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1. 发明授权

US06284774B1 4-Benzyl piperidine alkylsulfoxide heterocycles and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 4-苄基哌啶烷基亚砜杂环化合物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06284774B1
公开(公告)日：2001-09-04
申请号：US09674298
申请日：2000-10-31
申请人： Jonathan L. Wright , Suzanne Ross Kesten , Ravindra B. Upasani , Nancy C. Lan
发明人： Jonathan L. Wright , Suzanne Ross Kesten , Ravindra B. Upasani , Nancy C. Lan
IPC分类号： C07D40102
CPC分类号： C07D413/12 , A61K31/445 , A61K31/195 , A61K2300/00
摘要： Novel 4-Benzyl piperidine alkylsulfoxide heterocycles are disclosed and their use as subtype selective NMDA receptor antagonists, particularly for the treatment of Parkinson's disease, most preferably in combination with L-DOPA.
摘要翻译：公开了新的4-苄基哌啶烷基亚砜杂环，并且它们用作亚型选择性NMDA受体拮抗剂，特别是用于治疗帕金森病，最优选与L-DOPA组合。

2. 发明授权

US5925630A Neuroactive steroids of the androstane and pregnane series 失效
标题翻译：雄激素和孕烷系列的神经活性类固醇
公开(公告)号：US5925630A
公开(公告)日：1999-07-20
申请号：US659192
申请日：1996-06-06
申请人： Ravindra B. Upasani , David B. Fick , Derk J. Hogenkamp , Nancy C. Lan
发明人： Ravindra B. Upasani , David B. Fick , Derk J. Hogenkamp , Nancy C. Lan
IPC分类号： A61K31/565 , A61K31/57 , A61P25/00 , C07J1/00 , C07J5/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J43/00 , A61K31/56
CPC分类号： C07J31/006 , C07J1/0007 , C07J1/0029 , C07J1/0055 , C07J1/0077 , C07J17/00 , C07J21/00 , C07J41/0005 , C07J41/005 , C07J43/003
摘要： The invention relates to 3.alpha.-hydroxy, 17-(un)substituted derivatives of the androstane series and 3.alpha.-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R.sub.4 =methyl), 19-norandrostanes, and norpregnanes (R.sub.4 =H).
摘要翻译：本发明涉及雄甾烷基系列的3α-羟基，17-（未）取代衍生物和孕烷系列的3α-羟基，21-取代衍生物。这些衍生物能够在最近确定的GRC位点起作用，从而以减轻压力，焦虑，失眠，舒适于GRC活性剂（如抑郁症）和癫痫发作活动的情绪障碍的方式调节脑兴奋性。本发明的类固醇衍生物是具有以下结构式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在本文中进一步定义，虚线是单键或双键。该结构包括雄甾烷，孕烷（R4 =甲基），19-去雄孕烷和诺孕烷（R4 = H）。

3. 发明授权

US06780853B1 Neuroactive steroids of the androstane and pregnane series 失效
标题翻译：雄激素和孕烷系列的神经活性类固醇
公开(公告)号：US06780853B1
公开(公告)日：2004-08-24
申请号：US09321882
申请日：1999-05-28
申请人： Ravindra B. Upasani , David B. Fick , Derk J. Hogenkamp , Nancy C. Lan
发明人： Ravindra B. Upasani , David B. Fick , Derk J. Hogenkamp , Nancy C. Lan
IPC分类号： A61K3158
CPC分类号： C07J1/0029 , C07J1/0007 , C07J1/0055 , C07J1/0077 , C07J17/00 , C07J21/00 , C07J31/006 , C07J41/0005 , C07J41/005 , C07J43/003
摘要： The invention relates to 3&agr;-hydroxy, 17-(un)substituted derivatives of the androstane series and 3&agr;-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are farther defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R4=methyl), 19-norandrostanes, and norpregnanes (R4=H).
摘要翻译：本发明涉及雄甾烷基系列的3α-羟基，17-（未）取代的衍生物和孕烷系列的3α-羟基，21-取代的衍生物。这些衍生物能够在最近确定的GRC位点起作用，从而以减轻压力，焦虑，失眠，舒适于GRC活性剂（如抑郁症）和癫痫发作活动的情绪障碍的方式调节脑兴奋性。本发明的类固醇衍生物是具有以下结构式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在本文中进一步定义，虚线是单键或双键。该结构包括雄甾烷，孕烷（R4 =甲基），19-去雄孕烷和诺孕烷（R4 = H）。

4. 发明授权

US08426431B2 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：US08426431B2
公开(公告)日：2013-04-23
申请号：US12986587
申请日：2011-01-07
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： A61K31/505 , A61K31/47 , A61K31/165
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, anxiety, or manic depression, 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，预防或改善作为抗惊厥药物的抗痉挛剂的疼痛，焦虑或躁狂抑郁症，作为局部麻醉剂，作为抗心律失常药物和治疗或预防糖尿病性神经病变。

5. 发明授权

US06613803B1 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
公开(公告)号：US06613803B1
公开(公告)日：2003-09-02
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.

6. 发明授权

US5591733A Methods, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series 失效
标题翻译：通过雄甾烷和孕烷系列成员对gaba受体进行变构调节的方法，组合物和化合物
公开(公告)号：US5591733A
公开(公告)日：1997-01-07
申请号：US101497
申请日：1993-08-02
申请人： Michael B. Bolger , Kelvin W. Gee , Nancy C. Lan , Robert H. Purdy , Seid Mirsadeghi , Syed Hasan Tahir , Delia Belelli
发明人： Michael B. Bolger , Kelvin W. Gee , Nancy C. Lan , Robert H. Purdy , Seid Mirsadeghi , Syed Hasan Tahir , Delia Belelli
IPC分类号： A61K20060101 , A61K31/33 , A61K31/56 , A61K31/565 , A61K31/57 , A61K31/58 , A61K31/585 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J17/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J71/00
CPC分类号： A61K31/568 , A61K31/565 , A61K31/57 , A61K31/573 , A61K31/58 , C07J1/0022 , C07J13/005 , C07J13/007 , C07J21/00 , C07J21/005 , C07J3/005 , C07J41/005 , C07J43/003 , C07J5/0015 , C07J5/0053 , C07J51/00 , C07J7/002 , C07J7/0065 , C07J71/001 , C07J9/00
摘要： Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
摘要翻译：用于调节脑兴奋性以减轻应激，焦虑，失眠和癫痫发作活性的方法，组合物和化合物，其使用在γ-氨基丁酸受体 - 氯离子载体（GR）复合物上的新鉴定位点起作用的某些类固醇衍生物。

7. 发明申请

US20110269785A1 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：US20110269785A1
公开(公告)日：2011-11-03
申请号：US12986587
申请日：2011-01-07
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： A61K31/513 , A61P25/04 , A61K31/44 , A61K31/47 , A61K31/165 , A61K31/45
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, anxiety, or manic depression, 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，预防或改善作为抗惊厥药物的抗痉挛剂的疼痛，焦虑或躁狂抑郁症，作为局部麻醉剂，作为抗心律失常药物和治疗或预防糖尿病性神经病变。

8. 发明授权

US06696442B2 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
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：US06696442B2
公开(公告)日：2004-02-24
申请号：US10178477
申请日：2002-06-25
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
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-82-; 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-82-。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。

9. 发明授权

US06534522B2 Subtype-selective NMDA receptor ligands and the use thereof 失效
标题翻译：亚型选择性NMDA受体配体及其用途
公开(公告)号：US06534522B2
公开(公告)日：2003-03-18
申请号：US09779024
申请日：2001-02-07
申请人： Christopher F. Bigge , Gian Luca Araldi , Sui Xiong Cai , Anthony P. Guzikowski , Donald Lamunyon , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
发明人： Christopher F. Bigge , Gian Luca Araldi , Sui Xiong Cai , Anthony P. Guzikowski , Donald Lamunyon , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
IPC分类号： C07D40112
CPC分类号： C07D239/06 , C07D211/14 , C07D211/18 , C07D217/04 , C07D221/16 , C07D221/28 , C07D233/26 , C07D451/06 , C07D471/04
摘要： The invention relates to subtype-selective NMDA receptor ligands and the use thereof for 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 the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
摘要翻译：本发明涉及亚型选择性NMDA受体配体及其用于治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失的用途，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征，治疗或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑症，精神病，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，帕金森病，青光眼，CMV视网膜炎，尿失禁，阿片样物质容忍或戒断，诱导麻醉以及增强认知。

10. 发明授权

US06465472B1 Substituted quinazolines and analogs and use thereof 有权
标题翻译：取代的喹唑啉和类似物及其用途
公开(公告)号：US06465472B1
公开(公告)日：2002-10-15
申请号：US09654839
申请日：2000-09-01
申请人： Ravi Upasani , Sui X. Cai , Nancy C. Lan , Yan Wang , George Field , David B. Fick
发明人： Ravi Upasani , Sui X. Cai , Nancy C. Lan , Yan Wang , George Field , David B. Fick
IPC分类号： C07D23726
CPC分类号： C07D231/12 , C07D233/56 , C07D239/82 , C07D249/08 , C07D491/04
摘要： The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus. Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.
摘要翻译：本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环，以及其用于治疗，预防或改善与中风，全身和局灶性缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗或改善神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合征，治疗，预防或改善兴奋性氨基酸过度刺激的不良后果，治疗，预防或改善焦虑，精神病，惊厥，慢性疼痛，青光眼，视网膜炎，尿失禁，肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏症如精神分裂症，肌阵挛的不良后果。阿尔茨海默病和营养不良和神经发育不良，以及认知和学习增强剂。

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