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1. 发明授权

US07884124B2 Fluoro-substituted inhibitors of D-amino acid oxidase 有权
标题翻译：氟取代的D-氨基酸氧化酶抑制剂
公开(公告)号：US07884124B2
公开(公告)日：2011-02-08
申请号：US11772798
申请日：2007-07-02
申请人： Michele L. R. Heffernan , Robert J. Foglesong , Seth C. Hopkins , Mustapha Soukri , Steven W. Jones , Kerry L. Spear , Mark A. Varney
发明人： Michele L. R. Heffernan , Robert J. Foglesong , Seth C. Hopkins , Mustapha Soukri , Steven W. Jones , Kerry L. Spear , Mark A. Varney
IPC分类号： A61K31/40 , C07D487/02 , C07D491/02 , C07D495/02 , C07D497/02
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通式：其中A是NH或S.Q是选自CR1和N的成员.X和Y是独立地选自O，S，CR2，N和NH的成员。 R 1，R 2和R 4是独立地选自H和F的成员，条件是选自R 1，R 2和R 4中的至少一个是F.R 6是选自O-X +和OH的成员，其中X +是正离子，其中是选自无机正离子和有机正离子的成员。

2. 发明申请

US20090099248A1 INHIBITORS OF D-AMINO ACID OXIDASE 审中-公开
标题翻译： D-氨基酸氧化酶的抑制剂
公开(公告)号：US20090099248A1
公开(公告)日：2009-04-16
申请号：US12016954
申请日：2008-01-18
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： A61K31/404 , C07D209/02 , C07D209/42 , A61P25/00 , C12N9/99 , A61K31/403
CPC分类号： C07D209/52 , C07D209/42 , C07D209/94 , C07D487/04 , C07D491/04 , C07D495/04 , G01N21/253 , G01N21/255 , G01N21/3151
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。

3. 发明申请

US20100029737A1 INHIBITORS OF D-AMINO ACID OXIDASE 有权
标题翻译： D-氨基酸氧化酶的抑制剂
公开(公告)号：US20100029737A1
公开(公告)日：2010-02-04
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 , C07D209/52 , C07D209/56
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。

4. 发明申请

US20100029741A1 FUSED HETEROCYCLES 审中-公开
标题翻译：熔融杂环
公开(公告)号：US20100029741A1
公开(公告)日：2010-02-04
申请号：US12537896
申请日：2009-08-07
申请人： James M. Dorsey , Michele L. R. Heffernan , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
发明人： James M. Dorsey , 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： A61K31/407 , A61P25/00
CPC分类号： A61K31/407 , C07D491/04 , C07D495/04
摘要： This invention provides methods of improving cognitive function by administering to a subject a therapeutically effective amount of a fused heterocycle having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3 is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
摘要翻译：本发明提供了通过向受试者施用治疗有效量的具有下式的稠合杂环来提高认知功能的方法：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。索引n是从1到4的整数。

5. 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。

6. 发明申请

US20100022612A1 FUSED HETEROCYCLES 审中-公开
标题翻译：熔融杂环
公开(公告)号：US20100022612A1
公开(公告)日：2010-01-28
申请号：US12537925
申请日：2009-08-07
申请人： James M. Dorsey , Michele L. R. Heffernan , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
发明人： James M. Dorsey , 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： A61K31/407 , A61P29/00
CPC分类号： A61K31/407 , C07D491/04 , C07D495/04
摘要： This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3 is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
摘要翻译：本发明提供具有下式的稠合杂环：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。索引n是从1到4的整数。

7. 发明授权

US07579370B2 Fused heterocycles 失效
标题翻译：融合杂环
公开(公告)号：US07579370B2
公开(公告)日：2009-08-25
申请号：US11833903
申请日：2007-08-03
申请人： Michele L. R. Heffernan , James M. Dorsey , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
发明人： Michele L. R. Heffernan , James M. Dorsey , Qun Kevin Fang , Robert J. Foglesong , Seth C. Hopkins , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear
IPC分类号： A61K31/40 , A61K31/34 , A61K31/19 , A01N43/38 , A01N43/08 , A01N37/00
CPC分类号： A61K31/407 , C07D491/04 , C07D495/04
摘要： This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
摘要翻译：本发明提供具有下式的稠合杂环：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。索引n是从1到4的整数。

8. 发明申请

US20110034434A1 PRODRUGS OF FUSED HETEROCYCLIC INHIBITORS OF D-AMINO ACID OXIDASE 审中-公开
标题翻译： D-氨基酸氧化酶的融合杂环抑制剂的制备
公开(公告)号：US20110034434A1
公开(公告)日：2011-02-10
申请号：US12852215
申请日：2010-08-06
申请人： Michele L. R. Heffernan , Richard Dennis , James M. Dorsey , Robert J. Foglesong , Michael L. Jones , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear , Michael A. Orsini
发明人： Michele L. R. Heffernan , Richard Dennis , James M. Dorsey , Robert J. Foglesong , Michael L. Jones , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear , Michael A. Orsini
IPC分类号： A61K31/397 , C07D491/04 , A61K31/407 , C07D401/14 , A61K31/4439 , C07D413/14 , A61K31/5377 , A61K31/454 , C07D403/14 , A61K31/496 , A61K31/4178 , A61P29/00 , A61P25/28
CPC分类号： C07D491/04 , C07D491/14
摘要： The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
摘要翻译：本发明涉及D-氨基氧化酶（DAAO）的稠合杂环抑制剂的前药和治疗疾病和病症的方法，其中D-氨基酸氧化酶活性，D-丝氨酸水平，D-丝氨酸氧化产物和NMDA受体活性的调节哺乳动物受试者的神经系统是有效的。

9. 发明申请

US20100120740A1 PRODRUGS OF FUSED HETEROCYCLIC INHIBITORS OF D-AMINO ACID OXIDASE 审中-公开
标题翻译： D-氨基酸氧化酶的融合杂环抑制剂的制备
公开(公告)号：US20100120740A1
公开(公告)日：2010-05-13
申请号：US12537104
申请日：2009-08-06
申请人： Michele L. R. Heffernan , Richard Dennis , James M. Dorsey , Robert J. Foglesong , Michael L. Jones , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear , H. Scott Wilkinson , Michael Anthony Orsini
发明人： Michele L. R. Heffernan , Richard Dennis , James M. Dorsey , Robert J. Foglesong , Michael L. Jones , Cyprian O. Ogbu , Mustapha Soukri , Kerry L. Spear , H. Scott Wilkinson , Michael Anthony Orsini
IPC分类号： A61K31/407 , C07D491/048 , A61K31/497 , A61K31/5377
CPC分类号： C07D491/04
摘要： The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
摘要翻译：本发明涉及D-氨基氧化酶（DAAO）的稠合杂环抑制剂的前药和治疗疾病和病症的方法，其中D-氨基酸氧化酶活性，D-丝氨酸水平，D-丝氨酸氧化产物和NMDA受体活性的调节哺乳动物受试者的神经系统是有效的。

10. 发明申请

US20110319380A1 Compounds for Treating Disorders Mediated by Metabotropic Glutamate Receptor 5, and Methods of Use Thereof 有权
标题翻译：用于治疗由代谢型谷氨酸受体5介导的疾病的化合物及其使用方法
公开(公告)号：US20110319380A1
公开(公告)日：2011-12-29
申请号：US12972293
申请日：2010-12-17
申请人： Larry Wendell Hardy , Michele L. R. Heffernan , Frank Xinhe Wu , Kerry L. Spear , Lakshmi D. Saraswat
发明人： Larry Wendell Hardy , Michele L. R. Heffernan , Frank Xinhe Wu , Kerry L. Spear , Lakshmi D. Saraswat
IPC分类号： A61K31/517 , C07D417/10 , C07D413/04 , A61K31/5377 , A61P25/18 , C07D498/20 , C07D487/04 , A61P25/00 , A61P25/28 , C07D239/88 , C07D498/04
CPC分类号： C07D239/88 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/04 , C07D417/06 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/04 , C07D487/08 , C07D487/20 , C07D491/20 , C07D498/04
摘要： Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
摘要翻译：本文提供的化合物及其合成方法。本文所述的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍，神经变性疾病，神经精神障碍，认知障碍，学习或记忆障碍，胃肠道疾病，下尿路障碍和癌症。本文所述的化合物调节代谢型谷氨酸受体5（mGluR5）在中枢神经系统或周边的活性。本文还提供了含有化合物及其使用方法的药物制剂。

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