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31. 发明申请

WO2008148689A1 PROLINAMIDE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：丙酰胺衍生物作为NK3拮抗剂
公开(公告)号：WO2008148689A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056589
申请日：2008-05-29
申请人： F. HOFFMANN-LA ROCHE AG , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/16 , C07D401/06 , C07D487/10 , A61P25/16 , A61P25/18 , A61K31/401
CPC分类号： C07D207/16 , C07D401/06 , C07D471/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, or lower alkoxy substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 , R 4 form together with the N-atom to which they are attached a non aromatic heterocyclic group, selected from R 5 is hydrogen or halogen; R 6 is phenyl, unsubstituted or substituted by cyano, halogen, lower alkyl, lower alkoxy, CF 3 , -(CH 2 ) 2 O-lower alkyl, C(O)-lower alkyl or C(O)O-lower alkyl, or is pyridinyl, unsubstituted or substituted by CF 3 , or is -C(O)-phenyl; R 7 is hydrogen or lower alkoxy; R 8 is phenyl, lower alkyl or -C(O)O-lower alkyl; R 9 is hydrogen or S(O) 2 -lower alkyl; R 10 is hydrogen or cycloalkyl; X is -CH 2 - or -C(O)-; p is 1 or 2; n is 1, 2 or 3; o is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）化合物，其中R 1为氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢或低级烷基; R3，R4与它们所连接的N-原子一起形成非芳族杂环基，选自R5是氢或卤素; R 6为未取代或被氰基，卤素，低级烷基，低级烷氧基，CF 3， - （CH 2）2 O-低级烷基，C（O） - 低级烷基或C（O）O-低级烷基取代或被吡啶基取代的苯基，未取代或被CF 3取代，或为-C（O） - 苯基; R7是氢或低级烷氧基; R8是苯基，低级烷基或-C（O）O-低级烷基; R9是氢或S（O）2-低级烷基; R 10是氢或环烷基; X是-CH 2 - 或-C（O） - ; p为1或2; n为1,2或3; o是1或2; 或其药学上合适的酸加成盐，其是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

32. 发明申请

WO2008080844A1 AZASPIRO DERIVATIVES 审中-公开
标题翻译： AZASPIRO衍生物
公开(公告)号：WO2008080844A1
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064183
申请日：2007-12-19
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D491/20 , A61K31/438 , A61P9/12 , A61P25/24
CPC分类号： C07D491/20
摘要： The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R 1 to R 6 , U, V, W, X, Y and Z are as defined in the specification.
摘要翻译：本发明涉及新的吲哚-3-基 - 羰基 - 氮杂螺哌啶衍生物作为V1a受体拮抗剂，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑抑郁症和其它疾病。特别地，本发明涉及通式（I）的化合物，其中R 1至R 6，U，V，W，X，Y和Z分别为如说明书中所定义。

33. 发明申请

WO2008080842A1 INDOLES 审中-公开
标题翻译：吲哚
公开(公告)号：WO2008080842A1
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064176
申请日：2007-12-19
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D401/14 , A61K31/404 , A61P25/00 , A61P9/00
CPC分类号： C07D401/14
摘要： The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R 1 to R 10 are as described in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新的吲哚-3-基 - 羰基 - 哌啶 - 苯并吡咯啉酮 - 苯并恶唑酮和 - 苯并三唑衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。特别地，本发明涉及通式（I）的化合物，其中X，Y和R 1至R 10如说明书所述。

34. 发明申请

WO2008077811A1 SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译：螺旋哌啶衍生物
公开(公告)号：WO2008077811A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/063882
申请日：2007-12-13
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D211/16 , C07D471/10 , C07D491/10 , C07D519/00 , A61K31/438 , A61K31/5377 , A61P25/00
CPC分类号： C07D211/16 , C07D471/10 , C07D491/10 , C07D519/00
摘要： The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I), wherein R 1 to R 5 , R 5' , X, Y and A are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新型螺 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。特别地，本发明涉及通式（I）的化合物，其中R 1至R 5，R 5'， X，Y和A如说明书中所定义。

35. 发明申请

WO2008068159A1 SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译：螺旋哌啶衍生物
公开(公告)号：WO2008068159A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062857
申请日：2007-11-27
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D471/10 , C07D498/10 , A61K31/438 , A61P9/02
CPC分类号： C07D471/10 , C07D498/10
摘要： Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general Formula (I) wherein R 1 to R 11 and X are as defined in the description.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新的吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。本发明的化合物具有通式（I），其中R 1至R 11和X如说明书中所定义。

36. 发明申请

WO2007039438A1 INDOL-3-YL-CARBONYL-AZASPIRO DERIVATIVES AS VASOPRESSIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚-3-甲基亚苄基衍生物作为血管紧张素受体拮抗剂
公开(公告)号：WO2007039438A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066441
申请日：2006-09-18
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D491/10 , C07D471/10 , A61K31/4355 , A61K31/437 , A61P9/00 , A61P25/00
CPC分类号： C07D471/10 , C07D491/10
摘要： This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as Via receptor antagonists and which are represented by Formula (I) wherein the azaspiro-head group A and the residues R 1 , R 2 and R 3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in medicaments against dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
摘要翻译：本发明涉及作为Via受体拮抗剂并由式（I）表示的吲哚-3-基 - 羰基 - 氮杂螺环衍生物，其中阿扎头罗头基A和残基R 1，R ＆lt; SUP＆gt; 2＆gt;和＆lt; 3＆gt;如本文所定义。本发明还涉及含有这些化合物的药物组合物，其用于抗痛经，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍的药物中的用途及其制备方法。

37. 发明申请

WO2007014851A2 INDOL-3-YL-CARBONYL-PIPERIDIN AND PIPERAZIN DERIVATIVES 审中-公开
标题翻译：吲哚-3-基 - 碳 - 哌啶和哌嗪衍生物
公开(公告)号：WO2007014851A2
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064395
申请日：2006-07-19
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D401/06 , C07D405/14 , C07D209/22 , C07D209/42
CPC分类号： C07D209/42 , C07D209/22 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D495/04
摘要： The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula (I) wherein the residues R 1 to R 3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in medicaments against dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders, and methods of preparation thereof.
摘要翻译：本发明涉及作为V1a受体拮抗剂并由式（I）表示的吲哚-3-基 - 羰基 - 哌啶和哌嗪衍生物，其中残基R 1至R 3 如本文所定义。本发明还涉及含有这些化合物的药物组合物，它们在抗痛经药物，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍中的用途及其制备方法。

38. 发明申请

WO2005092856A8 TETRAHYDROCARBAZOLES AND DERIVATIVES 审中-公开
标题翻译：四氯化碳和衍生物
公开(公告)号：WO2005092856A8
公开(公告)日：2006-12-21
申请号：PCT/EP2005002869
申请日：2005-03-17
申请人： HOFFMANN LA ROCHE , DEHMLOW HENRIETTA , KUHN BERND , MASCIADRI RAFFAELLO , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
发明人： DEHMLOW HENRIETTA , KUHN BERND , MASCIADRI RAFFAELLO , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
IPC分类号： A61K31/40 , C07D209/70 , C07D209/86 , C07D209/88 , C07D401/12 , C07D403/06 , C07D403/12 , C07D411/06 , C07D411/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04
CPC分类号： C07D413/06 , C07D209/70 , C07D209/88 , C07D403/12 , C07D413/14 , C07D417/06
摘要： The present invention relates to compounds of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 , X 2 , X 3 , X 4 , n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXRa and/or LXRß agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，其中，R 5，X 5，X 1，X 2，X 3，X 4， SUP，n和k在说明书和权利要求书中被定义，以及其药学上可接受的盐和/或其药学上可接受的酯。该化合物可用于治疗和预防由LXRα和/或LXRβ激动剂调节的疾病，包括增加脂质和胆固醇水平，特别是低HDL-胆固醇，高LDL-胆固醇，动脉粥样硬化疾病，糖尿病，特别是非胰岛素依赖性糖尿病，代谢综合征，血脂异常，阿尔茨海默氏病，败血症，炎性疾病如结肠炎，胰腺炎，胆汁淤积/肝纤维化，以及具有炎性成分如阿尔茨海默病和受损/可改善的认知功能的疾病。

39. 发明申请

WO2013004642A1 1, 2, 4 -THIADIAZOL- 5 -YLPIPERAZINE DERIVATIVES USEFUL IN THE TREATMENT NEURODEGENERATIVE DISEASES 审中-公开
标题翻译： 1,2,4-噻二唑-5-基哌啶衍生物用于治疗神经损伤性疾病
公开(公告)号：WO2013004642A1
公开(公告)日：2013-01-10
申请号：PCT/EP2012/062778
申请日：2012-06-29
申请人： REMYND NV , GRIFFIOEN, Gerard , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , VIFIAN, Walter
发明人： GRIFFIOEN, Gerard , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/433 , A61P25/28
CPC分类号： C07D285/135 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
摘要翻译：本发明涉及式（IA）化合物本发明还涉及式IA化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

40. 发明申请

WO2012004207A1 (3 -METHYLPYRROLIDIN- 3 - YL) METHYL PYRIDINYL ETHER DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：（3-甲基吡咯烷-3-基）甲基吡啶基醚衍生物及其作为NK-3受体拮抗剂的用途
公开(公告)号：WO2012004207A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061168
申请日：2011-07-04
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
发明人： NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/4439 , A61P25/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The invention relates to a compound of general formula : (I) wherein A is selected from the groups (a), (b) or (c): formula (II) or formula (III) (b) or is cycloalkyl, (c) optionally substituted by lower alkyl (c);Ar 1 is phenyl or a six membered heteroaryl;X 1 is N or CH; X 2 is N-R 1 or O; R 1 is S(O) 2 -lower alkyl, C(O)-cycloalkyl substituted by lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano, cycloalkyl or is a six membered heteroaryl substituted by lower alkyl, cyano, C(O)-lower alkyl, halogen, lower alkyl substituted by halogen or lower alkoxy; or is phenyl substituted by cyano or halogen; R 2 is lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted by cyano, or is phenyl substituted by halogen, or is cyano, lower alkoxy, or is piperidin-2-one; or to pharmaceutically active salts, sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof..It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinsons disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及通式（I）的化合物，其中A选自（a），（b）或（c）：式（II）或式（III）（b）或环烷基，（c ），任选被（C）的低级烷基取代; Ar 1是苯基或6元杂芳基; X 1是N或CH; X2是N-R1或O; R 1是S（O）2-低级烷基，被低级烷基取代的C（O） - 环烷基，或是C（O） - 低级烷基，低级烷基，氰基，环烷基或是被低级烷基，氰基取代的六元杂芳基，C（O） - 低级烷基，卤素，被卤素或低级烷氧基取代的低级烷基; 或被氰基或卤素取代的苯基; R2是低级烷基，卤素，吡唑基，3-甲基 - [1,2,4]恶唑基，5-甲基 - [1,2,4]恶二唑-3-基，被氰基取代的吡啶基，或被卤素取代的苯基或氰基，低级烷氧基或哌啶-2-酮; 或药学活性盐，异构异构体形式，包括式I化合物的单独的非对映异构体和对映异构体，以及外消旋和非外消旋混合物。已经发现，本发明化合物是高潜在的NK-3受体拮抗剂抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的治疗。

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