公开(公告)号：WO2011009084A2

公开(公告)日：2011-01-20

申请号：PCT/US2010042340

申请日：2010-07-16

Applicant: VERTEX PHARMA ,  HENDERSON JAMES A ,  MAXWELL JOHN ,  VAILLANCOURT LOUIS ,  MORRIS MARK ,  GREY JR RONALD ,  GIROUX SIMON ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  LIU BINGCAN ,  POISSON CARL ,  CADILHAC CAROLINE ,  BUBENIK MONICA ,  REDDY T JAGADEESWAR ,  FALARDEAU GUY ,  YANNOPOULOS CONSTANTIN ,  WANG JIAN ,  PEREIRA OSWY Z ,  BENNANI YOUSSEF L ,  PIERCE ALBERT C ,  BHISETTI GOVINDA RAO ,  COTTRELL KEVIN M ,  MARONE VALERIE

Inventor： HENDERSON JAMES A ,  MAXWELL JOHN ,  VAILLANCOURT LOUIS ,  MORRIS MARK ,  GREY JR RONALD ,  GIROUX SIMON ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  LIU BINGCAN ,  POISSON CARL ,  CADILHAC CAROLINE ,  BUBENIK MONICA ,  REDDY T JAGADEESWAR ,  FALARDEAU GUY ,  YANNOPOULOS CONSTANTIN ,  WANG JIAN ,  PEREIRA OSWY Z ,  BENNANI YOUSSEF L ,  PIERCE ALBERT C ,  BHISETTI GOVINDA RAO ,  COTTRELL KEVIN M ,  MARONE VALERIE

IPC: C07D403/14 ,  A61K31/506

CPC classification number: C07K5/06052 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B', X, Y, R1, R1 ', R2, R2', R3, R3', R5, R5', R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6，m ，n或p如本文所定义，可用于治疗黄病毒科病毒感染。

公开(公告)号：WO2006000096A1

公开(公告)日：2006-01-05

申请号：PCT/CA2005/000999

申请日：2005-06-23

Applicant: VIROCHEM PHARMA INC. ,  CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  VAILLANCOURT, Louis ,  BUBENIK, Monica

Inventor： CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  VAILLANCOURT, Louis ,  BUBENIK, Monica

IPC: C07D471/10

CPC classification number: C07D471/10

Abstract: Novel compounds represented by formula (I): wherein R1, R2, R3 and R4 are as defined herein, and pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.

Abstract translation: 由式（I）表示的新型化合物：其中R 1，R 2，R 3和R 4如本文所定义，及其药学上可接受的盐，水合物和溶剂化物，可用于调节CCR5趋化因子受体活性。

公开(公告)号：WO2011079327A1

公开(公告)日：2011-06-30

申请号：PCT/US2010/062168

申请日：2010-12-27

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  LIU, Bingcan ,  POISSON, Carl ,  KONG, Laval Chan Chun ,  DAS, Sanjoy Kumar ,  YANNOPOULOS, Constantin ,  CADILHAC, Caroline ,  REDDY, T. Jagadeerswar ,  VAIILLANCOURT, Louis ,  FALARDEAU, Guy ,  PEREIRA, Oswy W. ,  BUBENIK, Monica ,  MAXWELL, John

Inventor： LIU, Bingcan ,  POISSON, Carl ,  KONG, Laval Chan Chun ,  DAS, Sanjoy Kumar ,  YANNOPOULOS, Constantin ,  CADILHAC, Caroline ,  REDDY, T. Jagadeerswar ,  VAIILLANCOURT, Louis ,  FALARDEAU, Guy ,  PEREIRA, Oswy W. ,  BUBENIK, Monica ,  MAXWELL, John

IPC: A61K31/4155 ,  A61P31/14 ,  C07D403/14

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D495/04

Abstract: Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 其中A，B，B'，X，Y，R1，R2，R2'，R3，R3'，R4，R4'，R5，R5'm， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

公开(公告)号：WO2006060918A1

公开(公告)日：2006-06-15

申请号：PCT/CA2005/001877

申请日：2005-12-09

Applicant: VIROCHEM PHARMA INC. ,  CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  COURCHESNE, Marc ,  VAILLANCOURT, Louis ,  BUBENIK, Monica

Inventor： CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  COURCHESNE, Marc ,  VAILLANCOURT, Louis ,  BUBENIK, Monica

IPC: C07D471/20 ,  A61K31/438

CPC classification number: C07D451/02

Abstract: Compounds according to formula (I): wherein the radical R 2 represents a hydrogen atom or one of the following structures: R, and R 7 _ 9 are as herein defined, and wherein ring A represents a 5 or 6 membered heteroring involving a nitrogen or oxygen atom and one or two keto substituent. These compounds and their pharmaceutical acceptable salt are used in combinations or pharmaceutical compositions and are useful in modulation of CCR5 chemokine receptor activity.

Abstract translation: 根据式（I）的化合物：其中基团R 2表示氢原子或以下结构之一：R 1和R 7 - SUB>如本文所定义，并且其中环A表示涉及氮或氧原子和一个或两个酮取代基的5或6元杂环。 这些化合物及其药学上可接受的盐以组合或药物组合物使用，并且可用于调节CCR5趋化因子受体活性。

公开(公告)号：WO2011009084A3

公开(公告)日：2011-01-20

申请号：PCT/US2010/042340

申请日：2010-07-16

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  HENDERSON, James A. ,  MAXWELL, John ,  VAILLANCOURT, Louis ,  MORRIS, Mark ,  GREY, JR., Ronald ,  GIROUX, Simon ,  KONG, Laval Chan Chun ,  DAS, Sanjoy Kumar ,  LIU, Bingcan ,  POISSON, Carl ,  CADILHAC, Caroline ,  BUBENIK, Monica ,  REDDY, T. Jagadeeswar ,  FALARDEAU, Guy ,  YANNOPOULOS, Constantin ,  WANG, Jian ,  PEREIRA, Oswy Z. ,  BENNANI, Youssef L. ,  PIERCE, Albert C. ,  BHISETTI, Govinda Rao ,  COTTRELL, Kevin M. ,  MARONE, Valerie

Inventor： HENDERSON, James A. ,  MAXWELL, John ,  VAILLANCOURT, Louis ,  MORRIS, Mark ,  GREY, JR., Ronald ,  GIROUX, Simon ,  KONG, Laval Chan Chun ,  DAS, Sanjoy Kumar ,  LIU, Bingcan ,  POISSON, Carl ,  CADILHAC, Caroline ,  BUBENIK, Monica ,  REDDY, T. Jagadeeswar ,  FALARDEAU, Guy ,  YANNOPOULOS, Constantin ,  WANG, Jian ,  PEREIRA, Oswy Z. ,  BENNANI, Youssef L. ,  PIERCE, Albert C. ,  BHISETTI, Govinda Rao ,  COTTRELL, Kevin M. ,  MARONE, Valerie

IPC: C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04 ,  A61K31/4184 ,  A61P3/00

Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B', X, Y, R 1 , R 1 ', R 2 , R 2 ', R 3 , R 3 ', R 5 , R 5 ', R 6 , m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

公开(公告)号：WO2009082819A8

公开(公告)日：2009-07-09

申请号：PCT/CA2008/002291

申请日：2008-12-23

Applicant: VIROCHEM PHARMA INC. ,  MOINET, Christophe ,  HALAB, Liliane ,  TURCOTTE, Nathalie ,  BUBENIK, Monica ,  COURCHESNE, Marc ,  POISSON, Carl ,  PEREIRA, Oswy, Z. ,  NGUYEN-BA, Paul ,  LIU, Bingcan ,  CHAURET, Nathalie ,  CADILHAC, Caroline ,  CHAN CHUN KONG, Laval

Inventor： MOINET, Christophe ,  HALAB, Liliane ,  TURCOTTE, Nathalie ,  BUBENIK, Monica ,  COURCHESNE, Marc ,  POISSON, Carl ,  PEREIRA, Oswy, Z. ,  NGUYEN-BA, Paul ,  LIU, Bingcan ,  CHAURET, Nathalie ,  CADILHAC, Caroline ,  CHAN CHUN KONG, Laval

IPC: C07J63/00 ,  A61K31/575 ,  A61K31/58 ,  A61K45/00 ,  A61P31/12 ,  A61P31/18 ,  C07J41/00 ,  C07J43/00 ,  C07J53/00

Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R 1 , X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.

公开(公告)号：WO2007143847A1

公开(公告)日：2007-12-21

申请号：PCT/CA2007/001062

申请日：2007-06-14

Applicant: VIROCHEM PHARMA INC. ,  MOINET, Christophe ,  BLAIS, Charles ,  BUBENIK, Monica ,  CHAN CHUN KONG, Laval ,  COURCHESNE, Marc ,  PEREIRA, Oswy, Z. ,  DENIS, Réal ,  VAILLANCOURT, Louis ,  YANNOPOULOS, Constantin, G.

Inventor： MOINET, Christophe ,  BLAIS, Charles ,  BUBENIK, Monica ,  CHAN CHUN KONG, Laval ,  COURCHESNE, Marc ,  PEREIRA, Oswy, Z. ,  DENIS, Réal ,  VAILLANCOURT, Louis ,  YANNOPOULOS, Constantin, G.

IPC: C07D451/00 ,  A61K31/46

CPC classification number: C07D471/20

Abstract: Compounds according to formula (I): (Insert formula from claim 1 here) wherein R 1 , R 2 , R 3 , n and X are defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity. Additionally, compounds according to Formula III: (Insert formula from claim 45 here) wherein Z, R' 1 , and R' 2 are defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful as intermediates for production of compounds that modulate CCR5 chemokine receptor activity.

Abstract translation: 根据式（I）的化合物：（其中R 1，R 2，R 3，n和X）中插入式 定义如本文所定义，其药学上可接受的盐，水合物和溶剂合物可用于调节CCR5趋化因子受体活性。 另外，根据式III的化合物（这里的插入式权利要求45），其中Z，R'1和R'2定义如本文所定义，并且药学上 可接受的盐，水合物和溶剂化物，可用作生产调节CCR5趋化因子受体活性的化合物的中间体。

公开(公告)号：WO2006060919A1

公开(公告)日：2006-06-15

申请号：PCT/CA2005/001878

申请日：2005-12-09

Applicant: VIROCHEM PHARMA INC. ,  CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  COURCHESNE, Marc ,  VAILLANCOURT, Louis ,  BLAIS, Charles ,  BUBENIK, Monica

Inventor： CHAN CHUN KONG, Laval ,  MOINET, Christophe ,  COURCHESNE, Marc ,  VAILLANCOURT, Louis ,  BLAIS, Charles ,  BUBENIK, Monica

IPC: C07D471/20 ,  A61K31/439 ,  C07D498/20

CPC classification number: C07D451/02

Abstract: Spiro compounds according to formula (I): wherein the radical R 1 represents NR 7 R 9 , R 2 , R 3 , R 7 , R 8 , R" 8 are as herein defined, and wherein ring A represents a 5 or 6 membered heteroring substituted once or twice with a keto substituent. These compounds and their pharmaceutical acceptable salts are used in combinations or in pharmaceutical compositions and are useful in the modulation of CCR5 chemokine receptor activity.

Abstract translation: 根据式（I）的螺环化合物：其中基团R 1表示NR 7 R 9，R 2， R 3，R 7，R 8，R“8如本文所定义，并且其中环A 表示用酮取代基取代一次或两次的5或6元杂环，这些化合物及其药学上可接受的盐以组合或药物组合物使用，并且可用于调节CCR5趋化因子受体活性。