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1. 发明申请

WO2019246300A1 BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT 审中-公开
公开(公告)号：WO2019246300A1
公开(公告)日：2019-12-26
申请号：PCT/US2019/038038
申请日：2019-06-19
申请人： AGENEBIO, INC. , MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing , PATEL, Hemantbhai , JIANG, Qin , HERR, Robert, Jason , MAYHEW, Nicholas, James , FREEMAN, Emily, Elizabeth
发明人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing , PATEL, Hemantbhai , JIANG, Qin , HERR, Robert, Jason , MAYHEW, Nicholas, James , FREEMAN, Emily, Elizabeth
IPC分类号： C07D487/14 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , A61P35/00 , A61K31/551 , A61K31/5517
摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABA A receptor agonist ( e.g ., an α5-containing GABA A receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease(AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABA A receptor agonist (e.g., an α5-containing GABA A receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

2. 发明申请

WO2016205739A1 BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT 审中-公开
标题翻译：苯并噻吩衍生物，组合物和治疗认知障碍的方法
公开(公告)号：WO2016205739A1
公开(公告)日：2016-12-22
申请号：PCT/US2016/038224
申请日：2016-06-17
申请人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing
发明人： MEKONNEN, Belew , BUTERA, John, A. , HUANG, Jianxing
IPC分类号： C07D487/14 , A61K31/5513 , A61P25/00
CPC分类号： A61K31/551 , A61K31/13 , A61K31/27 , A61K31/445 , A61K31/496 , A61K31/55 , A61K45/06 , C07D487/14 , A61K2300/00
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 GABA A receptor agonist ( e.g. , a α5-containing GABA A 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.
摘要翻译：本发明涉及苯并二氮杂衍生物，包含治疗有效量的那些苯并二氮杂衍生物的组合物和使用这些衍生物或组合物治疗与中枢神经系统（CNS）病症相关的认知障碍的方法。特别地，本发明涉及在本文所述的含有α5的GABA A受体激动剂（例如，含有α5的GABA A受体阳性变构调节剂）用于治疗有需要的受试者中与中枢神经系统（CNS）紊乱相关的认知障碍或其风险包括但不限于具有年龄相关认知障碍或轻度认知障碍（MCI），遗忘MCI（aMCI），年龄相关记忆障碍（AAMI），年龄相关认知衰退（ARCD）），痴呆，阿尔茨海默病（AD），前驱性AD，创伤后应激障碍（PTSD），精神分裂症，双相情感障碍，肌萎缩性侧索硬化（ALS），癌症治疗相关认知障碍，精神发育迟滞，帕金森病（PD），自闭症谱系障碍，脆性X病症，Rett综合征，强迫行为和物质成瘾。

3. 发明申请

WO2005063765A1 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译：环孢素依赖性激酶的抑制剂，组合物和与之相关的用途
公开(公告)号：WO2005063765A1
公开(公告)日：2005-07-14
申请号：PCT/US2004/043492
申请日：2004-12-21
申请人： GPC BIOTECH, INC. , BOCKOVICH, Nicholas , KLUGE, Arthur, F. , OALMANN, Chris , MURTHI, Krishna, K. , RAM, Siya , WANG, Zhongguo , HUANG, Jianxing
发明人： BOCKOVICH, Nicholas , KLUGE, Arthur, F. , OALMANN, Chris , MURTHI, Krishna, K. , RAM, Siya , WANG, Zhongguo , HUANG, Jianxing
IPC分类号： C07D487/04
CPC分类号： C07F9/6561
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) of formula (I) wherein the substituents are as defined in the claims 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：本发明涉及式（I）的新型细胞周期蛋白依赖性激酶抑制剂（cdks），其中取代基如权利要求中所定义，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。

4. 发明申请

WO2004092139A3 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译：环孢素依赖性激酶的抑制剂，组合物和与之相关的用途
公开(公告)号：WO2004092139A3
公开(公告)日：2005-03-31
申请号：PCT/US2004010381
申请日：2004-04-06
申请人： GPC BIOTECH INC , BOCKOVICH NICHOLAS , KLUGE ARTHUR , OALMANN CHRIS , MURTHI KRISHNA K , RAM SIYA , WANG ZHONGGUO , HUANG JIANXING
发明人： BOCKOVICH NICHOLAS , KLUGE ARTHUR , OALMANN CHRIS , MURTHI KRISHNA K , RAM SIYA , WANG ZHONGGUO , HUANG JIANXING
IPC分类号： A61P31/12 , A61P35/00 , C07D231/00 , C07F9/6558 , C07F9/6561 , C07D487/04 , A61K31/416 , A61K31/519 , A61K31/675 , C07D231/54 , C07D403/12 , C07D413/12 , C07D519/00
CPC分类号： C07F9/65583 , C07F9/6561
摘要： The invention pertains to novel cyclin dependent kinase inhibitors (cdks) of formulae (II) and (I) wherein the substituents are as defined in the claims 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：本发明涉及式（II）和（I）的新型细胞周期蛋白依赖性激酶抑制剂（cdks），其中取代基如权利要求中所定义，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。

5. 发明申请

WO2004092139A2 INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译：环孢素依赖性激酶的抑制剂，组合物和与之相关的用途
公开(公告)号：WO2004092139A2
公开(公告)日：2004-10-28
申请号：PCT/US2004/010381
申请日：2004-04-06
申请人： GPC BIOTECH, INC. , BOCKOVICH, Nicholas , KLUGE, Arthur , OALMANN, Chris , MURTHI, Krishna, K. , RAM, Siya , WANG, Zhongguo , HUANG, Jianxing
发明人： BOCKOVICH, Nicholas , KLUGE, Arthur , OALMANN, Chris , MURTHI, Krishna, K. , RAM, Siya , WANG, Zhongguo , HUANG, Jianxing
IPC分类号： C07D231/00
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。

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