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1. 发明公开

KR1020060128978A 벤조［디］이속사졸３올 디에이에이오 억제제 无效
标题翻译： BENZO [D] ISOXAZOL-3-OL DAAO抑制剂
公开(公告)号：KR1020060128978A
公开(公告)日：2006-12-14
申请号：KR1020067015383
申请日：2004-12-28
申请人： 선오비온 파마슈티컬스 인코포레이티드
发明人： 팡,큐.케빈 , 홉킨스,세쓰 , 헤퍼낸,미첼레 , 치틸,밀란 , 위프,피터
IPC分类号： C07D261/20 , C07D487/04
CPC分类号： C07D261/20
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D- Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: I wherein Z1 is N or CR3; Z2 is N or CR4; Z3 is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.
摘要翻译：增加D-丝氨酸浓度和减少D-丝氨酸氧化的毒性产物浓度，增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛或预防神经功能丧失的方法神经变性疾病的特征包括向需要治疗的受试者施用治疗量的式I化合物或其药学上可接受的盐或溶剂化物：其中Z 1是N或CR 3; Z2为N或CR4; Z3为O或S; A是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌或它们的混合物; R 1，R 2，R 3和R 4独立地选自氢，烷基，羟基烷氧基，芳基，酰基，卤素，氰基，卤代烷基，NHCOOR 5和SO 2 NH 2; R5是芳基，芳基烷基，杂芳基或杂芳基烷基; R 1，R 2，R 3和R 4中的至少一个不是氢; 并且Z1和Z2中的至少一个不是N.

2. 发明公开

KR1020060128976A 피롤 및 피라졸 디에이에이오 억제제 无效
标题翻译：吡咯和吡唑多糖抑制剂
公开(公告)号：KR1020060128976A
公开(公告)日：2006-12-14
申请号：KR1020067015379
申请日：2004-12-28
申请人： 선오비온 파마슈티컬스 인코포레이티드
发明人： 팡,큐.,케빈 , 홉킨스,세쓰 , 헤퍼낸,미첼레 , 치틸,밀란
IPC分类号： C07D231/14 , C07D231/56
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D- Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof: (I) wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7) n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R 1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula (I).
摘要翻译：增加D-丝氨酸浓度和降低D-丝氨酸氧化的毒性产物浓度，增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛或预防神经元功能特征丧失的方法的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式（I）化合物或其药学上可接受的盐或溶剂化物：（I）其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR 5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式（I）化合物一起共同施用。

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