公开(公告)号：WO2008156831A2

公开(公告)日：2008-12-24

申请号：PCT/US2008/007704

申请日：2008-06-20

Applicant: VITAE PHARMACEUTICALS, INC. ,  SMITHKLINE BEECHAM CORPORATION ,  BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David, A. ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  ISHCHENKO, Alexey, V. ,  JIA, Lanqi ,  MCGEEHAN, Gerard ,  SIMPSON, Robert, D ,  SINGH, Suresh, B. ,  TICE, Colin, M. ,  XU, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHUANG, Linghang ,  ZHANG, Jing

Inventor： BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David, A. ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  ISHCHENKO, Alexey, V. ,  JIA, Lanqi ,  MCGEEHAN, Gerard ,  SIMPSON, Robert, D ,  SINGH, Suresh, B. ,  TICE, Colin, M. ,  XU, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHUANG, Linghang ,  ZHANG, Jing

IPC: C07C237/24 ,  C07C237/32 ,  A61K31/165 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12

CPC classification number: C07C237/24 ,  C07C237/32 ,  C07C2601/08

Abstract: The present invention is directed to aspartic protease inhibitors. 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：WO2008156816A3

公开(公告)日：2008-12-24

申请号：PCT/US2008/007661

申请日：2008-06-20

Applicant: VITAE PHARMACEUTICALS, INC. ,  BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David, A. ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  ISHCHENKO, Alexey, V. ,  JIA, Lanqi ,  MCGEEHAN, Gerard ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  TICE, Colin, M. ,  XU, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHUANG, Linghang

Inventor： BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David, A. ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  ISHCHENKO, Alexey, V. ,  JIA, Lanqi ,  MCGEEHAN, Gerard ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  TICE, Colin, M. ,  XU, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHUANG, Linghang

IPC: C07C275/14 ,  C07C275/16 ,  C07C275/24 ,  C07D209/46 ,  C07D307/88 ,  C07D307/94 ,  C07D309/04 ,  C07D313/04 ,  A61K31/17 ,  A61K31/351 ,  A61K31/335 ,  A61K31/352 ,  A61K31/343 ,  A61K31/4035 ,  A61P9/00

Abstract: The present invention is directed to aspartic protease inhibitors. 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.

公开(公告)号：WO2008124575A8

公开(公告)日：2008-10-16

申请号：PCT/US2008/059384

申请日：2008-04-04

Applicant: VITAE PHARMACEUTICALS, INC. ,  BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  GHAVIMI-ALAGHA, Bahman ,  GHIRLANDA, Damiano ,  ISHCHENKO, Alexey, V. ,  KALLANDER, Lara, S. ,  LAWHORN, Brian ,  LEACH, Colin, A. ,  LU, Qing ,  MCGEEHAN, Gerald ,  PATTERSON, Jaclyn, R. ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  STOY, Patrick ,  TERRELL, Lamont, R. ,  TICE, Colin ,  XU, Zhenrong ,  YUAN, Jing ,  YUAN, Catherine, C., K. ,  ZHANG, Jing ,  ZHAO, Wei

Inventor： BALDWIN, John, J. ,  CACATIAN, Salvacion ,  CLAREMON, David ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  GHAVIMI-ALAGHA, Bahman ,  GHIRLANDA, Damiano ,  ISHCHENKO, Alexey, V. ,  KALLANDER, Lara, S. ,  LAWHORN, Brian ,  LEACH, Colin, A. ,  LU, Qing ,  MCGEEHAN, Gerald ,  PATTERSON, Jaclyn, R. ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  STOY, Patrick ,  TERRELL, Lamont, R. ,  TICE, Colin ,  XU, Zhenrong ,  YUAN, Jing ,  YUAN, Catherine, C., K. ,  ZHANG, Jing ,  ZHAO, Wei

IPC: A01N35/00 ,  A61K31/10 ,  A61K31/12

Abstract: Disclosed are compounds of Formula (I) wherein the R, R 1 , R 2 , R 3 , 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.

公开(公告)号：WO2007117560A3

公开(公告)日：2007-12-06

申请号：PCT/US2007008521

申请日：2007-04-05

Applicant: VITAE PHARMACEUTICALS INC ,  BALDWIN JOHN J ,  CLAREMON DAVID A ,  TICE COLIN M ,  CACATIAN SALVACION ,  DILLARD LAWRENCE W ,  ISHCHENKO ALEXEY V ,  YUAN JING ,  XU ZHENRONG ,  MCGEEHAN GERARD ,  ZHAO WEI ,  SIMPSON ROBERT D ,  SINGH SURESH B

Inventor： BALDWIN JOHN J ,  CLAREMON DAVID A ,  TICE COLIN M ,  CACATIAN SALVACION ,  DILLARD LAWRENCE W ,  ISHCHENKO ALEXEY V ,  YUAN JING ,  XU ZHENRONG ,  MCGEEHAN GERARD ,  ZHAO WEI ,  SIMPSON ROBERT D ,  SINGH SURESH B

IPC: C07D211/22 ,  A61K31/445 ,  A61P9/12 ,  C07D265/30

CPC classification number: C07D211/22 ,  C07D265/30

Abstract: Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.

Abstract translation: 描述的是具有口服活性并与肾素结合以抑制其活性的化合物。 它们可用于治疗或改善与肾素活性相关的疾病。 还描述了这些化合物用于治疗或改善受试者中肾素介导的病症的方法。

公开(公告)号：WO2007117557A3

公开(公告)日：2007-11-29

申请号：PCT/US2007008518

申请日：2007-04-05

Applicant: VITAE PHARMACEUTICALS INC ,  BALDWIN JOHN J ,  CLAREMON DAVID A ,  TICE COLIN M ,  CACATIAN SALVACION ,  DILLARD LAWRENCE W ,  ISHCHENKO ALEXEY V ,  YUAN JING ,  XU ZHENRONG ,  MCGEEHAN GERARD ,  ZHAO WEI ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  FLAHERTY PATRICK T

Inventor： BALDWIN JOHN J ,  CLAREMON DAVID A ,  TICE COLIN M ,  CACATIAN SALVACION ,  DILLARD LAWRENCE W ,  ISHCHENKO ALEXEY V ,  YUAN JING ,  XU ZHENRONG ,  MCGEEHAN GERARD ,  ZHAO WEI ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  FLAHERTY PATRICK T

IPC: C07D211/20 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61P9/00 ,  C07D207/08 ,  C07D265/30

CPC classification number: C07D211/22 ,  C07D207/08 ,  C07D265/30 ,  C07D413/12

Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.

Abstract translation: 描述其二氨基丙醇是口服活性的并且结合肾素以抑制其活性。 它们可用于治疗或改善与升高相关的疾病。 肾素活性水平或治疗天冬氨酸蛋白酶介导的病症。 还描述了在有需要的受试者中使用二氨基丙醇来改善或治疗肾素相关疾病的方法。

公开(公告)号：WO2006083924A1

公开(公告)日：2006-08-10

申请号：PCT/US2006/003489

申请日：2006-02-01

Applicant: VITAE PHARMACEUTICALS, INC. ,  MCGEEHAN, Gerard ,  SIMPSON, Robert D. ,  ZENG, Wenguang ,  BALDWIN, John J. ,  CLAREMON, David A. ,  DILLARD, Lawrence W. ,  ISHCHENKO, Alexey V. ,  YUAN, Jing ,  XU, Zhenrong ,  CACATIAN, Salvation ,  TICE, Colin ,  ZHAO, Wei

Inventor： MCGEEHAN, Gerard ,  SIMPSON, Robert D. ,  ZENG, Wenguang ,  BALDWIN, John J. ,  CLAREMON, David A. ,  DILLARD, Lawrence W. ,  ISHCHENKO, Alexey V. ,  YUAN, Jing ,  XU, Zhenrong ,  CACATIAN, Salvation ,  TICE, Colin ,  ZHAO, Wei

IPC: C07C233/36 ,  C07C233/62 ,  C07C275/24 ,  C07C311/13 ,  C07C335/12 ,  C07D295/20 ,  A61K31/165 ,  A61K31/17 ,  A61K31/18 ,  A61K31/4453 ,  A61P9/12 ,  C07D263/04

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-α-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：WO2010138901A1

公开(公告)日：2010-12-02

申请号：PCT/US2010/036709

申请日：2010-05-28

Applicant: BIOGEN IDEC MA INC ,  PENG, Hairuo ,  CUERVO, Julio, H. ,  ISHCHENKO, Alexey ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LUGOVSKOY, Alexey ,  TALREJA, Tina ,  TAVERAS, Arthur, G. ,  XIN, Zhili

Inventor： PENG, Hairuo ,  CUERVO, Julio, H. ,  ISHCHENKO, Alexey ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LUGOVSKOY, Alexey ,  TALREJA, Tina ,  TAVERAS, Arthur, G. ,  XIN, Zhili

IPC: A01N43/40

CPC classification number: A61K31/435 ,  C07C59/56 ,  C07C59/68 ,  C07C229/34 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/14 ,  C07D211/34 ,  C07D263/26 ,  C07D277/30 ,  C07D295/155

Abstract: Compounds that modulate gamma secretase (e.g., alter the cleavage pattern of gamma secretase) are described herein. Also disclosed are pharmaceutical compositions, methods of modulating the activity of gamma secretase, and methods of treating Alzheimer's Disease using the compounds described herein.

Abstract translation: 本文描述了调节γ-分泌酶（例如，改变γ-分泌酶的切割模式）的化合物。 还公开了药物组合物，调节γ-分泌酶的活性的方法，以及使用本文所述的化合物治疗阿尔茨海默病的方法。

公开(公告)号：WO2009096996A1

公开(公告)日：2009-08-06

申请号：PCT/US2008/067650

申请日：2008-06-20

Applicant: SMITHKLINE BEECHAM CORPORATION ,  VITAE PHARMACEUTICALS, INC. ,  BALDWIN, John J. ,  CACATIAN, Salvacion ,  CLAREMON, David ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  GHAVIMI-ALAGHA, Bahman ,  ISHCHENKO, Alexey, V. ,  GHIRLANDA, Damiano ,  KALLANDER, Lara, S. ,  LAWHORN, Brian ,  LU, Qing ,  MCGEEHAN, Gerard ,  KNAPP-REED, Beth, A. ,  SEMUS, Simon ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  TERRELL, Lamont, R. ,  TICE, Colin ,  TRAN, Tritin ,  Xu, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHAO, Yongdong Y.

Inventor： BALDWIN, John J. ,  CACATIAN, Salvacion ,  CLAREMON, David ,  DILLARD, Lawrence, W. ,  FLAHERTY, Patrick, T. ,  GHAVIMI-ALAGHA, Bahman ,  ISHCHENKO, Alexey, V. ,  GHIRLANDA, Damiano ,  KALLANDER, Lara, S. ,  LAWHORN, Brian ,  LU, Qing ,  MCGEEHAN, Gerard ,  KNAPP-REED, Beth, A. ,  SEMUS, Simon ,  SIMPSON, Robert, D. ,  SINGH, Suresh, B. ,  TERRELL, Lamont, R. ,  TICE, Colin ,  TRAN, Tritin ,  Xu, Zhenrong ,  YUAN, Jing ,  ZHAO, Wei ,  ZHAO, Yongdong Y.

IPC: C09K11/06

CPC classification number: C07D211/22 ,  C07D265/30

Abstract: Disclosed are compounds having the formula (I): wherein the R 1 , R 2 , R 3 , 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：WO2008156817A3

公开(公告)日：2009-06-04

申请号：PCT/US2008007662

申请日：2008-06-20

Applicant: VITAE PHARMACEUTICALS INC ,  BALDWIN JOHN J ,  CACATIAN SALVACION ,  CLAREMON DAVID A ,  DILLARD LAWRENCE W ,  FLAHERTY PATRICK T ,  ISHCHENKO ALEXEY V ,  MCGEEHAN GERARD ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  TICE COLIN M ,  XU ZHENRONG ,  YUAN JING ,  ZHAO WEI

Inventor： BALDWIN JOHN J ,  CACATIAN SALVACION ,  CLAREMON DAVID A ,  DILLARD LAWRENCE W ,  FLAHERTY PATRICK T ,  ISHCHENKO ALEXEY V ,  MCGEEHAN GERARD ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  TICE COLIN M ,  XU ZHENRONG ,  YUAN JING ,  ZHAO WEI

IPC: C07C271/16 ,  A61K31/27 ,  A61K31/335 ,  A61K31/351 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  C07D309/04 ,  C07D313/04

CPC classification number: C07C271/16 ,  C07C2601/14 ,  C07D309/04 ,  C07D313/04

Abstract: Described are compounds that 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：WO2008156828A3

公开(公告)日：2009-05-07

申请号：PCT/US2008007700

申请日：2008-06-20

Applicant: VITAE PHARMACEUTICALS INC ,  BALDWIN JOHN J ,  CACATIAN SALVACION ,  CLAREMON DAVID A ,  DILLARD LAWRENCE W ,  FLAHERTY PATRICK T ,  ISHCHENKO ALEXEY V ,  JIA LANQI ,  MCGEEHAN GERARD ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  TICE COLIN M ,  XU ZHENRONG ,  YUAN JING ,  ZHAO WEI

Inventor： BALDWIN JOHN J ,  CACATIAN SALVACION ,  CLAREMON DAVID A ,  DILLARD LAWRENCE W ,  FLAHERTY PATRICK T ,  ISHCHENKO ALEXEY V ,  JIA LANQI ,  MCGEEHAN GERARD ,  SIMPSON ROBERT D ,  SINGH SURESH B ,  TICE COLIN M ,  XU ZHENRONG ,  YUAN JING ,  ZHAO WEI

IPC: C07D211/60 ,  A61K31/351 ,  A61K31/44 ,  A61P9/00 ,  C07D309/04

CPC classification number: C07D211/60 ,  C07C271/20 ,  C07C2601/14 ,  C07D309/04

Abstract: Described are compounds that 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以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障碍的方法。