公开(公告)号：US07618971B2

公开(公告)日：2009-11-17

申请号：US11630224

申请日：2005-06-27

申请人： Paul J. Coleman ,  Christopher D. Cox ,  Mark E. Fraley ,  George D. Hartman ,  John Schreier

发明人： Paul J. Coleman ,  Christopher D. Cox ,  Mark E. Fraley ,  George D. Hartman ,  John Schreier

IPC分类号： A61K31/496 ,  A61K31/4196 ,  A61K31/4155 ,  C07D403/06 ,  C07D249/08 ,  C07D231/06

CPC分类号： C07D231/12 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D487/08 ,  C07D491/107 ,  C07D491/113

摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

公开(公告)号：US20090233896A1

公开(公告)日：2009-09-17

申请号：US11921598

申请日：2006-06-05

申请人： Kenneth L. Arrington ,  Vadim Y. Dudkin ,  Mark E. Fraley ,  Jacob M. Hoffman ,  Constantine Kreatsoulas ,  Cheng Wang

发明人： Kenneth L. Arrington ,  Vadim Y. Dudkin ,  Mark E. Fraley ,  Jacob M. Hoffman ,  Constantine Kreatsoulas ,  Cheng Wang

IPC分类号： A61K31/397 ,  C07D413/14 ,  A61K31/5377 ,  C07D401/14 ,  A61K31/506 ,  C07D403/00 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D417/14 ,  C07D417/04 ,  C07D417/12

摘要： The instant invention provides for compounds which comprise substituted pyridyl aminothiazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.

摘要翻译： 本发明提供了包含抑制CHK1活性的取代的吡啶基氨基噻唑的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。

公开(公告)号：US07553838B2

公开(公告)日：2009-06-30

申请号：US11630302

申请日：2005-06-27

申请人： Mark E. Fraley ,  George D. Hartman

发明人： Mark E. Fraley ,  George D. Hartman

IPC分类号： C07D403/06 ,  C07D403/14 ,  A61K31/496

CPC分类号： C07D231/06 ,  C07D487/08

摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的二氢吡唑化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：US07192949B2

公开(公告)日：2007-03-20

申请号：US11410341

申请日：2006-04-24

申请人： Mark E. Fraley ,  Robert M. Garbaccio

发明人： Mark E. Fraley ,  Robert M. Garbaccio

IPC分类号： C07D239/70 ,  C07D401/12 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D239/70 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06

摘要： The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的环烷基嘧啶酮化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：US07169788B2

公开(公告)日：2007-01-30

申请号：US10489647

申请日：2002-10-25

申请人： Kenneth L. Arrington ,  Mark E. Fraley ,  George D. Hartman

发明人： Kenneth L. Arrington ,  Mark E. Fraley ,  George D. Hartman

IPC分类号： A61K31/496 ,  A61K31/4704 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D401/14

摘要： The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

摘要翻译： 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化的方法 ，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

公开(公告)号：US5744486A

公开(公告)日：1998-04-28

申请号：US829406

申请日：1997-03-31

申请人： Philip E. Sanderson ,  Adel M. Naylor-Olsen ,  Dona L. Dyer ,  Joseph P. Vacca ,  Richard C. A. Isaacs ,  Bruce D. Dorsey ,  Mark E. Fraley

发明人： Philip E. Sanderson ,  Adel M. Naylor-Olsen ,  Dona L. Dyer ,  Joseph P. Vacca ,  Richard C. A. Isaacs ,  Bruce D. Dorsey ,  Mark E. Fraley

IPC分类号： A61K38/00 ,  C07K5/078 ,  A61K31/445 ,  C07D211/06

CPC分类号： C07K5/06139 ,  A61K38/00

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##

摘要翻译： 本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并具有以下结构：例如：

公开(公告)号：US08785481B2

公开(公告)日：2014-07-22

申请号：US13247009

申请日：2011-09-28

申请人： Douglas C. Beshore ,  Vadim Dudkin ,  Robert M. Garbaccio ,  Adam W. Johnson ,  Scott D. Kuduk ,  Jason W. Skudlarek ,  Cheng Wang ,  Mark E. Fraley

发明人： Douglas C. Beshore ,  Vadim Dudkin ,  Robert M. Garbaccio ,  Adam W. Johnson ,  Scott D. Kuduk ,  Jason W. Skudlarek ,  Cheng Wang ,  Mark E. Fraley

IPC分类号： A61K31/4245 ,  C07D249/04

CPC分类号： C07D249/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US08629275B2

公开(公告)日：2014-01-14

申请号：US13060775

申请日：2009-08-31

申请人： Antonella Converso ,  Timothy J. Hartingh ,  Mark E. Fraley

发明人： Antonella Converso ,  Timothy J. Hartingh ,  Mark E. Fraley

IPC分类号： C07D471/02

CPC分类号： C07D471/04

摘要： The present invention is directed to AHCY inhibitors of formula (I): which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.

摘要翻译： 本发明涉及式（I）的AHCY抑制剂：其可用于治疗以高同型半胱氨酸水平为特征的疾病，例如阿尔茨海默氏病。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗以高同型半胱氨酸水平为特征的疾病中的用途。

公开(公告)号：US20130143880A1

公开(公告)日：2013-06-06

申请号：US13814870

申请日：2011-08-05

申请人： Vadim Y. Dudkin ,  Mark E. Fraley ,  Kenneth L. Arrington ,  Mark E. Layton ,  Alexander J. Reif ,  Kevin J. Rodzinak ,  Joseph E. Pero

发明人： Vadim Y. Dudkin ,  Mark E. Fraley ,  Kenneth L. Arrington ,  Mark E. Layton ,  Alexander J. Reif ,  Kevin J. Rodzinak ,  Joseph E. Pero

IPC分类号： A61K31/4745 ,  C07D235/26 ,  A61K31/4439 ,  C07D417/14 ,  C07D405/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D409/10 ,  C07D405/10 ,  A61K31/4184 ,  C07D413/02 ,  C07D401/02 ,  C07D403/02 ,  A61K31/4709 ,  C07D471/04

CPC分类号： C07D235/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/06 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D513/14

摘要： The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.

摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的苯并咪唑酮衍生物，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病如精神分裂症中的用途。

公开(公告)号：US20120122900A1

公开(公告)日：2012-05-17

申请号：US13293177

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC分类号： A61K31/437 ,  A61K31/527 ,  A61P25/06 ,  C07D471/20

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.