公开(公告)号：EP2473041A1

公开(公告)日：2012-07-11

申请号：EP10814320.7

申请日：2010-08-27

申请人： Schering Corporation

发明人： POPOVICI-MULLER, Janeta ,  ROSNER, Kristin, E. ,  GUZI, Timothy, J.

IPC分类号： A01N43/04 ,  A61K31/70

CPC分类号： A61K31/70 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07H19/06 ,  C07H19/23

摘要： In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).

公开(公告)号：EP2209779A1

公开(公告)日：2010-07-28

申请号：EP08845907.8

申请日：2008-10-27

申请人： Schering Corporation

发明人： TADIKONDA, Praveen, K. ,  CAUBLE, David, F., Jr. ,  GUZI, Timothy, J. ,  SIDDIQUI, Arshad, M.

IPC分类号： C07D417/12 ,  A61K31/4439 ,  A61P35/00

CPC分类号： C07D417/12

摘要： The present invention relates to novel Heterocyclic Urea and Thiourea Derivatives of formula (I), compositions comprising the Heterocyclic Urea and Thiourea Derivatives, and methods for using the Heterocyclic Urea and Thiourea Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.

公开(公告)号：EP2155725A1

公开(公告)日：2010-02-24

申请号：EP08768096.3

申请日：2008-06-04

申请人： Schering Corporation

发明人： LABROLI, Marc, A. ,  POKER, Cory, Seth ,  GUZI, Timothy, J. ,  PARUCH, Kamil ,  DWYER, Michael, P. ,  KEERTIKAR, Kartik, M. ,  ALVAREZ, Carmen, S.

IPC分类号： C07D403/04

CPC分类号： C07D231/38 ,  C07D401/04 ,  C07D417/04

摘要： The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1′H-4,4′-bispyrazole.

公开(公告)号：EP2078003A1

公开(公告)日：2009-07-15

申请号：EP07853013.6

申请日：2007-10-29

申请人： Schering Corporation

发明人： SHIPPS, Gerald, W., Jr. ,  CHENG, Cliff, C. ,  HUANG, Xiaohua ,  FISCHMANN, Thierry, O. ,  DUCA, Jose, S. ,  RICHARDS, Matthew ,  ZENG, Hongbo ,  SUN, Binyuan ,  REDDY, Panduranga, A. ,  WONG, Tzu, T. ,  TADIKONDA, Praveen, K. ,  SIDDIQUI, M., Arshad ,  LABROLI, Marc, M. ,  POKER, Cory ,  GUZI, Timothy, J.

IPC分类号： C07D277/56 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  A61K31/426 ,  A61K31/427 ,  A61P35/00

CPC分类号： C07D277/56 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10

摘要： The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.

摘要翻译： 本发明涉及式（I）的新型苯胺基哌嗪衍生物，包含苯胺基哌嗪衍生物的组合物，以及使用苯胺基哌嗪衍生物治疗或预防增殖性疾病，癌症，抗增殖性疾病，炎症，关节炎，中枢神经 系统障碍，心血管疾病，脱发，神经元疾病，缺血性损伤，病毒性疾病，真菌感染或与蛋白激酶活性相关的病症。

公开(公告)号：EP2069349A2

公开(公告)日：2009-06-17

申请号：EP07839218.0

申请日：2007-10-02

申请人： 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 ,  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，含有一种或多种此类化合物的药物组合物，制备 包含一种或多种此类化合物的药物制剂，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。

公开(公告)号：EP1534709B1

公开(公告)日：2007-06-13

申请号：EP03749317.8

申请日：2003-09-03

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, 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 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel 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.

公开(公告)号：EP1720883A1

公开(公告)日：2006-11-15

申请号：EP05723498.1

申请日：2005-02-23

申请人： SCHERING CORPORATION

发明人： GUZI, Timothy, J. ,  PARUCH, Kamil

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, 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 kinases using such compounds or pharmaceutical compositions.

公开(公告)号：EP1534712A2

公开(公告)日：2005-06-01

申请号：EP03796321.2

申请日：2003-09-03

申请人： SCHERING CORPORATION ,  PHARMACOPEIA, INC.

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 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel 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.

公开(公告)号：EP1436281B1

公开(公告)日：2010-06-16

申请号：EP02773770.9

申请日：2002-10-15

申请人： Schering Corporation

发明人： GUZI, Timothy, J. ,  PARUCH, Kamil

IPC分类号： C07D401/06 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D211/34

摘要： There are disclosed compounds of the formula (I), prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

公开(公告)号：EP2178861A2

公开(公告)日：2010-04-28

申请号：EP08794560.6

申请日：2008-07-17

申请人： Schering Corporation

发明人： REDDY, Panduranga, Adulla, P. ,  ZHAO, Lianyun ,  TADIKONDA, Praveen, K. ,  WONG, Tzu, Tshin ,  TANG, Shuyi ,  TORRES, Luis, E. ,  CAUBLE, David, F., Jr. ,  GUZI, Timothy, J. ,  SIDDIQUI, M. Arshad

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compoundsfor treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.