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公开(公告)号：US20140128370A1
公开(公告)日：2014-05-08
申请号：US14151796
申请日：2014-01-09
申请人： Nigel Graham COOKE , Frédéric ZECRI , Nicolas SOLDERMANN , Romain WOLF , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Anette VON MATT , Ross Sinclair STRANG , Alexander Baxter SMITH , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Frank STOWASSER , Nicola TUFILLI
发明人： Nigel Graham COOKE , Frédéric ZECRI , Nicolas SOLDERMANN , Romain WOLF , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Anette VON MATT , Ross Sinclair STRANG , Alexander Baxter SMITH , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Frank STOWASSER , Nicola TUFILLI
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要： The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译： 本发明涉及式（I）的取代的四氢 - 吡啶并 - 嘧啶衍生物，其中Y，R 1，R 2和m如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。
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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：US20120277194A1
公开(公告)日：2012-11-01
申请号：US13546490
申请日：2012-07-11
IPC分类号： C07F9/09 , A61P37/06 , G01N30/96 , A61P37/00 , C07F9/572 , C07F9/653 , A61K31/661 , A61P29/00
CPC分类号： C07F9/5728 , C07D209/46 , C07D263/14 , C07F9/094 , C07F9/653 , Y10T436/163333
摘要： Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
摘要翻译： 式I化合物：其中R 1，R 2，n和m如说明书中所定义，其制备方法及其用途和含有它们的药物组合物。
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公开(公告)号：US07612238B2
公开(公告)日：2009-11-03
申请号：US10526760
申请日：2003-09-12
IPC分类号： C07C211/27 , C07F9/09 , A61K31/135
CPC分类号： C07C217/64 , C07C215/28 , C07C225/16 , C07F9/094
摘要： Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
摘要翻译： 其中R 1，R 2，R 3，R 4和R 5如说明书中所定义的式I化合物的制备方法，其用途和含有它们的药物组合物。
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公开(公告)号：US20120065183A1
公开(公告)日：2012-03-15
申请号：US13175050
申请日：2011-07-01
申请人： Nigel Graham COOKE , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Alexander Baxter SMITH , Nicolas SOLDERMANN , Frank STOWASSER , Ross STRANG , Nicola TUFILLI , Anette VON MATT , Romain WOLF , Frédéric ZECRI
发明人： Nigel Graham COOKE , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Alexander Baxter SMITH , Nicolas SOLDERMANN , Frank STOWASSER , Ross STRANG , Nicola TUFILLI , Anette VON MATT , Romain WOLF , Frédéric ZECRI
IPC分类号： A61K31/519 , A61K31/5377 , A61P19/02 , A61P17/00 , A61P37/08 , A61P7/06 , A61P25/00 , A61P21/04 , A61P35/00 , C07D471/04 , A61P7/04
CPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要： The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译： 本发明涉及式（I）的取代的四氢 - 吡啶并 - 嘧啶衍生物，其中Y，R 1，R 2和m如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。
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6.发明授权公开(公告)号：US07625950B2
公开(公告)日：2009-12-01
申请号：US10554556
申请日：2004-04-29
申请人： Klaus Hinterding , Carsten Spanka , Frédéric Zecri
发明人： Klaus Hinterding , Carsten Spanka , Frédéric Zecri
IPC分类号： A01N33/02 , A61K31/135 , A01N31/14 , A61K31/045 , A01N31/00
CPC分类号： C07D317/64 , C07C217/72 , C07F9/094 , C07F9/65744
摘要： Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and n are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
摘要翻译： 其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X，Y和n如说明书中所定义的式（I）化合物处理其制备方法，其用途和含有它们的药物组合物。
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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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8.发明授权公开(公告)号：US08921307B2
公开(公告)日：2014-12-30
申请号：US14082771
申请日：2013-11-18
申请人： Frédéric Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
发明人： Frédéric Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
摘要： The invention provides a synthetic polypeptide of Formula I′ (SEQ ID NO: 1): X1-X2-X3-R—X5-X6-X7-X8-X9-X10-X11-X12-X13 I or an amide, an ester or a salt thereof, wherein X1, X2, X3, 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'（SEQ ID NO：1）的合成多肽：X1-X2-X3-R-X5-X6-X7-X8-X9-X10-X11-X12-X13I或酰胺，酯 或其盐，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X 13如本文所定义。 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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9.发明申请公开(公告)号：US20150284446A1
公开(公告)日：2015-10-08
申请号：US14440198
申请日：2013-11-19
申请人： Frédéric ZECRI , Kayo YASOSHIMA , Philipp GROSCHE , Jun YUAN , Hongjuan ZHAO
发明人： Frederic Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
IPC分类号： C07K14/765 , A61K45/06 , A61K38/38
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apelin-13肽序列的新型组合物，其设计用于治疗其给药对象的心血管疾病，并且其表现出比其野生型对应物更大的降解抗性和等同或更大的生物活性。 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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10.发明申请公开(公告)号：US20140155315A1
公开(公告)日：2014-06-05
申请号：US14082771
申请日：2013-11-18
申请人： Frédéric Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
发明人： Frédéric Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
摘要： The invention provides a synthetic polypeptide of Formula I′ (SEQ ID NO: 1): X1-X2-X3-R—X5-X6-X7-X8-X9-X10-X11-X12-X13 I or an amide, an ester or a salt thereof, wherein X1, X2, X3, 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'（SEQ ID NO：1）的合成多肽：X1-X2-X3-R-X5-X6-X7-X8-X9-X10-X11-X12-X13I或酰胺，酯 或其盐，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X 13如本文所定义。 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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