公开(公告)号：EP2446894A3

公开(公告)日：2013-02-20

申请号：EP11185682.9

申请日：2005-10-27

申请人： UNIVERSITY OF DENVER ,  University of Florida ,  Oklahoma Medical Research Foundation

发明人： Brennan, Miles B. ,  Dores, Robert M. ,  Haskell-Luevano, Carrie ,  Hochgeschwender, Ute H. ,  Costa, Jessica I.

IPC分类号： A61K38/16 ,  A61K38/35

CPC分类号： C07K14/695 ,  A61K38/00

摘要： ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.

公开(公告)号：EP2446894A2

公开(公告)日：2012-05-02

申请号：EP11185682.9

申请日：2005-10-27

申请人： UNIVERSITY OF DENVER ,  University of Florida ,  OKLAHOMA MEDICAL RESEARCH FOUNDATION

发明人： Brennan, Miles B. ,  Dores, Robert M. ,  Haskell-Luevano, Carrie ,  Hochgeschwender, Ute H. ,  Costa, Jessica I.

IPC分类号： A61K38/16 ,  A61K38/35

CPC分类号： C07K14/695 ,  A61K38/00

摘要： ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.

摘要翻译： 本发明的ACTH类似物包括具有一个或多个结构修饰的ACTH肽序列的化合物，其可以具有以下优选的ACTH类似生物学功能中的一种或多种：（1）在存在下，肾上腺皮质激素分泌物减少 ACTH类似物与未经修饰的ACTH相比，（2）在内源性ACTH存在下肾上腺皮质类固醇分泌减少;（3）与未修饰的ACTH结合MC相比，MC-2R受体活化降低MC-2R结合亲和力增加 -2R黑皮质素。 因此，本发明的ACTH类似物化合物可用于治疗或预防与ACTH，ACTH受体或皮质类固醇分泌相关的疾病和病症，例如早产和库兴氏病。