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1. 发明申请

WO2010142650A1 NOVEL CYCLOPENTANE DERIVATIVES 审中-公开
标题翻译：新的环戊烷衍生物
公开(公告)号：WO2010142650A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/057945
申请日：2010-06-08
申请人： F. HOFFMANN-LA ROCHE AG , BANNER, David , CECCARELLI, Simona M. , GRETHER, Uwe , HAAP, Wolfgang , HILPERT, Hans , KUEHNE, Holger , MAUSER, Harald , PLANCHER, Jean-Marc , SANCHEZ, Rubén Alvarez
发明人： BANNER, David , CECCARELLI, Simona M. , GRETHER, Uwe , HAAP, Wolfgang , HILPERT, Hans , KUEHNE, Holger , MAUSER, Harald , PLANCHER, Jean-Marc , SANCHEZ, Rubén Alvarez
IPC分类号： C07C317/44 , C07D205/04 , C07D207/02 , C07D211/36 , C07D213/60 , C07D231/12 , C07D233/18 , C07D249/04 , C07D261/08 , C07D265/30 , C07D295/185 , C07D309/12 , C07D335/02 , A61K31/277 , A61P3/10
CPC分类号： C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D205/04 , C07D207/06 , C07D207/10 , C07D207/16 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/66 , C07D213/34 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D231/12 , C07D237/08 , C07D237/14 , C07D237/16 , C07D239/26 , C07D249/06 , C07D261/08 , C07D277/26 , C07D279/12 , C07D295/096 , C07D295/185 , C07D309/12 , C07D333/18 , C07D335/02 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D491/08 , C07D491/107
摘要： The invention relates to compounds of formula (I) wherein A 1 , R 1 , R 2 , R 3 , R 4 and R 5 are defined in the description and in the claims, which are preferential inhibitors of the cysteine protease cathepsin, in particular of the cysteine protease cathepsin S or L, making them useful as medicaments, particularly in the treatment of diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease or diabetic nephropathy.
摘要翻译：本发明涉及式（I）化合物，其中A1，R1，R2，R3，R4和R5在说明书和权利要求书中定义，其是半胱氨酸蛋白酶组织蛋白酶，特别是半胱氨酸蛋白酶组织蛋白酶S的优先抑制剂或L，使其用作药物，特别是用于治疗糖尿病，动脉粥样硬化，腹主动脉瘤，外周动脉疾病或糖尿病性肾病。

2. 发明申请

WO2010121918A1 PROLINE DERIVATIVES AS CATHEPSIN INHIBITORS 审中-公开
标题翻译：丙泊酚衍生物作为抑肽酶抑制剂
公开(公告)号：WO2010121918A1
公开(公告)日：2010-10-28
申请号：PCT/EP2010/054792
申请日：2010-04-13
申请人： F. HOFFMANN-LA ROCHE AG , ALVAREZ SANCHEZ, Ruben , BANNER, David , CECCARELLI, Simona M. , GRETHER, Uwe , HAAP, Wolfgang , HARTMAN, Peter , HARTMANN, Guido , HILPERT, Hans , KUEHNE, Holger , MAUSER, Harald , PLANCHER, Jean-Marc
发明人： ALVAREZ SANCHEZ, Ruben , BANNER, David , CECCARELLI, Simona M. , GRETHER, Uwe , HAAP, Wolfgang , HARTMAN, Peter , HARTMANN, Guido , HILPERT, Hans , KUEHNE, Holger , MAUSER, Harald , PLANCHER, Jean-Marc
IPC分类号： C07D207/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
CPC分类号： C07D207/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The invention relates to a compound of formula (I) wherein A, R 1 -R 6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A，R 1 -R 6如说明书和权利要求书中所定义。式（I）化合物可以用作药物。

3. 发明申请

WO2007062997A1 1,1-DIOXO-THIOMORPHOLINYL INDOLYL METHANONE DERIVATIVES FOR USE AS H3 MODULATORS 审中-公开
标题翻译：作为H3调制器使用的1,1-二氧基 - 苯并恶唑基甲醇衍生物
公开(公告)号：WO2007062997A1
公开(公告)日：2007-06-07
申请号：PCT/EP2006/068649
申请日：2006-11-20
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , TAYLOR, Sven
发明人： NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , TAYLOR, Sven
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , A61K31/445 , A61K31/404 , A61P3/04
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention relates to compounds of formula I wherein R 1 , R 2 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2和G如说明书和权利要求及其药学上可接受的盐所定义。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

4. 发明申请

WO2010028981A1 NEW BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新的苯并咪唑衍生物
公开(公告)号：WO2010028981A1
公开(公告)日：2010-03-18
申请号：PCT/EP2009/061252
申请日：2009-09-01
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven
IPC分类号： C07D235/18 , A61K31/31 , A61K31/41 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/444 , A61P19/00 , A61P21/00 , A61P3/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D495/04
CPC分类号： C07D235/18 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D495/04
摘要： The invention is concerned with novel benzimidazole derivatives of Formula (I) wherein A, n and R 1 to R 7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds act on Farnesyl X receptor (FXR) and against cholesterol and lipid illnesses, diabetes, obesity, psoriasis, cancer, osteoporosis, Parkinson's and Alzheimer's disease.
摘要翻译：本发明涉及式（I）的新的苯并咪唑衍生物，其中A，n和R 1至R 7如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物对法呢基X受体（FXR）和胆固醇和脂质疾病，糖尿病，肥胖症，牛皮癣，癌症，骨质疏松症，帕金森病和阿尔茨海默病起作用。

5. 发明申请

WO2009080555A3 CARBOXYL- OR HYDROXYL- SUBSTITUTED BENZIMIDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2009080555A3
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067399
申请日：2008-12-12
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven , YANG, Minmin
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , TAYLOR, Sven , YANG, Minmin
IPC分类号： C07D401/14 , C07D401/04 , C07D235/12 , C07D401/12 , A61K31/4184 , A61P3/10
摘要： This invention relates to novel carboxyl- or hydroxylsubstituted benzimidazole derivatives of formula (I) wherein R 1 to R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

6. 发明申请

WO2009013195A1 BENZOFURAN- AND BENZO[B]THIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AND USE THEREOF AS HISTAMINE 3 RECEPTOR MODULATORS 审中-公开
标题翻译：苯并呋喃和苯并[B]噻吩-2-羧酸酰胺衍生物及其作为组胺3受体调节剂的用途
公开(公告)号：WO2009013195A1
公开(公告)日：2009-01-29
申请号：PCT/EP2008/059281
申请日：2008-07-16
申请人： F. HOFFMANN-LA ROCHE AG , MOHR, Peter , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAKAHASHI, Tadakatsu , TAYLOR, Sven
发明人： MOHR, Peter , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAKAHASHI, Tadakatsu , TAYLOR, Sven
IPC分类号： C07D307/85 , C07D333/70 , C07D409/06 , C07D413/06 , C07D417/06 , A61K31/496 , A61P3/04
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I) wherein X, A and R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及其中X，A和R 1至R 4如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

7. 发明申请

WO2008095821A1 INDOL-2-YL-PIPERAZIN-1-YL-METHANONE DERIVATIVES 审中-公开
标题翻译：吲哚-2-基-L-哌嗪-1-基甲基酮衍生物
公开(公告)号：WO2008095821A1
公开(公告)日：2008-08-14
申请号：PCT/EP2008/050998
申请日：2008-01-29
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAYLOR, Sven
发明人： NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAYLOR, Sven
IPC分类号： C07D401/12 , C07D401/14 , C07D451/06 , A61K31/454 , A61P3/04
CPC分类号： C07D401/12 , C07D401/02 , C07D401/14 , C07D451/06
摘要： The present invention relates to compounds of formula (I), wherein A and R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中A和R 1至R 4如在说明书和权利要求书中所定义，以及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

8. 发明申请

WO2007065820A1 TRICYCLIC AMIDE DERIVATIVES USEFUL FOR TREATING OBESITY 审中-公开
标题翻译：用于治疗肥胖症的三酰胺衍生物
公开(公告)号：WO2007065820A1
公开(公告)日：2007-06-14
申请号：PCT/EP2006/069040
申请日：2006-11-29
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAYLOR, Sven
发明人： NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , TAYLOR, Sven
IPC分类号： C07D487/04 , C07D471/14 , A61K31/4985 , A61P25/00 , A61P3/00 , A61P1/00
CPC分类号： C07D487/04 , C07D471/14
摘要： The present invention relates to compounds of formula (I) wherein A, G, r and R 1 to R 5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中A，G，r和R 1至R 5如在说明书和权利要求书中所定义，以及药学上可接受的盐它们。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

9. 发明申请

WO2007062999A2 1,5-SUBSTITUTED INDOL-2-YL AMIDE DERIVATIVES 审中-公开
标题翻译： 1,5-取代的吲哚-2-基酰胺衍生物
公开(公告)号：WO2007062999A2
公开(公告)日：2007-06-07
申请号：PCT/EP2006/068655
申请日：2006-11-20
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , RUNTZ-SCHMITT, Valerie , TAYLOR, Sven
发明人： NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , RICHTER, Hans , ROCHE, Olivier , RUNTZ-SCHMITT, Valerie , TAYLOR, Sven
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds of formula I wherein R 1 to R 4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式I的化合物，其中R 1至R 4和G如说明书和权利要求书中所定义，并且药学上可接受的其盐。该化合物可用于治疗和/或预防与H3受体调节有关的疾病。

10. 发明申请

WO2010034657A1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 审中-公开
标题翻译： 3-氨基吲哚或3-氨基-4,5,6,7-四氢吲哚衍生物
公开(公告)号：WO2010034657A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/061966
申请日：2009-09-15
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , MARKUS, Rudolph , TAYLOR, Sven
发明人： BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , MARKUS, Rudolph , TAYLOR, Sven
IPC分类号： C07D231/56 , A61K31/416 , A61P3/06 , A61P3/10 , C07D401/12 , C07D407/12
CPC分类号： C07D231/56 , C07D401/12 , C07D407/12
摘要： This invention relates to novel indazole derivatives of formula (I), wherein R 1 to R 7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be use as medicaments. The compounds are selective modulators of the farnesoid-X-receptor, preferably agonists u j[ιe farnesoid-X-receptor (FXR) is a member of the nuclear hormone receptor superfamily of transcription factors. Diseases which are affected by FXR modulators include increased lipid and cholesterol levels, particularly high LDL-cholesterol, high triglycerides, low HDL-cholesterol, dyslipidemia, diseases of cholesterol absorption, atherosclerotic disease, peripheral occlusive disease, ischemic, stroke, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, diabetic nephropathy, obesity, cholesterol gallstone disease, cholestasis/fibrosis of the liver, non alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), psoriasis, cancer, particularly gastrointestinal cancer, osteoporosis, Parkinson's disease and Alzheimer's disease. Preferred diseases (and conditions) which are affected by FXR modulators are prevention or treatment of high LDL cholesterol levels high triglycerides, dyslipidemia, cholesterol gallstone disease, cancer, non-insulin dependent diabetes mellitus and metabolic syndrome. Particularly preferred diseases which arc affected by FXR modulators arc high LDL cholesterol, high triglyceride levels and dyslipidemia.
摘要翻译：本发明涉及式（I）的新的吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物是FXR调节剂，可用作药物。这些化合物是法呢基-X-受体的选择性调节剂，优选激动剂uj [法新颖-X-受体（FXR）是转录因子的核激素受体超家族的成员。受FXR调节剂影响的疾病包括增加脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酸酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周性闭塞性疾病，缺血性，中风，糖尿病，特别是非 - 胰岛素依赖性糖尿病，代谢综合征，糖尿病肾病，肥胖症，胆固醇胆结石疾病，肝脏胆汁郁积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪性肝病（NAFLD），牛皮癣，癌症，特别是胃肠癌，骨质疏松症，帕金森病和阿尔茨海默病。受FXR调节剂影响的首选疾病（和病症）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆结石疾病，癌症，非胰岛素依赖性糖尿病和代谢综合征。受FXR调节剂影响的特别优选的疾病具有高LDL胆固醇，高甘油三酯水平和血脂异常。

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