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公开(公告)号:LT4981B
公开(公告)日:2003-01-27
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: 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:PE09712002A1
公开(公告)日:2002-10-29
申请号:PE0001012002
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
CPC classification number: 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:NO20014837D0
公开(公告)日:2001-10-04
申请号:NO20014837
申请日:2001-10-04
Applicant: VERTEX PHARMA
Inventor: GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JAMES JANETKA , 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 , C07D
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:CA2381882A1
公开(公告)日:2001-02-22
申请号:CA2381882
申请日:2000-08-11
Applicant: VERTEX PHARMA
Inventor: GAO HUAI , HARRINGTON EDMUND , SALITURO FRANCIS , BAKER CHRISTOPHER , HALE MICHAEL , BEMIS GUY , GREEN JEREMY , CAO JINGRONG , LEDEBOER MARK , GRILLOT ANNE-LAURE
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 , C07D403/04 , C07D405/04
Abstract: The present invention provides compounds of formula (I) where R1 is H, CONH2 , T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as describe d 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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公开(公告)号:AU6111000A
公开(公告)日:2001-02-13
申请号:AU6111000
申请日:2000-07-19
Applicant: VERTEX PHARMA
Inventor: HALE MICHAEL , MALTAIS FRANCOIS , BAKER CHRISTOPHER , JANETKA JAMES , MOON YOUNG CHOON , SAUNDERS JEFFREY
IPC: A61K31/505 , A61K45/06 , A61K31/00
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公开(公告)号:ES2651439T3
公开(公告)日:2018-01-26
申请号:ES14163944
申请日:2005-05-13
Applicant: VERTEX PHARMA
Inventor: MARTINEZ-BOTELLA GABRIEL , HALE MICHAEL , MALTAIS FRANÇOIS , TANG QING , STRAUB JUDITH
IPC: C07D401/04 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P37/00 , C07F9/58 , C07F9/6558
Abstract: Un compuesto, en el que el compuesto es un compuesto de fórmula II:**Fórmula** o una de sus sales farmacéuticamente aceptables, en la que: R1 es un grupo C1-6 alifático, en el que R1 está opcionalmente sustituido con hasta 2 grupos seleccionados independientemente entre -OR, -OR4 o -C1-3 haloalquilo; cada R es independientemente hidrógeno o C1-6 alifático; cada R2 es independientemente R, fluoro o cloro; m es 0, 1 o 2; R3 es hidrógeno, C1-3 alifático, fluoro o cloro; cada R4 es independientemente hidrógeno, -C(R)2O-R5 o R5, siempre que al menos un grupo R4 o R8 no sea hidrógeno; cada R5 es independientemente -C(O)R6, -C(O)OR6, -C(O)-Q-R6, -C(O)-(CH2)n-C(O)OR6, -C(O)-(CH2)n- C(O)N(R7)2, -C(O)-(CH2)n-CH(R6)N(R7)2, -P(O)(OR6)2; cada R6 es independientemente hidrógeno, un grupo C1-6 alifático opcionalmente sustituido o un anillo de 5-8 miembros saturado, parcialmente insaturado o totalmente insaturado, opcionalmente sustituido, que tiene 0-4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre; cada R7 es independientemente hidrógeno, -C(O)R6, -C(O)OR6, -S(O)2R6, -OR6, un grupo C1-6 alifático opcionalmente sustituido o un anillo de 5-8 miembros saturado, parcialmente insaturado o totalmente insaturado, opcionalmente sustituido, que tiene 0-4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno o azufre, o: dos R6 en el mismo átomo de nitrógeno tomados juntos con el átomo de nitrógeno al que están unidos forman un anillo de 4-7 miembros saturado, parcialmente insaturado o totalmente insaturado que tiene 1-3 heteroátomos además del átomo de nitrógeno, seleccionados independientemente entre nitrógeno, oxígeno o azufre; cada n es 0-6; Q es una cadena C1-10 alquilideno opcionalmente sustituida en la que cero a cuatro unidades de metileno de Q son reemplazadas independientemente por -O-, -N(R)-, -S-, -S(O)-, -S(O)2- o - C(O)-; y R8 es hidrógeno o -C(R)2O-R5.
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公开(公告)号:CA2437767C
公开(公告)日:2010-05-04
申请号:CA2437767
申请日:2002-02-08
Applicant: VERTEX PHARMA
Inventor: CAO JINGRONG , GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , STRAUB JUDY , TANG QING , ARONOV ALEX
IPC: C07D403/04 , 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 , C07D403/14 , C07D405/14 , C07D413/14
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
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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.
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公开(公告)号:AT392421T
公开(公告)日:2008-05-15
申请号:AT02756943
申请日:2002-08-02
Applicant: VERTEX PHARMA
Inventor: HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , TANG QING
IPC: C07D403/04 , A61K31/4155 , A61K45/00 , A61L27/00 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P17/06 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R 1 , n, R 3 , Q and R 4 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:DE60122176T2
公开(公告)日:2007-07-05
申请号:DE60122176
申请日:2001-09-14
Applicant: VERTEX PHARMA
Inventor: HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , CAO JINGRONG , MASHAL ROBERT
IPC: C07D413/04 , A61K31/42 , A61K31/422 , A61K31/433 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , 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 , C07D413/14 , C07D417/14
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