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公开(公告)号：US07872129B2
公开(公告)日：2011-01-18
申请号：US12338129
申请日：2008-12-18
IPC分类号： C07D403/12 , C07D403/14 , C07D417/14 , A61K31/4162 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P9/10 , A61P25/18
CPC分类号： C07D403/12 , C07D471/04
摘要： The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. 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衍生物。 这些化合物是蛋白激酶的抑制剂，特别是GSK3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以及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。
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公开(公告)号：US07109357B2
公开(公告)日：2006-09-19
申请号：US10229981
申请日：2002-08-28
IPC分类号： C07D307/56
CPC分类号： C07D307/33 , C07D307/66 , C07F9/65515
摘要： Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P2—P4 moiety of a caspase inhibitor. Key intermediates include the azidolactones III and VIII:
摘要翻译： 本文公开了一种制备可用作式I的半胱天冬酶抑制剂前药的化合物的方法：其中R 1是选自脂族基团，芳烷基，杂环基烷基或芳基的任选取代的基团，和 R 2优选是半胱天冬酶抑制剂的P 2 -P 4 N 4个部分。 主要中间体包括叠氮内酯III和VIII：
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公开(公告)号：US06531474B1
公开(公告)日：2003-03-11
申请号：US09665503
申请日：2000-09-19
申请人： Marion W. Wannamaker , Guy W. Bemis , Paul S. Charifson , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , Keith P. Wilson , James W. Janetka , Robert J. Davies , Anne-Laure Grillot , Zhan Shi , Cornelia J. Forster
发明人： Marion W. Wannamaker , Guy W. Bemis , Paul S. Charifson , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , Keith P. Wilson , James W. Janetka , Robert J. Davies , Anne-Laure Grillot , Zhan Shi , Cornelia J. Forster
IPC分类号： C07D20724
CPC分类号： C07K5/0202 , A61K38/00 , C07D401/12 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; 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-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) 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-&ggr; production and methods for treating interleukin-1, apoptosis-, and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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公开(公告)号：US20110301096A1
公开(公告)日：2011-12-08
申请号：US13210712
申请日：2011-08-16
IPC分类号： A61K38/55 , C07D207/16 , A61P43/00
CPC分类号： C07K5/06034 , A61K38/00 , C07D207/16 , C07D307/02 , C07D477/02 , C07D477/20 , C07K5/0202 , C07K5/0205 , C07K5/06 , C07K5/06008 , C07K5/06191 , C07K5/08 , C07K5/0808 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
摘要翻译： 本发明描述了具有良好生物利用度的ICE抑制剂前药（I）。 化合物I可用于治疗IL-1介导的疾病，例如类风湿性关节炎，炎性肠病，克罗恩病，溃疡性结肠炎，炎性腹膜炎，败血性休克，胰腺炎，创伤性脑损伤，器官移植排斥，骨关节炎，哮喘，银屑病，阿尔茨海默病 心肌梗死，充血性心力衰竭，亨廷顿病，动脉粥样硬化，特应性皮炎，白血病和相关疾病，骨髓增生异常综合征，葡萄膜炎或多发性骨髓瘤。
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公开(公告)号：US20090118278A1
公开(公告)日：2009-05-07
申请号：US12338129
申请日：2008-12-18
IPC分类号： A61K31/506 , C07D471/04 , A61P37/00 , A61P25/00 , A61P3/10 , A61P29/00 , A61K31/5377
CPC分类号： C07D403/12 , C07D471/04
摘要： The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. 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衍生物。 这些化合物是蛋白激酶的抑制剂，特别是GSK3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。
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6.发明授权Azadecalin amides and thioamides as inhibitors of cholesterol biosynthesis 失效十八烷酰胺和硫代酰胺作为胆固醇生物合成的抑制剂
公开(公告)号：US5278171A
公开(公告)日：1994-01-11
申请号：US776143
申请日：1991-10-15
IPC分类号： A61K31/47 , A61K31/472 , A61P3/06 , A61P31/04 , A61P31/10 , C07D217/06 , C07D217/04
CPC分类号： C07D217/06
摘要： The present invention provides certain novel azadecalin amides and thioamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
摘要翻译： 本发明提供了一些可用作胆固醇生物合成抑制剂的新型十八烷酰胺和硫代酰胺，以及降低有需要的患者的总血清胆固醇的试剂。
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7.发明授权Azadecalin amides and thioamides as inhibitors of cholesterol biosynthesis 失效十八烷酰胺和硫代酰胺作为胆固醇生物合成的抑制剂
公开(公告)号：US5084461A
公开(公告)日：1992-01-28
申请号：US676149
申请日：1991-03-27
IPC分类号： A61K31/47 , A61K31/472 , A61P3/06 , A61P31/04 , A61P31/10 , C07D217/06
CPC分类号： C07D217/06
摘要： The present invention provides certain novel azadecalin amides and thioamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
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公开(公告)号：US08686143B2
公开(公告)日：2014-04-01
申请号：US13280670
申请日：2011-10-25
申请人： Marion W. Wannamaker , Francesco Salituro , Albert Pierce , Alex Aronov , Gabriel Martinez-Botella , Jian Wang , Luc Farmer , Mark Ledeboer , Tiansheng Wang , Randy Bethiel , Brian Ledford , Emilie Porter Huck
发明人： Marion W. Wannamaker , Francesco Salituro , Albert Pierce , Alex Aronov , Gabriel Martinez-Botella , Jian Wang , Luc Farmer , Mark Ledeboer , Tiansheng Wang , Randy Bethiel , Brian Ledford , Emilie Porter Huck
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14 , C07D213/74 , C07D239/42 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family 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.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂，特别是JAK家族激酶的化合物。 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。
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公开(公告)号：US08329662B2
公开(公告)日：2012-12-11
申请号：US13210712
申请日：2011-08-16
IPC分类号： A61K38/05
CPC分类号： C07K5/06034 , A61K38/00 , C07D207/16 , C07D307/02 , C07D477/02 , C07D477/20 , C07K5/0202 , C07K5/0205 , C07K5/06 , C07K5/06008 , C07K5/06191 , C07K5/08 , C07K5/0808 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
摘要翻译： 本发明描述了具有良好生物利用度的ICE抑制剂前药（I）。 化合物I可用于治疗IL-1介导的疾病，例如类风湿性关节炎，炎性肠病，克罗恩病，溃疡性结肠炎，炎性腹膜炎，败血性休克，胰腺炎，创伤性脑损伤，器官移植排斥，骨关节炎，哮喘，银屑病，阿尔茨海默病 心肌梗死，充血性心力衰竭，亨廷顿病，动脉粥样硬化，特应性皮炎，白血病和相关疾病，骨髓增生异常综合征，葡萄膜炎或多发性骨髓瘤。
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公开(公告)号：US08022041B2
公开(公告)日：2011-09-20
申请号：US12165838
申请日：2008-07-01
IPC分类号： C07K5/06
CPC分类号： C07K5/06034 , A61K38/00 , C07D207/16 , C07D307/02 , C07D477/02 , C07D477/20 , C07K5/0202 , C07K5/0205 , C07K5/06 , C07K5/06008 , C07K5/06191 , C07K5/08 , C07K5/0808 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
摘要翻译： 本发明描述了具有良好生物利用度的ICE抑制剂前药（I）。 化合物I可用于治疗IL-1介导的疾病，例如类风湿性关节炎，炎性肠病，克罗恩病，溃疡性结肠炎，炎性腹膜炎，败血性休克，胰腺炎，创伤性脑损伤，器官移植排斥，骨关节炎，哮喘，银屑病，阿尔茨海默病 心肌梗死，充血性心力衰竭，亨廷顿病，动脉粥样硬化，特应性皮炎，白血病和相关疾病，骨髓增生异常综合征，葡萄膜炎或多发性骨髓瘤。
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