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公开(公告)号:US20160159871A1
公开(公告)日:2016-06-09
申请号:US14905333
申请日:2014-07-21
申请人: Frédéric ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN
发明人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN
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。
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公开(公告)号:US20160145309A1
公开(公告)日:2016-05-26
申请号:US14905338
申请日:2014-07-21
申请人: Frédéric ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN
发明人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN
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。
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公开(公告)号:US20130196899A1
公开(公告)日:2013-08-01
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: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:US20150031604A1
公开(公告)日:2015-01-29
申请号:US14336262
申请日:2014-07-21
申请人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun Yuan , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla Giumaraes
发明人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun Yuan , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla Giumaraes
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 (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13 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(SEQ ID NO:1)的环状多肽:X1-R-X3-X4-LS-X7-X8-X9-X10-X11-X12-X13I或酰胺,酯或盐 或其生物缀合物,其中X1,X3,X4,X7,X8,X9,X10,X11,X12和X13在本文中定义。 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,潴留,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: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:US20160108091A1
公开(公告)日:2016-04-21
申请号:US14963391
申请日:2015-12-09
申请人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla GUIMARAES
发明人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla GUIMARAES
IPC分类号: C07K7/64 , C07K14/765
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 (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13 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.
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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:US20120264773A1
公开(公告)日:2012-10-18
申请号:US13490579
申请日:2012-06-07
申请人: Muneto MOGI , Ken YAMADA , Kayo YASOSHIMA , Toshio KAWANAMI , Ichiro UMEMURA , Yuki IWAKI , Hongbo QIN , Hidetomo IMASE
发明人: Muneto MOGI , Ken YAMADA , Kayo YASOSHIMA , Toshio KAWANAMI , Ichiro UMEMURA , Yuki IWAKI , Hongbo QIN , Hidetomo IMASE
IPC分类号: A61K31/506 , A61P3/06 , A61P9/10 , A61P9/04 , A61P7/02 , A61P9/12 , A61P3/10 , A61P3/04 , C07D401/14 , A61P9/00
CPC分类号: C07D401/14 , C07D413/14
摘要: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译: 本发明提供式(I)化合物:其中变体R1,R2,R3,R4,R5,R6,R7如本文所定义,并且其中所述化合物是CETP的抑制剂,因此可用于 治疗由CETP介导的或对CETP的抑制作用的疾病或疾病。
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公开(公告)号:US20120208816A1
公开(公告)日:2012-08-16
申请号:US13449347
申请日:2012-04-18
申请人: Muneto MOGI , Ken YAMADA , Kayo YASOSHIMA , Toshio KAWANAMI , Ichiro UMEMURA , Yuki IWAKI , Hongbo QIN , Hidetomo IMASE
发明人: Muneto MOGI , Ken YAMADA , Kayo YASOSHIMA , Toshio KAWANAMI , Ichiro UMEMURA , Yuki IWAKI , Hongbo QIN , Hidetomo IMASE
IPC分类号: A61K31/5377 , C07D401/14 , A61K31/506 , A61P9/00 , A61P3/04 , A61P3/00 , A61P9/10 , A61P3/10 , A61P9/12 , C07D413/14 , A61P3/06
CPC分类号: C07D401/14 , C07D413/14
摘要: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
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