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公开(公告)号：NO322745B1
公开(公告)日：2006-12-04
申请号：NO20014837
申请日：2001-10-04
Applicant: VERTEX PHARMA
Inventor： BEMIS GUY W , GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JAMES JANETKA , MULLICAN MICHAEL , XIE XIAOLING , STRAUB JUDITH , TANG QING , MASHAL ROBERT
IPC: A61B17/00 , C07D403/04 , A61F2/02 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/00 , A61L27/00 , A61P1/00 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P21/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D231/38 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R 1-4 , Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
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公开(公告)号：AT335737T
公开(公告)日：2006-09-15
申请号：AT01971002
申请日：2001-09-14
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , CAO JINGRONG , MASHAL ROBERT
IPC: A61K31/42 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P1/00 , A61P1/02 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/422 , A61K31/439
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公开(公告)号：AU782775B2
公开(公告)日：2005-08-25
申请号：AU3672301
申请日：2001-02-05
Applicant: VERTEX PHARMA
Inventor： GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JANETKA JAMES , MULLICAN MICHAEL , BEMIS GUY , XIE XIAOLING , STRAUB JUDITH , TANG QING , MASHALL ROBERT
IPC: A61B17/00 , A61F2/02 , A61K31/4155 , A61K31/4178 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/00 , A61L27/00 , A61P1/00 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P21/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D231/38 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D403/00
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R 1-4 , Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
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公开(公告)号：MXPA03007049A
公开(公告)日：2003-11-18
申请号：MXPA03007049
申请日：2002-02-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL
IPC: A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/06 , A61P19/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
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公开(公告)号：ECSP034715A
公开(公告)日：2003-10-28
申请号：ECSP034715
申请日：2003-08-07
Applicant: VERTEX PHARMA
Inventor： TANG QING , CAO JINGRONG , GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , STRAUB JUDY , ARONOV ALEX
IPC: A61K20060101 , A61P20060101 , C07D20060101 , C07D403/04
Abstract: El invento se refiere a la química medicinal y se refiere a los compuestos de pirazol que son inhibidores de protein quinasa, especialmente inhibidores de ERK, composiciones que contienen dichos compuestos y métodos de uso. Los compuestos son útiles para tratar el cáncer y otras enfermedades que son aliviados por los inhibidores de protein quinasa.
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Patent Agency Ranking
公开(公告)号：NO20031192D0
公开(公告)日：2003-03-14
申请号：NO20031192
申请日：2003-03-14
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , CAO JINGRONG , MASHAL ROBERT
IPC: A61K31/42 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P1/00 , A61P1/02 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D417/14 , C07D
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公开(公告)号：PE20020971A1
公开(公告)日：2002-10-29
申请号：PE2002000101
申请日：2002-02-11
Applicant: VERTEX PHARMA
Inventor： CAO JINGRONG , GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , STRAUB JUDITH , TANG QING , ARONOV ALEX
IPC: A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/06 , A61P19/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
Abstract: SE REFIERE A UN METODO PARA INHIBIR LA ACTIVIDAD DE ERK2 ADMINISTRANDO COMPUESTOS DE PIRAZOL DE FORMULA I DONDE Sp ES UN GRUPO ESPACIADOR QUE COMPRENDE UN ANILLO HETEROAROMATICO DE 5 MIEMBROS; EL ANILLO A Y QR2 ESTAN UNIDOS A SP EN POSICIONES NO ADYACENTES; Sp ESTA SUSTITUIDO CON R6; Z1 Y Z2 SON N, CH; T Y Q SON UN ENLACE; U ES NR7, NR7CO, NR7CONR7, NR7CO2, O, CO, CO2, ENTRE OTROS; m Y n SON 0-1; R1 ES H, CN, HALOGENO, R, N(R7)2, OR, OH; R2 ES (CH2)yR5; (CH2)yCH(R5)2, (CH2)yCH(R8)CH(R5)2, N(R4)2, NR4(CH2)yN(R4)2, y ES 0-6; R3 ES R7, R, (CH2)yCH(R8)R, CN, (CH2)yCH(R8)CH(R5)2, (CH2)yCH(R8)N(R4)2; R ES UN GRUPO ALIFATICO, ARILO, HETEROARILO, HETEROCICLICO; R4 ES R, R7, COR7, CO2R, CON(R7)2, SO2R7, ENTRE OTROS; R5 ES R, OR, CO2R, (CH2)yN(R7)2, N(R7)2, OR7, SR7, CN, ENTRE OTROS; R6 ES R7, F, Cl, (CH2)yN(R7)2, N(R7)2, ENTRE OTROS; R7 ES H, UN GRUPO ALIFATICO, DOS R7 JUNTO A N FORMAN UN HETEROCICLO, HETEROARILO; R8 ES R, (CH2)wOR7, (CH2)wN(R4)2, (CH2)wSR7; w ES 0-4. SON COMPUESTOS PREFERIDOS (2-HIDROXI-1-METIL-2-FENIL-ETIL)-AMIDA DEL ACIDO 4-(2-CIANOAMINO-5-METIL-PIRIMIDIN-4-IL]-1H-PIRROL-2-CARBOXILICO; (2-HIDROXI-1-HIDROXIMETIL-2-FENIL-ETIL)-AMIDA DEL ACIDO 4-(2-ETILAMINO-5-METIL-PIRIMIDIN-4-IL)-1H-PIRROL-2-CARBOXILICO, ENTRE OTROS. LOS COMPUESTOS SON INHIBIDORES DE QUINASAS REGULADA POR SENAL EXTRACELULAR Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE CANCER, APOPLEJIA, DIABETES, HEPATOMEGALIA, ENFERMEDAD CARDIOVASCULAR, ALZHEIMER, FIBROSIS QUISTICA
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公开(公告)号：LT2001103A
公开(公告)日：2002-10-25
申请号：LT2001103
申请日：2001-10-17
Applicant: VERTEX PHARMA
Inventor： GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JANETKA JAMES , MULLICAN MICHAEL , BEMIS GUY , XIE XIAOLING , STRAUB JUDITH , TANG QING , MARSHALL ROBERT
IPC: A61B17/00 , A61F2/02 , A61K31/4155 , A61K31/4178 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/00 , A61L27/00 , A61P1/00 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P21/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D231/38 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D403/00
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) where R1-4, Q and t are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
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49.发明专利
公开(公告)号：CZ20020534A3
公开(公告)日：2002-07-17
申请号：CZ20020534
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: 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 , C07D413/04 , C07D413/14 , C07D401/04 , A61K31/4196 , A61K31/4245 , A61P7/00 , A61P19/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/04 , C07D407/14 , C07D417/04 , C07D417/14
CPC classification number: C07D413/04 , A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , C07D413/14
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公开(公告)号：SK3572002A3
公开(公告)日：2002-07-02
申请号：SK3572002
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: 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 , C07D413/04 , C07D413/14 , C07D401/04 , C07D405/04 , C07D403/04
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.
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