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1. 发明申请

WO0222602A3 TRIAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：三唑化合物可用作蛋白激酶抑制剂
公开(公告)号：WO0222602A3
公开(公告)日：2002-06-27
申请号：PCT/US0142162
申请日：2001-09-14
申请人： VERTEX PHARMA , BEBBINGTON DAVID , KNEGTEL RONALD , BINCH HALEY , GOLEC JULIAN M C , LI PAN , CHARRIER JEAN-DAMIEN
发明人： BEBBINGTON DAVID , KNEGTEL RONALD , BINCH HALEY , GOLEC JULIAN M C , LI PAN , CHARRIER JEAN-DAMIEN
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel triazole compounds of formula (IX): wherein Z is nitrogen or CR and Z is nitrogen or CH, provided that at least one of Z and Z is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from -R ; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R and R are independently selected from T-R , or R and R are taken together with their intervening atoms to form a fused ring; R , R , and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
摘要翻译：本发明描述了式（IX）的新型三唑化合物：其中Z 1是氮或CR 9且Z 2是氮或CH，条件是Z 1和Z 2中的至少一个是氮; G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基环，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; R x和R y独立地选自T-R 3，或者R x和R y与它们的居间原子一起形成稠环; R 1，R 3和T如说明书中所述。该化合物可用作蛋白激酶抑制剂，特别是作为GSK-3和Aurora的抑制剂，用于治疗诸如糖尿病，癌症和阿尔茨海默氏病的疾病。

3. 发明申请

WO2007027528A2 PYRIDONES USEFUL AS INHIBITORS OF KINASES 审中-公开
标题翻译：吡咯啉作为金刚石的抑制剂有用
公开(公告)号：WO2007027528A2
公开(公告)日：2007-03-08
申请号：PCT/US2006033282
申请日：2006-08-25
申请人： VERTEX PHARMA , CHARRIER JEAN-DAMIEN , RAMAYA SHARN , DURRANT STEVEN , JIMENEZ JUAN-MIGUEL , GOLEC JULIAN M C , MORTIMORE MICHAEL
发明人： CHARRIER JEAN-DAMIEN , RAMAYA SHARN , DURRANT STEVEN , JIMENEZ JUAN-MIGUEL , GOLEC JULIAN M C , MORTIMORE MICHAEL
IPC分类号： C07D401/14 , A61K31/444 , A61P35/00 , A61P37/00 , C07D213/64 , C07D401/04
CPC分类号： C07D401/04 , C07D213/64 , C07D213/74 , C07D401/14 , C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein 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.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

4. 发明专利

ES2289279T3 COMPOSICIONES UTILES COMO INHIBIDORES DE PROTEINQUINASAS. 未知
公开(公告)号：ES2289279T3
公开(公告)日：2008-02-01
申请号：ES03716598
申请日：2003-03-14
申请人： VERTEX PHARMA , BINCH HAYLEY , CHARRIER JEAN-DAMIEN , EVERITT SIMON , GOLEC JULIAN M C , KAY DAVID
发明人： BEBBINGTON DAVID , BINCH HAYLEY , CHARRIER JEAN-DAMIEN , EVERITT SIMON , GOLEC JULIAN M C , KAY DAVID
IPC分类号： C07D403/12 , A61K31/517 , A61P35/00 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Un compuesto de fórmula I: o un derivado farmacéuticamente aceptable del mismo, en la que: Y es nitrógeno o CR2; R2 es R, oxo, halógeno, -CN, -NO2, -CO2R, -Ar, -T-Ar o T-R; X es azufre, oxígeno, o NR2''; R2'' es R, o R2 y R2'' se toman juntos para formar un anillo de 5-7 miembros, parcialmente insaturado o totalmente insaturado, opcionalmente sustituido, que tiene de cero a dos heteroátomos del anillo seleccionados independientemente entre nitrógeno, oxígeno o azufre, en los que: cada nitrógeno del anillo sustituible, del anillo formado por R2 y R2'' está opcionalmente sustituido; cada aparición de R es, independientemente, hidrógeno, un grupo alifático C1-6 opcionalmente sustituido, o Ar; Z1 es nitrógeno o CRx; Rx es -R, halógeno, -N(R)2, -NO2, -CN, -CO2R, -OR o -SR; en el que dos R unidos al mismo átomo de nitrógeno se pueden tomar junto con ese átomo de nitrógeno, para formar un anillo herocíclico o heteroarilo de cinco o seis miembros, que tiene de uno a dos heteroátomos adicionales, seleccionados independientemente entre oxígeno, nitrógeno o azufre; Z2 es nitrógeno o CRy, con la condición de que Z1 y Z2 no sean nitrógeno simultáneamente; Ry es -R1, -CN, halógeno, -NO2, -Ar, -T-Ar, o -T-R, o Rx y Ry se toman juntos para formar un anillo de 5-7 miembros, parcialmente insaturado o totalmente insaturado, opcionalmente sustituido, que tiene de cero a dos heteroátomos, seleccionados independientemente entre oxígeno, azufre y nitrógeno, en el que: cada nitrógeno del anillo sustituible del anillo formado por Rx y Ry está opcionalmente sustituido; R1 es hidrógeno o un grupo alifático C1-6 opcionalmente sustituido; cada Ar es independientemente un anillo heterocíclico de 3-6 miembros, opcionalmente sustituido, que tiene uno o dos heteroátomos, seleccionados independientemente entre nitrógeno, oxígeno y azufre; o un anillo arilo de 5 ó 6 miembros que tiene de cero a tres heteroátomos, seleccionados independientemente entre nitrógeno, oxígeno o azufre, en el que Ar está fusionado opcionalmente con un anillo de cinco o seis miembros, parcialmente insaturado o totalmente insaturado, que tiene de cero a dos heteroátomos, seleccionados independientemente entre nitrógeno, oxígeno o azufre; T es una cadena de alquilideno C1-4 en la que una unidad de metileno de T está reemplazada opcionalmente por -O-, -S-, -C(O)-, -CO2-, -NR-, -NRC(O)-, -NRC(O)NR-, -C(O)C(O)-, -OC(O)NR-, -NRCO2-, -SO2NR-, -NRSO2-, o -NRSO2NR-; Q es -N(R'')-, -S-, -O-, -C(R'')2-, o un enlace de valencia, siempre que Q sea distinto de un enlace de valencia cuando Ht es un anillo triazol; en el que cada R'' es, independientemente, hidrógeno o un C1-6 alifático; y El anillo D es un anillo arilo monocíclico de cinco ó seis miembros, opcionalmente sustituido, que tiene de cero a dos heteroátomos, seleccionados independientemente entre nitrógeno, oxígeno o azufre; o un anillo bicíclico de ocho a diez miembros, parcialmente insaturado o totalmente insaturado, opcionalmente sustituido, que tiene de cero a cuatro heteroátomos, seleccionados independientemente entre nitrógeno, oxígeno o azufre; con la condición de que se excluya el siguiente compuesto: (2-fenil-quinazolin-4-il)-tiazol-2-il-amina.

5. 发明申请

WO9824804A3 INHIBITORS OF INTERLEUKIN-1 BETA CONVERTING ENZYME 审中-公开
标题翻译： INTERLEUKIN-1 BETA转化酶的抑制剂
公开(公告)号：WO9824804A3
公开(公告)日：1998-09-03
申请号：PCT/US9722355
申请日：1997-12-05
申请人： VERTEX PHARMA , GOLEC JULIAN M C , LAUFFER DAVID J , LIVINGSTON DAVID J , MULLICAN MICHAEL D , NYCE PHILIP L , ROBIDOUX ANDREA L C , WANNAMAKER MARION W
发明人： GOLEC JULIAN M C , LAUFFER DAVID J , LIVINGSTON DAVID J , MULLICAN MICHAEL D , NYCE PHILIP L , ROBIDOUX ANDREA L C , WANNAMAKER MARION W
IPC分类号： A61K38/00 , A61P19/08 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07K5/02 , C07K5/078
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0202
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1beta converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-("IL-1"), apoptosis-, interferon-gamma inducing factor-(IGIF), or interferon-gamma-("IFN-gamma") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-gamma production and methods for treating interleukin-1, apoptosis- and interferon-gamma-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

6. 发明申请

WO2007022384A3 PYRAZINE KINASE INHIBITORS 审中-公开
标题翻译：吡嗪激酶抑制剂
公开(公告)号：WO2007022384A3
公开(公告)日：2007-04-05
申请号：PCT/US2006032191
申请日：2006-08-17
申请人： VERTEX PHARMA , MORTIMORE MICHAEL , GOLEC JULIAN M C
发明人： MORTIMORE MICHAEL , GOLEC JULIAN M C
IPC分类号： C07D403/12 , A61K31/497 , C07D417/12
CPC分类号： C07D241/18 , C07D403/12 , C07D417/12
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 inventions .
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。本发明还提供了制备本发明化合物的方法。

7. 发明申请

WO9722619A3 INHIBITORS OF INTERLEUKIN-1 BETA CONVERTING ENZYME 审中-公开
标题翻译： INTERLEUKIN-1 BETA转化酶的抑制剂
公开(公告)号：WO9722619A3
公开(公告)日：1997-10-16
申请号：PCT/US9620843
申请日：1996-12-20
申请人： VERTEX PHARMA
发明人： BATCHELOR MARK J , BEBBINGTON DAVID , BEMIS GUY W , FRIDMAN WOLF HERMAN , GILLESPIE ROGER J , GOLEC JULIAN M C , GU YONG , LAUFFER DAVID J , LIVINGSTON DAVID J , MATHARU SAROOP S , MULLICAN MICHAEL D , MURCKO MARK A , MURDOCH ROBERT , NYCE PHILIP L , ROBIDOUX ANDREA L C , SU MICHAEL , WANNAMAKER M WOODS , WILSON KEITH P , ZELLE ROBERT E
IPC分类号： C07D243/12 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/675 , A61K38/00 , A61K38/04 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55 , A61P13/12 , A61P19/08 , A61P19/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D243/10 , C07D243/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00 , C07F9/645 , C07F9/6561 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/078 , C07K5/097 , A61K38/08
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1² converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physiochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-³-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF-, and IFN-³-mediated diseases and decreasing IGIF, and IFN-³ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

8. 发明专利

DE602006020293D1 3,5-DISUBSTITUIERTE PYRID-2-ONE, DIE ALS HEMMER DER TEC-FAMILIE VON NICHT-REZEPTOR TYROSIN-KINASEN NÜTZLICH SIND 未知
公开(公告)号：DE602006020293D1
公开(公告)日：2011-04-07
申请号：DE602006020293
申请日：2006-08-25
申请人： VERTEX PHARMA
发明人： CHARRIER JEAN-DAMIEN , RAMAYA SHARN , DURRANT STEVEN , JIMENEZ JUAN-MIGUEL , GOLEC JULIAN M C , MORTIMORE MICHAEL
IPC分类号： C07D401/14 , A61K31/444 , A61P35/00 , A61P37/00 , C07D213/64 , C07D401/04

9. 发明专利

SK287422B6 Inhibitors of interleukin-1 beta converting enzyme, pharmaceutical composition containing the same and use thereof 未知
公开(公告)号：SK287422B6
公开(公告)日：2010-09-07
申请号：SK160996
申请日：1995-06-16
申请人： VERTEX PHARMA
发明人： BEMIS GUY W , GOLEC JULIAN M C , LAUFFER DAVID J , MULLICAN MICHAEL D , MURCKO MARK A , LIVINGSTON DAVID J
IPC分类号： C07D263/24 , A61K31/42 , C07K5/00 , A61K31/421 , A61K38/00 , A61K45/00 , A61P25/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07C229/22 , C07C233/41 , C07C233/83 , C07C311/30 , C07C317/26 , C07D521/00 , C07K5/02 , C07K5/023 , C07K5/04
摘要： The present invention relates to inhibitors of interleukin-1 beta converting enzyme of general formula alpha, pharmaceutical composition containing the same, and the use thereof for the preparation of a medicament for the treatment or prophylaxis of interleukin-1 mediated diseases, including autoimmune diseases, inflammatory diseases or neurodegenerative diseases, for the preparation of a medicament for inhibiting ICE activity, for the preparation of a medicament for promoting lesion and wound healing and for the treatment or prophylaxis of infectious diseases of a subject in need of such treatment or prophylaxis.

10. 发明专利

CA2422377C PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 未知
公开(公告)号：CA2422377C
公开(公告)日：2010-04-13
申请号：CA2422377
申请日：2001-09-14
申请人： VERTEX PHARMA
发明人： GOLEC JULIAN M C , CHARRIER JEAN-DAMIEN , KNEGTEL RONALD , BEBBINGTON DAVID , DAVIES ROBERT , LI PAN
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
摘要： This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII, wherein Z1 is N or C-R9, Z2 is N or CH, and Z3 is N or C-Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substitutents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2', R3 and R9 are as described inthe specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

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