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11. 发明授权

US06342611B1 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报道分子及其在全酶抑制剂中的应用及其用途
公开(公告)号：US06342611B1
公开(公告)日：2002-01-29
申请号：US09168888
申请日：1998-10-09
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： C07D31188
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
摘要翻译：本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性或器官。报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

12. 发明授权

US6130234A 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists 失效
标题翻译： 4-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US6130234A
公开(公告)日：2000-10-10
申请号：US91594
申请日：1996-12-20
申请人： Christopher F. Bigge , Jonathan Wright , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
发明人： Christopher F. Bigge , Jonathan Wright , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
IPC分类号： A61K31/00 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/498 , A61K31/505 , A61K31/517 , A61K31/529 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/00 , A61P25/02 , A61P25/04 , A61P43/00 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/54 , C07D211/58 , C07D211/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D235/08
CPC分类号： C07D401/06 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/54 , C07D211/58 , C07D405/06
摘要： Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.
摘要翻译： PCT No.PCT / US96 / 20766 Sec。 371日期：1998年9月16日 102（e）1998年9月16日PCT PCT 1996年12月20日PCT公布。公开号WO97 / 23214 PCT 日期1997年7月3日新颖的4-取代的哌啶类似物，含有它们的药物组合物和使用4-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，焦虑症，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，青光眼，CMV视网膜炎，慢性疼痛，阿片样物质耐受或戒断，或神经退行性疾病，如幻影，阿尔茨海默病，帕金森综合征并描述亨廷顿氏病。还描述了制备4-取代的哌啶类似物和4-取代的哌啶类似物的新中间体的新方法。

13. 发明授权

US06759207B2 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报告分子及其在半胱氨酸蛋白酶和其他酶的全细胞荧光筛选测定中的应用及其用途
公开(公告)号：US06759207B2
公开(公告)日：2004-07-06
申请号：US09947387
申请日：2001-09-07
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： G01N33573
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
摘要翻译：本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性或器官。报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

14. 发明授权

US06596693B1 Dipeptide apoptosis inhibitors and the thereof 失效
标题翻译：二肽凋亡抑制剂及其
公开(公告)号：US06596693B1
公开(公告)日：2003-07-22
申请号：US09653279
申请日：2000-08-31
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

15. 发明授权

US5863916A 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor 失效
标题翻译： 8-氮杂，6-氮杂和6,8-二氮杂-1,4-二氢喹喔啉-2,3-二酮及其作为甘氨酸/ NMDA受体拮抗剂的用途
公开(公告)号：US5863916A
公开(公告)日：1999-01-26
申请号：US795387
申请日：1997-02-04
申请人： Sui Xiong Cai , John F. W. Keana , Eckard Weber
发明人： Sui Xiong Cai , John F. W. Keana , Eckard Weber
IPC分类号： C07D487/04 , A61K31/495 , A61K31/4985 , A61K31/519 , A61P9/10 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/20 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D471/04 , C07D475/00 , C07D403/12
CPC分类号： C07D471/04 , A61K31/495 , A61K31/4985 , C07D475/00
摘要： Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof; wherein n is zero or 1; R.sup.4, R.sup.5, R.sup.6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R.sup.c and R.sup.d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor. Also disclosed are methods of treating pathophysiologic conditions associated with neuronal degeneration, convulsions, anxiety, chronic pain, pyschosis, opiate tolerance, and inducing anesthesia.
摘要翻译：公开了下式的化合物或其药学上可接受的盐; 其中n为0或1; R4，R5，R6独立地是氢，硝基，氨基，卤素，卤代烷基，氰基，烷基，环烷基，烯基，炔基，叠氮基，酰基氨基，烷基磺酰基，芳基，取代的芳基，杂芳基，烷氧基，三烷基甲硅烷基取代的烷氧基，芳氧基，杂芳氧基，杂环基，杂环氧基，芳烷氧基或卤代烷氧基; 并且在说明书中定义了Rc和Rd。这些化合物与NMDA受体的甘氨酸位点具有高度结合。还公开了治疗与神经元变性，抽搐，焦虑，慢性疼痛，慢性疼痛，阿片剂耐受和诱导麻醉相关的病理生理学病症的方法。

16. 发明授权

US5652368A 1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes 失效
标题翻译： 1,2,3,4-四氢喹啉2,3,4-三酮-3或4-肟
公开(公告)号：US5652368A
公开(公告)日：1997-07-29
申请号：US536937
申请日：1995-09-29
申请人： Sui Xiong Cai , John F. W. Keana , Eckard Weber
发明人： Sui Xiong Cai , John F. W. Keana , Eckard Weber
IPC分类号： A61K31/47 , A61K51/04 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/28 , C07D215/38 , C07D215/42 , C07D215/22 , C07D215/44 , C07D215/46
CPC分类号： C07D215/42 , A61K31/47 , A61K51/0455 , C07D215/38 , A61K2121/00
摘要： Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor and are usefully administered to animals for the treatment or prevention of the adverse consequences of the hyperactivity of the excitatory amino acids, or neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, for the treatment of anxiety, chronic pain, convulsions, and neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome; and for the inducement of anesthesia.
摘要翻译：本文公开了与甘氨酸受体具有高结合性的取代或未取代的1,2,3,4-四氢喹啉-2,3,4-三酮-3或4-肟或其药学上可接受的盐，并有用于动物给予治疗或预防兴奋性氨基酸多动症或与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失的不良后果，用于治疗焦虑，慢性疼痛，抽搐和神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿氏病和唐氏综合征; 并诱导麻醉。

17. 发明授权

US06680332B1 Substituted 5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyrans and benzothiopyrans and the use thereof as potentiators of AMPA 失效
标题翻译：取代的5-氧代-5,6,7,8-四氢-4H-1-苯并吡喃和苯并噻喃并将其作为AMPA的增效剂
公开(公告)号：US06680332B1
公开(公告)日：2004-01-20
申请号：US09980628
申请日：2002-05-20
申请人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
发明人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
IPC分类号： A61K4364
CPC分类号： C07D311/74
摘要： Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
摘要翻译：本发明公开了一种治疗患有AMPA受体AMPA受体阳性调节的病症的方法，其包括向有需要的动物施用式I化合物或其药学上可接受的盐或前药，其中：Y为NH 2， NHR和NHCOR; Z是O和S; 并且R1，R2，R3，R4和X在本文中定义。这些化合物可用作认知增强剂，用于治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病，帕金森病，AIDS相关性痴呆和唐氏综合征，以及治疗精神分裂症和肌阵挛。还公开了可用于治疗对AMPA受体的正调节起反应的病症的药物组合物和式I的新化合物。

18. 发明授权

US06184210B2 Dipeptide apoptosis inhibitors and the use thereof 有权
标题翻译：二肽凋亡抑制剂及其用途
公开(公告)号：US06184210B2
公开(公告)日：2001-02-06
申请号：US09270736
申请日：1999-03-16
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

19. 发明授权

US06800657B2 Substituted 5-oxo-5, 6, 7, 8-tetrahydro-4H-1-benzopyrans 失效
标题翻译：取代的5-氧代-5,6,7,8-四氢-4H-1-苯并吡喃
公开(公告)号：US06800657B2
公开(公告)日：2004-10-05
申请号：US10610871
申请日：2003-07-02
申请人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
发明人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
IPC分类号： A61K3138
CPC分类号： C07D311/74
摘要： Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
摘要翻译：本发明公开了一种治疗患有AMPA受体AMPA受体阳性调节的病症的方法，其包括向有需要的动物施用式I化合物或其药学上可接受的盐或前药，其中：Y为NH 2， NHR和NHCOR; Z是O和S; 并且R1，R2，R3，R4和X在本文中定义。这些化合物可用作认知增强剂，用于治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病，帕金森病，AIDS相关性痴呆和唐氏综合症，以及治疗精神分裂症和肌阵挛。还公开了可用于治疗对AMPA受体的正调节起反应的病症的药物组合物和式I的新化合物。

20. 发明授权

US5801183A Aza and aza (N-oxy) analogs of glycine/NMDA receptor antagonists 失效
标题翻译：甘氨酸/ NMDA受体拮抗剂的氮杂和氮杂（N-氧）类似物
公开(公告)号：US5801183A
公开(公告)日：1998-09-01
申请号：US466043
申请日：1995-06-06
申请人： John F. W. Keana , Sui Xiong Cai , Zhang-Lin Zhou , James M. Navratil
发明人： John F. W. Keana , Sui Xiong Cai , Zhang-Lin Zhou , James M. Navratil
IPC分类号： C07D241/44 , A61K31/4375 , A61K31/444 , A61K31/498 , A61K31/519 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D241/52 , C07D471/04 , C07D475/00 , C07D487/04 , A61K31/435
CPC分类号： C07D241/52 , C07D471/04 , C07D487/04
摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia, and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment or prevention a substituted or unsubstituted pyridine and pyridine (N-oxide) analogs of 4-hydroxydihydroquinolones, tetrahydroquinoline-trione-oximes and quinoxalones, tautomers and pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
摘要翻译：治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合症的治疗或预防方法，治疗或预防多动症的不良后果通过向需要这种治疗或预防的动物施用取代或未取代的吡啶和吡啶（N-氧化物）来公开兴奋性氨基酸以及治疗焦虑症，慢性疼痛，惊厥，诱导麻醉以及治疗或预防阿片剂耐受性的类似物，其与甘氨酸受体具有高结合性的4-羟基二氢喹诺酮，四氢喹啉 - 三酮 - 肟和喹喔啉酮，其互变异构体和药学上可接受的盐。

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