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公开(公告)号:US20150030594A1
公开(公告)日:2015-01-29
申请号:US14336290
申请日:2014-07-21
申请人: Jun YUAN , Frederic ZECRI , Philipp GROSCHE , Hongjuan ZHAO , Andrei GOLOSOV , Kayo YASOSHIMA , David Thomas PARKER , Eric PETERS , Aimee Richardson USERA , Shari Lynn CAPLAN , Aaron KANTER , Changgang LOU , Carla Guimaraes
发明人: Jun YUAN , Frederic ZECRI , Philipp GROSCHE , Hongjuan ZHAO , Andrei GOLOSOV , Kayo YASOSHIMA , David Thomas PARKER , Eric PETERS , Aimee Richardson USERA , Shari Lynn CAPLAN , Aaron KANTER , Changgang LOU , Carla Guimaraes
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′ (SEQ ID NO: 1): 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: 本发明提供包含式I'(SEQ ID NO:1)的合成多肽的生物缀合物或其酰胺,其酯或其盐,其中X 1,X 2,X 3,X 4,X 5,X 6,X 7,X 8,X 9 ,X10,X11,X12和X13在本文中定义并且半衰期延长部分,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。
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公开(公告)号:US08222425B2
公开(公告)日:2012-07-17
申请号:US13185683
申请日:2011-07-19
申请人: Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
发明人: Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
IPC分类号: C07D207/00
CPC分类号: C07D401/12 , C07D403/12 , C07K5/0812 , C07K5/1016
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
摘要翻译: 本申请描述了可用于治疗,预防和/或改善人类疾病的有机化合物。
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公开(公告)号:US08673848B2
公开(公告)日:2014-03-18
申请号:US13747621
申请日:2013-01-23
申请人: Frédéric Zecri , Andrei Golosov , Philipp Grosche , Kayo Yasoshima , Hongjuan Zhao , Qi-Ying Hu , Hidetomo Imase , David Thomas Parker
发明人: Frédéric Zecri , Andrei Golosov , Philipp Grosche , Kayo Yasoshima , Hongjuan Zhao , Qi-Ying Hu , Hidetomo Imase , David Thomas Parker
CPC分类号: A61M16/0816 , A61K38/00 , A61K38/10 , A61M16/0066 , A61M16/201 , A61M2016/0027 , A61M2016/003 , A61M2205/35 , A61M2205/502 , C07K7/08 , C07K7/56 , C07K7/60
摘要: The invention provides a synthetic polypeptide of Formula 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. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides 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,其中X1,X2,X3,X4,X5,X6,X7,X8,X9,X10,X11,X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽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( 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。
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公开(公告)号:US20120231998A1
公开(公告)日:2012-09-13
申请号:US13477866
申请日:2012-05-22
申请人: Trixi Brandl , Jiping Fu , Francois Lenoir , David Thomas Parker , Michael Patane , Branko Radetich , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic , Aregahegn Yifru , Rui Zheng
发明人: Trixi Brandl , Jiping Fu , Francois Lenoir , David Thomas Parker , Michael Patane , Branko Radetich , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic , Aregahegn Yifru , Rui Zheng
CPC分类号: A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D209/96 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/10 , C07D491/20 , C07D495/10 , C07D498/04 , C07D498/10 , C07K5/06034 , C07K5/06078 , C07K5/06165 , C07K5/0808 , C07K5/0812 , C07K5/101 , C07K5/1016
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
摘要翻译: 本申请描述了可用于治疗,预防和/或改善人类疾病的有机化合物。
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公开(公告)号:US08008263B2
公开(公告)日:2011-08-30
申请号:US12249186
申请日:2008-10-10
申请人: Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
发明人: Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
CPC分类号: C07D401/12 , C07D403/12 , C07K5/0812 , C07K5/1016
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
摘要翻译: 本申请描述了可用于治疗,预防和/或改善人类疾病的有机化合物。
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公开(公告)号:US07825152B2
公开(公告)日:2010-11-02
申请号:US11697894
申请日:2007-04-09
申请人: Trixi Brandl , Jiping Fu , Francois Lenoir , David Thomas Parker , Michael Patane , Branko Radetich , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic , Aregahegn Yifru , Rui Zheng
发明人: Trixi Brandl , Jiping Fu , Francois Lenoir , David Thomas Parker , Michael Patane , Branko Radetich , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic , Aregahegn Yifru , Rui Zheng
IPC分类号: C07D417/12 , C07D403/12 , C07D401/12 , C07D409/12 , C07D417/14 , C07D405/12 , C07D413/12 , C07D405/04 , C07D403/04 , C07D413/14 , C07D409/14 , C07D405/14 , C07D207/00 , C07D209/96 , A61K31/5377 , A61K31/506 , A61K31/497 , A61K31/4439 , A61K31/454 , A61K31/427 , A61K31/422 , A61K31/4178 , A61K31/4155 , A61K31/403
CPC分类号: A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D209/96 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/10 , C07D491/20 , C07D495/10 , C07D498/04 , C07D498/10 , C07K5/06034 , C07K5/06078 , C07K5/06165 , C07K5/0808 , C07K5/0812 , C07K5/101 , C07K5/1016
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
摘要翻译: 本申请描述了可用于治疗,预防和/或改善人类疾病的有机化合物。
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公开(公告)号:US20100204159A1
公开(公告)日:2010-08-12
申请号:US12440139
申请日:2007-09-11
申请人: Trixl Brandl , Sylvain Cottens , Claus Ehrhardt , Jiping Fu , Subramanian Karur , David Thomas Parker , Michael A. Patane , Prakash Raman , Stefan Andreas Randl , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic
发明人: Trixl Brandl , Sylvain Cottens , Claus Ehrhardt , Jiping Fu , Subramanian Karur , David Thomas Parker , Michael A. Patane , Prakash Raman , Stefan Andreas Randl , Pascal Rigollier , Mohindra Seepersaud , Oliver Simic
IPC分类号: A61K38/06 , C07D417/14 , A61P31/14 , A61K38/05 , C07K5/083
CPC分类号: C07D417/14 , C07D401/12 , C07D419/14 , C07K5/06078 , C07K5/0808 , C07K5/0823 , C12N2770/24211
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
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公开(公告)号:US20160166634A1
公开(公告)日:2016-06-16
申请号:US15053316
申请日:2016-02-25
申请人: Shari Lynn CAPLAN , Andrei GOLOSOV , Philipp GROSCHE , Carla GUIMARAES , Aaron KANTER , Changgang LOU , David Thomas PARKER , Eric C. Peters , Aimee Richardson USERA , Kayo YASOSHIMA , Jun YUAN , Federic ZECRI , Hongjuan ZHAO
发明人: Shari Lynn CAPLAN , Andrei GOLOSOV , Philipp GROSCHE , Carla GUIMARAES , Aaron KANTER , Changgang LOU , David Thomas PARKER , Eric C. Peters , Aimee Richardson USERA , Kayo YASOSHIMA , Jun YUAN , Federic ZECRI , Hongjuan ZHAO
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′ (SEQ ID NO: 1): 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.
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公开(公告)号:US20140142022A1
公开(公告)日:2014-05-22
申请号:US14165680
申请日:2014-01-28
申请人: Frederic ZECRI , Andrei GOLOSOV , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Qi-Ying HU , Hidetomo IMASE , David Thomas PARKER
发明人: Frederic ZECRI , Andrei GOLOSOV , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Qi-Ying HU , Hidetomo IMASE , David Thomas PARKER
IPC分类号: C07K7/08
CPC分类号: A61M16/0816 , A61K38/00 , A61K38/10 , A61M16/0066 , A61M16/201 , A61M2016/0027 , A61M2016/003 , A61M2205/35 , A61M2205/502 , C07K7/08 , C07K7/56 , C07K7/60
摘要: The invention provides a synthetic polypeptide of Formula 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. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides 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,其中X1,X2,X3,X4,X5,X6,X7,X8,X9,X10,X11,X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽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( 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。
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公开(公告)号:US20100120872A1
公开(公告)日:2010-05-13
申请号:US12557654
申请日:2009-09-11
申请人: Markus Rolf Dobler , Francois Lenoir , David Thomas Parker , Yunshan Peng , Grazia Piizzi , Sompong Wattanasin
发明人: Markus Rolf Dobler , Francois Lenoir , David Thomas Parker , Yunshan Peng , Grazia Piizzi , Sompong Wattanasin
IPC分类号: A61K31/44 , C07C233/16 , C12N1/20 , A61K31/16 , A61P31/04 , C07D213/00
CPC分类号: C07D309/22 , C07B2200/05 , C07C259/06 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07D211/70 , C07D213/30 , C07D307/42 , C07D307/80
摘要: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
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