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1. 发明申请

WO2007077005A1 3 , 5-SUBSTITΓUED PIPERIDINE COMPOUNDS AS RENIN INHIBITORS 审中-公开
标题翻译： 3,5-取代的哌啶化合物作为RININ抑制剂
公开(公告)号：WO2007077005A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/012581
申请日：2006-12-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , EHARA, Takeru , GROSCHE, Philipp , IRIE, Osamu , IWAKI, Yuki , KANAZAWA, Takanori , KAWAKAMI, Shimpei , KONISHI, Kazuhide , MOGI, Muneto , SUZUKI, Masaki , YOKOKAWA, Fumiaki
发明人： EHARA, Takeru , GROSCHE, Philipp , IRIE, Osamu , IWAKI, Yuki , KANAZAWA, Takanori , KAWAKAMI, Shimpei , KONISHI, Kazuhide , MOGI, Muneto , SUZUKI, Masaki , YOKOKAWA, Fumiaki
IPC分类号： C07D211/60 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545
CPC分类号： C07D401/12 , C07D211/60 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04
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。

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

WO2015013169A9 BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES 审中-公开
标题翻译：合成APELIN多肽的生物活性
公开(公告)号：WO2015013169A9
公开(公告)日：2016-10-20
申请号：PCT/US2014047378
申请日：2014-07-21
申请人： NOVARTIS AG , CAPLAN SHARI L , GOLOSOV ANDREI , GROSCHE PHILIPP , GUIMARAES CARLA , KANTER AARON , LOU CHANGGANG , PARKER DAVID THOMAS , PETERS ERIC C , USERA AIMEE RICHARDSON , YASOSHIMA KAYO , YUAN JUN , ZECRI FREDERIC , ZHAO HONGJUAN
发明人： CAPLAN SHARI L , GOLOSOV ANDREI , GROSCHE PHILIPP , GUIMARAES CARLA , KANTER AARON , LOU CHANGGANG , PARKER DAVID THOMAS , PETERS ERIC C , USERA AIMEE RICHARDSON , YASOSHIMA KAYO , YUAN JUN , ZECRI FREDERIC , ZHAO HONGJUAN
IPC分类号： A61K47/48
CPC分类号： A61K38/10 , A61K38/00 , A61K45/06 , A61K47/542 , A61K47/643 , A61K47/68 , A61K47/6811 , C07K14/47 , C07K14/765 , C07K2319/30 , C07K2319/31
摘要： The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I': I' or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了包含式I'的合成多肽：I'或其酰胺，其酯或其盐的生物缀合物，其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，X 9，X 10，X 11， X12和X13在本文中定义和半衰期延长部分，其中肽和半衰期延长部分任选地经由连接体共价连接或融合。多肽是APJ受体的激动剂。本发明还涉及本发明的生物缀合物的制备方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，布鲁加达综合征，室性心动过速，动脉粥样硬化，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤（包括晒伤）和先兆子痫。本发明还提供药理活性剂和药物组合物的组合。

4. 发明申请

WO2015013168A1 CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译：治疗心力衰竭的循环多糖
公开(公告)号：WO2015013168A1
公开(公告)日：2015-01-29
申请号：PCT/US2014/047377
申请日：2014-07-21
申请人： NOVARTIS AG , BRUCE, Alexandra Marshall , GROSCHE, Philipp , GUIMARAES, Carla , KANTER, Aaron , LOU, Changgang , USERA, Aimee Richardson , YASOSHIMA, Kayo , YUAN, Jun , ZECRI, Frederic , ZHAO, Hongjuan
发明人： BRUCE, Alexandra Marshall , GROSCHE, Philipp , GUIMARAES, Carla , KANTER, Aaron , LOU, Changgang , USERA, Aimee Richardson , YASOSHIMA, Kayo , YUAN, Jun , ZECRI, Frederic , ZHAO, Hongjuan
IPC分类号： C07K14/47 , A61K38/17 , A61P9/04
CPC分类号： C07K14/47 , A61K38/12 , A61K38/1709 , A61K45/06 , A61K47/542 , A61K47/60 , A61K47/643 , A61K47/6811 , C07K7/64 , C07K14/765 , C07K16/461 , C07K2319/30 , C07K2319/31
摘要： The invention provides a cyclic polypeptide of Formula I': I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I'的环状多肽：I或其酰胺，其酯或其盐或其生物缀合物，其中X1，X3，X4，X7，X8，X9，X10，X11，X12和X13被定义于此。多肽是APJ受体的激动剂。本发明还涉及制备本发明多肽或其生物缀合物的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，心室心动过速，动脉粥样硬化，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤（包括晒伤）和先兆子痫。本发明还提供药理活性剂和药物组合物的组合。

5. 发明申请

WO2015013167A1 DISULFIDE CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译：用于治疗心力衰竭的解决循环多糖
公开(公告)号：WO2015013167A1
公开(公告)日：2015-01-29
申请号：PCT/US2014/047375
申请日：2014-07-21
申请人： NOVARTIS AG , ZECRI, Frédéric , GROSCHE, Philipp , YASOSHIMA, Kayo , ZHAO, Hongjuan , YUAN, Jun
发明人： ZECRI, Frédéric , GROSCHE, Philipp , YASOSHIMA, Kayo , ZHAO, Hongjuan , YUAN, Jun
IPC分类号： C07K14/47 , A61K38/17 , A61P9/04
CPC分类号： C07K7/08 , A61K38/08 , A61K38/10 , A61K45/06 , C07K7/06 , C07K14/47
摘要： The invention provides a synthetic polypeptide of Formula I': X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I'的合成多肽：X1-RPR-X5-X6-X7-K-X9-P-X11-X12-X13或其酰胺，酯，盐或生物缀合物，其中X1，X5 ，X6，X7，X9，X11〜X13。多肽和生物缀合物是APJ受体的激动剂。本发明还涉及制备本发明的多肽或生物缀合物的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤受伤（包括晒伤）和先兆子痫。本发明还提供药理活性剂和药物组合物的组合。

6. 发明申请

WO2008028937A1 N-BIARYL (HETERO) ARYLSULPHONAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY LYMPHOCYTES INTERACTIONS 审中-公开
标题翻译：用于治疗由淋巴细胞相互作用介导的疾病的N-BIARYL（异氟醚）芳香酰胺衍生物
公开(公告)号：WO2008028937A1
公开(公告)日：2008-03-13
申请号：PCT/EP2007/059321
申请日：2007-09-06
申请人： NOVARTIS AG , BERST, Frederic , GROSCHE, Philipp , JANSER, Philipp , ZECRI, Frédéric , BOLLBUCK, Birgit
发明人： BERST, Frederic , GROSCHE, Philipp , JANSER, Philipp , ZECRI, Frédéric , BOLLBUCK, Birgit
IPC分类号： C07C311/21 , A61K31/18 , A61P19/02 , C07C311/29 , C07D207/16 , C07D213/30 , C07D213/76 , C07D231/18 , C07D233/84 , C07D241/24 , C07D257/04 , C07D277/36 , C07D307/79 , C07D333/34 , C07D333/62
CPC分类号： C07C311/21 , C07C311/29 , C07D205/04 , C07D207/16 , C07D213/30 , C07D213/76 , C07D231/18 , C07D233/84 , C07D241/04 , C07D241/24 , C07D257/04 , C07D277/36 , C07D307/79 , C07D307/82 , C07D333/34 , C07D333/62
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: Formula (I) wherein the groups R1-R5, R10 and X 1 -X 7 are as defined in the specification.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药酯：式（I）其中基团R 1 -R 5，R 10和X 1 -X 7是如说明书中所定义。

7. 发明申请

WO2015013165A1 CYCLIC APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译：用于治疗心力衰竭的循环APELIN衍生物
公开(公告)号：WO2015013165A1
公开(公告)日：2015-01-29
申请号：PCT/US2014/047372
申请日：2014-07-21
申请人： NOVARTIS AG , ZECRI, Frédéric , GROSCHE, Philipp , YASOSHIMA, Kayo , ZHAO, Hongjuan , YUAN, Jun
发明人： ZECRI, Frédéric , GROSCHE, Philipp , YASOSHIMA, Kayo , ZHAO, Hongjuan , YUAN, Jun
IPC分类号： C07K14/47 , A61K38/17 , A61P9/04
CPC分类号： C07K14/47 , A61K38/10 , A61K38/1709 , A61K45/06 , A61K47/643 , A61K47/6811
摘要： The invention provides a synthetic polypeptide of Formula I': X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I'的合成多肽：X1-R-X3-RL-X6-X7-K-X9-P-X11-X12-X13或其酰胺，酯，其盐或其生物缀合物，其中X1，X3，X6，X7，X9，X11，X12和X13在本文中定义。多肽和生物缀合物是APJ受体的激动剂。本发明还涉及本发明的多肽和生物缀合物的制备方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤受伤（包括晒伤）和先兆子痫。本发明还提供药理活性剂和药物组合物的组合。

8. 发明申请

WO2014081702A2 SYNTHETIC LINEAR APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译：用于治疗心脏衰竭的合成线性APELINMIMT
公开(公告)号：WO2014081702A2
公开(公告)日：2014-05-30
申请号：PCT/US2013/070742
申请日：2013-11-19
申请人： NOVARTIS AG , ZECRI, Frédéric , YASOSHIMA, Kayo , GROSCHE, Philipp , YUAN, Jun , ZHAO, Hongjuan
发明人： ZECRI, Frédéric , YASOSHIMA, Kayo , GROSCHE, Philipp , YUAN, Jun , ZHAO, Hongjuan
IPC分类号： A61K38/00 , C07K14/00
CPC分类号： C07K14/765 , A61K38/385 , A61K45/06 , C07K14/47 , A61K38/1709 , A61K2300/00
摘要： The invention provides a synthetic polypeptide of Formula I': or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X2, X3, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides or bioconjugates thereof are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I'的合成多肽：或其酰胺，酯或其盐或其生物缀合物，其中X 1，X 2，X 3，X 5，X 6，X 7，X 8，X 9，X 10，X 11，X 12和 X13在本文中定义。多肽或其生物缀合物是APJ受体的激动剂。本发明还涉及制备本发明的多肽或生物缀合物的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤受伤（包括晒伤）和先兆子痫。本发明还提供药理活性剂和药物组合物的组合。

9. 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。

10. 发明申请

WO2014081702A4 SYNTHETIC LINEAR APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译：用于治疗心力衰竭的合成线性APELIN模拟物
公开(公告)号：WO2014081702A4
公开(公告)日：2014-09-04
申请号：PCT/US2013070742
申请日：2013-11-19
申请人： NOVARTIS AG , ZECRI FRÉDÉRIC , YASOSHIMA KAYO , GROSCHE PHILIPP , YUAN JUN , ZHAO HONGJUAN
发明人： ZECRI FRÉDÉRIC , YASOSHIMA KAYO , GROSCHE PHILIPP , YUAN JUN , ZHAO HONGJUAN
IPC分类号： A61K38/00 , C07K14/00
CPC分类号： C07K14/765 , A61K38/385 , A61K45/06 , C07K14/47 , A61K38/1709 , A61K2300/00
摘要： The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.
摘要翻译：本发明涉及包含修饰的爱帕琳肽-13肽序列的新型组合物，其设计用于治疗施用受试者的心血管疾病，并且表现出比其野生型对应物更高的降解抗性和相等或更高的生物活性。本发明还涉及制备所述组合物并使用所述组合物作为药物活性剂治疗心血管疾病的方法。

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