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61. 发明授权

EP2855483B1 PYRROLOPYRROLIDINONE COMPOUNDS 有权
标题翻译：吡咯并吡咯烷酮化合物
公开(公告)号：EP2855483B1
公开(公告)日：2017-10-25
申请号：EP13734183.0
申请日：2013-05-22
申请人： Novartis AG
发明人： COTESTA, Simona , FURET, Pascal , GUAGNANO, Vito , HOLZER, Philipp , KALLEN, Joerg , MAH, Robert , MASUYA, Keiichi , SCHLAPBACH, Achim , STUTZ, Stefan , VAUPEL, Andrea
IPC分类号： C07D487/04 , A61K31/407 , A61P35/00
CPC分类号： C07D487/04 , A61K31/407 , A61K31/41 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06

62. 发明授权

EP2807164B1 IMIDAZOPYRROLIDINONE COMPOUNDS 有权
标题翻译：咪唑并吡啶酮化合物
公开(公告)号：EP2807164B1
公开(公告)日：2017-04-05
申请号：EP13711952.5
申请日：2013-01-25
申请人： Novartis AG
发明人： FURET, Pascal , GUAGNANO, Vito , HOLZER, Philipp , KALLEN, Joerg , LIAO, Lv , MAH, Robert , MAO, Liang , MASUYA, Keiichi , SCHLAPBACH, Achim , STUTZ, Stefan , VAUPEL, Andrea
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4188 , A61K31/4439 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06
摘要： The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译：本发明涉及式（I）化合物：如本文所述，包含此类化合物的药物制剂，用于此类化合物在治疗由MDM2和/或MDM4活性介导的病症或疾病中的用途和方法，以及包含这些化合物的组合

63. 发明公开

EP2948453A1 PYRAZOLO[3,4-D]PYRIMIDINONE COMPOUNDS AS INHIBITORS OF THE P53/MDM2 INTERACTION 有权
标题翻译：吡唑并[3,4-D] PYRIMIDINONVERBINDUNGEN ALS INHIBITOREN DER P53 / MDM2-INTERAKTION
公开(公告)号：EP2948453A1
公开(公告)日：2015-12-02
申请号：EP14704909.2
申请日：2014-01-21
申请人： Novartis AG
发明人： FURET, Pascal , GUAGNANO, Vito , HOLZER, Philipp , KALLEN, Joerg , MAH, Robert , MASUYA, Keiichi , SCHLAPBACH, Achim , VAUPEL, Andrea
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译：本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及包含这些化合物的组合。

65. 发明公开

EP2721007A1 CYCLOHEXYL ISOQUINOLINONE COMPOUNDS 有权
标题翻译：环己基异喹啉酮CONNECTIONS
公开(公告)号：EP2721007A1
公开(公告)日：2014-04-23
申请号：EP12728089.9
申请日：2012-06-19
申请人： Novartis AG
发明人： HOLZER, Philipp , MASUYA, Keiichi , GUAGNANO, Vito , FURET, Pascal , KALLEN, Joerg , STUTZ, Stefan
IPC分类号： C07D217/04 , C07D405/08 , A61K31/47 , A61P35/00
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , C07D217/04 , C07D401/08 , C07D405/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.

66. 发明公开

EP1915366A2 PIPERAZINE DERIVATIVE RENIN INHIBITORS 审中-公开
标题翻译：哌嗪衍生物肾素抑制剂
公开(公告)号：EP1915366A2
公开(公告)日：2008-04-30
申请号：EP06753947.8
申请日：2006-05-29
申请人： Novartis AG
发明人： NIHONYANAGI, Atsuko, Novartis Pharma K.K. , TOYAO, Atsushi, Novartis Pharma K.K. , IWAKI, Yuki, Novartis Pharma K.k. , MASUYA, Keiichi
IPC分类号： C07D403/12 , A61K31/496 , C07D417/14
CPC分类号： C07D417/14 , C07D403/12
摘要： The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula (I), wherein R1, R2, R11, C, E and D are as defined in the specification.
摘要翻译：本发明涉及取代的3,4-或更高取代的哌嗪化合物，其用于制备用于治疗取决于肾素活性的疾病的药物制剂的用途; 使用该类化合物治疗取决于肾素活性的疾病; 这些化合物用于诊断和治疗温血动物，特别是用于治疗取决于肾素活性的疾病（=病症）; 包含所述化合物的药物制剂或产品，和/或包括施用所述化合物的治疗方法，制备所述化合物的方法以及新的中间体，原料和/或其合成的部分步骤。该化合物尤其是式（I）的化合物，其中R 1，R 2，R 11，C，E和D如说明书中所定义。

67. 发明公开

EP1907359A2 3,5-SUBSTITUTED PIPERIDINE DERIVATIVES EFFECTIVE ON RENIN-RELATED DISORDERS 审中-公开
标题翻译：对肾素活性的诊断和治疗为本病SUITABLE哌啶
公开(公告)号：EP1907359A2
公开(公告)日：2008-04-09
申请号：EP06762515.2
申请日：2006-07-10
申请人： Novartis AG
发明人： BREITENSTEIN, Werner , EHRHARDT, Claus , MAIBAUM, Juergen, Klaus , OSTERMANN, Nils , ZIMMERMANN, Juerg , MASUYA, Keiichi , KONISHI, Kazuhide , YOKOKAWA, Fumiaki , KANAZAWA, Takanori , JACOBY, Edgar , MARZINZIK, Andreas , GROSCHE, Philipp , KAWAKAMI, Shimpei
IPC分类号： C07D211/56 , C07D409/12 , C07D403/12 , C07D417/12 , C07D413/12 , C07D413/14 , C07D403/14 , A61K31/55 , A61P9/00
CPC分类号： C07D403/14 , C07D211/56 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3, 5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1 , R2, T, R3 and R4 are as defined in the specification.

68. 发明授权

EP1592426B1 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： 2 CYANOPYRROLOPYRIMIDINE和它们的药物用途
公开(公告)号：EP1592426B1
公开(公告)日：2007-12-19
申请号：EP04708332.4
申请日：2004-02-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BUXTON, Francis, Paul , EHARA, Takeru , GANJU, Pamposh, Novartis Inst. Medical Sciences , HALLETT, Allan, Novartis Inst. Medical Sciences , IRIE, Ozamu , IWASAKI, Atsuko , KANAZAWA, Takanori , MASUYA, Keiichi , NONOMURA, Kazuhiko , SAKAKI, Junichi , SNELL, Christopher, Robert , SONG, Chuanheng , TANABE, Keiko , TENO, Naoki , UMEMURA, Ichiro , YOKOKAWA, Fumiaki
IPC分类号： A61K31/519 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.

69. 发明公开

EP1858849A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：EP1858849A1
公开(公告)日：2007-11-28
申请号：EP06707453.4
申请日：2006-03-07
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： MASUYA, Keiichi , YOKOKAWA, Fumiaki, Novartis Pharma K.K. , IRIE, Osamu, Novartis Pharma K.K. , NIHONYANAGI, Atsuko, Novartis Pharma K.K. , TOYAO, Atsushi, Novartis Pharma K.K. , EHARA, Takeru, Novartis Pharma K.K. , KONISHI, Kazuhide, Novartis Pharma K.K. , KANAZAWA, Takanori, Novartis Pharma K.K. , SUZUKI, Masaki, Novartis Pharma K.K.
IPC分类号： C07D211/60 , C07D401/12 , C07D413/12 , A61K31/4545 , A61P9/00
CPC分类号： C07D401/12 , C07D211/60 , C07D413/12
摘要： 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds are of the formula (I), wherein the substitutents are as defined in the specification.
摘要翻译： 3,4,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗取决于肾素活性的疾病（=病症）; 该类化合物在制备用于治疗取决于肾素活性的疾病的药物制剂中的用途; 使用该类化合物治疗取决于肾素活性的疾病; 包含3,4,5-取代哌啶化合物的药物制剂，和/或包括给予3,4,5-取代哌啶化合物的治疗方法，制备3,4,5-取代哌啶化合物的方法，以及新的中间体和其合成的部分步骤。化合物是式（I）的化合物，其中取代基如说明书中所定义。

70. 发明公开

EP1592426A1 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： 2 CYANOPYRROLOPYRIMIDINE和它们的药物用途
公开(公告)号：EP1592426A1
公开(公告)日：2005-11-09
申请号：EP04708332.4
申请日：2004-02-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BUXTON, Francis, Paul , EHARA, Takeru , GANJU, Pamposh,Novartis Inst. Medical Sciences , HALLETT, Allan,Novartis Inst. Medical Sciences , IRIE, Ozamu , IWASAKI, Atsuko , KANAZAWA, Takanori , MASUYA, Keiichi , NONOMURA, Kazuhiko , SAKAKI, Junichi , SNELL, Christopher, Robert , SONG, Chuanheng , TANABE, Keiko , TENO, Naoki , UMEMURA, Ichiro , YOKOKAWA, Fumiaki
IPC分类号： A61K31/519 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.

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