1617 ,  A61K31/428 ,  A61K47/10 ,  A61K47/14 ,  A61K47/26

Abstract: The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.

Abstract translation: 本发明涉及含有苯并噻唑衍生物的聚乙二醇甘油酯药物制剂。 具体而言，本发明涉及苯并噻唑硬脂酰聚乙二醇药物制剂，其制备方法和用途。

公开(公告)号：WO2003106455A1

公开(公告)日：2003-12-24

申请号：PCT/EP2003/050225

申请日：2003-06-13

Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. ,  Gaillard, Pascale ,  Gotteland, Jean-Pierre ,  Jeanclaude-Etter, Isabelle ,  Schwarz, Matthias ,  Thomas, Russel, J.

Inventor： Gaillard, Pascale ,  Gotteland, Jean-Pierre ,  Jeanclaude-Etter, Isabelle ,  Schwarz, Matthias ,  Thomas, Russel, J.

IPC: C07D417/06

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D495/10

Abstract: The present invention is related to azole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such azole derivatives. Said azole derivatives are modulators of the protein kinase signalling pathways, particularly the one involving c-Jun N-terminal kinase and/or Glycogen Kinase Synthase 3. The present invention is furthermore related to novel azole derivatives as well as to methods of their preparation. X is O, S or NR 0 , with R 0 being H or an unsubstituted or substituted C 1 -C 6 alkyl; A is 2-pyridyl, 3-pyridyl, 4-pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl group.

Abstract translation: 本发明涉及特别用作药物活性化合物的唑衍生物以及含有这种唑衍生物的药物制剂。 所述唑衍生物是蛋白激酶信号通路的调节剂，特别是涉及c-Jun N-末端激酶和/或糖原激酶合成酶3的调节剂。本发明还涉及新型唑衍生物及其制备方法。 X是O，S或NR 0，其中R 0是H或未取代或取代的C 1 -C 6烷基; A是2-吡啶基，3-吡啶基，4-吡啶基，哒嗪基，嘧啶基，吡嗪基或三嗪基。