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公开(公告)号：NO20031191A
公开(公告)日：2003-05-13
申请号：NO20031191
申请日：2003-03-14
Applicant: VERTEX PHARMA
Inventor： DAVIES ROBERT , BEBBINGTON DAVID , KNEGTEL RONALD , WANNAMAKER MARION W , LI PAN , FORSTER CORNELIA , PIERCE ALBERT , KAY DAVID
IPC: C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155 , A61K35/00
CPC classification number: C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
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公开(公告)号：NO20031189L
公开(公告)日：2003-05-13
申请号：NO20031189
申请日：2003-03-14
Applicant: VERTEX PHARMA
Inventor： BEBBINGTON DAVID , BINCH HALEY , KNEGTEL RONALD , GOLEC JULIAN M C , PATEL SANJAY , CHARRIER JEAN-DAMIEN , KAY DAVID , DAVIES ROBERT , LI PAN , WANNAMAKER MARION W , FORSTER CORNELIA , PIERCE ALBERT
IPC: C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155
Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
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公开(公告)号：CA2450769A1
公开(公告)日：2002-12-27
申请号：CA2450769
申请日：2002-06-14
Applicant: VERTEX PHARMA
Inventor： MOON YOUNG CHOON , CHOQUETTE DEB , DAVIES ROBERT , GREEN JEREMY , PIERCE ALBERT , LEDEBOER MARK
IPC: A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/635 , A61L27/00 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D401/14 , C07D409/14 , A61K31/505
Abstract: Described herein are benzisoxazole compounds of formula I or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N- O or O-N; Ar is an optionally substituted C5-10 aryl group; R1 is hydrogen or an optionally substituted group selected from C1-I0 aliphatic, C5-10 aryl, C6-1 2 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. The invention also provides pharmaceutically acceptable composition s comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various -, protein kinase mediated disorders.
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公开(公告)号：PE20020451A1
公开(公告)日：2002-06-06
申请号：PE2001000931
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： DAVIES ROBERT , BEBBINGTON DAVID , KNEGTEL RONALD , WANNAMAKER MARION , LI PAN , FORSTER CORNELIA J , LAUFFER DAVID , PIERCE ALBERT , KAY DAVID
IPC: C07D403/12 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/4427 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
Abstract: SE REFIERE A COMPUESTOS DE PIRAZOL DE FORMULA I DONDE EL ANILO C ES FENILO, PIRIDINILO, PIRIMIDINILO, PIRIDAZINILO, PIRAZINILO, 1,2,4-TRIAZINILO SUSTITUIDO EN LA POSICION ORTO POR HALO, CN, NO2, T-V-R6, FENILO, HETEROARILO, HETEROCICLO, UN GRUPO ALIFATICO C1-C6; EN LA POSICION DIFERENTE DE ORTO ES SUSTITUIDO POR R5; R1 Y R2 SON R, R-W-R6, ANILLO DE 5-8 MIEMBROS SUSTITUIDO CON HALO, OXO, CN, NO2R7, VR6; Rx Y Ry SON T-R3, ANILLO FUSIONADO SUSTITUIDO CON T-R3, OXO, R4; T ES ENLACE, ALQUILIDENO, C1-C4; R3 ES R, HALO, OR, COR, N(R4)2, CON(R7)2, ENTRE OTROS; R ES H, ARILO C6-C10, HETEROARILO C5-C10, HETEROCICLO 5-10 MIEMBROS; R4 ES R7, CON(R7)2, SO2R7; R7 ES H, GRUPO ALIFATICO, DOS R7 FORMAN HETEROARILO, HETEROCICLO; R5 ES R, HALO, OR, NR4COR, COCOR, ENTRE OTROS; V ES O, S, SO, SO2, NR6SO2, SO2NR6, CONR6, ENTRE OTROS; R6 ES H, GRUPO ALIFATICO C1-C4, DOS R6 FORMAN HETEROARILO, HETEROCICLO; W ES C(R6)2O, C(R6)2S, CO2, CONR6. TAMBIEN SE REFIERE A COMPUESTOS DE FORMULA A, B, ENTRE OTROS; R10 ES F, Br, HALOALQUILO C1-C6, NITRO, 1-PIRROLO; R1 ES Cl, F, CF3, CN, NO2; LOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE CINASAS GLICOGENO SINTASA GSK-3; SERINA TREONINA AURORA-2, AUMENTAN LA SINTESIS DE GLICOGENO, DISMINUYEN NIVEL SANGUINEO DE GLUCOSA, INHIBEN LA PRODUCCION DE PROTEINA TAU HIPERFOSFORILADA, INHIBEN LA FOSFORILACION DE ß-CATEINA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DIABETES, ALZHEIMER, ESQUIZOFRENIA, CANCER
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公开(公告)号：CA2422379A1
公开(公告)日：2002-03-21
申请号：CA2422379
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： KNEGTEL RONALD , WANNAMAKER MARION , FORESTER CORNELIA , LI PAN , BEBBINGTON DAVID , KAY DAVID , DAVIES ROBERT , PIERCE ALBERT
IPC: C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155
Abstract: This invention describes novel pyrazole compounds of formula II:wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, o r 1, 2, 4-triazinyl ring, and R2, R2, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2 are optionally taken together with the ir intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.
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Patent Agency Ranking
公开(公告)号：HUE057527T2
公开(公告)日：2022-05-28
申请号：HUE18207382
申请日：2014-03-12
Applicant: VERTEX PHARMA
Inventor： MAXWELL JOHN , CHARIFSON PAUL , TANG QING , RONKIN STEVEN , JACKSON KATRINA , PIERCE ALBERT , LAUFFER DAVID , LI PAN , GIROUX SIMON , XU JINWANG , MORRIS MARK , COURT JOHN , COTTRELL KEVIN , DENG HONGBO , WAAL NATHAN , GU WENXIN
IPC: C07D403/12 , A61P35/00 , C07D241/44 , C07D405/12 , C07D413/04 , C07D417/12
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公开(公告)号：AU2012203384A8
公开(公告)日：2012-08-02
申请号：AU2012203384
申请日：2012-06-08
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , WANG JIAN , PINDER JOANNE , WANG TIANSHENG , PIERCE ALBERT
IPC: C07D471/04 , C07D519/00
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：AU2012203384A1
公开(公告)日：2012-06-28
申请号：AU2012203384
申请日：2012-06-08
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , WANG JIAN , PINDER JOANNE , WANG TIANSHEN , PIERCE ALBERT
IPC: C07D471/04 , C07D519/00
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：AT540948T
公开(公告)日：2012-01-15
申请号：AT06770824
申请日：2006-05-22
Applicant: VERTEX PHARMA
Inventor： WANNAMAKER MARION , LEDEBOER MARK , PIERCE ALBERT , WANG TIANSHENG , FARMER LUC , MARTINEZ-BOTELLA GABRIEL , BEMIS GUY , BETHIEL RANDY , COME JON , ARNOST MICHAEL , SALITURO FRANCESCO , WANG JIAN , MARHEFKA CRAIG , STEWART MICHELLE , GREEN JEREMY
IPC: C07D471/04 , A61K31/437 , A61P35/00 , C07D487/04
Abstract: The present invention relates to compounds of formula (I) wherein Q, Z, R 1 , R 2 , and R 3 are as described in claim 1 useful as inhibitors of protein kinases, particularly of JAK family and ROCK family kinases. 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.
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公开(公告)号：PL1730146T3
公开(公告)日：2011-10-31
申请号：PL05756052
申请日：2005-03-30
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , PINDER JOANNE , WANG TIANSHENG , PIERCE ALBERT , WANG JIAN
IPC: C07D471/04 , C07D519/00
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