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1. 发明申请

US20010044428A1 Aminopyridines and methods of using thereof 有权
标题翻译：氨基吡啶及其使用方法
公开(公告)号：US20010044428A1
公开(公告)日：2001-11-22
申请号：US09819693
申请日：2001-03-29
申请人： CoCensys, Inc.
发明人： Derk J. Hogenkamp
IPC分类号： C07D213/36 , A61K031/655
CPC分类号： C07D213/74
摘要： This invention relates to aminopyridines of Formula I: 1 or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1-R8, X and m are set in the specification. The invention is also directed to the use of compounds of Formula I 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 both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及式I的氨基吡啶或其药学上可接受的盐，前药或溶剂化物，其中R1-R8，X和m在说明书中设定。本发明还涉及式I化合物用于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）以及治疗，预防或改善的用途作为抗惊厥剂，作为抗惊厥剂，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。

2. 发明申请

US20020061886A1 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：US20020061886A1
公开(公告)日：2002-05-23
申请号：US10003249
申请日：2001-12-06
申请人： CoCensys, Inc.
发明人： Yan Wang , Sui Xiong Cai , John FW Keana
IPC分类号： A61K031/535 , A61K031/495 , A61K031/445 , A61K031/175
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: 1 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。

3. 发明申请

WO0066614A8 3 alpha -HYDROXY-3 beta METHOXYMETHYL-21-HETEROCYCLE SUBSTITUTED STEROIDS WITH ANESTHETIC ACTIVITY 审中-公开
标题翻译： 3α-羟基-3β甲氧基甲基-21-杂交取代的具有神经活性的甾体
公开(公告)号：WO0066614A8
公开(公告)日：2001-03-15
申请号：PCT/US0011680
申请日：2000-04-28
申请人： COCENSYS INC , HOGENKAMP DERK J
发明人： HOGENKAMP DERK J
IPC分类号： A61K31/573 , A61K31/58 , A61P23/00 , A61P25/20 , C07J31/00 , C07J33/00 , C07J43/00
CPC分类号： C07J43/003
摘要： This invention relates to compounds having Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein; R1 is H or methyl; R2 is 5 alpha - or 5 beta - H; R3 is an optionally substituted N-attached heteroaryl group or a group -X-R4; R4 is an optionally substituted carbon-attached heteroaryl group; and X is O, S or N. The invention also is directed to the use of 3 alpha - hydroxy-3 beta - methoxymethyl-substituted steroids as sedative/hypnotics and for inducing anesthesia.
摘要翻译：本发明涉及具有式（I）的化合物或其药学上可接受的盐，前药或溶剂合物，其中： R1是H或甲基; R2是5个α或5个β-H; R3是任选取代的N-连接的杂芳基或基团-X-R4; R4是任选取代的含碳杂芳基; 并且X是O，S或N.本发明还涉及3α-羟基-3β-甲氧基甲基取代的类固醇作为镇静/催眠药和诱导麻醉的用途。

4. 发明申请

WO0172714A2 ARYL SUBSTITUTED PYRAZOLES, TRIAZOLES AND TETRAZOLES, AND THE USE THEREOF 审中-公开
标题翻译： ARYL取代的吡咯，三唑和四氢呋喃及其用途
公开(公告)号：WO0172714A2
公开(公告)日：2001-10-04
申请号：PCT/US0108972
申请日：2001-03-22
申请人： COCENSYS INC , HOGENKAMP DERK , NGUYEN PHONG , YANG JI
发明人： HOGENKAMP DERK , NGUYEN PHONG , YANG JI
IPC分类号： C07D249/08 , A61K31/415 , A61K31/4196 , A61P9/04 , A61P9/06 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/24 , A61P27/16 , C07D231/12 , C07D231/14 , C07D249/12 , C07D521/00 , C07D231/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： This invention relates to compounds having the Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5 - R8 are set in the specification. The invention also is directed to the use of compounds of Formula (I) 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 both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及具有式（I）化合物或其药学上可接受的盐，前药或溶剂合物，其中Het和R5-R8被置于说明书中。本发明还涉及式（I）化合物用于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）以及用于治疗，预防或改善急性或慢性疼痛，作为抗惊厥剂，抗惊厥药，抗抑郁药，作为局部麻醉剂，作为抗心律失常药，以及用于治疗或预防糖尿病性神经病变。

5. 发明申请

WO1996016076A1 ANDROSTANE AND PREGNANE SERIES FOR ALLOSTERIC MODULATION OF GABA RECEPTOR 审中-公开
标题翻译：安哥拉和普罗米亚系列用于GABA受体的单独调控
公开(公告)号：WO1996016076A1
公开(公告)日：1996-05-30
申请号：PCT/US1995015210
申请日：1995-11-22
申请人： COCENSYS, INC.
发明人： COCENSYS, INC. , LAN, Nancy, C. , GEE, Kelvin, W. , BOLGER, Michael, B. , TAHIR, Hasan , PURDY, Robert , UPASANI, Ravindra, B.
IPC分类号： C07J09/00
CPC分类号： C07J41/005 , C07J5/0015 , C07J7/002 , C07J7/007 , C07J9/00
摘要： Methods, compositions, and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
摘要翻译：用于调节GABA A受体 - 氯离子载体复合物以缓解压力，焦虑，癫痫发作，情绪障碍，PMS和PND并诱导麻醉的方法，组合物和化合物。

6. 发明申请

WO0168612A3 ARYL SUBSTITUTED PYRIDINES, PYRIMIDINES, PYRAZINES AND TRIAZINES AND THE USE THEREOF 审中-公开
标题翻译：亚芳基取代的吡啶，吡啶，吡咯并吡啶及其用途
公开(公告)号：WO0168612A3
公开(公告)日：2002-03-14
申请号：PCT/US0107797
申请日：2001-03-12
申请人： COCENSYS INC , HOGENKAMP DERK J , NGUYEN PHONG , SHAO BIN
发明人： HOGENKAMP DERK J , NGUYEN PHONG , SHAO BIN
IPC分类号： C07D251/22 , A61K31/44 , A61K31/4453 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/53 , A61P9/06 , A61P9/10 , A61P23/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/10 , A61P29/02 , C07D213/81 , C07D239/00 , C07D239/26 , C07D239/28 , C07D239/38 , C07D241/24 , C07D241/26 , C07D251/24 , C07D253/06 , C07D295/12 , C07D403/04 , C07D413/04
CPC分类号： C07D213/81 , C07D239/28 , C07D239/38 , C07D241/24 , C07D251/24 , C07D403/04
摘要： This invention relates aryl substituted pyridines, pyrimides, pyrazines and triazines of Formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I 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 both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhytmics and for the treatment of prevention of diabetic neuropathy.
摘要翻译：本发明涉及式（I）的芳基取代的吡啶，嘧啶，吡嗪和三嗪：或其药学上可接受的盐，前药或溶剂合物，其中A1，A2，A3，R1-R4，X和Y置于说明书中。本发明还涉及式I化合物用于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）以及治疗，预防或改善的用途作为抗惊厥剂，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预防糖尿病性神经病变的治疗。

7. 发明申请

WO1998005337A1 USE OF GABA AND NMDA RECEPTOR LIGANDS FOR THE TREATMENT OF MIGRAINE HEADACHE 审中-公开
标题翻译： GABA和NMDA受体配体用于治疗疟原虫的用途
公开(公告)号：WO1998005337A1
公开(公告)日：1998-02-12
申请号：PCT/US1997013430
申请日：1997-07-31
申请人： COCENSYS, INC. , LAN, Nancy, C.
发明人： COCENSYS, INC.
IPC分类号： A61K31/56
CPC分类号： A61K31/56 , A61K31/495 , A61K2300/00
摘要： Methods of treating or preventing migraine headache are disclosed by administering to an animal a GABA receptor agonist and/or an NMDA receptor antagonist. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of migraine headache.
摘要翻译：通过向动物施用GABA受体激动剂和/或NMDA受体拮抗剂来公开治疗或预防偏头痛头痛的方法。还公开了用于治疗或预防偏头痛的药物组合物和试剂盒。

8. 发明申请

WO1993018053A1 METHOD FOR MAKING 3'alpha'-HYDROXY,3'beta'-SUBSTITUTED-PREGNANES 审中-公开
标题翻译：制备3α-羟基的方法，3β-去磷酸化-PREGNANES
公开(公告)号：WO1993018053A1
公开(公告)日：1993-09-16
申请号：PCT/US1993001602
申请日：1993-02-22
申请人： COCENSYS, INC.
发明人： COCENSYS, INC. , TAHIR, Syed, Hasan , BOLGER, Michael, Bruce , BUSWELL, Richard , GABRIEL, Richard , STEARNS, Jay
IPC分类号： C07J41/00
CPC分类号： A61K31/565 , A61K31/568 , A61K31/57 , A61K31/573 , A61K31/58 , C07J1/0022 , C07J3/005 , C07J5/0015 , C07J5/0053 , C07J7/002 , C07J7/0065 , C07J9/00 , C07J13/005 , C07J13/007 , C07J21/00 , C07J21/005 , C07J41/005 , C07J43/003 , C07J51/00 , C07J71/001
摘要： This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3 alpha -hydroxy,3 beta -substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3 alpha -hydroxy,3 beta -substituted-20-one form, which can be further modified at the 20-keto position. Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
摘要翻译：本发明提供了将孕烷-3,20-二酮化合物转化为3个α-羟基，3β-取代孕烷的简化方法。通过选择性使用试剂，将未保护的二酮转化为化学选择性和非对映选择性地转化为3（R） - 孕烷-3-螺 - 2 - 环氧乙烷-20-酮中间体。然后可以通过第二组反应转化为3α-羟基，3β-取代的20-一种形式来区域选择地转化，其可以在20-酮位置进一步修饰。通过该方法，每个酮基团被独立地处理。通过一次修饰一个酮，可以在每个位点获得所需的立体特异性。

9. 发明申请

WO1997023458A1 SUBTYPE-SELECTIVE NMDA RECEPTOR LIGANDS AND THE USE THEREOF 审中-公开
标题翻译：亚型选择性NMDA受体配体及其用途
公开(公告)号：WO1997023458A1
公开(公告)日：1997-07-03
申请号：PCT/US1996020746
申请日：1996-12-20
申请人： WARNER-LAMBERT COMPANY , COCENSYS, INC. , BIGGE, Christopher, F. , CAI, Sui Xiong , KEANA, John, F., W. , LAN, Nancy, C. , GUZIKOWSKI, Anthony, P. , ZHOU, Zhang-Lin , ARALDI, Gian, Luca , LAMUNYON, Donald , WEBER, Eckard
发明人： WARNER-LAMBERT COMPANY , COCENSYS, INC.
IPC分类号： C07D211/06
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. 发明申请

WO1997023215A1 2-SUBSTITUTED PIPERIDINE ANALOGS AND THEIR USE AS SUBTYPE-SELECTIVE NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-取代的哌嗪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：WO1997023215A1
公开(公告)日：1997-07-03
申请号：PCT/US1996020767
申请日：1996-12-20
申请人： WARNER-LAMBERT COMPANY , COCENSYS, INC. , BIGGE, Christopher, F. , CAI, Sui, Xiong , WEBER, Eckard , WOODWARD, Richard , LAN, Nancy, C. , KEANA, John, F., W. , GUZIKOWSKI, Anthony, P.
发明人： WARNER-LAMBERT COMPANY , COCENSYS, INC.
IPC分类号： A61K31/445
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-asparate (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：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，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，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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