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1. 发明申请

WO2013060751A1 NOVEL PYRAZINE DERIVATIVES 审中-公开
标题翻译：新型吡嗪衍生物
公开(公告)号：WO2013060751A1
公开(公告)日：2013-05-02
申请号：PCT/EP2012/071093
申请日：2012-10-25
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , DHURWASULU, Baledi , GRETHER, Uwe , HAZRA, Anindya , HEBEISEN, Paul , ROEVER, Stephan , ROGERS-EVANS, Mark
发明人： BISSANTZ, Caterina , DHURWASULU, Baledi , GRETHER, Uwe , HAZRA, Anindya , HEBEISEN, Paul , ROEVER, Stephan , ROGERS-EVANS, Mark
IPC分类号： C07D241/12 , C07D241/18 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/497 , A61P9/00
CPC分类号： C07D413/12 , C07D241/12 , C07D241/18 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention relates to a compound of formula (I), wherein R 1 to R 4 are defined as 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R 1至R 4如在说明书和权利要求书中所定义。式（I）化合物可以用作药物。

2. 发明申请

WO2011020806A1 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINE DERIVATIVES 审中-公开
标题翻译： 3-氨基-5-苯基-5,6-二氢-2H- [1,4]氧杂衍生物
公开(公告)号：WO2011020806A1
公开(公告)日：2011-02-24
申请号：PCT/EP2010/061875
申请日：2010-08-16
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , ANDREINI, Matteo , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , TRAVAGLI, Massimiliano , VALACCHI, Michela , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： ANDREINI, Matteo , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , TRAVAGLI, Massimiliano , VALACCHI, Michela , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5377
CPC分类号： C07D413/12 , C07D265/30 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[l,4]oxazine derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明涉及具有BACE1和/或BACE2抑制活性的式（I）的3-氨基-5-苯基-5,6-二氢-2H- [1,4]恶嗪衍生物，其制备方法，含有它们的药物组合物和它们作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

3. 发明申请

WO2010012620A1 PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS 审中-公开
标题翻译：吡咯烷-3-基甲基胺作为OREXIN拮抗剂
公开(公告)号：WO2010012620A1
公开(公告)日：2010-02-04
申请号：PCT/EP2009/059271
申请日：2009-07-20
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/423 , A61P25/00
CPC分类号： C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要： The present invention is concerned with compounds of formula (I) wherein R 1 , R 2 , Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，Ar，杂芳基，m和n如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗其中涉及食欲素途径的病症。

4. 发明申请

WO2009153180A1 HETEROAROMATIC MONOAMIDES AS OREXININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为OREXININ受体拮抗剂的异种单体
公开(公告)号：WO2009153180A1
公开(公告)日：2009-12-23
申请号：PCT/EP2009/056992
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D231/40 , C07D261/08 , C07D277/46 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07K5/02 , A61K31/44 , A61K31/4406
CPC分类号： C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D231/40 , C07D261/08 , C07D277/46 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention is concerned with novel sulfonamides of formula I wherein R 1 , R 2 , R 3 , R 4 , R 5 , Ar, Ar 1 , Ar 2 , n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及式I的新型磺酰胺，其中R 1，R 2，R 3，R 4，R 5，Ar，Ar 1，Ar 2，n，o和p如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗涉及食欲素途径的病症。

5. 发明申请

WO2008122513A1 HETEROCYCLES AS OREXIN ANTAGONISTS 审中-公开
标题翻译：杂交体作为OREXIN拮抗剂
公开(公告)号：WO2008122513A1
公开(公告)日：2008-10-16
申请号：PCT/EP2008/053545
申请日：2008-03-26
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D471/04 , C07D495/04 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61P25/00 , A61P43/00
CPC分类号： C07D471/04 , C07D495/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 /R 2 are independently from each other hydrogen or lower alkyl; R 3 is independently from the number of substituents hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; hetaryl is a one or two membered heteroaromatic ring, connected to the carbon atoms of the piperidine group selected from the group consisting of (II), (II), (IV) or (V) or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2彼此独立地为氢或低级烷基; R 3独立于取代基的数目，氢，卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或低级烷氧基; R 4是卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或低级烷氧基; 杂芳基是与选自（II），（II），（IV）或（V）的哌啶基团的碳原子连接的一个或两个元杂芳环，或者与药学上合适的酸加成盐，光学上纯的对映异构体，外消旋体或非对映体混合物。已经发现，式I化合物是食欲素受体拮抗剂，并且相关化合物可用于治疗其中食欲素途径如睡眠障碍的疾病。

6. 发明申请

WO2008068183A1 INDOLES 审中-公开
标题翻译：吲哚
公开(公告)号：WO2008068183A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062983
申请日：2007-11-29
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： C07D401/04 , C07D413/14 , A61K31/404 , A61P29/00
CPC分类号： C07D401/04 , C07D413/14
摘要： The present invention is concerned with novel indol-2-yl-carbonyl-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 5 and other diseases. Present invention is concerned with compounds of the general formula (I), A: (a), (b), (c) wherein R 1 to R 6 , R 8 to R 14 , R 12' , R 13' , X and Y are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新的吲哚-2-基 - 羰基 - 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/或治疗焦虑和抑郁障碍5及其它疾病。本发明涉及通式（I）的化合物：A：（a），（b），（c）其中R 1至R 6， R 8，R 14，R 12，R 13，X和Y如说明书中所定义。

7. 发明申请

WO2007077122A1 INDOL-3-YL-CARBONYL-SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译：吲哚-3-基 - 碳 - 螺 - 哌啶衍生物
公开(公告)号：WO2007077122A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/069897
申请日：2006-12-19
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： C07D471/10 , C07D498/10 , A61K31/438 , A61P9/02
CPC分类号： C07D471/10
摘要： This invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula (I) wherein the spiropiperidine-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V1a受体拮抗剂的吲哚-3-基 - 羰基 - 螺 - 哌啶衍生物，其由式（I）表示，其中spiropiperidine-head基团A和残基R 1 R 2和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，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。

8. 发明申请

WO2007014851A3 INDOL-3-YL-CARBONYL-PIPERIDIN AND PIPERAZIN DERIVATIVES 审中-公开
标题翻译： INDOL-3-YL-羰基哌啶和哌嗪衍生物
公开(公告)号：WO2007014851A3
公开(公告)日：2007-05-31
申请号：PCT/EP2006064395
申请日：2006-07-19
申请人： HOFFMANN LA ROCHE , 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 , A61K31/454 , A61P9/12 , C07D209/22 , C07D209/42 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D495/04
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受体拮抗剂起作用的吲哚-3-基 - 羰基 - 哌啶和哌嗪衍生物，其由式（I）表示，其中残基R 1至R 3 如本文所定义。本发明进一步涉及含有这些化合物的药物组合物，它们在抗痛经，高血压，慢性心力衰竭，血管加压素分泌不当，肝硬化，肾病综合征，强迫症，焦虑和抑郁症的药物中的用途，以及它们的制备方法。

9. 发明申请

WO2013068306A1 [1, 2, 3] TRIAZOLO [4, 5 -D] PYRIMIDINE DERIVATIVES AS AGONISTS OF THE CANNABINOID RECEPTOR 2 审中-公开
标题翻译： [1,2,3]三唑并[4,5-D]吡啶衍生物作为CANNABINOID受体2的激动剂
公开(公告)号：WO2013068306A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/071788
申请日：2012-11-05
申请人： F. HOFFMANN-LA ROCHE AG , ADAM, Jean-Michel , BISSANTZ, Caterina , GRETHER, Uwe , KIMBARA, Atsushi , NETTEKOVEN, Matthias , ROEVER, Stephan , ROGERS-EVANS, Mark
发明人： ADAM, Jean-Michel , BISSANTZ, Caterina , GRETHER, Uwe , KIMBARA, Atsushi , NETTEKOVEN, Matthias , ROEVER, Stephan , ROGERS-EVANS, Mark
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10 , A61P9/10 , A61P27/06
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/2054 , A61K9/4866 , A61K31/519 , A61K47/10 , C07D491/107
摘要： The invention relates to a compound of formula (I), wherein A, R 1 and R 2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament as agonists of the cannabinoid receptor 2.
摘要翻译：本发明涉及式（I）化合物，其中A，R 1和R 2如描述和权利要求中所定义。式（I）化合物可以用作大麻素受体2的激动剂的药物。

10. 发明申请

WO2013024168A1 PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物
公开(公告)号：WO2013024168A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/066136
申请日：2012-08-17
申请人： REMYND NV , GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
发明人： GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , A61K31/433 , A61P25/28
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G 1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is -NR 2 R 3 ; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl; tetrahydropyran-4-yl; -CH 2 -cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R 2 and R 3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is -CH 2 - or -(CH 2 ) 2 -; Ar is phenyl or pyridinyl; R 4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a 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，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基; 四氢吡喃-4-基; 苯; 被一个或多个卤素取代的苯乙基; 苯氧基; 被一个或多个卤素取代的苯氧基甲基; 苄氧; 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基; 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。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。

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