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1. 发明授权

US07902252B2 Inhibitors of D-amino acid oxidase 有权
标题翻译： D-氨基酸氧化酶抑制剂
公开(公告)号：US07902252B2
公开(公告)日：2011-03-08
申请号：US12506204
申请日：2009-07-20
申请人： Michele L. R. Heffernan , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
发明人： Michele L. R. Heffernan , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D209/42 , C07D209/52 , C07D209/94 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.
摘要翻译：本发明提供D-氨基酸氧化酶酶的新型抑制剂。本发明的化合物可用于治疗或预防疾病和/或病症，其中D-丝氨酸水平和/或其氧化产物的调节在改善症状中是有效的。本发明还提供增强学习，记忆和/或认知的方法。例如，本发明提供了治疗或预防与神经变性疾病如阿尔茨海默病有关的记忆丧失和/或认知丧失的方法。本发明还提供了用于预防神经变性疾病的神经元功能特征丧失的方法。此外，提供了用于治疗或预防神经精神疾病（例如精神分裂症）和用于治疗或预防疼痛和共济失调的方法。

2. 发明申请

US20110053945A1 SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-DIHY-DRO-5H-PYRROLO[3,4-B]PYRAZINE 审中-公开
标题翻译： -6 - （5-氯-2-吡啶基）-5 - [（4-甲基-1-哌嗪基）羰基] -7-氧代-6,7-二氢-6H-吡咯并[3,4-B ] PYRAZINE
公开(公告)号：US20110053945A1
公开(公告)日：2011-03-03
申请号：US12808025
申请日：2008-12-18
申请人： H. Scott Wilkinson , Richard Hsia , Tushar Misra , Kostas Saranteas
发明人： H. Scott Wilkinson , Richard Hsia , Tushar Misra , Kostas Saranteas
IPC分类号： A61K31/4985 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel mesylate, (R)-mandelate, succinate, citrate, fumarate, D-malate, D-tartrate, sulfate and L-tartrate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
摘要翻译：（6-（5-氯-2-吡啶基）-5 - [（4-甲基）丙烯酸的新型甲磺酸酯，（R） - 扁桃酸酯，琥珀酸盐，柠檬酸盐，富马酸盐，D-苹果酸盐，D-酒石酸盐，硫酸盐和L-酒石酸盐 -1-哌嗪基）羰基氧基] -7-氧代-6,7-二氢-5H-吡咯并[3,4-b]吡嗪）。

3. 发明申请

US20100272654A1 LEVALBUTEROL SALT 审中-公开
标题翻译： LEVALBUTEROL盐
公开(公告)号：US20100272654A1
公开(公告)日：2010-10-28
申请号：US12833882
申请日：2010-07-09
申请人： Paul McGlynn , Roger Bakale , Craig Sturge
发明人： Paul McGlynn , Roger Bakale , Craig Sturge
IPC分类号： A61K9/12 , A61K31/138 , A61P11/00
CPC分类号： C07C215/60 , A61K9/008 , A61K9/14 , A61K31/205 , A61M15/002 , A61M15/009 , A61M2202/0484 , A61M2202/0488 , A61M2202/064 , C07B2200/07 , C07B2200/13 , C07C59/255 , C09K3/30
摘要： Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
摘要翻译：莱伐珠特醇L-酒石酸盐提供具有期望用于计量剂量吸入器的性质的晶体。

4. 发明授权

US07816375B2 Ligands for monoamine receptors and transporters, and methods of use thereof 有权
标题翻译：单胺受体和转运蛋白的配体及其使用方法
公开(公告)号：US07816375B2
公开(公告)日：2010-10-19
申请号：US12403311
申请日：2009-03-12
申请人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
发明人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
IPC分类号： A61P25/00 , A61K31/445 , C07D211/00
CPC分类号： C40B40/04 , C07B2200/11 , C07C255/46 , C07C2601/04 , C07D205/02 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/12 , C07D211/16 , C07D211/18 , C07D211/20 , C07D211/26 , C07D211/32 , C07D211/40 , C07D211/42 , C07D211/60 , C07D233/04 , C07D233/10 , C07D265/30 , C07D267/10 , C07D303/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C40B30/04 , C40B50/14
摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
摘要翻译：本发明的一个方面涉及杂环化合物。本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

5. 发明授权

US07812035B2 4-substituted piperidines, and methods of use thereof 有权
标题翻译： 4-取代的哌啶，及其使用方法
公开(公告)号：US07812035B2
公开(公告)日：2010-10-12
申请号：US10317014
申请日：2002-12-11
申请人： Heike Radeke , Liming Shao
发明人： Heike Radeke , Liming Shao
IPC分类号： A61K31/445 , C07D211/44 , C07D211/22
CPC分类号： C07D211/62 , C07D211/22 , C07D211/46
摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
摘要翻译：本发明的一个方面涉及杂环化合物。本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

6. 发明申请

US20100204336A1 Formoterol Tartrate Process and Polymorph 有权
标题翻译：福莫特罗酒石酸盐过程和多晶型物
公开(公告)号：US20100204336A1
公开(公告)日：2010-08-12
申请号：US12767043
申请日：2010-04-26
申请人： Gerald J. Tanoury , Chris H. Senanayake , Donald W. Kessler
发明人： Gerald J. Tanoury , Chris H. Senanayake , Donald W. Kessler
IPC分类号： A61K31/167 , C07C233/24 , A61P11/08
CPC分类号： A61K31/205 , C07B2200/13 , C07C231/24 , C07C233/25 , C07C233/43
摘要： A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
摘要翻译：公开了制备R，R-福莫特醇L-酒石酸盐的高纯度盐的方法。该方法通过重结晶新型多晶型物提供最热力学稳定的多晶型物。

7. 发明申请

US20090292026A1 Treatment of CNS Disorders With trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine 有权
标题翻译：用反式4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理中枢神经系统疾病
公开(公告)号：US20090292026A1
公开(公告)日：2009-11-26
申请号：US12538583
申请日：2009-08-10
申请人： Thomas P. Jerussi , Qun Kevin Fang , Mark G. Currie
发明人： Thomas P. Jerussi , Qun Kevin Fang , Mark G. Currie
IPC分类号： A61K31/135 , A61P25/00
CPC分类号： C07C211/42 , C07B2200/07 , C07C2602/10 , C07C2602/28
摘要： Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.
摘要翻译：用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理CNS病症; 和（1S，4R） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺。还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺的方法。该方法包括制备N- [4-（3,4-二氯苯基）-1,2,3,4-四氢萘-1-基]甲酰胺的全部四种异构体，它们也是有用的。

8. 发明申请

US20090060922A1 Acetamide Stereoisomer 有权
标题翻译：乙酰胺立体异构体
公开(公告)号：US20090060922A1
公开(公告)日：2009-03-05
申请号：US12196520
申请日：2008-08-22
申请人： Craig R. Abolin , H. Scott Wilkinson , Paul McGlynn , William K. McVicar
发明人： Craig R. Abolin , H. Scott Wilkinson , Paul McGlynn , William K. McVicar
IPC分类号： C07C233/07 , A61K31/167 , A61K31/46 , A61K31/40 , A61K31/352 , A61K31/195 , A61P11/00 , A61K39/395 , A61P13/00
CPC分类号： C07C233/43 , A61K9/0075 , A61K9/008 , A61K31/167 , A61K31/4015 , A61K45/06 , C07B2200/13 , C07C231/18
摘要： The compound of formula (I) is a water-stable, long acting β2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
摘要翻译：式（I）化合物是用作治疗与可逆性阻塞性气道疾病等相关的支气管收缩剂的支气管扩张剂的水稳定的长效β2-选择性肾上腺素受体激动剂。

9. 发明授权

US07390796B2 Fatty acid modified forms of glucocorticoids 有权
标题翻译：脂肪酸修饰形式的糖皮质激素
公开(公告)号：US07390796B2
公开(公告)日：2008-06-24
申请号：US11599124
申请日：2006-11-14
申请人： Mark G. Currie , Steven Jones , Charles M. Zepp
发明人： Mark G. Currie , Steven Jones , Charles M. Zepp
IPC分类号： A61K31/56 , C07J5/00
CPC分类号： C07J5/00 , C07J5/0076 , C07J5/0092 , C07J71/0031 , Y10S514/826 , Y10S514/886
摘要： Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
摘要翻译：公开了下列化学式的化合物，其中R 3为C 8 -C 24烃或米索前列醇的残基。该化合物可用于治疗鼻炎和哮喘，特别是通过吸入治疗和治疗炎症，特别是通过局部或局部给药治疗炎症。

10. 发明申请

US20080004327A1 FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE 有权
标题翻译： D-氨基酸氧化酶的荧光取代抑制剂
公开(公告)号：US20080004327A1
公开(公告)日：2008-01-03
申请号：US11772798
申请日：2007-07-02
申请人： Michele Heffernan , Robert Foglesong , Seth Hopkins , Mustapha Soukri , Steven Jones , Kerry Spear , Mark Varney
发明人： Michele Heffernan , Robert Foglesong , Seth Hopkins , Mustapha Soukri , Steven Jones , Kerry Spear , Mark Varney
IPC分类号： A61K31/407 , C07D491/02
CPC分类号： C07D495/04 , C07D491/04
摘要： This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O−X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
摘要翻译：本发明提供了D-氨基酸氧化酶酶的新型抑制剂以及包含本发明化合物的药物组合物。本发明还提供了治疗和预防神经系统疾病如神经精神和神经退行性疾病以及疼痛，共济失调和惊厥的方法。本发明的化合物具有以下一般结构：其中A是NH或S.Q是选自CR 1和N的成员.X和Y是独立地选自O，S，CR < > 2，N和NH。 R 1，R 2和R 4都是独立地选自H和F的成员，条件是选自R 1，R 2， R 1，R 2，R 4和R 4是F.R 6是选自O - >其中X + +为正离子，其为选自无机正离子和有机正离子的成员。

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