公开(公告)号：AT547412T

公开(公告)日：2012-03-15

申请号：AT04759362

申请日：2004-04-09

Applicant: VERTEX PHARMA

Inventor： FARMER LUC ,  PERNI ROBERT ,  BHISETTI GOVINDA ,  WILSON KEITH

IPC: C07D403/12 ,  A61K31/401 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/4745 ,  A61K31/4965 ,  A61K38/04 ,  C07D417/12 ,  C07D471/02

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.

公开(公告)号：ES2381548T3

公开(公告)日：2012-05-29

申请号：ES04759362

申请日：2004-04-09

Applicant: VERTEX PHARMA

Inventor： FARMER LUC ,  PERNI ROBERT ,  BHISETTI GOVINDA ,  WILSON KEITH

IPC: C07D403/12 ,  A61K31/401 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/4745 ,  A61K31/4965 ,  A61K38/04 ,  C07D417/12 ,  C07D471/02

Abstract: Un compuesto seleccionado de: **Fórmula**

公开(公告)号：DE69512220T2

公开(公告)日：2000-03-16

申请号：DE69512220

申请日：1995-02-24

Applicant: VERTEX PHARMA

Inventor： TUNG ROGER ,  SALITURO FRANCESCO ,  DEININGER DAVID ,  MURCKO MARK ,  NOVAK PERRY ,  BHISETTI GOVINDA

IPC: A61K31/18 ,  A61K31/27 ,  A61K31/34 ,  A61K31/341 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61P31/12 ,  A61P43/00 ,  C07C311/16 ,  C07C311/29 ,  C07C311/37 ,  C07C311/41 ,  C07C311/51 ,  C07D211/60 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D217/24 ,  C07D217/26 ,  C07D231/38 ,  C07D233/54 ,  C07D233/76 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D235/28 ,  C07D241/04 ,  C07D249/18 ,  C07D261/08 ,  C07D263/22 ,  C07D263/32 ,  C07D263/56 ,  C07D263/58 ,  C07D277/06 ,  C07D277/20 ,  C07D277/26 ,  C07D277/36 ,  C07D277/44 ,  C07D277/46 ,  C07D307/10 ,  C07D307/20 ,  C07D307/33 ,  C07D309/08 ,  C07D309/10 ,  C07D317/18 ,  C07D317/34 ,  C07D319/06 ,  C07D333/36 ,  C07D333/38 ,  C07D333/48 ,  C07D335/02 ,  C07D401/06 ,  C07D487/04 ,  C07D493/04 ,  C07D521/00 ,  C07C241/04 ,  C07D317/36

Abstract: PCT No. PCT/US95/02420 Sec. 371 Date Apr. 1, 1996 Sec. 102(e) Date Apr. 1, 1996 PCT Filed Feb. 24, 1995 PCT Pub. No. WO95/24385 PCT Pub. Date Sep. 14, 1995This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

公开(公告)号：DE69512220D1

公开(公告)日：1999-10-21

申请号：DE69512220

申请日：1995-02-24

Applicant: VERTEX PHARMA

Inventor： TUNG ROGER ,  SALITURO FRANCESCO ,  DEININGER DAVID ,  MURCKO MARK ,  NOVAK PERRY ,  BHISETTI GOVINDA

IPC: A61K31/18 ,  A61K31/27 ,  A61K31/34 ,  A61K31/341 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61P31/12 ,  A61P43/00 ,  C07C311/16 ,  C07C311/29 ,  C07C311/37 ,  C07C311/41 ,  C07C311/51 ,  C07D211/60 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D217/24 ,  C07D217/26 ,  C07D231/38 ,  C07D233/54 ,  C07D233/76 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D235/28 ,  C07D241/04 ,  C07D249/18 ,  C07D261/08 ,  C07D263/22 ,  C07D263/32 ,  C07D263/56 ,  C07D263/58 ,  C07D277/06 ,  C07D277/20 ,  C07D277/26 ,  C07D277/36 ,  C07D277/44 ,  C07D277/46 ,  C07D307/10 ,  C07D307/20 ,  C07D307/33 ,  C07D309/08 ,  C07D309/10 ,  C07D317/18 ,  C07D317/34 ,  C07D319/06 ,  C07D333/36 ,  C07D333/38 ,  C07D333/48 ,  C07D335/02 ,  C07D401/06 ,  C07D487/04 ,  C07D493/04 ,  C07D521/00 ,  C07C241/04 ,  C07D317/36

Abstract: PCT No. PCT/US95/02420 Sec. 371 Date Apr. 1, 1996 Sec. 102(e) Date Apr. 1, 1996 PCT Filed Feb. 24, 1995 PCT Pub. No. WO95/24385 PCT Pub. Date Sep. 14, 1995This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

公开(公告)号：AT542815T

公开(公告)日：2012-02-15

申请号：AT08726147

申请日：2008-02-27

Applicant: VERTEX PHARMA

Inventor： CONNELLY PATRICK ,  KADIYALA IRINA ,  STAVROPOLUS KATHY ,  ZHANG YUEGANG ,  JOHNSTON STEVE ,  BHISETTI GOVINDA ,  JURKAUSKAS VALDAS ,  ROSE PETER

IPC: C07D403/12 ,  A61K31/497 ,  A61K38/07 ,  C07K5/10

Abstract: The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicyclic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.

公开(公告)号：AT443044T

公开(公告)日：2009-10-15

申请号：AT03813772

申请日：2003-12-19

Applicant: VERTEX PHARMA

Inventor： BANDARAGE UPUL ,  COME JON ,  PEROLA EMANUELE ,  BHISETTI GOVINDA ,  SAUNDERS JEFFREY ,  WANG TIANSHENG

IPC: C07D207/12 ,  A61K31/40 ,  A61P35/00 ,  C07C323/65 ,  C07D205/04 ,  C07D261/04 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.

公开(公告)号：ES2240446T3

公开(公告)日：2005-10-16

申请号：ES01924516

申请日：2001-03-29

Applicant: VERTEX PHARMA

Inventor： PERNI ROBERT ,  COURT JOHN ,  O'MALLEY ETHAN ,  BHISETTI GOVINDA

IPC: A61K31/13 ,  A61K31/7052 ,  A61K38/00 ,  A61K38/21 ,  C12N9/99 ,  A61K45/00 ,  A61P31/14 ,  C07K5/103 ,  C07K7/06 ,  C07K5/117 ,  A61K38/07 ,  A61L2/16

Abstract: Un compuesto de **fórmula**, en la que: R1 se selecciona de alquilo (C1-C6) lineal o ramificado, o alquenilo o alquinilo (C2-C6) lineal o ramificado, en las que hasta 4 átomos de carbono en R1 están opcional e independientemente sustituidos con un halógeno; y en las que cualquier átomo de hidrógeno unido a cualquier átomo de carbono terminal en R1 está opcional e independientemente sustituido con ¿SH u ¿OH; R3 se selecciona de en las que cada R2 se selecciona independientemente de ¿R11, -Ar, -O-R11, -O-Ar, -O-R11-Ar, -R11-C(O)-R11, -N(R11)2, -N(R11)-C(O)O-R11, -N(R11)-C(O)O-R11-Ar, - C(O)O-R11, -O-C(O)-N(R11)2, halo, -CN, -NO2, -R11-C(O)-R11, -R11-C(O)O-R11, -C(O)-N(R11)2, -C(O)-N(R11)-Ar, -S(O)2-R11, o ¿S(O)2-N(R11)2; en las que hasta 2 átomos de hidrógeno en R2 se sustituyen opcional e independientemente con un grupo diferente seleccionado de ¿R11, -Ar, -O-R11, -O-Ar, -O- R11-Ar, -R11-C(O)-R11, -NH-(R11)2, -N(R11)-C(O)O-R11, - N(R11)-C(O)O-R11-Ar, -C(O)O-R11, -O-C(O)- N(R11)2, halo, -CN, -NO2, -R11-C(O)-R11, -R11-C(O)O-R11, -O-C(O)-R11, -C(O)-N(R11)2, -C(O)-N(R11)-Ar, -N(R11)-C(O)- R11, -R11-C(O)-N(R11)2, -S(O)2-R11 o ¿S(O)2-N(R11)2; en las que cada R11 se selecciona de hidrógeno, alquilo (C1-C6) lineal o ramificado o alquenilo o alquinilo (C2-C6) lineal o ramificado, y en las que hasta 3 átomos de hidrógeno en dicho alquilo, alquenilo o alquinilo están opcional e independientemente sustituidos con halo.