公开(公告)号：WO2007025307A3

公开(公告)日：2007-04-26

申请号：PCT/US2006033770

申请日：2006-08-28

Applicant: VERTEX PHARMA ,  COTTRELL KEVIN M ,  MAXWELL JOHN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  LE TIRAN ARNAUD ,  PEROLA EMANUELE

Inventor： COTTRELL KEVIN M ,  MAXWELL JOHN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  LE TIRAN ARNAUD ,  PEROLA EMANUELE

IPC: C07D498/10 ,  C07K5/08

CPC classification number: C07D498/10 ,  A61K38/00 ,  C07D498/20 ,  C07D519/00 ,  C07K5/06026 ,  C07K5/06191 ,  C07K5/0804 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0827

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式（I）化合物或其药学上可接受的盐或混合物。

公开(公告)号：WO2009020470A3

公开(公告)日：2010-10-21

申请号：PCT/US2007087411

申请日：2007-12-13

Applicant: VERTEX PHARMA ,  GUTIERREZ COREY DON ,  TERMIN ANDREAS ,  HADIDA-RUAH SARA ,  BERGERON DANIELE ,  YOO SANGHEE ,  BINCH HAYLEY ,  JOSHI PRAMOD ,  COME JON ,  NANTHAKUMAR SUGANTHI ,  CAO JINGRONG ,  KRUEGER ELAINE ,  MAXWELL JOHN ,  LE TIRAN ARNAUD ,  LIAO YUSHENG

Inventor： GUTIERREZ COREY DON ,  TERMIN ANDREAS ,  HADIDA-RUAH SARA ,  BERGERON DANIELE ,  YOO SANGHEE ,  BINCH HAYLEY ,  JOSHI PRAMOD ,  COME JON ,  NANTHAKUMAR SUGANTHI ,  CAO JINGRONG ,  KRUEGER ELAINE ,  MAXWELL JOHN ,  LE TIRAN ARNAUD ,  LIAO YUSHENG

IPC: C07D277/14 ,  A61K31/4468 ,  A61K31/517 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D498/10 ,  C07D513/10

CPC classification number: C07D277/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D498/10 ,  C07D513/10

Abstract: The present invention relates to CGRP receptor antagonists of formula I, wherein: X is S, Si, or SO2; pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.

Abstract translation: 本发明涉及式I的CGRP受体拮抗剂，其中：X是S，Si或SO 2; 其药物组合物及其用于治疗CGRP受体介导的疾病和病症的方法。

公开(公告)号：WO2009076200A3

公开(公告)日：2009-08-27

申请号：PCT/US2008085673

申请日：2008-12-05

Applicant: VERTEX PHARMA ,  ALARGOVA ROSSITZA ,  KADIYALA IRINA ,  LE TIRAN ARNAUD ,  MACIKENAS DAINIUS ,  ZHANG YUEGANG

Inventor： ALARGOVA ROSSITZA ,  KADIYALA IRINA ,  LE TIRAN ARNAUD ,  ZHANG YUEGANG

IPC: C07D401/14 ,  A61K31/4184 ,  A61P31/00

CPC classification number: C07D401/14

Abstract: Solid forms of crystalline1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)- 1H-benzo[d]imidazol-2-yl)urea, compositions containing solid forms of crystalline 1- ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d]imidazol-2-yl)urea and methods of using the same are described.

Abstract translation: 结晶1-乙基-3-（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）脲的固体形式，含有固体形式的组合物 的结晶1-乙基-3-（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）脲及其使用方法 被描述。

公开(公告)号：CA2785499C

公开(公告)日：2017-05-02

申请号：CA2785499

申请日：2010-12-21

Applicant: VERTEX PHARMA

Inventor： ARONOV ALEX ,  COME JON H ,  DAVIES ROBERT J ,  PIERCE ALBERT CHARLES ,  WANG JIAN ,  NANTHAKUMAR SUGANTHINI S ,  CAO JINGRONG ,  BANDARAGE UPUL KEERTHI ,  KRUEGER ELAINE B ,  LE TIRAN ARNAUD ,  LIAO YUSHENG ,  MESSERSMITH DAVID ,  COLLIER PHILIP N ,  GREY RONALD LEE JR ,  O'DOWD HARDWIN ,  HENDERSON JAMES A ,  GRILLOT ANNE-LAURE

IPC: C07D401/04 ,  A61K31/352 ,  A61K31/424 ,  A61K31/429 ,  A61P9/00 ,  A61P29/00 ,  A61P37/00 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/20 ,  C07D491/20

Abstract: The present invention relates to compounds having the formula: (see formula I) useful as inhibitors of PI3K, particularly of PI3K.gamma.. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：NZ612961A

公开(公告)日：2015-10-30

申请号：NZ61296112

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： PEROLA EMANUELE ,  LE TIRAN ARNAUD ,  GRILLOT ANNE-LAURE ,  CHARIFSON PAUL S ,  BENNANI YOUSSEF LAAFIRET ,  O’DOWD HARDWIN

IPC: C07D405/14 ,  A61K31/506 ,  A61P31/04 ,  C07F9/6558

Abstract: NZ 612961 The disclosure relates to solid forms of compound of formula (I) and pharmaceutically acceptable salts thereof, wherein the variables X and R are as defined herein, particularly the methanesulfonic acid salt, which inhibit bacterial enzymes gyrase and/or topoisomerase IV. The compounds of formula (I) either possess a broad range of anti bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity. Also disclosed are pharmaceutical compositions comprising said compound of formula (I) or its salts and their use for treating nosocomial or a non-nosocomial bacterial infections which are characterized by the presence of one or more of Streptococcus pneumoniae, Staphylococcus epidermidis, Enterococcus faecalis, Staphylococcus aureus, Clostridium difJicile, Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, ycobacterium avium complex, Mycobacterium abscessus, Mycobacterium kansasii, Mycobacterium ulcerans, Chlamydophila pneumoniae, Chlamydia trachomatis, Haemophilus injluenzae, Streptococcus pyogenes or &bgr;-haemolytic streptococci.

公开(公告)号：CY1109385T1

公开(公告)日：2014-07-02

申请号：CY091100962

申请日：2009-09-17

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL S ,  DEININGER DAVID D ,  GRILLOT ANNE-LAURE ,  LIAO YUSHENG ,  RONKIN STEVEN M ,  STAMOS DEAN ,  PEROLA EMANUELE ,  WANG TIANSHENG ,  LE TIRAN ARNAUD ,  DRUMM JOSEPH

IPC: C07D403/14 ,  A61K31/4184 ,  A61P31/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: Ηπαρούσαεφεύρεσηαφοράενώσειςοιοποίεςαναστέλλουνβακτηριακήγυράσηκαι/ή Topo IV καιφαρμακευτικώςαποδεκτέςσυνθέσειςπουπεριλαμβάνουντιςαναφερθείσεςενώσεις. Αυτέςοιενώσεις, καισυνθέσειςαυτών, είναιχρήσιμεςστηνθεραπείαβακτηριακήςμόλυνσης. Συνεπώς, ηπαρούσαεφεύρεσηεπίσηςαφοράμεθόδουςγιατηνθεραπείαβακτηριακώνμολύνσεωνσεθηλαστικά. Τύπος (Ι).

公开(公告)号：SG191946A1

公开(公告)日：2013-08-30

申请号：SG2013053426

申请日：2012-01-13

Applicant: VERTEX PHARMA

Inventor： LE TIRAN ARNAUD ,  GRILLOT ANNE-LAURE ,  CHARIFSON PAUL S ,  BENNANI YOUSSEF LAAFIRET ,  O'DOWD HARDWIN ,  PEROLA EMANUELE

Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti¬ bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.

公开(公告)号：NZ579296A

公开(公告)日：2012-10-26

申请号：NZ57929608

申请日：2008-02-27

Applicant: VERTEX PHARMA

Inventor： COTTRELL KEVIN M ,  MAXWELL JOHN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  LE TIRAN ARNAUD ,  PEROLA EMANUELE

IPC: C07D498/10 ,  A61K31/24 ,  A61P31/12

Abstract: Disclosed are spiro compounds of formula (I), salts thereof, and methods for their preparation. A specific example of compounds of formula (I) is: 7-((S)-3-(benzo[b]thiophen-3-yl)-2-(2-cyclohexylacetamido)propanoyl)-3-(3-chlorophenyl)-N-((3R)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide, Compounds of formula (I) are useful for treating hepatitis C virus

公开(公告)号：AU2006282771B2

公开(公告)日：2012-08-09

申请号：AU2006282771

申请日：2006-08-28

Applicant: VERTEX PHARMA

Inventor： GRILLOT ANNE-LAURE ,  MAXWELL JOHN ,  COTTRELL KEVIN M ,  PEROLA EMANUELE ,  LE TIRAN ARNAUD ,  TANG QING

IPC: C07D498/10 ,  C07K5/08

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.

公开(公告)号：AU2004322641B2

公开(公告)日：2012-05-31

申请号：AU2004322641

申请日：2004-10-21

Applicant: VERTEX PHARMA

Inventor： PEROLA EMANUELE ,  DEININGER DAVID D ,  LE TIRAN ARNAUD ,  GRILLOT ANNE-LAURE ,  RONKIN STEVEN M ,  WANG TIANSHENG ,  STAMOS DEAN ,  CHARIFSON PAUL S ,  LIAO YUSHENG ,  DRUMM JOSEPH

IPC: C07D491/04 ,  A61K31/4439 ,  A61K31/506 ,  A61P31/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.