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31. 发明授权

US06794400B2 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译： 4-取代-1-（芳基亚甲基）氨基硫脲，4-取代-1-（芳基羰基）氨基硫脲和类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US06794400B2
公开(公告)日：2004-09-21
申请号：US10158827
申请日：2002-06-03
申请人： Sui Xiong Cai , Bao Ngoc Nguyen , John Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Azra Pervin
发明人： Sui Xiong Cai , Bao Ngoc Nguyen , John Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Azra Pervin
IPC分类号： A61K3144
CPC分类号： C07D207/335 , A61K31/175 , A61K31/435 , A61K31/44 , A61K31/4965 , C07C281/14 , C07C337/08 , C07C2602/42 , C07D213/53 , C07D213/61 , C07D213/84 , C07D213/86 , C07D231/16 , C07D233/64 , C07D277/28 , C07D277/56 , C07D285/06 , C07D295/135 , C07D307/52 , C07D307/76 , C07D333/22 , C07D333/44 , A61K2300/00
摘要： The present invention is directed to optionally substituted 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs thereof, represented by the Formulae I and II: wherein A1, A2, Q and R1-R3 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及由式I和II表示的任选取代的4-取代-1-（芳基亚甲基）氨基硫脲，4-取代-1-（芳基羰基）氨基硫脲及其类似物：其中A1，A2，Q和R1- R3在本文中定义。本发明还涉及具有式I和II的化合物是胱天蛋白酶的活化剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于在异常细胞发生不受控制的生长和扩散的各种临床病症中诱导细胞死亡。

32. 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。

33. 发明授权

US06500825B2 Substituted 2-aminoacetamides and the use thereof 有权
标题翻译：取代的2-氨基乙酰胺及其用途
公开(公告)号：US06500825B2
公开(公告)日：2002-12-31
申请号：US09933203
申请日：2001-08-21
申请人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
发明人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
IPC分类号： A61K31445
CPC分类号： C07C233/05 , A61K31/165 , C07C237/06 , C07C237/08 , C07C2601/14 , C07D211/46 , C07D213/65 , C07D213/68 , C07D215/20 , C07D239/34 , C07D241/08 , C07D309/12 , C07D317/64
摘要： This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is 0, 1, 2 or 3. The invention also is directed to the use substituted 2-aminoacetamides for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及由式II表示的取代的2-氨基乙酰胺或其药学上可接受的盐或前药，其中：R 1，R 2，R 3和R 4独立地为氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟烷基，烷氧基烷基或羧基烷基; R5，R6和R7独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基，或R5如上所定义，R 6和R 7与它们所在的氮原子一起连接形成杂环，包括哌啶，哌嗪，吗啉; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR8，CH2，C（O），NR8C（O），C（O）NR8，SO，SO2或共价键; 其中R8是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 本发明还涉及使用取代的2-氨基乙酰胺用于治疗全身和局灶性缺血后的神经元损伤，用于治疗或预防神经变性病症如肌萎缩性侧索硬化（ALS），作为抗惊厥药，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变的治疗，预防或改善。

34. 发明授权

US06458843B1 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
标题翻译：碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途
公开(公告)号：US06458843B1
公开(公告)日：2002-10-01
申请号：US09421403
申请日：1999-10-21
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要翻译：本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

35. 发明授权

US6124317A 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-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：US6124317A
公开(公告)日：2000-09-26
申请号：US91593
申请日：1998-11-18
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31/445 , A61K31/454 , C07D211/14 , C07D401/12 , A01N43/40
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartatc (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, amioglycoside antibiotics-induced hearing loss, migraine headaches, chronic pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译： PCT No.PCT / US96 / 20767 Sec。 371日期：1998年11月18日 102（e）1998年11月18日日期PCT 1996年12月20日PCT公布。出版物WO97 / 23215 PCT 日期1997年7月3日新颖的2-取代的哌啶类似物，含有它们的药物组合物和使用2-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，焦虑症，惊厥，阿糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，青光眼，CMV视网膜炎，精神病，尿失禁，阿片样物质耐受或戒断，或神经退行性疾病，阿尔茨海默病，帕金森综合征和亨廷顿氏病。

36. 发明授权

US07872127B2 Substituted 2-aminoacetamides and the use thereof 失效
标题翻译：取代的2-氨基乙酰胺及其用途
公开(公告)号：US07872127B2
公开(公告)日：2011-01-18
申请号：US12473887
申请日：2009-05-28
申请人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
发明人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
IPC分类号： C07D211/94 , C07D211/96 , C07D211/98
CPC分类号： C07C233/05 , A61K31/165 , C07C237/06 , C07C237/08 , C07C2601/14 , C07D211/46 , C07D213/65 , C07D213/68 , C07D215/20 , C07D239/34 , C07D241/08 , C07D309/12 , C07D317/64
摘要： The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及由式（II）表示的取代的2-氨基乙酰胺及其药学上可接受的盐和前药，其中取代基在本文中定义。本发明还涉及取代的2-氨基乙酰胺在治疗全球和局灶性缺血后的神经元损伤的方法中的用途，以及用作治疗，预防或改善疼痛的抗惊厥药作为抗痉挛剂，作为局部麻醉剂，如抗心律失常药物和治疗或预防糖尿病性神经病变。

37. 发明授权

US07528164B2 Substituted 4-aryl-4h-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的4-芳基-4H-吡咯并[2,3-h]色烯和类似物作为胱天蛋白酶的激活剂和凋亡诱导剂及其用途
公开(公告)号：US07528164B2
公开(公告)日：2009-05-05
申请号：US10514427
申请日：2003-05-16
申请人： Sui Xiong Cai , Songchun Jiang , William E. Kemnitzer , Hong Zhang , Giorgio Attardo , Real Denis
发明人： Sui Xiong Cai , Songchun Jiang , William E. Kemnitzer , Hong Zhang , Giorgio Attardo , Real Denis
IPC分类号： A61K31/407
CPC分类号： C07D491/04
摘要： The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及由式（I）表示的取代的4H-色烯及其类似物：其中R1，R3-R5，A，D，Y和Z如本文所定义。本发明还涉及具有式（I）的化合物是胱天蛋白酶的激活剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

38. 发明授权

US07476741B2 Substituted 4H-chromens, 2H-chromenes, chromans and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的4H-色素，2H-色烯，着色剂和类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07476741B2
公开(公告)日：2009-01-13
申请号：US10514426
申请日：2003-05-16
申请人： Sui Xiong Cai , Songchun Jiang , Giorgio Attardo , Réal Denis , Richard Storer , Rabindra Rej
发明人： Sui Xiong Cai , Songchun Jiang , Giorgio Attardo , Réal Denis , Richard Storer , Rabindra Rej
IPC分类号： C07D405/00
CPC分类号： C07D311/04 , C07D311/74 , C07D311/76
摘要： The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R5, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及其中R5，A，B，X，Y，Z和虚线由本文定义的通式（I）表示的取代的4H-色烯，2H-色烯，色满及其类似物。本发明还涉及具有式（I）的化合物是胱天蛋白酶的激活剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

39. 发明申请

US20080300191A1 PROTEASE INHIBITORS FOR CORONAVIRUSES AND SARS-COV AND THE USE THEREOF 失效
标题翻译：冠状病毒和SARS-COV的蛋白酶抑制剂及其用途
公开(公告)号：US20080300191A1
公开(公告)日：2008-12-04
申请号：US10839753
申请日：2004-05-06
申请人： Sui Xiong Cai , William E. Kemnitzer , Hong Zhang , Han-Zhong Zhang
发明人： Sui Xiong Cai , William E. Kemnitzer , Hong Zhang , Han-Zhong Zhang
IPC分类号： A61K38/05 , A61K38/04 , C07K5/04 , C07K5/06
CPC分类号： C07K5/06043 , A61K38/00 , C07K5/06026 , C07K5/06052 , C07K5/06086 , C07K5/06095 , C07K5/06191 , Y02A50/463 , Y02A50/465
摘要： Disclosed are protease inhibitors for coronaviruses and SARS-CoV, or picornaviruses, and the use of these protease inhibitors for preventing, reducing, ameliorating and treating a disease or condition caused by coronaviruses and SARS-CoV, or picornaviruses. Also disclosed are methods of reducing or preventing the spread of coronavirus, or picornaviruses, and preventing or reducing the replication of coronavirus, or picornaviruses, with the compounds of the present invention
摘要翻译：公开了用于冠状病毒和SARS-CoV或微小核糖核酸病毒的蛋白酶抑制剂，以及这些蛋白酶抑制剂用于预防，减少，改善和治疗由冠状病毒和SARS-CoV或小核糖核酸病毒引起的疾病或病症的用途。还公开了减少或预防冠状病毒或小核糖核酸病毒的扩散以及预防或减少冠状病毒或小核糖核酸病毒与本发明化合物复制的方法

40. 发明授权

US06534525B1 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-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：US06534525B1
公开(公告)日：2003-03-18
申请号：US09598162
申请日：2000-06-21
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31445
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist 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, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译：新的2-取代的哌啶类似物，含有它们的药物组合物和使用2-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，脊髓痛，青光眼，CMV视网膜炎，精神病，尿失禁，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。

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