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公开(公告)号：NO20052888D0
公开(公告)日：2005-06-10
申请号：NO20052888
申请日：2005-06-10
Applicant: VERTEX PHARMA
Inventor： ARNOST MICHAEL J , FORSTER CORNELIA J , DAVIES ROBERT J , PIERCE ALBERT , BINCH HAYLEY , LEDEBOER MARK , LEDFORD BRIAN E , GALULLO VINCENT , GREY RONALD , TIAN SHI-KAI , XU JINWANG , MESSERSMITH DAVID , NANTHAKUMAR SUGHANTHI , JAYARAJ ANDREW
IPC: A61K31/4196 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D249/10 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07D495/04 , C07D
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：DE60110616D1
公开(公告)日：2005-06-09
申请号：DE60110616
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： BEBBINGTON DAVID , BINCH HAYLEY , KNEGTEL RONALD , GOLEC JULIAN M C , PATEL SANJAY , CHARRIER JEAN-DAMIEN , KAY DAVID , DAVIES ROBERT , LI PAN , WANNAMAKER MARION , 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：PL361676A1
公开(公告)日：2004-10-04
申请号：PL36167601
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： DAVIES ROBERT , BEBBINGTON DAVID , KNEGTEL RONALD , WANNAMAKER MARION , LI PAN , FORESTER 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
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：NO20031191L
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
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：NO20031189D0
公开(公告)日：2003-03-14
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 , C07D
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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Patent Agency Ranking
公开(公告)号：PE04512002A1
公开(公告)日：2002-06-06
申请号：PE0009312001
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
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
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：AU9091401A
公开(公告)日：2002-03-26
申请号：AU9091401
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： KNEGTEL RONALD , BEBBINGTON DAVID , BINCH HAYLEY , GOLEC JULIAN , PATEL SANJAY , CHARRIER JEAN-DAMIEN , KAY DAVID , DAVIES ROBERT , LI PAN , WANNAMAKER MARION , 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 , A61K31/4427 , 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：CA2422378A1
公开(公告)日：2002-03-21
申请号：CA2422378
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： PATEL SANJAY , BINCH HAYLEY , CHARRIER JEAN-DAMIEN , FORSTER CORNELIA , WANNAMAKER MARION , LI PAN , BEBBINGTON DAVID , DAVIES ROBERT , KAY DAVID , PIERCE ALBERT , GOLEC JULIAN M C , KNEGTEL RONALD
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 (IV) wherein Ri ng 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 taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ri ng having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R 2, R2', and T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 an d GSK-3, for treating diseases such as cancer, diabetes and Alzehimer's diseas e.
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公开(公告)号：HUE037516T2
公开(公告)日：2018-09-28
申请号：HUE14800181
申请日：2014-10-17
Applicant: VERTEX PHARMA
Inventor： CHARIFSON PAUL , COTTRELL KEVIN , DENG HONGBO , DUFFY JOHN , GAO HUAI , GIROUX SIMON , GREEN JEREMY , JACKSON KATRINA , KENNEDY JOSEPH , LAUFFER DAVID , LEDEBOER MARK , LI PAN , MAXWELL JOHN , MORRIS MARK , PIERCE ALBERT , WAAL NATHAN , XU JINWANG
IPC: A61P35/00
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公开(公告)号：LT3057959T
公开(公告)日：2018-06-11
申请号：LT14800181
申请日：2014-10-17
Applicant: VERTEX PHARMA
Inventor： CHARIFSON PAUL , COTTRELL KEVIN , DENG HONGBO , DUFFY JOHN , GAO HUAI , GIROUX SIMON , GREEN JEREMY , JACKSON KATRINA , KENNEDY JOSEPH , LAUFFER DAVID , LEDEBOER MARK , LI PAN , MAXWELL JOHN , MORRIS MARK , PIERCE ALBERT , WAAL NATHAN , XU JINWANG
IPC: C07D403/12 , A61K31/506 , A61P35/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07D493/04
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