公开(公告)号：US20100130471A1

公开(公告)日：2010-05-27

申请号：US12450619

申请日：2008-04-04

Applicant: John J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  Damiamo Ghirlanda ,  Xiaoping Hou ,  Alexey V. Ishebenko ,  Lara S. Kallander ,  Beth A. Knapp-Reed ,  Brian Lawhorn ,  Qing Lu ,  Gerard McGeehan ,  Simon Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Lamont R. Terrell ,  Colin Tice ,  Tritin Tran ,  Zhenrong Xu ,  Jing Yuan ,  Jing Zhang ,  Wei Zhao

Inventor： John J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  Damiamo Ghirlanda ,  Xiaoping Hou ,  Alexey V. Ishebenko ,  Lara S. Kallander ,  Beth A. Knapp-Reed ,  Brian Lawhorn ,  Qing Lu ,  Gerard McGeehan ,  Simon Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Lamont R. Terrell ,  Colin Tice ,  Tritin Tran ,  Zhenrong Xu ,  Jing Yuan ,  Jing Zhang ,  Wei Zhao

IPC: A61K31/445 ,  A61K31/554 ,  A61K31/55 ,  A61K31/551 ,  A61K31/549 ,  A61K31/5377 ,  A61K31/5375 ,  A61K31/4545 ,  C07D417/12 ,  C07D265/30 ,  C07D401/06 ,  C07D401/10 ,  C07D211/34 ,  A61P25/00 ,  A61P9/12 ,  A61P9/10

CPC classification number: C07D401/06 ,  C07D211/22 ,  C07D265/30

Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract translation: 描述了结合天冬氨酸蛋白酶抑制其活性的化合物。 它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还描述了本文所述化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。

公开(公告)号：US20080103113A1

公开(公告)日：2008-05-01

申请号：US11934666

申请日：2007-11-02

Applicant: Robert HORMANN ,  Colin TICE ,  Orestes CHORTYK ,  Howard SMITH ,  Thomas METEYER

Inventor： Robert HORMANN ,  Colin TICE ,  Orestes CHORTYK ,  Howard SMITH ,  Thomas METEYER

IPC: A61K31/4412 ,  A61K31/166 ,  A61K31/695 ,  C12N5/00 ,  C12P21/00 ,  C12N15/63 ,  A61K31/357

CPC classification number: C07C243/38 ,  C07D213/87 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  C07F7/1896 ,  C12N9/0069 ,  C12N15/85 ,  C12N2830/002

Abstract: The present invention relates to methods to use non-steroidal ligands in nuclear receptor-based inducible gene expression system to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

Abstract translation: 本发明涉及在基于核受体的诱导型基因表达系统中使用非甾体配体以调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合结构域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。

公开(公告)号：US20060020146A1

公开(公告)日：2006-01-26

申请号：US10787906

申请日：2004-02-26

Applicant: Robert Hormann ,  David Potter ,  Orestes Chortyk ,  Colin Tice ,  Glenn Carlson ,  Andrew Meyer ,  Thomas Opie

Inventor： Robert Hormann ,  David Potter ,  Orestes Chortyk ,  Colin Tice ,  Glenn Carlson ,  Andrew Meyer ,  Thomas Opie

IPC: C07C237/38 ,  C07D271/12 ,  C07D235/04

CPC classification number: C07C241/04 ,  A61K31/166 ,  A61K31/222 ,  A61K31/357 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/455 ,  A61K31/4965 ,  C07C243/18 ,  C07C243/24 ,  C07C243/38 ,  C07C251/08 ,  C07C251/38 ,  C07C255/66 ,  C07C281/10 ,  C07C309/59 ,  C07C315/02 ,  C07C317/44 ,  C07C317/46 ,  C07D209/42 ,  C07D213/81 ,  C07D213/82 ,  C07D213/86 ,  C07D213/87 ,  C07D231/14 ,  C07D231/56 ,  C07D235/06 ,  C07D235/24 ,  C07D237/24 ,  C07D239/52 ,  C07D241/24 ,  C07D271/12 ,  C07D317/68 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D405/12 ,  C12N9/0069 ,  C12N15/635 ,  C12P21/00 ,  Y02A50/471

Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.