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1. 发明专利

JP2010215675A Pyrazolopyrimidine derivative as cyclin dependent kinase inhibitor 审中-公开
标题翻译：作为CYCLIN依赖性激酶抑制剂的吡唑并嘧啶衍生物
公开(公告)号：JP2010215675A
公开(公告)日：2010-09-30
申请号：JP2010157338
申请日：2010-07-09
申请人： Pharmacopeia Drug Discovery Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコペイアドラッグディスカバリー, インコーポレイテッド
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL , MALLAMS ALAN , ALVAREZ CARMEN S , KEERTIKAR KARTIK M , RIVERA JOCELYN , CHAN TIN-YAU , MADISON VINCENT , FISCHMANN THIERRY O , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON , PARADKAR VIDYADHAR M , HOBBS DOUGLAS WALSH
IPC分类号： C07D487/04 , A61K31/437 , A61K31/444 , A61K31/495 , A61K31/519 , A61K31/5355 , A61K41/00 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D453/02
CPC分类号： C07D487/04 , A61K31/495
摘要： PROBLEM TO BE SOLVED: To provide cyclin dependent kinase inhibitors. SOLUTION: The invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing one or more kind of 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. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供细胞周期蛋白依赖性激酶抑制剂。解决方案：本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备一种或多种这类化合物的方法，含有一种或多种这类化合物的药物组合物，方法制备包含一种或多种这样的化合物的药物制剂，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。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2010180235A New pyrazolopyrimidine as cyclin-dependent kinase inhibitor 审中-公开
标题翻译：新型吡唑啉酮作为循环激酶激酶抑制剂
公开(公告)号：JP2010180235A
公开(公告)日：2010-08-19
申请号：JP2010088212
申请日：2010-04-06
申请人： Pharmacopeia Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコピア, インコーポレイテッド
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL , ALVAREZ CARMEN S , CHAN TIN-YAU , KNUTSON CHAD , MADISON VINCENT , FISCHMANN THIERRY O , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/00 , A61P1/04 , A61P1/16 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/02 , A61P13/08 , A61P13/12 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/08 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/10 , A61P31/12 , A61P31/14 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D519/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a compound useful for treating, preventing or ameliorating a disease or disorder associated with a CDK. SOLUTION: A novel class of a pyrazolo[1,5-α]pyrimidine compound as an inhibitor of a cyclin-dependent kinase is provided in its many embodiments. A pharmacologically acceptable salt or solvate of the compound, a method for preparing such a compound, a method for preparing a pharmacological composition comprising one or more such compounds, and a method for treating, preventing, inhibiting or restoring from one or more diseases associated with a CDK using such a compound or such a pharmacological composition are also provided. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用于治疗，预防或改善与CDK相关的疾病或病症的化合物。解决方案：在许多实施方案中提供了一类新颖的作为细胞周期蛋白依赖性激酶抑制剂的吡唑并[1,5-α]嘧啶化合物。化合物的药理学上可接受的盐或溶剂合物，制备这种化合物的方法，制备包含一种或多种这样的化合物的药物组合物的方法，以及用于治疗，预防，抑制或恢复与一种或多种与还提供了使用这种化合物或这种药物组合物的CDK。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2012082233A Pyrazolopyrimidine as protein kinase inhibitor 审中-公开
标题翻译：作为蛋白激酶抑制剂的吡唑并嘧啶
公开(公告)号：JP2012082233A
公开(公告)日：2012-04-26
申请号：JP2012015794
申请日：2012-01-27
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： PARUCH KAMIL , GUZI TIMOTHY J , DWYER MICHAEL P , ALVAREZ CARMEN S
IPC分类号： C07D487/04 , A61K31/519 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide effective inhibitors of protein kinases in order to treat or prevent disease states associated with abnormal cell proliferation.SOLUTION: In its many embodiments, the present invention provides a novel class of amino- substituted pyrazolo[1,5-a] pyrimidine compounds represented by the structural formula (I) 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.
摘要翻译：要解决的问题：提供蛋白激酶的有效抑制剂，以治疗或预防与异常细胞增殖相关的疾病状态。解决方案：在其许多实施方案中，本发明提供了由结构式（I）表示的氨基取代的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检测点激酶的抑制剂的新类型，方法制备这些化合物的药物组合物，包括一种或多种这样的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，以及使用以下方法治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法：这样的化合物或药物组合物。版权所有（C）2012，JPO＆INPIT

4. 发明专利

JP2010168406A Pyrazolopyrimidine as cyclin dependent kinase inhibitor 审中-公开
标题翻译：作为CYCLIN依赖性激酶抑制剂的吡唑并嘧啶
公开(公告)号：JP2010168406A
公开(公告)日：2010-08-05
申请号：JP2010112695
申请日：2010-05-14
申请人： Pharmacopeia Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコピアインコーポレーテッドPharmacopeia, Inc
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON
IPC分类号： C07D487/04 , A61K31/519 , A61K45/00 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： C07D487/04 , A61K31/519 , A61K31/52 , A61K31/704 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide compounds useful for treatment, prevention, or amelioration of diseases and trouble associated with the CDKs.
SOLUTION: The invention provides in its many embodiments, a new class of pyrazolo[1,5-α]pyrimidine 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.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗，预防或改善与CDK有关的疾病和麻烦的化合物。解决方案：本发明在其许多实施方案中提供了一类新的作为细胞周期蛋白依赖性激酶抑制剂的吡唑并[1,5-α]嘧啶化合物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，方法制备包含一种或多种这样的化合物的药物制剂，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。版权所有（C）2010，JPO＆INPIT

5. 发明专利

JP2010180247A Pyrazolotriazine as kinase inhibitor 审中-公开
标题翻译：吡唑啉酮作为激酶抑制剂
公开(公告)号：JP2010180247A
公开(公告)日：2010-08-19
申请号：JP2010118852
申请日：2010-05-24
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： GUZI TIMOTHY J , PARUCH KAMIL
IPC分类号： C07D487/04 , A61K31/53 , A61K45/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/02 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a compound useful on treating, preventing or ameliorating a disease or disorder associated with a CDK. SOLUTION: A new class of a pyrazolo[1,5-a]triazine compound as an inhibitor of a kinase (for example, a cyclin-dependent kinase) is provided in many embodiments. A method for preparing such a compound, a pharmaceutical composition comprising one or more such compounds, a method for preparing a pharmaceutical compound comprising one or more such compounds, and a method for treating, preventing, inhibiting or ameliorating one or more diseases associated with a kinase using such a compound or such a pharmaceutical formulation are also provided. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用于治疗，预防或改善与CDK相关的疾病或病症的化合物。解决方案：在许多实施方案中提供了一类新的激酶抑制剂（例如，细胞周期蛋白依赖性激酶）的吡唑并[1,5-a]三嗪化合物。一种制备这种化合物的方法，包含一种或多种这样的化合物的药物组合物，包含一种或多种这样的化合物的药物组合物的制备方法，以及治疗，预防，抑制或改善一种或多种与还提供了使用这种化合物或这种药物制剂的激酶。版权所有（C）2010，JPO＆INPIT

6. 发明专利

JP2010138204A 17β-HYDROXYSTEROID DEHYDROGENASE TYPE 3 INHIBITOR FOR TREATMENT OF ANDROGEN DEPENDENT DISEASE 审中-公开
标题翻译：用于治疗依恋性疾病的17β-羟基甾体脱氢酶3型抑制剂
公开(公告)号：JP2010138204A
公开(公告)日：2010-06-24
申请号：JP2010058356
申请日：2010-03-15
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： PARUCH KAMIL , GUZI TIMOTHY J
IPC分类号： C07D401/12 , A61K31/4545 , A61K31/496 , A61K45/00 , A61P5/28 , A61P13/08 , A61P15/00 , A61P17/00 , A61P17/10 , A61P17/14 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/46 , C07D211/58
CPC分类号： C07D211/46 , C07D211/58
摘要： PROBLEM TO BE SOLVED: To provide a useful compound in the treatment, prevention or improvement of diseases or disorders associated with type 3 17β-hydroxysteroid dehydrogenase. SOLUTION: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing the pharmaceutical compositions containing one or more such compounds, and methods of treatment, prevention, inhibition or improvement of one or more diseases associated with type 3 17β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供治疗，预防或改善与3型17β-羟类固醇脱氢酶相关的疾病或病症的有用化合物。解决方案：在其许多实施方案中，本发明提供了一类新型化合物作为3β17β-羟类固醇脱氢酶的抑制剂，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物组合物的方法含有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3型17β-羟类固醇脱氢酶相关的一种或多种疾病的方法。版权所有（C）2010，JPO＆INPIT

7. 发明专利

JP2012082234A Use of pyrazolo [1,5-a] pyrimidine derivative for inhibiting protein kinase, and method for inhibiting protein kinase 有权
标题翻译：使用吡唑并[1,5-A]吡啶衍生物抑制蛋白激酶，以及抑制蛋白激酶的方法
公开(公告)号：JP2012082234A
公开(公告)日：2012-04-26
申请号：JP2012015831
申请日：2012-01-27
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , PARRY DAVID A
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P9/00 , A61P17/14 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D519/00
CPC分类号： A61K31/519 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide methods for inhibiting a protein kinase selected from a group comprising AKT, Checkpoint kinases, Aurora kinases, Pim kinases, and tyrosine kinases, using pyrazolo[1,5-a]pyrimidine compounds; and to provide methods of treating, preventing, inhibiting and ameliorating one or more diseases related to the protein kinase by using the compounds.SOLUTION: In one aspect, the present invention provides a method of inhibiting activity of one or more kinases in a patient, wherein the kinases are selected from the group consisting of Akt kinases, Checkpoint kinases, Pim kinases and Aurora kinases, the method including a step of administering a therapeutically effective amount of at least one compound, or a pharmaceutically acceptable salt, solvate, ester, isomer or prodrug of the compound, to a patient in need thereof.
摘要翻译：待解决的问题：使用吡唑并[1,5-a]嘧啶化合物提供抑制选自AKT，检查点激酶，极光激酶，Pim激酶和酪氨酸激酶的蛋白激酶的方法; 并提供通过使用该化合物来治疗，预防，抑制和改善与蛋白激酶相关的一种或多种疾病的方法。解决方案：一方面，本发明提供一种抑制患者中一种或多种激酶活性的方法，其中所述激酶选自Akt激酶，检查点激酶，Pim激酶和极光激酶，方法，其包括向有需要的患者施用治疗有效量的化合物或其药学上可接受的盐，溶剂合物，酯，异构体或前药。版权所有（C）2012，JPO＆INPIT

8. 发明专利

JP2012072189A New pyrazolopyrimidines as a cyclin-dependent kinase inhibitor 审中-公开
标题翻译：作为循环依赖型激酶抑制剂的新型吡唑并嘧啶
公开(公告)号：JP2012072189A
公开(公告)日：2012-04-12
申请号：JP2012003526
申请日：2012-01-11
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , LABROLI MARC , KEERTIKAR KARTIK M
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/00 , A61P9/00 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D519/00
CPC分类号： C07D487/04 , Y02P20/582
摘要： PROBLEM TO BE SOLVED: To provide novel pyrazolopyrimidines as cyclin dependent kinase inhibitors.SOLUTION: The present invention relates to: a novel class of pyrazolo[1, 5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases; methods of preparing such compounds; pharmaceutical compositions comprising 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. The compounds are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. The compounds further useful in the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
摘要翻译：要解决的问题：提供新的吡唑并嘧啶作为细胞周期蛋白依赖性激酶抑制剂。解决方案：本发明涉及：作为细胞周期蛋白依赖性激酶抑制剂的新一类吡唑并[1,5-a]嘧啶化合物; 制备这些化合物的方法; 包含一种或多种这样的化合物的药物组合物; 制备包含一种或多种这样的化合物的药物制剂的方法; 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。该化合物可用于治疗和预防增殖性疾病，例如癌症，炎症和关节炎。还可用于治疗和预防神经变性疾病如阿尔茨海默氏病，心血管疾病，病毒性疾病和真菌疾病的化合物。版权所有（C）2012，JPO＆INPIT

9. 发明专利

JP2011074088A Pyrazolopyrimidine as cyclin dependent kinase inhibitor 审中-公开
标题翻译：作为CYCLIN依赖性激酶抑制剂的吡唑并嘧啶
公开(公告)号：JP2011074088A
公开(公告)日：2011-04-14
申请号：JP2011005344
申请日：2011-01-13
申请人： Pharmacopeia Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコピア, インコーポレイテッド
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL , KNUTSON CHAD , MCKITTRICK BRIAN , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON
IPC分类号： C07D487/04 , A61K31/519 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/02 , A61P37/06 , A61P43/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide new compounds, formulations, treatment and therapy for treating diseases and disorders associated with CDK.
SOLUTION: In its many embodiments, there are provided a new class of pyrazolo[1,5-a]pyrimidine 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.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供新的化合物，制剂，治疗和治疗用于治疗与CDK相关的疾病和病症。解决方案：在其许多实施方案中，提供了一类新的作为细胞周期依赖性激酶抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，方法制备包含一种或多种这样的化合物的药物制剂，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。版权所有（C）2011，JPO＆INPIT

10. 发明专利

JP2010180234A Pyrazolopyrimidine as cyclin-dependent kinase inhibitor 审中-公开
标题翻译：作为CYCLIN依赖性激酶抑制剂的吡唑并嘧啶
公开(公告)号：JP2010180234A
公开(公告)日：2010-08-19
申请号：JP2010088210
申请日：2010-04-06
申请人： Pharmacopeia Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコピア, インコーポレイテッド
发明人： GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL , MALLAMS ALAN , ALVAREZ CARMEN S , KEERTIKAR KARTIK M , RIVERA JOCELYN , CHAN TIN-YAU , MADISON VINCENT , FISCHMANN THIERRY O , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON , PARADKAR VIDYADHAR M , HOBBS DOUGLAS WALSH
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D519/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as a protein kinase inhibitor. SOLUTION: A new class of a pyrazolo[1,5-a]pyrimidine compound represented by the formula as an inhibitor of a cyclin-dependent kinase is provided in many embodiments. A method for preparing such a compound, a pharmacological composition comprising one or more such compounds, a method for preparing a pharmacological formulation comprising one or more such compounds, and a method for treating, preventing, inhibiting or ameliorating one or more diseases associated with a CDK using such a compound or such a pharmacological composition are also provided. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用作蛋白激酶抑制剂的化合物。解决方案：在许多实施方案中提供了一类新的由式表示的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂。一种制备这种化合物的方法，包含一种或多种这样的化合物的药物组合物，包含一种或多种这样的化合物的药物制剂的制备方法，以及治疗，预防，抑制或改善一种或多种与还提供使用这种化合物的CDK或这样的药物组合物。版权所有（C）2010，JPO＆INPIT

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