公开(公告)号：US08598163B2

公开(公告)日：2013-12-03

申请号：US13147637

申请日：2010-02-03

Applicant: David Claremon ,  Colin Tice ,  Suresh Singh ,  Yuanjie Ye ,  Katerina Leftheris ,  Linghang Zhuang

Inventor： David Claremon ,  Colin Tice ,  Suresh Singh ,  Yuanjie Ye ,  Katerina Leftheris ,  Linghang Zhuang

IPC: A61K31/5355 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: This invention relates to novel compounds of an 11 β-HSD1 inhibitor disclosed herein, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11/3-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract translation: 本发明涉及本文公开的11β-HSD1抑制剂的新化合物，其药学上可接受的盐及其药物组合物，其可用于治疗与哺乳动物中11/3-HSD1的调节或抑制相关的疾病的治疗。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇的产生或抑制细胞中可的松转化为皮质醇的方法。

公开(公告)号：US08487108B2

公开(公告)日：2013-07-16

申请号：US12084928

申请日：2006-11-13

Applicant: John J. Baldwin ,  David A. Claremon ,  Colin Tice ,  Salvacion Cacatian ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Wei Zhao ,  Patrick T. Flaherty

Inventor： John J. Baldwin ,  David A. Claremon ,  Colin Tice ,  Salvacion Cacatian ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Wei Zhao ,  Patrick T. Flaherty

IPC: C07D211/22 ,  C07D211/60

CPC classification number: C07D211/26 ,  C07D211/22 ,  C07D401/12 ,  C07D407/12 ,  C07D409/06 ,  C07D417/06 ,  Y02P20/55

Abstract: The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

Abstract translation: 本发明涉及天冬氨酸蛋白酶抑制剂。 本发明的某些天冬氨酸蛋白酶抑制剂可以由以下结构式表示或其药学上可接受的盐。 本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。 本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。

公开(公告)号：US20080293701A1

公开(公告)日：2008-11-27

申请号：US11883518

申请日：2006-02-01

Applicant: John J. Baldwin ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Wenguang Zeng ,  Salvacion Cacatian ,  Colin Tice ,  Robert D. Simpson ,  Wei Zhao

Inventor： John J. Baldwin ,  David A. Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Wenguang Zeng ,  Salvacion Cacatian ,  Colin Tice ,  Robert D. Simpson ,  Wei Zhao

IPC: A61K31/546 ,  C07C233/62 ,  A61K31/164 ,  A61K31/4453 ,  C07D211/60 ,  A61K31/145 ,  C07C381/00 ,  A61P9/12 ,  A61P9/00

CPC classification number: C07D263/04 ,  C07C233/36 ,  C07C233/62 ,  C07C275/24 ,  C07C307/06 ,  C07C311/13 ,  C07C2601/14 ,  C07D263/06 ,  C07D263/22 ,  C07D295/215 ,  C07D303/36

Abstract: 1-Acylamino-2-hydroxy-3-amino-ω-arylalkanes of formula I. and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.

Abstract translation: 式I的1-酰基氨基-2-羟基-3-氨基-ω-芳基烷烃及其盐具有肾素抑制性质，可用作抗高血压药物活性成分。

公开(公告)号：US20100048636A1

公开(公告)日：2010-02-25

申请号：US12084928

申请日：2006-11-13

Applicant: John J. Baldwin ,  David A. Claremon ,  Colin Tice ,  Salvacion Cacatian ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Wei Zhao ,  Patrick T. Flaherty

Inventor： John J. Baldwin ,  David A. Claremon ,  Colin Tice ,  Salvacion Cacatian ,  Lawrence W. Dillard ,  Alexey V. Ishchenko ,  Jing Yuan ,  Zhenrong Xu ,  Gerard McGeehan ,  Robert D. Simpson ,  Suresh B. Singh ,  Wei Zhao ,  Patrick T. Flaherty

IPC: A61K31/4523 ,  C07D211/78 ,  A61K31/445 ,  C07D405/02 ,  A61P9/00 ,  A61P9/12 ,  A61P9/10

CPC classification number: C07D211/26 ,  C07D211/22 ,  C07D401/12 ,  C07D407/12 ,  C07D409/06 ,  C07D417/06 ,  Y02P20/55

Abstract: The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

Abstract translation: 本发明涉及天冬氨酸蛋白酶抑制剂。 本发明的某些天冬氨酸蛋白酶抑制剂可以由以下结构式表示或其药学上可接受的盐。 本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。 本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。

公开(公告)号：US20050228016A1

公开(公告)日：2005-10-13

申请号：US10460820

申请日：2003-06-12

Applicant: Enrique Michelotti ,  Colin Tice ,  Subba Palli ,  Christine Thompson ,  Tarlochan Dhadialla

Inventor： Enrique Michelotti ,  Colin Tice ,  Subba Palli ,  Christine Thompson ,  Tarlochan Dhadialla

IPC: A61K31/47 ,  C07D215/42 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  A61K31/4709 ,  C07D215/38 ,  C07D45/02 ,  C07D49/02

CPC classification number: C07D215/44 ,  A61K31/47 ,  C07D215/42 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

Abstract: This invention relates to 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. The ligands comprise a class of 4-tetrahydroquinolines.

Abstract translation: 本发明涉及一种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。 配体包括一类4-四氢喹啉。

公开(公告)号：US20100280005A1

公开(公告)日：2010-11-04

申请号：US12450620

申请日：2008-04-04

Applicant: Jonh J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  John Gleason ,  Alexey V. Ishchenko ,  Brian Lawhorn ,  Gerard McGeehan ,  Jaclyn R. Patterson ,  Simon F. Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin Tice ,  Tritin Tran ,  Zhenrong Xu ,  Jing Yuan ,  Wei Zhao

Inventor： Jonh J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  John Gleason ,  Alexey V. Ishchenko ,  Brian Lawhorn ,  Gerard McGeehan ,  Jaclyn R. Patterson ,  Simon F. Semus ,  Robert D. Simpson ,  Suresh B. Singh ,  Colin Tice ,  Tritin Tran ,  Zhenrong Xu ,  Jing Yuan ,  Wei Zhao

IPC: A61K31/445 ,  C07D211/60 ,  C07D401/02 ,  C07D413/02 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/58 ,  A61P9/12

CPC classification number: C07D211/22 ,  C07D401/06

Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract translation: 公开了式I的化合物，其中R，R 1，R 2，R 3，X，Y，A，Q，E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性，并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I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：US20050209283A1

公开(公告)日：2005-09-22

申请号：US10775883

申请日：2004-02-09

Applicant: Robert Hormann ,  Colin Tice ,  Orestes Chortyk ,  Howard Smith ,  Thomas Meteyer

Inventor： Robert Hormann ,  Colin Tice ,  Orestes Chortyk ,  Howard Smith ,  Thomas Meteyer

IPC: C07C243/38 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  A61K31/455 ,  A61K31/165 ,  A61K31/277

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 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.

Abstract translation: 本发明涉及用于基于核受体的诱导型基因表达系统的非甾体配体，以及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：US20080064741A1

公开(公告)日：2008-03-13

申请号：US11841568

申请日：2007-08-20

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: A61K31/16 ,  A61K31/335 ,  A61P43/00 ,  C07C233/00 ,  C07D311/00 ,  C12N5/06 ,  C12P21/04

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.

Abstract translation: 本发明涉及用于基于核受体的诱导型基因表达系统的非甾体配体，以及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：US20100317697A1

公开(公告)日：2010-12-16

申请号：US12665217

申请日：2008-06-20

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

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

IPC: A61K31/445 ,  C07D211/06

CPC classification number: C07D211/22 ,  C07D265/30

Abstract: Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract translation: 公开了具有式（I）的化合物：其中R1，R2，R3，X，Y，A，L和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性，并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I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：US20100179109A1

公开(公告)日：2010-07-15

申请号：US12450631

申请日：2008-04-04

Applicant: Jonh J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  Damiano Ghirlanda ,  Alexey V. Ishchenko ,  Lara S. Kallander ,  Brian Lawhorn ,  Colin A. Leach ,  Qing Lu ,  Gerard McGeehan ,  Jaclyn R. Patterson ,  Robert D. Simpson ,  Suresh B. Singh ,  Patrick Stoy ,  Lamont R. Terrell ,  Colin Tice ,  Zhenrong Xu ,  Jing Yuan ,  Catherine C. K. Yuan ,  Jing Zhang ,  Wei Zhao

Inventor： Jonh J. Baldwin ,  Salvacion Cacatian ,  David Claremon ,  Lawrence W. Dillard ,  Patrick T. Flaherty ,  Bahman Ghavimi-Alagha ,  Damiano Ghirlanda ,  Alexey V. Ishchenko ,  Lara S. Kallander ,  Brian Lawhorn ,  Colin A. Leach ,  Qing Lu ,  Gerard McGeehan ,  Jaclyn R. Patterson ,  Robert D. Simpson ,  Suresh B. Singh ,  Patrick Stoy ,  Lamont R. Terrell ,  Colin Tice ,  Zhenrong Xu ,  Jing Yuan ,  Catherine C. K. Yuan ,  Jing Zhang ,  Wei Zhao

IPC: A61K31/675 ,  C07D211/34 ,  A61K31/445 ,  C07D265/30 ,  A61K31/5375 ,  C07D413/06 ,  A61K31/5377 ,  A61K31/535 ,  A61K31/517 ,  A61K31/554 ,  A61K31/4965 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/47 ,  A61K31/566 ,  A61P25/28 ,  A61P33/06 ,  A61P31/18 ,  A61P9/12 ,  A61P9/10 ,  A61P25/22 ,  A61P27/06

CPC classification number: C07D211/96 ,  C07D211/22 ,  C07D401/10 ,  C07D401/12

Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract translation: 公开了式（I）的化合物，其中R，R 1，R 2，R 3，X，Y，A，Q，E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性，并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I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。