公开(公告)号：PE20120508A1

公开(公告)日：2012-05-09

申请号：PE2011002120

申请日：2010-06-17

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL ,  CLARK MICHAEL P ,  BANDARAGE UPUL K ,  BETHIEL RANDY S ,  COURT JOHN J ,  DENG HONGO ,  DRUTU IONA ,  DUFFY JOHN P ,  FARMER LUC ,  GAO HUAI ,  GU WEXIN ,  JACOBS DYLAN H ,  KENNEDY JOSEPH M ,  LEDEBOER MARK W ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  PEROLA EMANUELE ,  WANG TIANSHENG ,  WANNAMAKER M WOODS ,  BYRN RANDAL ,  ZHOU YI ,  LIN CHAO ,  JIANG MIN ,  JONES STEVEN ,  GERMANN URSULA A ,  SALITURO FRANCESCO G ,  KWONG ANN DAK-YEE

IPC: C07D471/04 ,  A61K31/437 ,  A61P31/16

Abstract: REFERIDA A UN DERIVADO DE PIRROLOPIRIDINA DE FORMULA (IA), DONDE Z1 ES F, Cl, CN, NO2, ENTRE OTROS; Z2 ES R*, OR*, CO2R*, ENTRE OTROS; Z3 ES H, OH, NH2, HALOGENO, ENTRE OTROS; R1 ES H O ALQUILO C1-C6; R2 ES H, F, NH2, NH(ALQUILO C1-C4), ENTRE OTROS; R3 ES H, Cl, F, OH, O(ALQUILO C1-C4), ENTRE OTROS; R4 ES (a), (b) O (c); T ES UN CARBOCICLO NO AROMATICO C3-C10 OPCIONALMENTE SUSTITUIDO CON JA O UN HETEROCICLO NO AROMATICO DE 3 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JB; J ES UN HETEROCICLO NO AROMATICO DE 3 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JB; D ES UN HETEROCICLO NO AROMATICO DE 4 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JD1; JA Y JB SON HALOGENO, CN, NCO, ENTRE OTROS; R9 ES H, HALOGENO, CN, OH, AMINO, ALQUILO C1-C6, ENTRE OTROS; R* ES H, ALQUILO C1-C6, CARBOCICLO C3-C8 NO AROMATICO, ENTRE OTROS; JD1 ES HALOGENO, CN, OXO, ENTRE OTROS; R13 Y R14 SON H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; j Y z SON 1 O 2; t ES 0, 1 O 2. SON COMPUESTOS PREFERIDOS: ACIDO (R)-3-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDINA-1-CARBONIL)PIRAZINA-2-CARBOXILICO, (S)-1-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDIN-1-IL)-2-METOXIETANONA, (S)-1-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDIN-1-IL)PROPAN-1-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA REPLICACION DEL VIRUS DE LA INFLUENZA

公开(公告)号：DE602004024572D1

公开(公告)日：2010-01-21

申请号：DE602004024572

申请日：2004-10-14

Applicant: VERTEX PHARMA

Inventor： JIMENEZ JUAN-MIGUEL ,  GREEN JEREMY ,  GAO HUAI ,  MOON YOUNG-CHOON ,  BRENCHLEY GUY ,  KNEGTEL RONALD ,  PIERARD FRANCOISE

IPC: C07D495/04 ,  A61K31/496 ,  A61K31/505 ,  A61K31/519 ,  A61P35/00 ,  C07D239/70 ,  C07D239/84 ,  C07D333/22 ,  C07D333/38 ,  C07D333/54 ,  C07D333/70 ,  C07D471/04 ,  C07D487/04 ,  C07D491/14 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：AU2008282156A1

公开(公告)日：2009-02-05

申请号：AU2008282156

申请日：2008-07-31

Applicant: VERTEX PHARMA

Inventor： JIMENEZ JUAN-MIGUEL ,  COLLIER PHILIP ,  DROS ALBERT CORNELIS ,  GAO HUAI ,  MILLER ANDREW ,  GREEN JEREMY ,  HAMON SYLVAIN LOIC JEAN-LUC

IPC: C07D471/04

公开(公告)号：NO20084652A

公开(公告)日：2008-12-03

申请号：NO20084652

申请日：2008-11-05

Applicant: VERTEX PHARMA

Inventor： FORSTER CORNELIA J ,  CAO JINGRONG ,  PIERCE ALBERT ,  MALTAIS FRANCOIS ,  LEDEBOER MARK ,  MESSERSMITH DAVID ,  WANG TIANSHENG ,  GAO HUAI ,  MARTINEZ-BOTELLA GABRIEL ,  SALITURO FRANCESCO ,  FARMER LUC ,  WANNAMAKER MARION ,  DUFFY JOHN ,  MARONE VALERIE

IPC: C07D487/04

CPC classification number: C07D487/04

公开(公告)号：DE60039616D1

公开(公告)日：2008-09-04

申请号：DE60039616

申请日：2000-08-11

Applicant: VERTEX PHARMA

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

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 R 1 is H, CONH 2 , T( n )-R, or T( n )-Ar 2 , 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：DE60214701T2

公开(公告)日：2007-09-13

申请号：DE60214701

申请日：2002-04-10

Applicant: VERTEX PHARMA

Inventor： CAO JINGRONG ,  GREEN JEREMY ,  MOON YOUNG-CHOON ,  WANG JIAN ,  LEDEBOER MARK ,  HARRINGTON EDMUND ,  GAO HUAI

IPC: C07D409/00 ,  C12N15/09 ,  A61K31/427 ,  A61K31/506 ,  A61L33/00 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P3/14 ,  A61P5/14 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C12N9/99

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, R a , R 1 , R 2 , R 3 , and R 4 are as described in the specification. 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; Lck and Src kinase. 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：MXPA06011328A

公开(公告)日：2006-12-15

申请号：MXPA06011328

申请日：2005-04-04

Applicant: VERTEX PHARMA

Inventor： COURT JOHN J ,  GREEN JEREMY ,  MILLER ANDREW ,  JIMENEZ JUAN-MIGUEL ,  MARHEFKA CRAIG ,  CAO JINGRONG ,  BANDARAGE UPUL K ,  GAO HUAI ,  NANTHAKUMAR SUGANTHINI

IPC: A61K31/437 ,  A61P29/00 ,  A61P37/08 ,  C07D471/04

Abstract: La presente invencion se relaciona con compuestos utiles como inhibidores de proteinas cinasas. La invencion tambien proporciona composiciones farmaceuticas que comprenden los compuestos de la invencion y los metodos para utilizar las composiciones en el tratamiento de diversas enfermedades, condiciones y desordenes.

公开(公告)号：NO20064976A

公开(公告)日：2006-10-31

申请号：NO20064976

申请日：2006-10-31

Applicant: VERTEX PHARMA

Inventor： GREEN JEREMY ,  CAO JINGRONG ,  MILLER ANDREW ,  COURT JOHN J ,  JIMENEZ JUAN-MIGUEL ,  MARHEFKA CRAIG ,  BANDRAGE UPUL K ,  GAO HUAI ,  NANTHAKUMAR SUGANTHINI

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

公开(公告)号：AT337312T

公开(公告)日：2006-09-15

申请号：AT02744355

申请日：2002-06-14

Applicant: VERTEX PHARMA

Inventor： BEMIS GUY ,  GAO HUAI ,  HARRINGTON EDMUND MARTIN ,  LEDEBOER MARK ,  SALITURO FRANCESCO ,  WANG JIAN

IPC: A61K31/506 ,  A61P1/04 ,  A61P1/16 ,  A61P3/14 ,  A61P5/14 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P27/16 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A-B is N-O or O-N and G, R , R , R , and R are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of Src and Lck kinase. 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：AU2004282172A1

公开(公告)日：2005-04-28

申请号：AU2004282172

申请日：2004-10-14

Applicant: VERTEX PHARMA

Inventor： JIMENEZ JUAN-MIGUEL ,  KNEGTEL RONALD ,  GAO HUAI ,  GREEN JEREMY ,  PIERARD FRANCOISE ,  BRENCHLEY GUY ,  MOON YOUNG-CHOON

IPC: A61K31/496 ,  C07D239/70 ,  C07D239/84 ,  C07D333/22 ,  C07D333/38 ,  C07D333/54 ,  C07D333/70 ,  C07D471/04 ,  C07D487/04 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.