公开(公告)号：MY133159A

公开(公告)日：2007-10-31

申请号：MYPI20003684

申请日：2000-08-11

Applicant: VERTEX PHARMA

Inventor： FRANCIS SALITURO ,  GUY BEMIS ,  HUAI GAO ,  JEREMY GREEN ,  ANNE-LAURE GRILLOT ,  MARK LEDEBOER ,  EDMUND HARRINGTON ,  CHRISTOPHER BAKER ,  MICHAEL HALE ,  JINGRONG CAO

IPC: C07D401/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14

Abstract: THE PRESENT INVENTION PROVIDES COMPOUNDS OF FORMULA I: WHERE R1 IS H, CONH2, T(N) -R, OR T(N) -AR2, N MAY BE ZERO OR ONE, AND G, XYZ, AND Q ARE AS DESCRIBED BELOW. THESE COMPOUNDS ARE INHIBITORS OF PROTEIN KINASE, PARTICULARLY INHIBITORS OF JNK,A MAMMALIAN PROTEIN KINASE INVOLVED CELL PROLIFERATION, CELL DEATH AND RESPONSE TO EXTRACELLULAR STIMULI. THE INVENTION ALSO RELATES TO METHODS FOR PRODUCING THESE INHIBITORS. THE INVENTION ALSO PROVIDES PHARMACEUTICAL COMPOSITIONS COMPRISING THE INHIBITORS OF THE INVENTION AND METHODS OF UTILIZING THOSE COMPOSITIONS IN THE TREATMENT AND PREVENTION OF VARIOUS DISORDERS.

公开(公告)号：HK1046276A1

公开(公告)日：2003-01-03

申请号：HK02107512

申请日：2002-10-16

Applicant: VERTEX PHARMA

Inventor： JEREMY GREEN ,  JINGRONG CAO ,  MICHAEL HALE ,  CHRISTOPHER BAKER ,  FRANCOIS MALTAIS ,  JAMES JANETKA ,  MICHAEL MULLICAN ,  GUY BEMIS ,  XIAOLING XIE ,  JUDITH STRAUB ,  QING TANG ,  ROBERT MASHALL

IPC: A61B17/00 ,  C07D20060101 ,  A61F2/02 ,  A61K20060101 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/00 ,  A61L27/00 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/00 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D231/38 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

公开(公告)号：HK1045507A1

公开(公告)日：2002-11-29

申请号：HK02106918

申请日：2002-09-23

Applicant: VERTEX PHARMA

Inventor： JEREMY GREEN ,  GUY BEMIS ,  ANNE-LAURE GRILLOT ,  MARK LEDEBOER ,  FRANCIS SALITURO ,  EDMUND HARRINGTON ,  HUAI GAO ,  CHRISTOPHER BAKER ,  JINGRONG CAO ,  MICHAEL HALE

IPC: C07D20060101 ,  A61K20060101 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14

公开(公告)号：HK1021737A1

公开(公告)日：2000-06-30

申请号：HK00100695

申请日：2000-02-03

Applicant: VERTEX PHARMA

Inventor： ROBERT TUNG ,  MICHAEL HALE ,  CHRISTOPHER BAKER ,  STEVEN FURFINE ERIC ,  ISTVAN KALDOR ,  MIECZYSLAW KAZMIERSKI WIESLAW ,  ANDREW SPALTENSTEIN

IPC: C07D20060101 ,  A61K20060101 ,  A61K31/18 ,  A61K31/215 ,  A61K31/265 ,  A61K31/27 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4025 ,  A61K31/496 ,  A61K31/66 ,  A61K31/661 ,  A61K31/664 ,  A61K31/7048 ,  A61K45/00 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07C20060101 ,  C07C311/15 ,  C07C311/18 ,  C07C311/37 ,  C07D277/30 ,  C07D307/20 ,  C07D405/12 ,  C07D407/12 ,  C07D417/12 ,  C07F20060101 ,  C07F9/655 ,  C07F9/6584 ,  C07H20060101 ,  C07H15/04 ,  C07H15/26

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.