公开(公告)号：US20170253603A2

公开(公告)日：2017-09-07

申请号：US15104494

申请日：2014-12-19

申请人： Jianxing HUANG ,  Belew MEKONNEN ,  John A. BUTERA ,  Jianxing HUANG

发明人： Belew MEKONNEN ,  John A. BUTERA

IPC分类号： C07D487/14 ,  A61K45/06 ,  A61K31/5517 ,  A61K31/551

CPC分类号： C07D487/14 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US07893057B2

公开(公告)日：2011-02-22

申请号：US12456539

申请日：2009-06-18

申请人： Nicholas Bockovich ,  Arthur Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

发明人： Nicholas Bockovich ,  Arthur Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07F9/65583 ,  C07F9/6561

摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

摘要翻译： 本发明涉及新的细胞周期蛋白依赖性激酶抑制剂（cdks），具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。 如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，最终控制细胞生长和分化。 这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。

公开(公告)号：US07786112B2

公开(公告)日：2010-08-31

申请号：US10819899

申请日：2004-04-06

申请人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

发明人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07F9/65583 ,  C07F9/6561

摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

公开(公告)号：US08097619B2

公开(公告)日：2012-01-17

申请号：US10584485

申请日：2004-12-21

申请人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

发明人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07F9/6561

摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, untimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

摘要翻译： 本发明涉及新的细胞周期蛋白依赖性激酶抑制剂（cdks），具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。 如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，非常重要地控制细胞生长和分化。 这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。

公开(公告)号：US20100004207A1

公开(公告)日：2010-01-07

申请号：US12456539

申请日：2009-06-18

申请人： Nicholas Bockovich ,  Arthur Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

发明人： Nicholas Bockovich ,  Arthur Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

IPC分类号： A61K31/5377 ,  C07D413/14 ,  C07D487/04 ,  C07D413/10 ,  A61K31/519 ,  A61K31/675 ,  A61P31/18 ,  A61P35/00

CPC分类号： C07F9/65583 ,  C07F9/6561

摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

摘要翻译： 本发明涉及新的细胞周期蛋白依赖性激酶抑制剂（cdks），具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。 如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，最终控制细胞生长和分化。 这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。

公开(公告)号：US20090209530A1

公开(公告)日：2009-08-20

申请号：US10584485

申请日：2004-12-21

申请人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

发明人： Nicholas Bockovich ,  Arthur F. Kluge ,  Chris Oalmann ,  Krishna K. Murthi ,  Siya Ram ,  Zhongguo Wang ,  Jianxing Huang

IPC分类号： A61K31/5377 ,  C07D413/14 ,  C07D413/12 ,  C07D403/12 ,  C07F9/08 ,  C07D401/14 ,  C07D403/14 ,  A61P35/00 ,  A61P31/12 ,  A61P17/14

CPC分类号： C07F9/6561

摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

摘要翻译： 本发明涉及新的细胞周期蛋白依赖性激酶抑制剂（cdks），具体而非排他地作为cdk /细胞周期蛋白复合物的抑制剂。 如本文所述，本发明的抑制剂能够抑制细胞周期机制，因此可用于调节细胞周期进程，最终控制细胞生长和分化。 这样的化合物可用于治疗患有与过度细胞增殖相关的疾病的受试者。