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1. 发明申请

WO2007056468A1 METHODS FOR INHIBITING PROTEIN KINASES 审中-公开
标题翻译：抑制蛋白激酶的方法
公开(公告)号：WO2007056468A1
公开(公告)日：2007-05-18
申请号：PCT/US2006/043512
申请日：2006-11-08
申请人： SCHERING CORPORATION , GUZI, Timothy J. , PARUCH, Kamil , DWYER, Michael P. , PARRY, David, A. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, Adulla, P. , SIDDIQUI, M. Arshad , TADIKONDA, Praveen, K.
发明人： GUZI, Timothy J. , PARUCH, Kamil , DWYER, Michael P. , PARRY, David, A. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, Adulla, P. , SIDDIQUI, M. Arshad , TADIKONDA, Praveen, K.
IPC分类号： A61K31/4985 , A61P35/00
CPC分类号： A61K31/4985 , A61K31/498
摘要： The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
摘要翻译：本发明提供使用咪唑并[1,2-a]吡嗪化合物抑制选自AKT，检查点激酶，极光激酶，Pim-1激酶和酪氨酸激酶的蛋白激酶的方法，以及治疗，预防，抑制，或使用这些化合物改善与蛋白激酶相关的一种或多种疾病。

2. 发明申请

WO2008057512A3 IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2008057512A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/023329
申请日：2007-11-06
申请人： SCHERING CORPORATION , BELANGER, David, B. , SIDDIQUI, M. Arshad , GUZI, Timothy, J. , CURRAN, Patrick, J. , TADIKONDA, Praveen, K. , HAMANN, Blake , REDDY, Panduranga, Adulla P. , ZHAO, Lianyun
发明人： BELANGER, David, B. , SIDDIQUI, M. Arshad , GUZI, Timothy, J. , CURRAN, Patrick, J. , TADIKONDA, Praveen, K. , HAMANN, Blake , REDDY, Panduranga, Adulla P. , ZHAO, Lianyun
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
摘要： In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds of following formula (1) as inhibitors of protein and/or Aurora kinases. methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions, such as cancer and leukemia.

3. 发明申请

WO2008082487A2 NOVEL JNK INHIBITORS 审中-公开
标题翻译：诺维奇抑制剂
公开(公告)号：WO2008082487A2
公开(公告)日：2008-07-10
申请号：PCT/US2007/025764
申请日：2007-12-17
申请人： SCHERING CORPORATION , BELANGER, David, B. , SIDDIQUI, M. Arshad , CURRAN, Patrick J. , HAMANN, Blake , ZHAO, Lianyun , REDDY, Panduranga, Adulla, P. , TADIKONDA, Praveen, K. , SHIPPS, Gerald W., Jr. , MANSOOR, Umar, Faruk
发明人： BELANGER, David, B. , SIDDIQUI, M. Arshad , CURRAN, Patrick J. , HAMANN, Blake , ZHAO, Lianyun , REDDY, Panduranga, Adulla, P. , TADIKONDA, Praveen, K. , SHIPPS, Gerald W., Jr. , MANSOOR, Umar, Faruk
IPC分类号： C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/44 , A61P29/00
CPC分类号： C07D417/12 , C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR 5 . Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
摘要翻译：公开了式（I）的化合物，其中X是N或CH，Y是N或CR 5。还公开了使用式1.0化合物治疗JNK和ERK介导的疾病的方法。

4. 发明申请

WO2008045266A2 NOVEL PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：新型吡唑并嘧啶类作为周期蛋白依赖性激酶抑制剂
公开(公告)号：WO2008045266A2
公开(公告)日：2008-04-17
申请号：PCT/US2007/021273
申请日：2007-10-02
申请人： SCHERING CORPORATION , GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , SIDDIQUI, M., Arshad , REDDY, Panduranga, Adulla, P. , BELANGER, David, B. , HAMANN, Blake , CURRAN, Patrick, J.
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , SIDDIQUI, M., Arshad , REDDY, Panduranga, Adulla, P. , BELANGER, David, B. , HAMANN, Blake , CURRAN, Patrick, J.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类作为细胞周期蛋白依赖性激酶（CDK）抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这类化合物的方法，含有一种或更多此类化合物，制备包含一种或多种此类化合物的药物制剂的方法以及使用此类化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

5. 发明申请

WO2007058942A3 IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2007058942A3
公开(公告)日：2007-05-24
申请号：PCT/US2006/043786
申请日：2006-11-08
申请人： SCHERING CORPORATION , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, A. , PARUCH, Kamil , GUZI, Timothy. J. , DWYER, Michael, P. , SIDDIQUI, M., Arshad , TADIKONDA, Praveen, K.
发明人： ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, A. , PARUCH, Kamil , GUZI, Timothy. J. , DWYER, Michael, P. , SIDDIQUI, M., Arshad , TADIKONDA, Praveen, K.
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00
摘要： In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

6. 发明申请

WO2007058873A2 NOVEL IMIDAZOPYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：新型咪达唑仑作为循环依赖性激酶抑制剂
公开(公告)号：WO2007058873A2
公开(公告)日：2007-05-24
申请号：PCT/US2006/043592
申请日：2006-11-08
申请人： SCHERING CORPORATION , GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, A. , SIDDIQUI, Arshad, M.
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, A. , SIDDIQUI, Arshad, M.
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡嗪化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

7. 发明申请

WO2003033010A1 CYCLOSPORIN ANALOGS FOR THE TREATMENT OF AUTOIMMUNE DISEASES 审中-公开
标题翻译：用于治疗自身免疫性疾病的环磷酰胺类似物
公开(公告)号：WO2003033010A1
公开(公告)日：2003-04-24
申请号：PCT/US2002/032118
申请日：2002-10-11
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake , CHEN, Jason
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake , CHEN, Jason
IPC分类号： A61K38/00
CPC分类号： C07K7/645 , Y10S514/828
摘要： The present invention relates to a cyclosporin analog of the following , formula (I) or a pro-drug or pharmaceutically acceptable salt thereof: Formula (I). In particular, residue A maybe represented by either formula A1 or A2 as illustrated below: Formulas (A1) or (A2) where X is absent, -C1-C6-alkyl- or -C3-C6-cycloalkyl-; Y is selected from the groups: aryl, substituted aryl, heteroaryl, and substituted heteroaryl; residue B is - aAbu-, -Val-, -Thr- or -Nva-; and residue U is -(D)Ala-, -(D)Ser-, -[0-(2- hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- or -[0-(2-acyloxyethyl)(D)Ser]-. In a second embodiment, the present invention relates to the use of the cyclosporin analogs of the present invention or a pro-drug or pharmaceutically acceptable salt 20 thereof in pharmaceutical compositions for the treatment of autoimmune diseases or for the prevention of organ transplantation rejection in a subject. In a third embodiment, the present invention relates to processes for the production of novel cyclosporin analogs of the present invention. The present invention also contemplates method(s) of treatment of autoimmune diseases or prevention of 25 organ transplant rejection in a subject by administering to the subject therapeutically effective amounts of the cyclosporin analogs of the present invention with or without the concurrent use of other drugs or pharmaceutically acceptable carriers or excipients.
摘要翻译：本发明涉及以下的式（I）的环孢菌素类似物或其前药或其药学上可接受的盐：式（I）。特别地，残基A可以由式A1或A2表示，如下所示：式（A1）或（A2）其中X不存在，-C 1 -C 6 - 烷基 - 或-C 3 -C 6 - 环烷基 - ; Y选自芳基，取代的芳基，杂芳基和取代的杂芳基; 残基B是-aAbu-，-Val-，-Thr-或-Nva-; 并且残基U是 - （D）Ala-， - （D）Ser-， - [O-（2-羟乙基）（D）Ser] - ， - [O-酰基（D）Ser] - 或 - （2-酰氧基乙基）（D）丝氨酸] - 。在第二个实施方案中，本发明涉及本发明的环孢菌素类似物或其前药或其药学上可接受的盐20在药物组合物中用于治疗自身免疫疾病或用于预防器官移植排斥反应的用途学科。在第三个实施方案中，本发明涉及用于生产本发明的新型环孢菌素类似物的方法。本发明还考虑了通过给予本发明治疗有效量的本发明的环孢菌素类似物来治疗自身免疫疾病或预防受试者的器官移植排斥反应的方法，所述方法在或不同时使用其它药物或药学上可接受的载体或赋形剂。

8. 发明公开

EP2069348A2 NOVEL PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权转让
标题翻译：吡唑并嘧啶新型AS细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP2069348A2
公开(公告)日：2009-06-17
申请号：EP07839217.2
申请日：2007-10-02
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , SIDDIQUI, M., Arshad , REDDY, Panduranga, Adulla, P. , BELANGER, David, B. , HAMANN, Blake , CURRAN, Patrick, J.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

9. 发明公开

EP1945216A1 METHODS FOR INHIBITING PROTEIN KINASES 审中-公开
标题翻译：用于抑制蛋白激酶
公开(公告)号：EP1945216A1
公开(公告)日：2008-07-23
申请号：EP06827636.9
申请日：2006-11-08
申请人： Schering Corporation
发明人： GUZI, Timothy J. , PARUCH, Kamil , DWYER, Michael P. , PARRY, David, A. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, Adulla, P. , SIDDIQUI, M. Arshad , TADIKONDA, Praveen, K.
IPC分类号： A61K31/4985 , A61P35/00
CPC分类号： A61K31/4985 , A61K31/498
摘要： The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.

10. 发明公开

EP1945643A2 IMIDAZOPYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：咪唑并吡嗪AS细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP1945643A2
公开(公告)日：2008-07-23
申请号：EP06837219.2
申请日：2006-11-08
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , ZHAO, Lianyun , CURRAN, Patrick, J. , BELANGER, David, B. , HAMANN, Blake , REDDY, Panduranga, A. , SIDDIQUI, Arshad, M.
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

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