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1. 发明授权

US07399823B1 Antimicrobial theta defensins and methods of using same 有权
标题翻译：抗微生物θ防御素及其使用方法
公开(公告)号：US07399823B1
公开(公告)日：2008-07-15
申请号：US10009317
申请日：2000-05-10
申请人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
发明人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
IPC分类号： A61K38/00
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa8, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also provides nucleic acids encoding theta defensins and antibodies that specifically bind a theta defensin. In addition, the invention relates to methods of using theta defensin to reduce or inhibit microbial growth or survival.
摘要翻译：本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa8，其中Xaa1至Xaa8是定义其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。例如，本发明提供具有氨基酸序列Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。本发明还提供编码θ防御素和特异性结合θ防御素的抗体的核酸。此外，本发明涉及使用θ防御素来减少或抑制微生物生长或存活的方法。

2. 发明授权

US06890537B2 Antimicrobial theta defensins and methods of using same 有权
标题翻译：抗微生物θ防御素及其使用方法
公开(公告)号：US06890537B2
公开(公告)日：2005-05-10
申请号：US10313994
申请日：2002-12-05
申请人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
发明人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
IPC分类号： A61K38/00 , A61K38/10 , A61K38/12 , C07K7/08 , C07K14/47 , C12N15/12 , C12P21/00 , A61K39/00 , A61K39/38
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.
摘要翻译：本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5，其中Xaa1至Xaa8是定义其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。例如，本发明提供具有氨基酸序列Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。本发明还涉及特异性结合θ防御素和编码θ防御素的分离的核酸分子的抗体。此外，本发明涉及使用θ防御素或θ防御素类似物以通过使环境与θ防御素接触来在能够维持微生物生长或存活的环境中减少或抑制微生物生长或存活的方法。

3. 发明授权

US06514727B1 Antimicrobial theta defensins and methods of using same 有权
公开(公告)号：US06514727B1
公开(公告)日：2003-02-04
申请号：US09967808
申请日：2001-09-26
申请人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
发明人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
IPC分类号： C12N1509
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.

4. 发明授权

US06335318B1 Antimicrobial theta defensins and methods of using same 有权
标题翻译：抗微生物θ防御素及其使用方法
公开(公告)号：US06335318B1
公开(公告)日：2002-01-01
申请号：US09309487
申请日：1999-05-10
申请人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
发明人： Michael E. Selsted , Yi-Quan Tang , Jun Yuan , Andre J. Ouellette
IPC分类号： A61K3800
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5 -Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.
摘要翻译：本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5 -Xaa1-Xaa3-Xaa7-Xaa5，其中Xaa1至Xaa8是定义其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。例如，本发明提供具有氨基酸序列Gly-Phe-Cys-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。本发明还涉及特异性结合θ防御素和编码θ防御素的分离的核酸分子的抗体。此外，本发明涉及使用θ防御素或θ防御素类似物以通过使环境与θ防御素接触来在能够维持微生物生长或存活的环境中减少或抑制微生物生长或存活的方法。

5. 发明申请

US20050261193A1 Antimicrobial theta defensins and methods of using same 审中-公开
标题翻译：抗微生物θ防御素及其使用方法
公开(公告)号：US20050261193A1
公开(公告)日：2005-11-24
申请号：US11126468
申请日：2005-05-10
申请人： Michael Selsted , Yi-Quan Tang , Jun Yuan , Andre Ouellette
发明人： Michael Selsted , Yi-Quan Tang , Jun Yuan , Andre Ouellette
IPC分类号： A61K38/00 , A61K38/10 , A61K38/12 , C07K7/08 , C07K14/47 , C12N15/12 , C12P21/00
CPC分类号： C07K7/08 , A61K38/12 , C07K14/4723 , C12P21/00 , Y02A50/473 , Y02A50/481
摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.
摘要翻译：本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5，其中Xaa1至Xaa8是定义其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。例如，本发明提供具有氨基酸序列Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。本发明还涉及特异性结合θ防御素和编码θ防御素的分离的核酸分子的抗体。此外，本发明涉及使用θ防御素或θ防御素类似物以通过使环境与θ防御素接触来在能够维持微生物生长或存活的环境中减少或抑制微生物生长或存活的方法。

6. 外观设计

USD1049616S1 Travel case for toothbrush 有权
公开(公告)号：USD1049616S1
公开(公告)日：2024-11-05
申请号：US29949301
申请日：2024-06-26
申请人： Jun Yuan
设计人： Jun Yuan
摘要： FIG. 1 is a front, top perspective view of a travel case for toothbrush, showing my new design;
FIG. 2 is a rear, bottom perspective view thereof;
FIG. 3 is a front elevation view thereof;
FIG. 4 is a rear elevation view thereof;
FIG. 5 is a left side elevation view thereof;
FIG. 6 is a right side elevation view thereof;
FIG. 7 is a top plan view thereof;
FIG. 8 is a bottom plan view thereof;
FIG. 9 is another front, top perspective view of the travel case for toothbrush, shown in a position of use; and,
FIG. 10 is a rear, bottom perspective view thereof.
The evenly space broken lines are shown for the purpose of illustrating both parts of the travel case for toothbrush as well as environmental subject matter. None of the broken lines form part of the claimed design.

7. 发明授权

US09683019B2 Cyclic polypeptides for the treatment of heart failure 有权
公开(公告)号：US09683019B2
公开(公告)日：2017-06-20
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： A61K38/12 , C07K7/64 , C07K16/46 , A61K45/06 , C07K14/47 , A61K47/48 , 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.

8. 发明授权

US09340582B2 Bioconjugates of synthetic apelin polypeptides 有权
标题翻译：合成apelin多肽的生物缀合物
公开(公告)号：US09340582B2
公开(公告)日：2016-05-17
申请号：US14336290
申请日：2014-07-21
申请人： Jun Yuan , Frederic Zecri , Philipp Grosche , Hongjuan Zhao , Eric Peters , Shari Lynn Caplan , Changgang Lou
发明人： Jun Yuan , Frederic Zecri , Philipp Grosche , Hongjuan Zhao , Eric Peters , Shari Lynn Caplan , Changgang Lou
IPC分类号： C07K14/47 , C07K7/08 , A61K47/48 , A61K45/06 , A61K38/10 , C07K16/00 , A61K39/395
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。

9. 发明授权

US09036570B2 Method and system for providing an uplink structure and improved channelization scheme in a wireless communication network 有权
标题翻译：在无线通信网络中提供上行链路结构和改进的信道化方案的方法和系统
公开(公告)号：US09036570B2
公开(公告)日：2015-05-19
申请号：US13264936
申请日：2010-04-16
申请人： Sophie Vrzic , Mo-Han Fong , DongSheng Yu , Robert Novak , Jun Yuan
发明人： Sophie Vrzic , Mo-Han Fong , DongSheng Yu , Robert Novak , Jun Yuan
IPC分类号： H04W4/00 , H04W72/00 , H04W36/38 , H04W72/04 , H04J13/16
CPC分类号： H04W36/385 , H04J13/16 , H04L5/0007 , H04L5/0037 , H04L5/0092 , H04W72/042 , H04W72/0453
摘要： A method and system are provided to perform channelization in a wireless communication network, wherein the wireless communication network including at least one base station that is communicatively coupled to at least one mobile terminal. A bandwidth of the wireless communication network is divided into a plurality of zones at the base station. Resource blocks are provided at the base station to receive data symbols transmitted in the wireless communication network. A plurality of resource blocks are combined at the base station to form a physical basic channel unit which are allocated to one of the plurality of zones at the base station. A permutation is performed on the physical basic channel unit to form a logical basic channel unit. A channel is provided to communicatively couple the base station and the mobile terminal so that the mobile terminal may send an access grant message and a user identification to the base station to transmit data in the logical basic channel unit.
摘要翻译：提供了一种在无线通信网络中执行信道化的方法和系统，其中所述无线通信网络包括通信地耦合到至少一个移动终端的至少一个基站。无线通信网络的带宽在基站被分成多个区域。在基站处提供资源块以接收在无线通信网络中发送的数据符号。在基站处组合多个资源块，以形成分配给基站的多个区域之一的物理基本信道单元。在物理基本信道单元上执行置换以形成逻辑基本信道单元。提供了一种通信来通信地耦合基站和移动终端，使得移动终端可以向基站发送接入许可消息和用户标识以在逻辑基本信道单元中发送数据。

10. 发明申请

US20150031604A1 CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 有权
标题翻译：治疗心力衰竭的循环多糖
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
IPC分类号： C07K7/64 , A61K38/12 , A61K45/06 , C07K16/46
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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