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公开(公告)号:US20240002433A1
公开(公告)日:2024-01-04
申请号:US18189057
申请日:2023-03-23
Inventor: Kleomenis Barlos , Dimitrios Gatos , Kostas K. Barlos , Zoi Vasileiou
IPC: C07K1/107 , C07K14/505 , C07K14/575 , C07K14/62 , C07K14/635 , C07K14/695 , C07K1/04 , C07K14/605 , A61K47/54 , C07C269/04 , C07C269/06 , C07C271/02 , C07C323/60 , C07K14/00 , C07K14/47
CPC classification number: C07K1/1075 , C07K14/505 , C07K14/57509 , C07K14/62 , C07K14/635 , C07K14/695 , C07K1/04 , C07K1/1077 , C07K14/575 , C07K14/605 , A61K47/542 , C07C269/04 , C07C269/06 , C07C271/02 , C07C323/60 , C07K14/00 , C07K14/4703 , C07K14/473 , C07C2603/18 , A61K38/00
Abstract: The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.
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公开(公告)号:US09572866B2
公开(公告)日:2017-02-21
申请号:US14802812
申请日:2015-07-17
Inventor: Wylie W. Vale, Jr. , Joan M. Vaughan , Cindy Donaldson , Wolfgang Fischer , Jean E. F. Rivier
IPC: C07K14/47 , A61K38/22 , C07K14/575
CPC classification number: A61K38/2228 , C07K14/4705 , C07K14/57509 , Y10T428/13
Abstract: Disclosed are polypeptides that are analogs of urocortin 2 that have pharmacological activity similar to urocortin 2 but have improved water solubility compared to urocortin 2, and pharmaceutical compositions of the polypeptides of the present invention. Also disclosed are polynucleotides encoding the polypeptides, and methods of treating pathophysiological states employing pharmaceutical compositions of the polypeptides and polynucleotides of the present invention. In addition, disclosed are vectors and host cells that include a nucleic acid encoding a polypeptide of the present invention, and kits that include pharmaceutical compositions of the present invention.
Abstract translation: 公开的是具有类似于尿皮质素2但具有与尿皮质素2相比具有改善的水溶性的药理学活性的尿皮质素2的类似物的多肽和本发明的多肽的药物组合物。 还公开了编码多肽的多核苷酸,以及使用本发明的多肽和多核苷酸的药物组合物治疗病理生理状态的方法。 此外,所公开的是包含编码本发明多肽的核酸的载体和宿主细胞,以及包括本发明的药物组合物的试剂盒。
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公开(公告)号:US20160375102A1
公开(公告)日:2016-12-29
申请号:US15206083
申请日:2016-07-08
Applicant: Research Development Foundation
Inventor: Wylie W. VALE, JR. , Kathy A. LEWIS , Marilyn H. PERRIN , Koichi KUNITAKE , Jean E. F. RIVIER , Jozsef GULYAS
IPC: A61K38/22
CPC classification number: A61K38/2228 , A61K38/00 , C07K14/57509 , C07K14/695
Abstract: A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to b e identified receptor.
Abstract translation: 公众人类基因组数据库的搜索确定了人类EST,GenBank登录号AW293249,其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示,该序列编码了一种新的人类urocortin,其命名为urocortin III(UcnIII)。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力,但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够激活表达CRF-R2α或β的细胞中的环AMP产生。 因此,亲和力足够高,使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而,尿细胞素III也可能是尚未被鉴定的受体的更强的激动剂。
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公开(公告)号:US09388229B2
公开(公告)日:2016-07-12
申请号:US14179543
申请日:2014-02-12
Applicant: Research Development Foundation
Inventor: Wylie W. Vale, Jr. , Kathy A. Lewis , Marilyn H. Perrin , Koichi Kunitake , Jean E. F. Rivier , Jozsef Gulyas
IPC: C07K14/00 , C07K14/695 , C07K14/575 , A61K38/00
CPC classification number: A61K38/2228 , A61K38/00 , C07K14/57509 , C07K14/695
Abstract: A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.
Abstract translation: 公众人类基因组数据库的搜索确定了人类EST,GenBank登录号AW293249,其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示,该序列编码了一种新的人类urocortin,其命名为urocortin III(UcnIII)。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力,但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2α或bgr的细胞中的环AMP产生。 因此,亲和力足够高,使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而,urocortin III也可能是未被鉴定的受体的更强的激动剂。
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公开(公告)号:US09035022B2
公开(公告)日:2015-05-19
申请号:US13996186
申请日:2011-12-22
Applicant: Jean E. F. Rivier
Inventor: Jean E. F. Rivier
IPC: A61K38/00 , C07K14/47 , C07K14/575
CPC classification number: C07K14/47 , A61K38/00 , C07K14/57509
Abstract: Cyclic CRF antagonist peptides having improved properties of “drugability”. The peptides are 33 residues in length with a lactam bond between the residues in position 22 and 25; however, they may be N-terminally shortened by up to 3 residues.
Abstract translation: 循环CRF拮抗剂肽具有改善的“药物性”性质。 所述肽的长度为33个残基,位置22和25之间的残基之间具有内酰胺键; 然而,它们可以被N末端缩短多达3个残基。
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公开(公告)号:US20120270792A1
公开(公告)日:2012-10-25
申请号:US13328821
申请日:2011-12-16
Applicant: Wylie W. Vale, JR. , Kathy A. Lewis , Marilyn H. Perrin , Koichi S. Kunitake , Jean E. Rivier , Jozsef Gulyas
Inventor: Wylie W. Vale, JR. , Kathy A. Lewis , Marilyn H. Perrin , Koichi S. Kunitake , Jean E. Rivier , Jozsef Gulyas
CPC classification number: A61K38/2228 , A61K38/00 , C07K14/57509 , C07K14/695
Abstract: A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.
Abstract translation: 公众人类基因组数据库的搜索确定了人类EST,GenBank登录号AW293249,其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示,该序列编码了一种新的人类urocortin,其命名为urocortin III(UcnIII)。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力,但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2α或bgr的细胞中的环AMP产生。 因此,亲和力足够高,使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而,urocortin III也可能是未被鉴定的受体的更强的激动剂。
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公开(公告)号:US20080287650A1
公开(公告)日:2008-11-20
申请号:US12074454
申请日:2008-03-03
Applicant: Avi Tovi , Chaim Eidelman , Shimon Shushan , Shai Elster , Alon Hagi , Alexander Ivchenko , Gabriel-Marcus Butilca , Gil Zaoui , Eleonora Alterman , Leah Bar-Oz
Inventor: Avi Tovi , Chaim Eidelman , Shimon Shushan , Shai Elster , Alon Hagi , Alexander Ivchenko , Gabriel-Marcus Butilca , Gil Zaoui , Eleonora Alterman , Leah Bar-Oz
CPC classification number: C07K14/58 , C07K1/02 , C07K1/04 , C07K1/20 , C07K14/575 , C07K14/57509 , C07K14/57563 , C07K14/57581 , C07K14/60 , C07K14/635 , C07K14/815
Abstract: The invention relates to methods for the preparation of highly purified peptides. The peptides are prepared in high optical purity of at least about 98.5%, and preferably at least about 99%. Specifically, Nesiritide (SEQ. ID NO. 1) having a purity of at least 99% as measured by HPLC and containing about 0.05% to about 0.5% [D-His]-Nesiritide (SEQ. ID NO. 1) as measured by chiral GC/MS.
Abstract translation: 本发明涉及制备高纯度肽的方法。 肽以高光学纯度制备为至少约98.5%,优选至少约99%。 具体地,通过HPLC测量纯度为至少99%,含有约0.05%至约0.5%[D-His] -Nesiritide(SEQ ID NO:1)的奈西立肽(SEQ ID NO:1),通过 手性GC / MS。
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公开(公告)号:US07226743B2
公开(公告)日:2007-06-05
申请号:US10814760
申请日:2004-03-31
Applicant: Fiona C. Buchanan , Tracy D. Thue , Dianne Winkelman-Sim
Inventor: Fiona C. Buchanan , Tracy D. Thue , Dianne Winkelman-Sim
IPC: C12Q1/68
CPC classification number: C12Q1/6888 , C07K14/57509 , C12Q2600/156
Abstract: The present invention provides for selection of bovine animals that will display phenotypes associated with increased rates of growth. These phenotypes include hot carcass weight, average daily gain, shipping weight, end of test rib eye area, and adjusted weaning weight which is a measure of post-natal growth, based on the knowledge of their CRH, POMC and MC4R genotypes. The predictive value comes from the discovery that certain single nucleotide polymorphisms (SNPs) in these genes are linked to higher growth rate phenotypes. Specifically, the phenotypes that correlated with specific SNP's are end-of-test rib-eye area, adjusted weaning weight, average daily gain, shipping weight and hot carcass weight. The invention also provides novel kits that can be used in making the determination of these genotypes. The invention further provides for methods of screening bovines to predict which animals will have higher growth rate, allowing producers to selectively breed and manage animals based on desired characteristics, thereby maximizing productivity and profitability in commercial meat production operations.
Abstract translation: 本发明提供了选择将显示与增长的生长速率相关的表型的牛动物。 基于其CRH,POMC和MC4R基因型的知识,这些表型包括热胴体重,平均日增重,运输重量,测试肋眼面积的结束和调整的断奶重量,这是产后生长的量度。 预测值来自发现这些基因中的某些单核苷酸多态性(SNPs)与较高生长速率表型相关联。 具体来说,与特异性SNP相关的表型是测试结束面积,调整的断奶重量,平均日增重,运输重量和热胴体重。 本发明还提供可用于确定这些基因型的新型试剂盒。 本发明还提供了筛选牛的方法以预测哪些动物具有较高的生长速率,允许生产者基于期望的特征来选择性繁殖和管理动物,从而最大限度地提高商业肉类生产操作中的生产率和获利能力。
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公开(公告)号:US07192923B2
公开(公告)日:2007-03-20
申请号:US10315964
申请日:2002-12-11
Applicant: Robert Joseph Isfort , Wieslaw Adam Mazur
Inventor: Robert Joseph Isfort , Wieslaw Adam Mazur
IPC: A61K38/16 , A61K38/22 , C07K14/435 , C07K14/575
CPC classification number: C07K14/57509 , A61K38/00
Abstract: Isolated corticotropin releasing factor derivatives, and nucleic acids encoding the same, are effective for treating corticotropin releasing factor 2 receptor modulated disorders such as muscular dystrophy.
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公开(公告)号:US20060025339A1
公开(公告)日:2006-02-02
申请号:US11121612
申请日:2005-05-04
Applicant: Robert Isfort , Wieslaw Mazur
Inventor: Robert Isfort , Wieslaw Mazur
IPC: A61K38/22
CPC classification number: C07K14/57509 , A61K38/00
Abstract: Isolated corticotropin releasing factor derivatives, and nucleic acids encoding the same, are effective for treating corticotropin releasing factor 2 receptor modulated disorders such as muscular dystrophy.
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