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71. 发明专利

NO20073170L 未知
公开(公告)号：NO20073170L
公开(公告)日：2007-06-22
申请号：NO20073170
申请日：2007-06-22
申请人： VERTEX PHARMA
发明人： MORTIMORE MICHAEL , KNEGTEL RONALD , CHARRIER JEAN-DAMIEN , STUDLEY JOHN R
IPC分类号： C07D213/75
摘要： The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.

72. 发明专利

NZ537807A Caspase inhibitors and uses thereof 未知
公开(公告)号：NZ537807A
公开(公告)日：2007-05-31
申请号：NZ53780703
申请日：2003-06-27
申请人： VERTEX PHARMA
发明人： KNEGTEL RONALD , MORTIMORE MICHAEL , STUDLEY JOHN , MILLAN DAVID
IPC分类号： C07D239/88 , A61K31/473 , A61K31/517 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/06 , A61P31/14 , A61P31/18 , A61P31/20 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/06 , A61P43/00 , C07D217/24 , C07D239/90 , A61K31/472
摘要： Disclosed are caspase inhibitor of formula I and methods of preparing them wherein: X is CH; Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R2 is ethyl, n-propyl or isopropyl; R3 is H, halo, OCF3, CH, or CF3; and R4 is H, halo, OCF3, SR, CH, CF3, Ar or T-Ar wherein R, Ar and T are as defined in the specification. Compounds of the type disclosed are useful in the preparation of medicaments for treating diseases where caspase activity is indicated.

73. 发明专利

CA2627857A1 AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS 未知
公开(公告)号：CA2627857A1
公开(公告)日：2007-05-18
申请号：CA2627857
申请日：2006-11-03
申请人： VERTEX PHARMA
发明人： RUTHERFORD ALISTAIR , STUDLEY JOHN , PINDER JOANNE , BINCH HAYLEY , MILLER ANDREW , MORTIMORE MICHAEL , FRAYSSE DAMIEN , RAMAYA SHARN , ROBINSON DANIEL , EVERITT SIMON , DAVIS CHRIS , BOYALL DEAN , O'DONNELL MICHAEL
IPC分类号： A61K31/505 , C07D239/02
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

74. 发明专利

AU2006311797A1 Aminopyrimidines useful as kinase inhibitors 未知
公开(公告)号：AU2006311797A1
公开(公告)日：2007-05-18
申请号：AU2006311797
申请日：2006-11-03
申请人： VERTEX PHARMA
发明人： ROBINSON DANIEL , O'DONNELL MICHAEL , STUDLEY JOHN , DAVIS CHRIS , RUTHERFORD ALISTAIR , MORTIMORE MICHAEL , BINCH HAYLEY , PINDER JOANNE , EVERITT SIMON , RAMAYA SHARN , MILIER ANDREW , FRAYSSE DAMIEN , BOYALL DEAN
IPC分类号： A61K31/505 , C07D239/02
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

75. 发明专利

AU2005260689A1 Azaindoles useful as inhibitors of protein kinases 未知
公开(公告)号：AU2005260689A1
公开(公告)日：2006-01-12
申请号：AU2005260689
申请日：2005-06-29
申请人： VERTEX PHARMA
发明人： KENGTEL RONALD , MORTIMORE MICHAEL , PIERARD FRANCOISE , JIMENEZ JUAN-MIGUEL , MAZZEI FRANCESCA , BRENCHLEY GUY
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61P35/00 , C07D209/00 , C07D221/00

76. 发明专利

NO20056192L 未知
公开(公告)号：NO20056192L
公开(公告)日：2005-12-27
申请号：NO20056192
申请日：2005-12-27
申请人： VERTEX PHARMA
发明人： CHARRIER JEAN-DAMIEN , KNEGTEL RONALD , BRENCHLEY GUY , MORTIMORE MICHAEL , DURRANT STEVEN , STUDLEY JOHN R
IPC分类号： C07D213/74 , A61K31/4412 , C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula I: wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.

77. 发明专利

AR044770A1 DERIVADOS DE PIRIDINA COMO INHIBIDORES DE CASPASA Y SUS USOS 未知
公开(公告)号：AR044770A1
公开(公告)日：2005-10-05
申请号：ARP040101830
申请日：2004-05-27
申请人： VERTEX PHARMA
发明人： BRENCHLEY GUY , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KNEGTEL RONALD , MORTIMORE MICHAEL , STUDLEY JOHN
IPC分类号： C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12 , C07D213/74 , C07D213/81 , A61K31/4427 , A61P37/00
摘要： La presente provee composiciones farmacéuticas y métodos para utilizar dichas composiciones para el tratamiento de enfermedades mediadas por la caspasa y los procesos para preparar dichos compuestos. Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque: R1 es R6C(O)-, HC(O)-, R6SO2-, R6OC(O)-, (R6)2NC(O)-, (R6)(H)NC(O)-, R6C(O)C(O)-, R6-, (R6)2NC(O)C(O)-, (R6)(H)NC(O)C(O)-, o R6OC(O)C(O)-; R2 es hidrógeno, -CF3, halo, -OR7, -NO2, -OCF3, -CN, o R8; R3 es hidrógeno o alifático-(C1-4)-; R4 es -COOH o -COOR8; R5 es -CH2F o -CH2O-2,3,5,6-tetrafluorofenilo; R6 es alifático-(C1-12)-cicloalifático-(C3-10)-, arilo-(C6-10)-, heterociclilo-(C3-10)-, heteroarilo-(C5-10)-, cicloalifático-(C3-10)-alifático-(C1-12)-, aril-(C6-10)-alifático-(C1-12)-, heterociclil-(C3-10)-alifático-(C1-12)-, heteroaril-(C5-10)-alifático(C1-12)-, o dos grupos R6 enlazados al mismo átomo forman junto con dicho átomo un anillo aromático o no aromático de 3 a 10 miembros; donde el anillo está opcionalmente fusionado a arilo-(C6-10), heteroarilo-(C5-10), cicloalquilo-(C3-10), o heterociclilo-(C3-10); donde hasta 3 átomos de carbono alifáticos pueden ser reemplazados por un grupo seleccionado entre O, N(H), N(R), S, SO, y SO2; y donde R6 está sustituido con hasta 6 sustituyentes seleccionados de manera independiente de R; R es halógeno, -OR7, -OC(O)N(R7)2, -NO2, -CN, -CF3, -OCF3, -R7, oxo, =NR7, =N(OR7), tioxo, 1,2-metilendioxi, 1,2-etilendioxi, -N(R7)2, -SR7, -SOR7, -SO2R7, -SO2N(R7)2, -SO3R7, -C(O)R7, -C(O)C(O)R7, -C(O)C(O)OR7, -C(O)C(O)N(R7)2, -C(O)CH2C(O)R7, -C(S)R7, -C(S)OR7, -C(O)OR7, -OC(O)R7, -C(O)N(R7)2, -OC(O)N(R7)2, -C(S)N(R7)2, -(CH2)0-2NHC(O)R7, -N(R7)N(R7)COR7, -N(R7)N(R7)C(O)OR7, -N(R7)N(R7)CON(R7)2, -N(R7)SO2R7, -N(R7)SO2N(R7)2, -N(R7)C(O)OR7, -N(R7)C(O)R7, -N(R7)C(S)R7, -N(R7)C(O)N(R7)2, -N(R7)C(S)N(R7)2, -N(COR7)COR7, -N(OR7)R7, -C(=NH)N(R7)2, -C(O)N(OR7)R7, -C(=NOR7)R7, -OP(O)(OR7)2, -P(O)(R7)2, -P(O)(OR7)2, o -P(O)(H)(OR7); dos grupos R7 junto con los átomos a los cuales están enlazados forman un anillo aromático o no aromático de 3 a 10 miembros que tienen hasta 3 heteroátomos seleccionados independientemente entre N(H), N(R), O, S, SO, o SO2, donde el anillo está opcionalmente fusionado a arilo (C6-10), heteroarilo (C5-10), cicloalquilo (C3-10), o heterociclilo (C3-10), y donde cualquier anillo tiene hasta 3 sustituyentes seleccionados de manera independiente de J2; o cada R7 se selecciona, de manera independiente, de: hidrógeno-, alifático-(C1-12)-; cicloalifático-(C3-10)-; cicloalifático-(C3-10)-alifático-(C1-12)-; arilo-(C6-10)-; aril-(C6-10)-alifático-(C1-12)-; heterociclilo-(C3-10)-; heterociclil-(C6-10)-alifático-(C1-12)-; heteroarilo-(C5-10)-, o heteroaril-(C5-10)-alifático-(C1-12)-; donde R7 tiene hasta 3 sustituyentes seleccionados, de manera independiente, de J2; y J2 es halógeno, -OR7, -OC(O)N(R7)2, -NO2, -CN, -CF3, -OCF3, -R7, oxo, tioxo, =NR7, =NOR7, 1,2-metilendioxi, 1,2-etilendioxi, -N(R7)2, -SR7, -SOR7, -SO2R7, -SO2N(R7)2, -SO3R7, -C(O)R7, -C(O)C(O)R7, -C(O)C(O)OR7, -C(O)CH2C(O)R7, -C(S)R2, -C(S)OR7, -OC(O)R7, -C(O)N(R7)2, -OC(O)N(R7)2, -C(S)N(R7)2, -(CH2)0-2NHC(O)R7, -N(R7)N(R7)COR7, -N(R7)N(R7)C(O)OR7, -N(R7)N(R7)CON(R7)2, -N(R7)SO2R7, -N(R7)SO2N(R7)2, -N(R7)C(O)OR7, -N(R7)C(O)R7, -N(R7)C(S)R7, -N(R7)C(O)N(R7)2, -N(R7)C(S)N(R7)2, -N(COR7)COR7, -N(OR7)R7, -CN, -C(=NH)N(R7)2, -C(O)N(OR7)R7, -C(=NOR7)R7, -OP(O)(OR7)2, -P(O)(R7)2, -P(O)(OR7)2, o -P(O)(H)(OR7); y R8 es alifático-(C1-12)-cicloalifático (C3-10)-, (C6-10)-arilo-, heterociclilo-(C3-10)-, heteroarilo-(C5-10)-, cicloalifático-(C3-10)-alifático-(C1-12)-, aril-(C6-10)-alifático-(C1-12)-, heterociclil-(C3-10)-alifático-(C1-12), heteroaril-(C5-10)-alifático-(C1-12)-, donde hasta 3 átomos de carbono alifáticos pueden estar reemplazados con un grupo seleccionado entre O, N(H), N(R), S, SO, y SO2; y donde R8 está opcionalmente sustituido con hasta 6 sustituyentes seleccionados independientemente de R.

78. 发明专利

CA2557645A1 CASPASE INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2557645A1
公开(公告)日：2005-09-15
申请号：CA2557645
申请日：2005-02-28
申请人： VERTEX PHARMA
发明人： CHARRIER JEAN-DAMIEN , RUTHERFORD ALISTAIR , STUDLEY JOHN R , DURRANT STEVEN , LOOKER ADAM , TRUDEAU MARTIN , O'DONNELL MICHAEL , MORTIMORE MICHAEL , RAMAYA SHARN
IPC分类号： C07D405/12 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/443 , A61K38/04 , A61K38/06 , A61P37/00 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , 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.

79. 发明专利

PE07282004A1 INHIBIDORES DE CASPASA 未知
公开(公告)号：PE07282004A1
公开(公告)日：2004-10-23
申请号：PE0006532003
申请日：2003-06-27
申请人： VERTEX PHARMA
发明人： KNEGTEL RONALD , STUDLEY JOHN , MORTIMORE MICHAEL , MILLAN DAVID
IPC分类号： C07D239/88 , A61K31/472 , A61K31/473 , A61K31/517 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/06 , A61P31/14 , A61P31/18 , A61P31/20 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/06 , A61P43/00 , C07D217/24 , C07D239/90
CPC分类号： C07D239/90 , C07D217/24
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I DONDE X ES CH, N; Y ES HALO, TRIFLUOROFENOXI, TETRAFLUOROFENOXI; R2 ES ALQUILO C1-C6 DE CADENA RECTA O RAMIFICADA; R3 ES H; HALO, OCF3, CN, CF3; R4 ES H, HALO, OCF3, CN, Ar, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (S)-3-[2-(7-CLORO-1-OXO-1H-ISOQUINOLIN-2-IL)-BUTIRILAMINO]-5-FLUORO-4-OXO-ACIDO PENTANOICO; (S,S)-3-[2-(6-CLORO-4-OXO-4H-QUINAZOLIN-3-IL)-BUTIRILAMINO]-4-OXO-5-(2,3,5,6-TETRAFLUOROFENOXI)-ACIDO PENTANOICO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE CASPASAS UTILES EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR IL-1, ENFERMEDADES INFECCIOSAS, INFLAMATORIAS, ENTRE OTROS

80. 发明专利

PL358430A1 CARBAMATE CASPASE INHIBITORS AND USES THEREOF 未知
公开(公告)号：PL358430A1
公开(公告)日：2004-08-09
申请号：PL35843001
申请日：2001-03-29
申请人： VERTEX PHARMA
发明人： BEBBINGTON DAVID , CHARRIER JEAN-DAMIEN , KAY DAVID , KNEGTEL RONALD , GOLEC JULIAN , MORTIMORE MICHAEL , STUDLEY JOHN
IPC分类号： A61K31/403 , A61K31/404 , A61K31/473 , A61K31/496 , A61K31/5415 , A61K31/55 , A61K31/575 , A61P9/00 , A61P19/02 , A61P19/08 , A61P25/32 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/04 , C07D209/08 , C07D209/82 , C07D209/86 , C07D221/12 , C07D223/22 , C07D223/26 , C07D223/28 , C07D279/30 , C07D279/36 , C07D403/12 , C07J9/00 , C07D209/00 , A61K31/395
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R 1 is hydrogen, -CHN 2 , R, CH 2 OR, CH 2 SR, or -CH 2 Y; Y is an electronegative leaving group; R 2 is CO 2 H, CH 2 CO 2 H, or esters, amides or isosteres thereof; R 3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R 4 and R 5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1beta secretion.

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