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1. 发明申请

WO2011154327A1 NITROGEN CONTAINING HETEROARYL COMPOUNDS 审中-公开
标题翻译：含氮异氰酸酯化合物
公开(公告)号：WO2011154327A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059234
申请日：2011-06-06
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
发明人： BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P25/00 , A61P35/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A 1 , A 2 , (a), R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基化合物，其中A1，A2，（a），R1，R2，R3，R4，R5和R6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。这些化合物抑制PDE10A，可用作药物。

2. 发明申请

WO2008052898A1 INDAZOLE DERIVATIVES USEFUL AS L-CPT1 INHIBITORS 审中-公开
标题翻译：吲哚衍生物作为L-CPT1抑制剂有用
公开(公告)号：WO2008052898A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/061251
申请日：2007-10-22
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , BLEICHER, Konrad , CECCARELLI, Simona M. , CHOMIENNE, Odile , MATTEI, Patrizio
发明人： ACKERMANN, Jean , BLEICHER, Konrad , CECCARELLI, Simona M. , CHOMIENNE, Odile , MATTEI, Patrizio
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K31/416 , A61K31/4245 , A61K31/4439 , A61P3/00
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention is concerned with novel indazole derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的吲唑衍生物，其中R 1，R 2，R 3，R 4， R 5，R 6，X 6，X和Y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。这些化合物抑制L-CPT1，可用作药物。

3. 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。

4. 发明申请

WO2007093507A1 HETEROBICYCLIC SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的异环琥珀酰胺衍生物
公开(公告)号：WO2007093507A1
公开(公告)日：2007-08-23
申请号：PCT/EP2007/051013
申请日：2007-02-02
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , BLEICHER, Konrad , CECCARELLI, Simona, M. , CHOMIENNE, Odile , MATTEI, Patrizio , OBST SANDER, Ulrike
发明人： ACKERMANN, Jean , BLEICHER, Konrad , CECCARELLI, Simona, M. , CHOMIENNE, Odile , MATTEI, Patrizio , OBST SANDER, Ulrike
IPC分类号： C07D241/42 , C07D263/56 , C07D265/14 , C07D265/36 , C07D267/14 , C07D279/16 , C07D413/12 , C07D417/12 , C07D491/04 , C07D498/04 , A61K31/495 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/00
CPC分类号： C07D265/36 , C07D241/42 , C07D263/56 , C07D265/14 , C07D267/14 , C07D279/16 , C07D413/12 , C07D417/12 , C07D491/04
摘要： The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPTl and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型杂双环衍生物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，V，W，X和Y如说明书和权利要求书中所定义，以及生理上可接受的盐和酯它们。这些化合物抑制L-CPT1，可用作药物。

5. 发明申请

WO2006045478A1 NEW INDOLE OR BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新的吲哚或苯并咪唑衍生物
公开(公告)号：WO2006045478A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011176
申请日：2005-10-18
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , NETTEKOVEN, Matthias, Heinrich , PFLIEGER, Philippe , ROEVER, Stephan
发明人： BLEICHER, Konrad , NETTEKOVEN, Matthias, Heinrich , PFLIEGER, Philippe , ROEVER, Stephan
IPC分类号： C07D235/12 , C07D401/06 , C07D209/12 , A61K31/4184 , A61P3/04
CPC分类号： C07D235/12 , C07D209/12 , C07D401/06
摘要： The present invention relates to compounds of the formula (I), wherein R 1 to R 7 , X and Y are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
摘要翻译：本发明涉及式（I）的化合物，其中R 1至R 7，X和Y如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/或预防与调节CB1受体相关的疾病。

6. 发明申请

WO2011117163A1 CYCLOPENTYL - AND CYCLOHEPTYLPYRAZOLES AS FXR MODULATORS 审中-公开
标题翻译：作为FXR调节剂的环丙基和环己基
公开(公告)号：WO2011117163A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054176
申请日：2011-03-21
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , RICHTER, Hans , TAYLOR, Sven
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , GRETHER, Uwe , KUHN, Bernd , RICHTER, Hans , TAYLOR, Sven
IPC分类号： C07D231/54 , C07D401/12 , C07D403/12 , A61K31/416 , A61K31/4439 , A61P3/04 , A61P3/06 , A61P3/10 , A61P25/16 , A61P25/28 , A61P35/00
CPC分类号： C07D231/54 , A61K9/0019 , A61K9/0095 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2866 , A61K9/4825 , A61K9/4858 , C07D401/12 , C07D403/12
摘要： This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula (I) wherein A and R 1 to R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof, to compositions including these compounds and methods of using the compounds.
摘要翻译：本发明涉及式（I）的新的环戊基 - 和环庚基吡唑衍生物，其中A和R 1至R 4如在说明书和权利要求书中所定义，以及其生理上可接受的盐，包括这些化合物的组合物和使用的方法化合物。

7. 发明申请

WO2011036127A1 IMIDAZOPYRIDINE OR IMIDAZOPYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10A INHIBITORS 审中-公开
标题翻译：作为磷酸二酯酶10A抑制剂的咪唑并吡啶或咪唑并嘧啶衍生物
公开(公告)号：WO2011036127A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/063830
申请日：2010-09-21
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5025 , A61K31/5377 , A61K31/553 , C07D487/04
摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A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。这些化合物抑制PDE10A，可用作药物。

8. 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。

9. 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.

10. 发明申请

WO2008122510A1 1-(1-BENZYLPIPERIDIN-4-YL)BENZIMIDAZ0LE -5-CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF DIABETES MELLITUS 审中-公开
标题翻译：用于治疗糖尿病的1-（1-苄基哌啶-4-基）苯并咪唑-5-羧酸衍生物
公开(公告)号：WO2008122510A1
公开(公告)日：2008-10-16
申请号：PCT/EP2008/053513
申请日：2008-03-26
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , CHRIST, Andreas D. , MARTIN, Rainer E. , MOHR, Peter
发明人： BLEICHER, Konrad , CHRIST, Andreas D. , MARTIN, Rainer E. , MOHR, Peter
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04 , A61K31/454 , A61P5/50
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04
摘要： This invention relates to compounds of the formula (I) wherein A, R 1 to R 3 are as defined in the specification and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridinone and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的化合物，其中A，R 1至R 3如说明书中所定义，G为苯并咪唑，喹喔啉，苯并三唑，二氢 - 咪唑并[4,5-c]吡啶酮和二氢异吲哚酮基及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

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