首页> 外国专利> compound, methods for increasing the concentration of d-serine and / or decreasing the concentration of toxic d-serine oxidation by donation in a mammal, to treat schizophrenia, to treat or prevent associated memory and / or cognition loss. with Alzheimer's disease, to treat ataxia or to prevent loss of neuronal function characteristic of neurodegenerative diseases, to enhance learning, memory and / or cognition and to treat neuropathic pain, and, pharmaceutical composition

compound, methods for increasing the concentration of d-serine and / or decreasing the concentration of toxic d-serine oxidation by donation in a mammal, to treat schizophrenia, to treat or prevent associated memory and / or cognition loss. with Alzheimer's disease, to treat ataxia or to prevent loss of neuronal function characteristic of neurodegenerative diseases, to enhance learning, memory and / or cognition and to treat neuropathic pain, and, pharmaceutical composition

机译:化合物,通过在哺乳动物中捐献来增加d-丝氨酸浓度和/或降低毒性d-丝氨酸氧化浓度的方法,以治疗精神分裂症,以治疗或预防相关的记忆和/或认知丧失。阿尔茨海默氏病,治疗共济失调或预防神经退行性疾病的神经元功能丧失,增强学习,记忆和/或认知并治疗神经性疼痛以及药物组合物

摘要

"COMPOSITE, METHODS FOR INCREASING CONCENTRATION OF D-SERINE AND / OR DECREASING CONCENTRATION OF DAAO TOXIC D-SERINE OXIDATION IN A MAMMER, TO TREAT SCHIZOPHRENIA, TO TREAT OR PRECERATE OR PRECERATE ASSOCIATED WITH ALZHEIMER EVIL, TO TREAT ATAXIA OR TO PREVENT LOSS OF NEURONAL FUNCTION CHARACTERISTIC OF NEURODEGENERATIVE DISEASES, TO INCREASE LEARNING, MEMORY AND / OR COGNITION, AND TO TREAT NEURODIA. Methods for increasing the concentration of D-Serine and reducing the concentration of toxic D-Serine oxidation products, 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 disorders involves administering to a patient in need of treatment a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein R¬1¬ and R¬2 ¬ are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl and XYR¬ 5¬; or R 1 and R 2 taken together form a substituted or unsubstituted 5-, 6-, 7- or 8-membered carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH and (CR¬ 6¬R¬ 7¬) ~ n ~; R¬ 3¬ is hydrogen, alkyl or M +; M is aluminum ion, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; Z is N or CR¬4¬; R¬ 4¬ is selected from hydrogen, halo, nitro, alkyl, alkylaryl and XYR¬ 5¬; R¬5¬ is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R¬6¬ and R¬7¬ are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R¬ 1¬, R¬ 2¬ and R¬ 4¬ is other than hydrogen; and at least one of X and Y is (CR¬ 6¬R¬ 7¬) ~ n ~. D-serine or cycloserine may be co-administered together with the compound of formula (I).
机译:“在孕妇中增加D-丝氨酸浓度和/或降低DAAO毒性D-丝氨酸氧化,治疗精神分裂症,治疗或预防或预防与老年痴呆有关的方法,预防或预防失语的复合物,方法神经退行性疾病的神经功能特征,以增加学习,记忆和/或认知,以及治疗神经病。增加D-丝氨酸浓度和降低有毒D-丝氨酸氧化产物浓度的方法,以增强学习,记忆和/认知或用于治疗精神分裂症,阿尔茨海默氏病,共济失调或神经性疼痛或预防神经退行性疾病特征的神经元功能丧失涉及向需要治疗的患者给药治疗有效量的式(I)化合物或药学上可接受的盐或其溶剂化物:其中R 1和R 2各自独立地选自氢,卤素,硝基,烷基,酰基,烷基芳基和XYR 5-; R 1和R 2一起形成取代或未取代的5、6、7或8元碳环或杂环基;或X和Y独立地选自O,S,NH和(CR 6 -R 7-)〜n〜; R 3-是氢,烷基或M +; M为铝离子,钙,锂,镁,钾,钠,锌或其混合物; Z是N或CR 4-; R 4选自氢,卤素,硝基,烷基,烷基芳基和XYR 5; R 5-选自芳基,取代的芳基,杂芳基和取代的杂芳基; R 6和R 7独立地选自氢和烷基; n为1至6的整数; R 1,R 2和R 4中的至少一个不是氢。 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)化合物一起共同给药。

著录项

  • 公开/公告号BRPI0418244A

    专利类型

  • 公开/公告日2007-04-17

    原文格式PDF

  • 申请/专利权人 SEPRACOR INC.;

    申请/专利号BR2004PI18244

  • 发明设计人 Q. KEVIN FANG;SETH HOPKINS;STEVEN JONES;

    申请日2004-12-28

  • 分类号C07D231/54;A61K31/401;A61K31/403;A61K31/405;A61K31/415;A61K31/416;C07D207/34;C07D209/42;C07D209/44;C07D231/14;C07D231/16;C07D231/56;C07D491/04;

  • 国家 BR

  • 入库时间 2022-08-21 20:59:24

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