-
公开(公告)号：US07790713B2
公开(公告)日：2010-09-07
申请号：US11655938
申请日：2007-01-18
申请人： Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L. C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
发明人： Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L. C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
IPC分类号： C07D243/12 , A61K31/55 , A61P29/00
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-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical 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-γ-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-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing-N-acylamino compounds.
摘要翻译： 本发明涉及作为白介素-1和bgr的抑制剂的新型化合物。 转化酶。 本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。 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IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，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，退行性疾病和坏死性疾病。 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，用于治疗白细胞介素-1，细胞凋亡，IGIF和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。 本发明还涉及N-酰基氨基化合物的制备方法。
-
公开(公告)号：US07691853B2
公开(公告)日：2010-04-06
申请号：US11369220
申请日：2006-03-06
申请人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M. C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert J. Davies , Pan Li , Marion W. Wannamaker , Cornelia J. Forster , Albert C. Pierce
发明人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M. C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert J. Davies , Pan Li , Marion W. Wannamaker , Cornelia J. Forster , Albert C. Pierce
IPC分类号： C07D403/12 , C07D239/94 , A61K31/517 , A61K31/506 , A61P25/18 , A61P25/28
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 , C07D491/10 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the 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.
摘要翻译： 本发明描述了式IV的新型吡唑化合物：其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R x和R y独立地选自T-R 3，或与它们的插入原子一起形成具有1-3个选自氧，硫或氮的环杂原子的稠合的，不饱和的或部分不饱和的5-8元环; R2，R2'，T和R3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
-
公开(公告)号：US20090312543A1
公开(公告)日：2009-12-17
申请号：US12545347
申请日：2009-08-21
IPC分类号： C07D401/12 , C07D413/14
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , 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 pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the 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.
摘要翻译： 本发明描述了式IIIa的新型吡唑化合物：其中R1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; Rx，Ry，R2和R2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。
-
34.发明授权公开(公告)号：US07008948B2
公开(公告)日：2006-03-07
申请号：US10624800
申请日：2003-07-22
申请人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
发明人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P5/48 , A61P35/00
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 , C07D491/10 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the 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.
摘要翻译： 本发明描述了式IV的新型吡唑化合物：其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R“x”和“R”独立地选自TR 3，或者与它们的插入原子一起形成稠合的，不饱和的或部分不饱和的， 具有1-3个选自氧，硫或氮的环杂原子的5-8元环; 和R 2，R 2，R 3和R 3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
-
公开(公告)号：US06787541B1
公开(公告)日：2004-09-07
申请号：US09958948
申请日：2002-03-13
申请人： Roger John Gillespie , Joanne Lerpiniere , Paul Richard Giles , Claire Elizabeth Dawson , David Bebbington
发明人： Roger John Gillespie , Joanne Lerpiniere , Paul Richard Giles , Claire Elizabeth Dawson , David Bebbington
IPC分类号： C07D49504
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of formula (I): wherein X is S. Compounds can be used for treating a disorder in which the blocking of purine receptors is beneficial.
摘要翻译： 式（I）化合物：其中X为S.化合物可用于治疗嘌呤受体阻断有益的病症。
-
公开(公告)号：US06727251B2
公开(公告)日：2004-04-27
申请号：US10034019
申请日：2001-12-20
IPC分类号： A61K3153
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , 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 pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Ry, R2, and R2′ are as described in the 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.
摘要翻译： 本发明描述了式II的新型吡唑化合物：其中Z 1是氮或CR 8; Q是-S-，-O-，-N（R 4） - 或-CH（R 6） - ; R 1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; 和R y，R 2和R 2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。
-
公开(公告)号：US06638926B2
公开(公告)日：2003-10-28
申请号：US09953505
申请日：2001-09-14
IPC分类号： C07D40312
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 provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as cancer, diabetes and Alzheimer's disease. The compounds are represented by formula VI: wherein 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 —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Ry is T—R3′; T is a valence bond or a C1-4 alkylidene chain; R3′ is an optionally substituted group selected from C1-6 aliphatic, C3-10 carbocyclyl, C6-10 aryl, a heteroaryl ring having 5-10 ring atoms, or a heterocyclyl ring having 5-10 ring atoms; and R1, R2, and R2′ are as described in the specification.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新型吡唑化合物，特别是作为极光-2和GSK-3的抑制剂。 该化合物可用于治疗导致癌症，糖尿病和阿尔茨海默病等疾病的异常生理功能。 化合物由式VI表示：其中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，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 y是T-R 3; T是价键或C 1-4亚烷基链; R 3是任选取代的基团，其选自C 1-6脂族基，C 3-10碳环基，C 6-10芳基，具有5-10个环原子的杂芳基环，或具有5-10个环原子的杂环基环; 和R 1，R 2和R 2'如说明书中所述。
-
公开(公告)号：US06613776B2
公开(公告)日：2003-09-02
申请号：US09952836
申请日：2001-09-14
申请人： Ronald Knegtel , David Bebbington , Hayley Binch , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
发明人： Ronald Knegtel , David Bebbington , Hayley Binch , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
IPC分类号： C07D40112
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 pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 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 —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T are as described in the 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.
摘要翻译： 本发明描述了包含药学上可接受的载体和式V化合物的新型吡唑组合物：其中Z1是N，CRa或CH，Z2是N或CH，其中Z1和Z2之一是氮; 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，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; Rx和Ry独立地选自T-R3，或Rx和Ry与它们的插入原子一起形成稠环; R1，R2，R2'，R3和T如说明书所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
-
公开(公告)号：US07982037B2
公开(公告)日：2011-07-19
申请号：US12545347
申请日：2009-08-21
IPC分类号： C07D403/12
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , 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 pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the 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.
摘要翻译： 本发明描述了式IIIa的新型吡唑化合物：其中R1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; Rx，Ry，R2和R2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。
-
公开(公告)号：US07625913B2
公开(公告)日：2009-12-01
申请号：US10026992
申请日：2001-12-19
IPC分类号： C07D403/12 , A61K31/506
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , 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 pyrazole compounds of formula IIIc: wherein R1 is T—Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the 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.
摘要翻译： 本发明描述了式IIIc的新型吡唑化合物：其中R1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; Rx，Ry，R2和R2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。
-
-
-
-
-
-
-
-
-
搜索结果
58 条记录 (耗时 0.07 秒)
