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1. 发明申请

WO2014009833A2 COMPLEMENT PATHWAY MODULATORS AND USES THEREOF 审中-公开
标题翻译：补充道路调节器及其用途
公开(公告)号：WO2014009833A2
公开(公告)日：2014-01-16
申请号：PCT/IB2013055302
申请日：2013-06-27
申请人： NOVARTIS AG , HOMMEL ULRICH , LORTHIOIS EDWIGE LILIANE JEANNE , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , RANDL STEFAN ANDREAS , VULPETTI ANNA
发明人： HOMMEL ULRICH , LORTHIOIS EDWIGE LILIANE JEANNE , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , RANDL STEFAN ANDREAS , VULPETTI ANNA , ROGEL OLIVIER
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , A61K31/4155 , A61K31/416 , A61K31/437 , A61K45/06 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了式I化合物：制备本发明化合物的方法及其治疗用途。本发明进一步提供药理活性剂和药物组合物的组合。

2. 发明申请

WO2007006534A3 PIPERIDINE DERIVATIVES USEFUL IN THE DIAGNOSTIC AND THERAPEUTIC TREATMENT OF DISEASES DEPENDING ON RENIN ACTIVITY 审中-公开
标题翻译：依托仁活性诊断和治疗疾病治疗有效的哌啶衍生物
公开(公告)号：WO2007006534A3
公开(公告)日：2007-04-19
申请号：PCT/EP2006006733
申请日：2006-07-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , 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
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 , A61K31/55 , A61P9/00 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
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.
摘要翻译：本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法和新的中间体和部分其合成步骤。优选的化合物（其也可以盐形式存在）具有式I，其中R 1，R 2，T，R 3和R 4如说明书中所定义。

3. 发明申请

WO2014002051A2 COMPLEMENT PATHWAY MODULATORS AND USES THEREOF 审中-公开
标题翻译：补充道路调节器及其用途
公开(公告)号：WO2014002051A2
公开(公告)日：2014-01-03
申请号：PCT/IB2013055292
申请日：2013-06-27
申请人： NOVARTIS AG , ALTMANN EVA , HOMMEL ULRICH , LORTHIOIS EDWIGE LILIANE JEANNE , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , QUANCARD JEAN , RANDL STEFAN ANDREAS , VULPETTI ANNA
发明人： ALTMANN EVA , HOMMEL ULRICH , LORTHIOIS EDWIGE LILIANE JEANNE , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , QUANCARD JEAN , RANDL STEFAN ANDREAS , VULPETTI ANNA , ROGEL OLIVIER
IPC分类号： C07D403/06
CPC分类号： C07D403/06 , A61K31/416 , A61K31/4162 , A61K45/06 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了式I化合物：（I）制备本发明化合物的方法及其治疗用途。本发明进一步提供药理活性剂和药物组合物的组合。

4. 发明申请

WO2007006534A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007006534A2
公开(公告)日：2007-01-18
申请号：PCT/EP2006/006733
申请日：2006-07-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , 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
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 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
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.
摘要翻译：本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法和新的中间体和部分其合成步骤。优选的化合物（其也可以盐形式存在）具有式I，其中R 1，R 2，T，R 3和R 4如说明书中所定义。

5. 发明申请

WO2006066896A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006066896A2
公开(公告)日：2006-06-29
申请号：PCT/EP2005/013786
申请日：2005-12-21
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BREITENSTEIN, Werner , COTTENS, Sylvain , EHRHARDT, Claus , JACOBY, Edgar , LORTHIOIS, Edwige, Liliane, Jeanne , MAIBAUM, Juergen, Klaus , OSTERMANN, Nils , SELLNER, Holger , SIMIC, Oliver
发明人： BREITENSTEIN, Werner , COTTENS, Sylvain , EHRHARDT, Claus , JACOBY, Edgar , LORTHIOIS, Edwige, Liliane, Jeanne , MAIBAUM, Juergen, Klaus , OSTERMANN, Nils , SELLNER, Holger , SIMIC, Oliver
IPC分类号： C07D207/09 , C07D207/14 , C07D401/12 , C07D405/12 , C07D403/12 , C07D409/12 , C07D207/08 , C07D413/12 , C07D417/12 , C07D491/10 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/54 , A61P9/00
CPC分类号： C07D207/08 , C07D207/09 , C07D207/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/10
摘要： Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine 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 inappropriate 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 inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as described in the specificacion.
摘要翻译：新型3-单，3,4-二和3,4,4-三取代的吡咯烷化合物，用于诊断和治疗温血动物，特别是用于治疗疾病的化合物（=无序），取决于肾素的不适当活动; 使用该类化合物制备用于治疗依赖于肾素不适当活性的疾病的药物制剂; 使用该类化合物治疗依赖肾素不适当活动的疾病; 包括所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的方法，制备所述取代的吡咯烷化合物的方法和新的中间体及其合成的部分步骤。取代的吡咯烷化合物特别是式（I）的化合物，其中取代基如在分子中所述。

6. 发明申请

WO2005054177A1 DELTA-AMINO-GAMMA-HYDROXY-OMEGA-ARYL-ALKANOIC ACID AMIDES AND USE AS RENIN INHIBITORS 审中-公开
标题翻译： DELTA-氨基 - 氨基 - 羟基 - 欧米亚 - 阿尔卡酸 - 氨基酸和用作RENIN抑制剂
公开(公告)号：WO2005054177A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013589
申请日：2004-11-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SELLNER, Holger , GROSS, Gerhard , MAIBAUM, Juergen, Klaus , COTTENS, Sylvain
发明人： SELLNER, Holger , GROSS, Gerhard , MAIBAUM, Juergen, Klaus , COTTENS, Sylvain
IPC分类号： C07C237/22
CPC分类号： C07C237/22
摘要： The invention relates to novel δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amides of formula (I), or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）的新型δ-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺或其药学上可接受的盐。

7. 发明申请

WO2014005150A1 CRYSTALLINE FORMS OF L-(2-((LR,3S,5R)-3-( (2 -FLUORO-3 - (TRIFLUOROMETHOXY) PHENYL) CARBAMOYL) - 2 -AZABICYCL O [3.1.0] HEXAN- 2 -YL) - 2 -OXOETHYL) - 5 -METHYL - 1H - PYRAZOLO [3, 4 -C] PYRIDINE - 3 - CARBOXAMI DE AND SALTS THEREOF 审中-公开
标题翻译： L-（2 - （（LR，3S，5R）-3-（（2-氟-3-（三氟甲酰基）苯基）羰基）-2-氨基] O [3.1.0]庚烷-2-基） -2-乙氧基）-5-甲基-1H-吡唑并[3,4-C]吡啶-3-羧酸酯及其盐
公开(公告)号：WO2014005150A1
公开(公告)日：2014-01-03
申请号：PCT/US2013/048960
申请日：2013-07-01
申请人： NOVARTIS AG , TOWLER, Christopher , ALTMANN, Eva , HOMMEL, Ulrich , LORTHIOIS, Edwige Liliane Jeanne , MAIBAUM, Juergen Klaus , OSTERMANN, Nils , QUANCARD, Jean , RANDL, Stefan Andreas , SIMIC, Oliver , VULPETTI, Anna
发明人： TOWLER, Christopher , ALTMANN, Eva , HOMMEL, Ulrich , LORTHIOIS, Edwige Liliane Jeanne , MAIBAUM, Juergen Klaus , OSTERMANN, Nils , QUANCARD, Jean , RANDL, Stefan Andreas , SIMIC, Oliver , VULPETTI, Anna
IPC分类号： C07D471/04 , A61K31/437 , A61P27/02
CPC分类号： C07D471/04
摘要： Crystalline forms and pharmaceutically acceptable salts of l-(2- ((1 R,3S,5R)-3-((2-fluoro- 3-(trifluoromethoxy)phenyl)carbamoyl)-2- azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4- c]pyridine-3-carboxamide. l-(2-((l R,3S,5R)3-((2-fluoro-3- (trifluoromethoxy)phenyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl) -2-oxoethyl)-5- methyl-1 H-pyrazolo[3,4-c]pyridine-3-carboxamide is useful in treating Age-related Macular Degeneration (AMD).
摘要翻译： 1-（2-（（1R，3S，5R）-3 - （（2-氟-3-（三氟甲氧基）苯基）氨基甲酰基）-2-氮杂双环[3.1.0]己烷 - -2-氧代乙基）-5-甲基-1H-吡唑并[3,4-c]吡啶-3-甲酰胺。 1-（2 - （（1R，3S，5R）3 - （（2-氟-3-（三氟甲氧基）苯基）氨基甲酰基）-2-氮杂双环[3.1.0]己-2-基）-2-氧代乙基）-5-甲基-1H-吡唑并[3,4-c]吡啶-3-甲酰胺可用于治疗年龄相关性黄斑变性（AMD）。

8. 发明申请

WO2014002051A3 COMPLEMENT PATHWAY MODULATORS AND USES THEREOF 审中-公开
公开(公告)号：WO2014002051A3
公开(公告)日：2014-01-03
申请号：PCT/IB2013/055292
申请日：2013-06-27
申请人： NOVARTIS AG , ALTMANN, Eva , HOMMEL, Ulrich , LORTHIOIS, Edwige Liliane Jeanne , MAIBAUM, Juergen Klaus , OSTERMANN, Nils , QUANCARD, Jean , RANDL, Stefan Andreas , VULPETTI, Anna
发明人： ALTMANN, Eva , HOMMEL, Ulrich , LORTHIOIS, Edwige Liliane Jeanne , MAIBAUM, Juergen Klaus , OSTERMANN, Nils , QUANCARD, Jean , RANDL, Stefan Andreas , VULPETTI, Anna
IPC分类号： C07D403/06 , A61K31/401 , A61K31/416 , A61K31/4162 , A61P27/02
摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

9. 发明申请

WO2007144129A3 PYRROLIDINE DERIVATIVES USEFUL AGAINST DISEASES THAT DEPENDS ON ACTIVITY OF RENIN 审中-公开
标题翻译：吡咯烷衍生物有效应用于依赖于仁氏活性的疾病
公开(公告)号：WO2007144129A3
公开(公告)日：2008-03-06
申请号：PCT/EP2007005131
申请日：2007-06-11
申请人： NOVARTIS AG , MAIBAUM JUERGEN KLAUS , LORTHIOIS EDWIGE LILIANE JEANN
发明人： MAIBAUM JUERGEN KLAUS , LORTHIOIS EDWIGE LILIANE JEANN
IPC分类号： C07D405/12 , A61K31/4025
CPC分类号： C07D405/12 , C07D207/14
摘要： Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine 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 inappropriate 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 inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I) wherein the substituents are as described in the specification.
摘要翻译：新型3,4-二，3,3,4-二，3,4,4， - 和3,3,4,4-四取代的吡咯烷化合物，用于诊断和治疗的这些化合物治疗温血动物，特别是用于治疗依赖于肾素不适当活动的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素不适当活性的疾病的药物制剂; 使用该类化合物治疗依赖肾素不适当活动的疾病; 包括所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的方法，制备所述取代的吡咯烷化合物的方法和新的中间体及其合成的部分步骤。取代的吡咯烷化合物特别是式（I），其中取代基如说明书中所述。

10. 发明申请

WO2005051895A8 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2005051895A8
公开(公告)日：2006-07-20
申请号：PCT/EP2004013412
申请日：2004-11-25
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAESCHLIN DANIEL KASPAR , MAIBAUM JUERGEN KLAUS , SELLNER HOLGER
发明人： BAESCHLIN DANIEL KASPAR , MAIBAUM JUERGEN KLAUS , SELLNER HOLGER
IPC分类号： A61K31/165 , A61K31/275 , A61K31/325 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/402 , A61K31/44 , A61K31/5377 , C07C237/20 , C07C237/24 , C07C255/50 , C07C255/60 , C07C271/22 , C07C271/24 , C07C323/29 , C07C323/41 , C07D207/09 , C07D295/02 , C07D295/027 , C07D307/79 , C07D313/08 , C07D319/18 , C07D333/08
CPC分类号： C07C237/20 , C07C237/24 , C07C255/60 , C07C271/22 , C07C271/24 , C07C323/41 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07D207/09 , C07D295/027 , C07D307/79 , C07D313/08 , C07D319/18 , C07D333/08
摘要： Disclosed are d-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
摘要翻译：公开了具有肾素抑制性质的式（I）的d-氨基-β-羟基-α-芳基 - 链烷酰胺化合物及其盐。还公开了包含这些化合物的药物组合物及其用于治疗高血压，动脉粥样硬化，不稳定型冠状动脉综合征，充血性心力衰竭，心脏肥大，心脏纤维化，心肌梗死后心肌梗塞，不稳定型冠状动脉综合征，舒张功能障碍，慢性肾脏疾病，肝脏纤维化，糖尿病引起的并发症，如肾病，血管病变和神经病变，冠状动脉血管疾病，血管成形术后再狭窄，眼内压升高，青光眼，异常血管生长，醛固酮增多症，认知障碍，阿尔茨海默病，痴呆，焦虑状态和认知障碍。

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