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1. 发明公开

EP2580207A1 NITROGEN CONTAINING HETEROARYL COMPOUNDS 有权
标题翻译： STICKSTOFFHALTIGE HETEROARYLVERBINDUNGEN
公开(公告)号：EP2580207A1
公开(公告)日：2013-04-17
申请号：EP11723077.1
申请日：2011-06-06
申请人： F.Hoffmann-La Roche AG
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，R1，R2，R3，R4，R5和R6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的酯。这些化合物抑制PDE10A，可用作治疗剂。

2. 发明公开

EP2552918A1 N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDE DERIVATIVES AND THEIR USE AS PDE10A INHIBITORS 失效
标题翻译： N-（咪唑并嘧啶-7-基）-HETEROARYLAMID-衍生物及其作为抑制剂PDE10A
公开(公告)号：EP2552918A1
公开(公告)日：2013-02-06
申请号：EP11711068.4
申请日：2011-03-23
申请人： F.Hoffmann-La Roche AG
发明人： ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P25/00 , A61P25/18
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 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 pharmaceuticals.

3. 发明公开

EP2550254A1 CYCLOPENTYL - AND CYCLOHEPTYLPYRAZOLES AS FXR MODULATORS 审中-公开
标题翻译：环戊二烯并吡咯并吡唑（FXR-MODULATOREN）
公开(公告)号：EP2550254A1
公开(公告)日：2013-01-30
申请号：EP11711495.9
申请日：2011-03-21
申请人： F.Hoffmann-La Roche AG
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如说明书和权利要求书中所定义，以及其生理上可接受的盐。本发明还涉及包括这些化合物的组合物和使用该化合物的方法。

4. 发明公开

EP1926711A1 NOVEL HETEROBICYCLIC DERIVATIVES USEFUL AS INHIBITORS OF LIVER CARNITINE PALMITOYL TRANSFERASE 有权
标题翻译：新杂衍生物肝脏肉碱棕榈酰TRANSFERASEHEMMER
公开(公告)号：EP1926711A1
公开(公告)日：2008-06-04
申请号：EP06793207.9
申请日：2006-09-05
申请人： F.HOFFMANN-LA ROCHE AG
发明人： ACKERMANN, Jean , BLEICHER, Konrad , CECCARELLI, Simona Maria , CHOMIENNE, Odile , MATTEI, Patrizio , SCHULZ-GASCH, Tanja
IPC分类号： C07D209/10 , C07D403/12 , C07D413/12 , C07D215/58 , C07D223/16
CPC分类号： C07D223/16 , C07D209/10 , C07D215/58 , C07D403/12 , C07D413/12
摘要： The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, 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.

5. 发明公开

EP2935312A1 PEPTIDES AS OXYTOCIN AGONISTS 失效
标题翻译：肽类ALS氧化还原
公开(公告)号：EP2935312A1
公开(公告)日：2015-10-28
申请号：EP13814079.3
申请日：2013-12-17
申请人： F.Hoffmann-La Roche AG
发明人： BISSANTZ, Caterina , BLEICHER, Konrad , GRUNDSCHOBER, Christophe
IPC分类号： C07K7/16
CPC分类号： C07K7/64 , A61K38/00 , A61K38/08 , C07K7/16
摘要： It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.

6. 发明授权

EP2346834B1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 有权
标题翻译： 3-氨基 - 吲唑或3-氨基-4,5,6,7-四氢 - 吲唑衍生物
公开(公告)号：EP2346834B1
公开(公告)日：2013-11-20
申请号：EP09783046.7
申请日：2009-09-15
申请人： F.Hoffmann-La Roche AG
发明人： BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , RUDOLPH, Markus , 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 R1 to R7 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 used as medicaments.
摘要翻译：本发明涉及式I的新型吲唑衍生物：其中R 1至R 7如说明书和权利要求中所定义，以及其生理上可接受的盐。这些化合物是FXR调节剂，可以用作药物。

7. 发明公开

EP2483247A1 NEW BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS FXR AGONISTS 审中-公开
标题翻译：新的苯并咪唑衍生物和它们作为FXR激动剂的用途
公开(公告)号：EP2483247A1
公开(公告)日：2012-08-08
申请号：EP10757215.8
申请日：2010-09-27
申请人： F.Hoffmann-La Roche AG
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , PLANCHER, Jean-Marc , RICHTER, Hans , RUDOLPH, Markus , TAYLOR, Sven
IPC分类号： C07D235/18 , C07D401/04 , C07D403/10 , C07D403/12 , C07D405/14 , C07D417/14 , A61K31/4184 , A61K31/4439
CPC分类号： C07D401/04 , C07D235/18 , C07D403/10 , C07D403/12 , C07D405/14 , C07D417/14
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A, B, R
1 , R
2 , R
3 , R
4 , R
5 , n, m and p have the significance given in claim 1.

8. 发明授权

EP1996563B1 HETEROBICYCLIC SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF DIABETES 有权
标题翻译：杂磺胺对于糖尿病的治疗
公开(公告)号：EP1996563B1
公开(公告)日：2012-03-21
申请号：EP07726290.5
申请日：2007-02-02
申请人： F.Hoffmann-La Roche AG
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 R1, R2, R3, R4, R5, R6, 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.

9. 发明公开

EP2346834A1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 有权
标题翻译： 3-氨基 - 吲唑或3-氨基-4,5,6,7-四氢 - 吲唑衍生物
公开(公告)号：EP2346834A1
公开(公告)日：2011-07-27
申请号：EP09783046.7
申请日：2009-09-15
申请人： F.Hoffmann-La Roche AG
发明人： BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , RUDOLPH, Markus , 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）的新型吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，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。该化合物是法尼醇-X-受体的选择性调节剂，优选激动剂，其中法尼醇-X-受体（FXR）是转录因子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的脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周阻塞病，局部缺血，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，胆固醇胆结石病，肝胆汁淤积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪肝病（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调节剂影响的优选疾病（和条件）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆石病，癌症，非胰岛素依赖型糖尿病和代谢综合征。特别优选的受FXR调节剂影响的疾病是高LDL胆固醇，高甘油三酯水平和血脂异常。

10. 发明公开

EP2038259A1 BENZIMIDAZOLE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS FXR AGONISTS AND PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME 审中-公开
标题翻译：苯并咪唑衍生物，PROCESS所周之，它们作为FXR激动剂和含筹备PHARAMZEUTISCHE
公开(公告)号：EP2038259A1
公开(公告)日：2009-03-25
申请号：EP07765461.4
申请日：2007-06-18
申请人： F.HOFFMANN-LA ROCHE AG
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , CHUCHOLOWSKI, Alexander , DEHMLOW, Henrietta , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , NIESOR, Eric J. , PANDAY, Narendra , RICHTER, Hans , SCHULER, Franz , WAROT, Xavier Marie , WRIGHT, Matthew , YANG, Minmin
IPC分类号： C07D235/18 , C07D409/10 , C07D409/04 , C07D403/04 , C07D403/10 , A61K31/4184 , A61P3/00 , A61P25/00 , A61P35/00
CPC分类号： C07D235/18 , C07D235/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/06
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 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.

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