公开(公告)号：US06794489B2

公开(公告)日：2004-09-21

申请号：US10040547

申请日：2002-01-04

申请人： Christine H. Blood ,  Annette M. Shadiack ,  Joanna K. Bernstein ,  Guy H. Herbert

发明人： Christine H. Blood ,  Annette M. Shadiack ,  Joanna K. Bernstein ,  Guy H. Herbert

IPC分类号： A61K3800

CPC分类号： C07K14/685 ,  A61K38/00 ,  Y10S436/811

摘要： Compositions and methods are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction. In one embodiment, a peptide-based composition including the peptide sequence Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH is administered. Methods of administration include injection, oral, nasal and mucosal administration.

摘要翻译： 提供用于治疗哺乳动物性功能障碍的组合物和方法，包括男性性功能障碍，如勃起功能障碍和女性性功能障碍。 在一个实施方案中，施用包含肽序列Ac-Nle-cyclo（-Asp-His-D-Phe-Arg-Trp-Lys）-OH的基于肽的组合物。 给药方法包括注射，口服，鼻腔和粘膜给药。

公开(公告)号：US06579968B1

公开(公告)日：2003-06-17

申请号：US09606501

申请日：2000-06-28

申请人： Christine H. Blood ,  Annette M. Shadiack ,  Joanna K. Bernstein ,  Guy H. Herbert

发明人： Christine H. Blood ,  Annette M. Shadiack ,  Joanna K. Bernstein ,  Guy H. Herbert

IPC分类号： A61K3800

CPC分类号： C07K14/685 ,  A61K38/00 ,  Y10S436/811

摘要： Compositions and methods are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction. In one embodiment, a peptide-based composition including the peptide sequence Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH is administered. Methods of administration include injection, oral, nasal and mucosal administration.

公开(公告)号：US06228985B1

公开(公告)日：2001-05-08

申请号：US09082787

申请日：1998-05-21

申请人： Christine H. Blood ,  Bernard R. Neustadt ,  Elizabeth M. Smith

发明人： Christine H. Blood ,  Bernard R. Neustadt ,  Elizabeth M. Smith

IPC分类号： C07K200

CPC分类号： C07C229/38 ,  A61K38/00 ,  C07C237/36 ,  C07D209/18 ,  C07D209/20

摘要： The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. The compounds are useful for treating uPA- or uPAR-mediated disorders, e.g., tumor metastasis, tumor angiogenesis, restenosis, chronic inflammation, or corneal angiogenesis.

摘要翻译： 本发明提供具有下式的化合物：其中n为0或1; R为-NH 2，其中R1和R2独立地选自H，烷基，芳烷基，杂芳烷基，羧基，羧基烷基和氨基甲酰基; Q为R3C （O） - 或其中R 5选自H，烷基，芳烷基，杂芳烷基和氨基甲酰基烷基，R 3和R 4选自H，烷基，烷氧基，芳基烷氧基，芳烷基，杂芳烷基和氨基甲酰基烷基; 式I化合物的Q-NH-（CH 2）n - 和-C（O）R取代基相对于形成所述取代基的两个苯基之间的键的碳原子独立地位于邻位，间位或对位 条件是所述取代基不都位于邻位; 和式II化合物的Q-NH-（CH 2）n和-C（O）R取代基彼此定位在间或其生物不稳定酯或其药学上可接受的盐中。 该化合物可用于治疗uPA或uPAR介导的病症，例如肿瘤转移，肿瘤血管发生，再狭窄，慢性炎症或角膜血管生成。