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1. 发明授权

US07982018B2 Modified corticotropin releasing factor peptides and uses thereof 失效
标题翻译：修饰的促肾上腺皮质激素释放因子肽及其用途
公开(公告)号：US07982018B2
公开(公告)日：2011-07-19
申请号：US11873291
申请日：2007-10-16
申请人： Thomas R. Ulich , Jean-Philippe Estradier , Karen Thibaudeau
发明人： Thomas R. Ulich , Jean-Philippe Estradier , Karen Thibaudeau
IPC分类号： A61K38/35 , A61K38/38 , C07K14/695 , C07K14/76 , C07K14/765
CPC分类号： C07K14/57509 , A61K38/00 , A61K47/64 , A61K47/643 , A61K47/644 , A61K47/6889
摘要： The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and preferably exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
摘要翻译：本发明涉及包含修饰的促肾上腺皮质激素释放因子肽，特别是尿皮质素和尿皮质素相关肽，其修饰的衍生物，以及这些修饰肽和衍生物与血清成分，优选血清蛋白或肽的缀合物的化合物。本发明的化合物和缀合物包含反应性基团，其任选地通过连接基团共价连接到修饰的肽或衍生物上。本发明还提供了将修饰的肽或衍生物共价连接到血清蛋白或肽以形成本发明的缀合物的方法。与相应的未结合的肽相比，本发明的缀合物优选表现出更长的体内循环半衰期。本发明的缀合物还保留非共轭肽的至少一些生物活性，并且与非共轭多肽相比优选表现出增加的生物学活性。本发明还提供了治疗和预防疾病或病症的方法，包括将本发明的一种或多种化合物或缀合物施用于需要这种治疗或预防的受试者。

2. 发明申请

US20080167231A1 Modified Corticotropin Releasing Factor Peptides and Uses Thereof 失效
标题翻译：改性促肾上腺皮质激素释放因子肽及其用途
公开(公告)号：US20080167231A1
公开(公告)日：2008-07-10
申请号：US11873291
申请日：2007-10-16
申请人： Thomas R. Ulich , Jean-Philippe Estradier , Karen Thibaudeau
发明人： Thomas R. Ulich , Jean-Philippe Estradier , Karen Thibaudeau
IPC分类号： A61K38/00 , C07K16/00
CPC分类号： C07K14/57509 , A61K38/00 , A61K47/64 , A61K47/643 , A61K47/644 , A61K47/6889
摘要： The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and preferably exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
摘要翻译：本发明涉及包含修饰的促肾上腺皮质激素释放因子肽，特别是尿皮质素和尿皮质素相关肽，其修饰的衍生物，以及这些修饰肽和衍生物与血清成分，优选血清蛋白或肽的缀合物的化合物。本发明的化合物和缀合物包含反应性基团，其任选地通过连接基团共价连接到修饰的肽或衍生物上。本发明还提供了将修饰的肽或衍生物共价连接到血清蛋白或肽以形成本发明的缀合物的方法。与相应的未结合的肽相比，本发明的缀合物优选表现出更长的体内循环半衰期。本发明的缀合物还保留非共轭肽的至少一些生物活性，并且与非共轭多肽相比优选表现出增加的生物学活性。本发明还提供了治疗和预防疾病或病症的方法，包括将本发明的一种或多种化合物或缀合物施用于需要这种治疗或预防的受试者。

3. 发明申请

US20090186819A1 FORMULATION OF INSULINOTROPIC PEPTIDE CONJUGATES 审中-公开
标题翻译：胰岛素诱导剂配方
公开(公告)号：US20090186819A1
公开(公告)日：2009-07-23
申请号：US12333276
申请日：2008-12-11
申请人： Marieve Carrier , Byeong Seon Chang , Omar Quraishi , Thomas R. Ulich , Maggie Wang , Jean-Philippe Estradier
发明人： Marieve Carrier , Byeong Seon Chang , Omar Quraishi , Thomas R. Ulich , Maggie Wang , Jean-Philippe Estradier
IPC分类号： A61K38/38 , A61P3/10
CPC分类号： A61K9/0019 , A61K47/643
摘要： The present invention provides pharmaceutical formulations comprising insulinotropic peptide conjugates, particularly a conjugate of albumin to exendin-4, or a derivative thereof, and methods of administration thereof. The present invention also provides methods for treating diabetes and insulinotropic peptides related diseases or conditions by administering the pharmaceutical formulations described herein.
摘要翻译：本发明提供包含促胰岛素肽缀合物，特别是白蛋白与毒蜥外泌肽-4的缀合物或其衍生物的药物制剂及其施用方法。本发明还提供了通过施用本文所述的药物制剂治疗糖尿病和促胰岛素肽相关疾病或病症的方法。

4. 发明授权

US5300292A Composition and method for treating inflammation 失效
标题翻译：用于治疗炎症的组合物和方法
公开(公告)号：US5300292A
公开(公告)日：1994-04-05
申请号：US989959
申请日：1992-12-10
申请人： Thomas R. Ulich
发明人： Thomas R. Ulich
IPC分类号： A61K38/20 , C07G7/00 , A61K37/02
CPC分类号： A61K38/204
摘要： A method for treatment of inflammation, comprising the step of administering to a patient in need thereof an effective, inflammation-inhibiting amount of a composition comprising IL-6, or IL-6 and TGF.beta. together in a weight ratio of from about 5:95 to 95:5, preferably from about 20:80 to 80:20. Also disclosed is a composition for treatment of inflammation, comprising as active ingredients IL-6 and TGF.beta. in a weight ratio of from about 5:95 to about 95:5, optionally comprising a carrier in combination with the active ingredients, and a method of reducing migration of neutrophils into tissue of an animal which has received an inflammatory stimulus, comprising the step of administering to the tissue an effective neutrophil-migration-inhibiting amount of a composition as defined above.
摘要翻译：一种治疗炎症的方法，包括以下步骤：向有需要的患者施用有效的炎症抑制量的包含IL-6或IL-6和TGF（β）的组合物，其重量比为约 5:95至95:5，优选约20:80至80:20。还公开了用于治疗炎症的组合物，其包含重量比为约5:95至约95:5的活性成分IL-6和TGF（β），任选地包含与活性成分组合的载体，以及一种减少嗜中性粒细胞向接受炎性刺激的动物组织中的迁移的方法，包括向组织施用有效的中性粒细胞迁移抑制量的上述组合物的步骤。

5. 发明授权

US5376368A Composition and method for treating inflammation 失效
标题翻译：用于治疗炎症的组合物和方法
公开(公告)号：US5376368A
公开(公告)日：1994-12-27
申请号：US186762
申请日：1994-01-25
申请人： Thomas R. Ulich
发明人： Thomas R. Ulich
IPC分类号： A61K38/20 , A61K37/02 , C07G7/00
CPC分类号： A61K38/204
摘要： A method for treatment of inflammation, comprising the step of administering to a patient in need thereof an effective, inflammation-inhibiting amount of a composition comprising IL-6, or IL-6 and TGF.beta. together in a weight ratio of from about 5:95 to 95:5, preferably from about 20:80 to 80:20. Also disclosed is a composition for treatment of inflammation, comprising as active ingredients IL-6 and TGF.beta. in a weight ratio of from about 5:95 to about 95:5, optionally comprising a carrier in combination with the active ingredients, and a method of reducing migration of neutrophils into tissue of an animal which has received an inflammatory stimulus, comprising the step of administering to the tissue an effective neutrophil-migration-inhibiting amount of a composition as defined above.
摘要翻译：一种用于治疗炎症的方法，包括以下步骤：向有需要的患者施用有效的炎症抑制量的包含IL-6或IL-6和TGFβ的组合物，其重量比为约5： 95至95:5，优选约20:80至80:20。还公开了用于治疗炎症的组合物，其包含重量比为约5:95至约95:5的活性成分IL-6和TGFβ，任选地包含与活性成分组合的载体，以及方法减少嗜中性粒细胞迁移到已经接受炎症刺激的动物的组织中，包括向组织施用有效的中性粒细胞迁移抑制量的上述组合物的步骤。

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