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1. 发明申请

WO2007107298A1 PHTHALAZINONE PYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：苯并噻唑酮衍生物及其制备方法及用作药物代理
公开(公告)号：WO2007107298A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/002332
申请日：2007-03-16
申请人： F. HOFFMANN-LA ROCHE AG , BOYD, Edward , BROOKFIELD, Frederick , COURTNEY, Steve , GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , PRIME, Michael , RUEGER, Petra , RUETH, Matthias
发明人： BOYD, Edward , BROOKFIELD, Frederick , COURTNEY, Steve , GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , PRIME, Michael , RUEGER, Petra , RUETH, Matthias
IPC分类号： C07D403/12 , C07D401/14 , A61K31/495 , A61P35/00
CPC分类号： C07D403/12 , C07D401/14
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

2. 发明申请

WO2007107346A1 SUBSTITUTED INDAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：取代的吲哚衍生物，其制造和用作药物代理
公开(公告)号：WO2007107346A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/002487
申请日：2007-03-21
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
发明人： GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

3. 发明申请

WO2006108489A1 AMINOPYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：氨基吡唑衍生物，其制造和用作药物代理
公开(公告)号：WO2006108489A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/002478
申请日：2006-03-17
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KUENKELE, Klaus-Peter , LEMARCHAND, Aude , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
发明人： GEORGES, Guy , GOLLER, Bernhard , KUENKELE, Klaus-Peter , LEMARCHAND, Aude , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

4. 发明申请

WO2006133885A1 TRICYCLIC FUSED INDOLE DERIVATIVES AND THEIR USE AS AURORA KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC FUSED INDOLE DERIVATIVES AND THE E USUR作为AURORA KINASE INHIBITORS
公开(公告)号：WO2006133885A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005633
申请日：2006-06-13
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
发明人： GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
IPC分类号： C07D487/04 , A61P35/00 , A61K31/4155 , C07D209/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法以及上述用途所述化合物可用于控制或预防诸如癌症等疾病。

5. 发明申请

WO2008017465A1 BICYCLIC LACTAM DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：双相乳酸衍生物，其制造和用作药物代理
公开(公告)号：WO2008017465A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/007006
申请日：2007-08-08
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias
发明人： GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00 , A61P25/00 , A61P9/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述化合物在控制或预防癌症等疾病。

6. 发明申请

WO2006108488A1 TRICYCLIC AZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：三氯化钛衍生物，其制造和用作药物代理
公开(公告)号：WO2006108488A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/002477
申请日：2006-03-17
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
发明人： GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00 , A61P43/00 , C07D209/00 , C07D235/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）的化合物，其药学上可接受的盐，对映体形式，非对映异构体和外消旋物，上述化合物的制备，含有它们的药物及其制备，以及上述用途控制或预防疾病如癌症的化合物。

7. 发明申请

WO2006063841A3 TRYCYCLIC HETEROCYCLES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
公开(公告)号：WO2006063841A3
公开(公告)日：2006-06-22
申请号：PCT/EP2005/013557
申请日：2005-12-16
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KUENKELE, Klaus-Peter , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine
发明人： GEORGES, Guy , GOLLER, Bernhard , KUENKELE, Klaus-Peter , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine
IPC分类号： C07D487/04 , A61K31/4188
摘要： Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

8. 发明申请

WO2007068465A1 TRICYCLIC LACTAM DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：三聚赖氨酸衍生物，其制造和用作药物代理
公开(公告)号：WO2007068465A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/011998
申请日：2006-12-13
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
发明人： GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , LIMBERG, Anja , REIFF, Ulrike , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
IPC分类号： C07D487/04 , A61K31/4164 , A61P35/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）的化合物，其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述用途所述化合物可用于控制或预防诸如癌症等疾病。

9. 发明申请

WO2006032519A1 TRICYCLES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译： TRICYCLES，他们的制造和用作药物代理
公开(公告)号：WO2006032519A1
公开(公告)日：2006-03-30
申请号：PCT/EP2005/010312
申请日：2005-09-23
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , KUENKELE, Klaus-Peter , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias
发明人： GEORGES, Guy , GOLLER, Bernhard , KRELL, Hans-Willi , KUENKELE, Klaus-Peter , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias
IPC分类号： A61K31/4188 , A61K31/4745 , C07D487/04 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Objects of the present invention are the compounds of Formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋物，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

10. 发明申请

WO2009019163A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
公开(公告)号：WO2009019163A1
公开(公告)日：2009-02-12
申请号：PCT/EP2008/059908
申请日：2008-07-29
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
IPC分类号： C07D401/08 , C07D401/06
CPC分类号： C07D401/06 , C07D401/08
摘要： The invention relates to a compound of general formula (I) wherein Ar 1 is aryl or a five or six membered heteroaryl; Ar 2 is aryl or a five or six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O) 2 -lower alkyl, -S(O) 2 -di-lower alkyl amino, -(CH 2 ) q R, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl or CH 2 OH; R 4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R 1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R 2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R 4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, 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, Parkinson's 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Ar 1是芳基或五或六元杂芳基; Ar 2是芳基或五或六元杂芳基; R 1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O）氨基， - （CH 2）q R，氰基，氨基，一或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n为1,2或3; 在n为2或3的情况下，R 1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R 2可以相同或不同; p为1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q为1或2; 或其药物活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。已经发现，本发明化合物是用于治疗抑郁症，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。

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