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1.发明公开INHIBITORS OF c-JUN N-TERMINAL KINASES (JNK) AND OTHER PROTEIN KINASES 有权c-Jun N-末端激酶（JNK）AND OTHER蛋白抑制剂KINASES-
公开(公告)号：EP1218369A4
公开(公告)日：2005-06-22
申请号：EP00957485
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 , C07D403/04 , C07D405/04
CPC classification number: C07D413/04 , A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , C07D413/14
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公开(公告)号：CA2381882C
公开(公告)日：2011-01-25
申请号：CA2381882
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: C07D413/04 , 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 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/14
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 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：CO5200770A1
公开(公告)日：2002-09-27
申请号：CO00060686
申请日：2000-08-14
Applicant: VERTEX PHARMA
Inventor： GREEN JEREMY , BEMIS GUY , GRILLOT ANNE-LAURE , LEDEBOER MARK , SALITURO FRANCIS , HARRINGTON EDMUND , HUAI GAO , BAKER CHRISTOPHER
IPC: A61K31/341 , A61K31/39 , A61K31/40 , 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
Abstract: Un compuesto que tiene la fórmula: En dondeX-Y-Z se seleccionan de uno de los siguientes: R1 es H, CONH2, T(n)-R, o T(n) -Ar2;R es un grupo alifático o grupo alifático sustituido;N es cero o uno;T es C(=0), CO2, CONH, S(O)2, S(O)2NH, COCH2 o CH2; cada R2 es independiente seleccionado de hidrógeno, -R, CH2OR, -CH2OH, -CH=O, CH2SR, CH2S(O)R, CH2(C=O)R, CH2CO2, CH2CO2H, CH2CN, CH2NHR, CH2N(R)2, -CH=N-OR, -CH=NNHR, -CH=NNHR, -CH=NN(R)2, -CH=NNHCCOR, -CH=NNHCO2R, -CH=NNHSO2R,-arilo, -arilo sustituido), (-heterociclilo, o -heterociclilo sustituido);Cada R3 es independiente seleccionado de hidrógeno, R, COR, CO2R o S(O)2R;G es R o Ar1;Ar1 es arilo, arilo sustituido, aralquilo, aralquilo sustituido, heterociclilo, o heterociclilo sustituido, en donde Ar1 está opcionalmente fusionado a un anillo de 5 a 7 miembros parcial o completamente insaturado que contiene de 0 a 3 heteroátomos;Q-NH es en donde el H de Q-NH es opcionalmente reemplazado por R3; A es N o CR3;U es CR3, O S, o NR;Ar2 es arilo, arilo sustituido, heterociclilo, o heterociclilo sustituido, en donde Ar2 está opcionalmente fusionado a un anillo de 5 a 7 miembros parcial o completamente insaturado que contiene de 0 a 3 heteroátomos; yen donde cada átomo de carbono sustituible en Ar2, que incluye el anillo fusionado cuando está presente, es opcional e independiente sustituido por halo, R, OR, SR, OH, NO2, CN, NH2, NHR, N(R)2, NHCOR, NHCONHR, NHCON(R)2, NRCOR, NHCO2R, CO2R, CO2H, COR, CONHR, CON(R)2, S(O)2R, SONH2, S(O)R, SO2NHR, o NHS(O)2R, y en donde cada carbono saturado en el anillo fusionado es además opcional e independientemente sustituido por =O, =S, =NNHR, =NNR2, =N-OR, =NNHCOR, =NNHCO2, =NNHSO2R, o =NR;en donde cada átomo de nitrógeno sustituible en Ar2 es opcionalmente sustituido por R, COR, S(O)2R, o CO2R.
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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：MY132496A
公开(公告)日：2007-10-31
申请号：MYPI9901841
申请日：1999-05-10
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCIS , GALULLO VINCENT , BELLON STEVEN , BEMIS GUY , COCHRAN JOHN
IPC: C07D213/56 , A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: THE PRESENT INVENTION RELATES TO INHIBITORS OF P38, 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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Patent Agency Ranking
公开(公告)号：NZ517694A
公开(公告)日：2005-03-24
申请号：NZ51769400
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 , AKER 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: Disclosed herein are compounds of formula (I), wherein R1 is H, CONH2, T(n)-R, or T(n)-Ar2; G is R or Ar1; R is an aliphatic or substituted aliphatic group; n may be zero or one; and Ar1, Ar2, XYZ, and Q 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. Also disclosed are methods for producing these inhibitors, and pharmaceutical compositions comprising these inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号：NO20020713A
公开(公告)日：2002-04-12
申请号：NO20020713
申请日：2002-02-12
Applicant: VERTEX PHARMA
Inventor： GREEN JEREMY , BEMIS GUY , GRILLOT ANNE-LAURE , LEDERBOER 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
CPC classification number: C07D413/04 , A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , C07D413/14
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公开(公告)号：AU2006203676B2
公开(公告)日：2010-04-22
申请号：AU2006203676
申请日：2006-08-24
Applicant: VERTEX PHARMA
Inventor： BAKER CHRISTOPHER , HARRINGTON EDMUND , GRILLOT ANNE-LAURE , BEMIS GUY , GREEN JEREMY , HALE MICHAEL , LEDEBOER MARK , GAO HUAI , CAO JINGRONG , SALITURO FRANCIS
IPC: C07D413/14 , A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , C07D413/04
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公开(公告)号：HU0300340A2
公开(公告)日：2003-06-28
申请号：HU0300340
申请日：2000-08-11
Applicant: VERTEX PHARMA
Inventor： BAKER CHRISTOPHER , BEMIS GUY , CAO JINGRONG , GAO HUAI , GREEN JEREMY , GRILLOT ANNE-LAURE , HALE MICHAEL , HARRINGTON EDMUND , LEDEBOER MARK , SALITURO FRANCIS
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
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：AU6909600A
公开(公告)日：2001-03-13
申请号：AU6909600
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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