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1. 发明申请

WO1998024805A1 INHIBITORS OF INTERLEUKIN-1'beta' CONVERTING ENZYME 审中-公开
标题翻译： INTERLEUKIN-1转化酶的抑制剂
公开(公告)号：WO1998024805A1
公开(公告)日：1998-06-11
申请号：PCT/US1997022289
申请日：1997-12-05
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GOLEC, Julian, M., C. , LAUFFER, David, J. , LIVINGSTON, David, J. , MULLICAN, Michael, D. , MURCKO, Mark, A. , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , WANNAMAKER, Marion, W.
发明人： VERTEX PHARMACEUTICALS INCORPORATED
IPC分类号： C07K05/023
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 beta 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), interferon- gamma -("IFN- gamma ") mediated diseases, excess dietary alcohol intake diseases, or viral 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.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）），干扰素-γ-（“IFN-γ”）介导的疾病，过度饮食酒精摄入疾病或病毒性疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，细胞凋亡和干扰素-γ-介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

2. 发明申请

WO0157022A2 PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF ERK 审中-公开
标题翻译：作为ERK的抑制剂有用的吡咯类组合物
公开(公告)号：WO0157022A2
公开(公告)日：2001-08-09
申请号：PCT/US0103911
申请日：2001-02-05
申请人： VERTEX PHARMA , GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JANETKA JAMES , MULLICAN MICHAEL , BEMIS GUY , XIE XIAOLING , STRAUB JUDITH , TANG QING , MASHALL ROBERT
发明人： GREEN JEREMY , CAO JINGRONG , HALE MICHAEL , BAKER CHRISTOPHER , MALTAIS FRANCOIS , JANETKA JAMES , MULLICAN MICHAEL , BEMIS GUY , XIE XIAOLING , STRAUB JUDITH , TANG QING , MASHALL ROBERT
IPC分类号： 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
CPC分类号： C07D401/14 , C07D231/38 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04
摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula: (I) where R , Q, and T are described inthe 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.
摘要翻译：本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中R 1-4，Q和T在说明书中描述。该化合物可用于治疗由蛋白激酶抑制剂，特别是诸如癌症，炎症性疾病，再狭窄和心血管疾病等疾病减轻的哺乳动物的疾病状态。

3. 发明申请

WO0102363A3 N-SUBSTITUTED GLYCINE DERIVATIVES 审中-公开
标题翻译： N-取代的甘氨酸衍生物
公开(公告)号：WO0102363A3
公开(公告)日：2001-07-05
申请号：PCT/US0018564
申请日：2000-07-06
申请人： VERTEX PHARMA , LAUFFER DAVID , LEDFORD BRIAN , MULLICAN MICHAEL
发明人： LAUFFER DAVID , LEDFORD BRIAN , MULLICAN MICHAEL
IPC分类号： A61K31/4409 , A61K31/444 , A61K38/22 , A61P9/10 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , C07D213/40 , A61K31/4465
CPC分类号： C07D213/40
摘要： The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
摘要翻译：本发明涉及用于治疗或预防与神经疾病相关的神经元损伤的N-取代甘氨酸衍生物。本发明还提供了包含本发明化合物的组合物和利用这些组合物治疗或预防神经元损伤的方法。

4. 发明申请

WO2004058749A1 BENZISOXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：苄嘧菌衍生物作为蛋白激酶的抑制剂有用
公开(公告)号：WO2004058749A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/039989
申请日：2003-12-17
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDEBOER, Mark , DAVIES, Robert, J. , MESSERSMITH, David , MOON, Young-Choon , MULLICAN, Michael, D.
发明人： LEDEBOER, Mark , DAVIES, Robert, J. , MESSERSMITH, David , MOON, Young-Choon , MULLICAN, Michael, D.
IPC分类号： C07D413/14
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3, JAK-3, FLT-3, PIM-1, SYK, or PDK-1 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐。这些化合物是蛋白激酶的抑制剂，特别是GSK-3，JAK-3，FLT-3，PIM-1，SYK或PDK-1哺乳动物蛋白激酶的抑制剂。本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

5. 发明申请

WO2002098876A1 CAK INHIBITORS AND USES THEREOF 审中-公开
标题翻译： CAK抑制剂及其用途
公开(公告)号：WO2002098876A1
公开(公告)日：2002-12-12
申请号：PCT/US2002/018102
申请日：2002-06-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDFORD, Brian , MOODY, Cameron, Stuver , MULLICAN, Michael , NAMCHUK, Mark
发明人： LEDFORD, Brian , MOODY, Cameron, Stuver , MULLICAN, Michael , NAMCHUK, Mark
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/437
摘要： The present invention provides a method of inhibiting CAK comprising the step of contacting said CAK with a compound of formula I wherein X is N or = C; Y is= C when X is N; Y is N when X is =C; ring A, taken together with X, is a 5-7 membered monocyclic carbocyclic or heterocyclic aromatic or non-aromatic ring; one of Z 1 and Z 3 is selected from -CN, -N 3 , acetenyl or cyclopropyl, and the other of Z 1 and Z 3 is wherein n is 0 or 1; W is O or S; V is -NH-; ar is a 5-10 membered monocyclic or bicyclic aromatic carbocyclic or aromatic heterocyclic ring; Z 2 is NHR 1 ; wherein R 1 is H or C1-C6 straight or branched alkyl. The present invention also provides compounds useful in inhibiting CAK, and compositions comprising said compound and a pharmaceutically acceptable carrier. The rpesent invention also provides methods of treating CAK-mediated diseases and fungal infections.
摘要翻译：本发明提供一种抑制CAK的方法，包括使所述CAK与式I化合物接触的步骤，其中X为N或= C; 当X为N时，Y为= C; 当X = C时，Y为N; 环A与X一起是5-7元单环碳环或杂环芳族或非芳香环; Z 1和Z 3中的一个选自-CN，-N 3，炔基或环丙基，Z 1和Z 3中的另一个是其中n是0或1; W为O或S; V是-NH-; ar是5-10元单环或双环芳族碳环或芳族杂环; Z 2是NHR 1; 其中R 1是H或C 1 -C 6直链或支链烷基。本发明还提供了可用于抑制CAK的化合物和包含所述化合物和药学上可接受的载体的组合物。本发明还提供了治疗CAK介导的疾病和真菌感染的方法。

6. 发明申请

WO0158891A3 Piperazine and piperidine derivatives for treatment or prevention of neuronal damage 审中-公开
标题翻译：哌嗪和哌啶衍生物用于治疗或预防神经元损伤
公开(公告)号：WO0158891A3
公开(公告)日：2002-04-25
申请号：PCT/US0104210
申请日：2001-02-09
申请人： TOMLINSON RONALD , LAUFFER DAVID , MULLICAN MICHAEL , VERTEX PHARMA
发明人： TOMLINSON RONALD , LAUFFER DAVID , MULLICAN MICHAEL
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4995 , A61K31/506 , A61K38/22 , A61K38/27 , A61P19/04 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , C07D20060101 , C07D205/04 , C07D207/16 , C07D209/52 , C07D211/26 , C07D211/60 , C07D211/62 , C07D211/78 , C07D277/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/06 , C07D417/12 , C07D487/08
CPC分类号： C07D401/04 , C07D205/04 , C07D207/16 , C07D211/60 , C07D211/62 , C07D277/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D487/08
摘要： The present invention relates to piperazine and piperidine derivatives of Formula (1), with Q, X, Y, A, B and P as defined herein, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

7. 发明申请

WO0102358A3 CYCLIZED AMIDE DERIVATIVES FOR TREATING OR PREVENTING NEURONAL DAMAGE 审中-公开
标题翻译：用于治疗或预防神经损伤的循环酰胺衍生物
公开(公告)号：WO0102358A3
公开(公告)日：2001-07-12
申请号：PCT/US0018418
申请日：2000-07-05
申请人： VERTEX PHARMA , LAUFFER DAVID , MULLICAN MICHAEL , LEDFORD BRIAN
发明人： LAUFFER DAVID , MULLICAN MICHAEL , LEDFORD BRIAN
IPC分类号： C07D243/12 , A61K31/4015 , A61K31/45 , A61K31/4545 , A61K31/55 , A61K31/5513 , A61K38/27 , A61P19/08 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D211/76 , C07D223/12 , C07D223/16 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/14 , A61K31/554 , C07D211/72 , C07D413/14 , C07D417/14
CPC分类号： C07D207/273 , C07D211/76 , C07D223/16 , C07D243/24 , C07D401/14
摘要： The present invention relates to cyclized amide derivatives of formula (I) for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
摘要翻译：本发明涉及用于治疗或预防与神经疾病相关的神经元损伤的式（I）的环化酰胺衍生物。本发明还提供包含本发明化合物的组合物和利用这些组合物治疗或预防神经元损伤的方法。

8. 发明申请

WO9947545A3 INHIBITORS OF CASPASES 审中-公开
标题翻译： CASPASES的抑制剂
公开(公告)号：WO9947545A3
公开(公告)日：1999-11-25
申请号：PCT/US9905919
申请日：1999-03-19
申请人： VERTEX PHARMA , WANNAMAKER MARION W , BEMIS GUY W , CHARIFSON PAUL S , LAUFFER DAVID J , MULLICAN MICHAEL D , MURCKO MARK A , WILSON KEITH P , JANETKA JAMES W , DAVIES ROBERT J , GRILLOT ANNE LAURE , SHI ZHAN , FORSTER CORNELIA J
发明人： WANNAMAKER MARION W , BEMIS GUY W , CHARIFSON PAUL S , LAUFFER DAVID J , MULLICAN MICHAEL D , MURCKO MARK A , WILSON KEITH P , JANETKA JAMES W , DAVIES ROBERT J , GRILLOT ANNE-LAURE , SHI ZHAN , FORSTER CORNELIA J
IPC分类号： C07D207/273 , A61K31/47 , A61K38/00 , A61K38/03 , A61K38/04 , A61P5/48 , A61P7/00 , A61P9/00 , A61P17/00 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D401/12 , C07K5/02 , C07K5/023
CPC分类号： C07K5/0202 , A61K38/00 , C07D401/12
摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1 beta converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase 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 caspase 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.
摘要翻译：本发明涉及新型的化合物，它们是半胱天冬酶抑制剂，特别是白细胞介素-1β转化酶（“ICE”）抑制剂。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制半胱天冬酶活性，因此可以有利地用作抗白细胞介素-1（“IL-1”），细胞凋亡 - ，干扰素-γ诱导因子 - （IGIF），或干扰素-γ-（“IFN-γ”）介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及抑制半胱天冬酶活性并降低IGIF产生和IFN-γ产生的方法以及使用本发明的化合物和组合物治疗白细胞介素-1，细胞凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

9. 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.

10. 发明申请

WO1998024804A2 INHIBITORS OF INTERLEUKIN-1'beta' CONVERTING ENZYME 审中-公开
标题翻译： INTERLEUKIN-1转化酶的抑制剂
公开(公告)号：WO1998024804A2
公开(公告)日：1998-06-11
申请号：PCT/US1997022355
申请日：1997-12-05
申请人： VERTEX PHARMACEUTICALS INCORPORATED , 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： VERTEX PHARMACEUTICALS INCORPORATED
IPC分类号： C07K05/02
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 beta 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.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF），或干扰素-γ-（“IFN-γ”）介导的疾病，包括炎性疾病，自身免疫疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，细胞凋亡和干扰素-γ-介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

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