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71. 发明专利

CA2591413A1 PYRID-2-ONES USEFUL AS INHIBITORS OF TEC FAMILY PROTEIN KINASES FOR THE TREATMENT OF INFLAMMATORY, PROLIFERATIVE AND IMMUNOLOGICALLY-MEDIATED DISEASES 未知
公开(公告)号：CA2591413A1
公开(公告)日：2006-06-22
申请号：CA2591413
申请日：2005-12-15
申请人： VERTEX PHARMA
发明人： RAMAYA SHARN , JIMENEZ JUAN-MIGUEL , DURRANT STEVEN , RUTHERFORD ALISTAIR , CHARRIER JEAN-DAMIEN
IPC分类号： C07D213/22 , A61K31/4412 , A61K31/4427 , A61K31/444 , A61P29/00 , A61P35/00 , A61P37/00 , C07D213/64 , C07D213/75 , C07D401/14 , C07D407/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of protein 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. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.

72. 发明专利

AU2005219861A1 Caspase inhibitors and uses thereof 未知
公开(公告)号：AU2005219861A1
公开(公告)日：2005-09-15
申请号：AU2005219861
申请日：2005-02-28
申请人： VERTEX PHARMA
发明人： STUDLEY JOHN R , MORTIMORE MICHAEL , CHARRIER JEAN-DAMIEN , RUTHERFORD ALISTAIR , LOOKER ADAM , O'DONNELL MICHAEL , TRUDEAU MARTIN , RAMAYA SHARN , DURRANT STEVEN
IPC分类号： C07D207/16 , A61K38/04 , A61K38/06 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04
摘要： The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

73. 发明专利

AR038202A1 COMPUESTOS DE INDAZOL UTILES COMO INHIBIDORES DE LA PROTEINA QUINASA 未知
公开(公告)号：AR038202A1
公开(公告)日：2005-01-05
申请号：ARP030100171
申请日：2003-01-21
申请人： VERTEX PHARMA
发明人： BINCH HAYLEY , BRENCHLEY GUY , GOLEC JULIAN M C , KNEGTEL RONALD , MORTIMORE MICHAEL , PATEL SANJAY , RUTHERFORD ALISTAIR
IPC分类号： A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K45/00 , A61P1/16 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P19/00 , A61P19/10 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/02 , A61P43/00 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D401/02
摘要： Los compuestos son inhibidores de la proteína quinasa, en particular, son inhibidores de quinasa AKT, PKA, PDK1, p70S6K o ROCK, proteínas quinasas de mamífero involucradas en trastornos proliferativos y neurodegenerativos. Además se proporciona composiciones farmacéuticas que comprenden a los compuestos de la presente y a los métodos para utilizar dichas composiciones en el tratamiento de varios trastornos. Reivindicación 1: Un método para inhibir la quinasa AKT, PKA, PDK1, p70S6K o ROCK en: (a) un paciente; o (b) una muestra biológica; estando dicho método caracterizado porque comprende administrar a dicho paciente, o poner en contacto dicha muestra biológica con un compuesto de la fórmula (1) o una sal del mismo aceptable para uso farmacéutico, donde R1 se selecciona de halógeno, CN, N(R4)2, T-R, o T-Ar; cada T se selecciona, de manera independiente, de un enlace de valencia o una cadena de alquilideno C1-6, donde hasta dos unidades de metileno de T están, de manera opcional e independiente, reemplazadas por -O-, -N(R)-, -S-, -N(R)C(O), -C(O)N(R)-, -C(O)-, o -SO2-, T' es una cadena de alquilideno C1-6 donde hasta dos unidades de metileno de T' son reemplazadas, de manera opcional e independiente, por -O-, -N(R)-, -S-, -N(R)C(O)-, -C(O)N(R)-, -C(O)-, o -SO2; cada R se selecciona, de manera independiente, de H o un grupo alifático C1-6 opcionalmente sustituido, o: dos grupos R en el mismo N, tomados junto con el átomo de N unido allí, forman un anillo saturado, parcialmente insaturado o aromático de 5-7 miembros que tiene 1-3 heteroátomos seleccionados, de manera independiente, de N, O ó S; R2 se selecciona de Q-Ar, Q-N(R5)2, o Q-C(R)(Q-Ar)R3, donde: R y R3 forman de manera opcional, un anillo saturado o parcialmente insaturado de 5-7 miembros que tiene 0-4 heteroátomos seleccionados, de manera independiente, de N, O, o S; cada Q se selecciona, de manera independiente, de un enlace de valencia o una cadena de alquilideno C1-4; cada Ar es, independientemente, un anillo opcionalmente sustituido, seleccionado entre un anillo monocíclico, saturado, parcialmente insaturado o completamente insaturado de 5-7 miembros que tiene de 0-4 heteroátomos seleccionados, de manera independiente, de N, O, o S, o un anillo bicíclico saturado, parcialmente insaturado o completamente insaturado de 8-10 miembros que tiene de 0-4 heteroátomos seleccionados, de manera independiente, de N, O, o S; R3 se selecciona de R', Ar1, Q-OR5, Q-OC(O)R5, Q-CONHR5, Q-OC(O)NHR5, Q-SR5, Q-N(R4)2, N(R)(Q-Ar), N(R)C(O)Q-N(R4)2, o N(R)Q-N(R4)2; R' es un grupo alifático C1-6 opcionalmente sustituido; cada R4 se selecciona de manera independiente de R, COR5, CO2R5, CON(R5)2, SO2R5, SO2N(R5)2, o Ar1; cada R5 se selecciona, de manera independiente, de R o Ar; V1, V2, y V3 se seleccionan, de manera independiente, de N o C(R6); cada R6 se selecciona, de manera independiente de R, Ar1, halógeno, CN, NO2, OR, SR, N(R4)2, N(R)COR, N(R)CON(R4)2, N(R)C(O)OR, CON(R4)2, OC(O)N(R4)2, CO2R, OC(O)R, N(R)SO2R, N(R)SO2N(R4)2, SO2R, o SO2N(R4)2; y cada Ar1 se selecciona, de manera independiente, de un anillo monocíclico, opcionalmente sustituido, saturado, parcialmente insaturado o completamente insaturado de 5-7 miembros que tiene 0-4 heteroátomos seleccionados, de manera independiente, de N, O, o S; con la condición de que; cuando V1, V2 y V3 son, cada uno, CH y R1 es H, entonces R2 es Q-C(R)(Q-Ar)R3, donde R3 es diferente de R', Q-OC(O)R5 o OCH2fenilo.

75. 发明专利

AU2016222396B2 Pyrazine derivatives useful as inhibitors of ATR kinase 未知
公开(公告)号：AU2016222396B2
公开(公告)日：2018-04-05
申请号：AU2016222396
申请日：2016-08-31
申请人： VERTEX PHARMA
发明人： CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KAY DAVID , KNEGTEL RONALD , MACCORMICK SOMHAIRLE , MORTIMORE MICHAEL , O'DONNELL MICHAEL , PINDER JOANNE , RUTHERFORD ALISTAIR , YOUNG STEPHEN , REAPER PHILIP MICHAEL , VIRANI ANISA NIZARALI
IPC分类号： C07D413/04 , A61K31/497 , A61P35/00 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04
摘要： The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I): wherein the variables are as defined herein. N (L)n-R'

76. 发明专利

SG10201607592PA PYRAZINE DERIVATIVES USEFUL AS INHIBITORS OF ATR KINASE 未知
公开(公告)号：SG10201607592PA
公开(公告)日：2016-11-29
申请号：SG10201607592P
申请日：2009-12-18
申请人： VERTEX PHARMA
发明人： CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KAY DAVID , KNEGTEL RONALD , MACCORMICK SOMHAIRLE , MORTIMORE MICHAEL , O'DONNELL MICHAEL , PINDER JOANNE , RUTHERFORD ALISTAIR , VIRANI ANISA NIZARALI , YOUNG STEPHEN , REAPER PHILIP MICHAEL
摘要： The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

77. 发明专利

MX2014003491A COMPUESTOS UTILES COMO INHIBIDORES DE COLINA CINASA. 未知
公开(公告)号：MX2014003491A
公开(公告)日：2014-07-22
申请号：MX2014003491
申请日：2012-09-21
申请人： VERTEX PHARMA
发明人： MORTIMORE MICHAEL , EVERITT SIMON , RUTHERFORD ALISTAIR , KNEGTEL RONALD
IPC分类号： C07D453/02 , A61K31/439 , A61P33/06 , A61P35/00
摘要： La presente invención se relaciona con compuestos útiles como inhibidores de colina cinasa. La presente invención proporciona, además, composiciones farmacéuticamente aceptables que comprenden los compuestos y métodos para usar las composiciones en el tratamiento de diversas enfermedades, condiciones o trastornos. La presente invención proporciona, además, procesos para preparar los compuestos de las invenciones.

78. 发明专利

AU2012312301A8 Compounds useful as inhibitors of choline kinase 未知
公开(公告)号：AU2012312301A8
公开(公告)日：2014-03-27
申请号：AU2012312301
申请日：2012-09-21
申请人： VERTEX PHARMA
发明人： EVERITT SIMON , KNEGTEL RONALD , MORTIMORE MICHAEL , RUTHERFORD ALISTAIR
IPC分类号： C07D453/00 , A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/538 , A61P1/00 , A61P3/00 , A61P7/00 , A61P9/00 , A61P13/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00
摘要： The present invention relates to compounds useful as inhibitors of choline kinase. 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. The invention also provides processes for preparing compounds of the inventions.

79. 发明专利

AU2012312302A1 Compounds useful as inhibitors of choline kinase 未知
公开(公告)号：AU2012312302A1
公开(公告)日：2014-03-20
申请号：AU2012312302
申请日：2012-09-21
申请人： VERTEX PHARMA
发明人： MORTIMORE MICHAEL , EVERITT SIMON , RUTHERFORD ALISTAIR , KNEGTEL RONALD
IPC分类号： C07D453/02 , A61K31/439 , A61P33/06 , A61P35/00
摘要： The present invention relates to compounds useful as inhibitors of choline kinase. 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. The invention also provides processes for preparing compounds of the inventions.

80. 发明专利

CA2847186A1 COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE 未知
公开(公告)号：CA2847186A1
公开(公告)日：2013-03-28
申请号：CA2847186
申请日：2012-09-21
申请人： VERTEX PHARMA
发明人： MORTIMORE MICHAEL , EVERITT SIMON , RUTHERFORD ALISTAIR , KNEGTEL RONALD
IPC分类号： C07D453/02 , A61K31/439 , A61P33/06 , A61P35/00
摘要： The present invention relates to compounds useful as inhibitors of choline kinase. 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. The invention also provides processes for preparing compounds of the inventions.

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