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    • 8. 发明授权
    • Isoxazolopyridone derivatives and their use
    • 异恶唑吡啶酮衍生物及其用途
    • US07053219B2
    • 2006-05-30
    • US10732988
    • 2003-12-10
    • Masayuki NakamuraHideki KuriharaMitsuru OhkuboNaohiro Tsukamoto
    • Masayuki NakamuraHideki KuriharaMitsuru OhkuboNaohiro Tsukamoto
    • C07D471/22A61K31/44
    • C07D498/04
    • The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substituted phenyl or heteroaryl group, and R3a represents a methyl group, provided that, (1) when R1a is an unsubstituted phenyl group, then R2a must not be a para-substituted phenyl group of which the substituent is any of a methoxy group, a chloro group, a methyl group, a trifluoromethyl group, a fluoro group, a bromomethyl group or a dimethylaminomethyl group, and R2a must not be an unsubstituted heteroaryl group, and (2) when R1a is a 4-tolyl group or a 4-fluorophenyl group, then R2a must not be an unsubstituted phenyl group, a 4-methoxyphenyl group or a 4-fluorophenyl group, or their pharmaceutically-acceptable salts. The isoxazolopyridone derivatives or their pharmaceutically-acceptable salts of the invention have a metabotropic glutamic acid receptor-antagonistic effect, and are useful for remedy of, for example, anxiety disorders, psychosomatic disorders, obsessive-compulsive neurosis, bipolar disorders, melancholia, eating disorders, schizophrenia, multi-infarct dementia, Alzheimer disease, epilepsy, Parkinson disease, Huntington's chorea, pain or retrograde neurosis.
    • 本发明涉及式(Ia)的异恶唑吡啶酮衍生物:其中R 1a表示任选取代的杂芳基或苯基,R 2a表示任选取代的苯基或杂芳基 基团,且R 3a表示甲基,条件是(1)当R 1a为未取代的苯基时,R 2a必须 不是取代基是甲氧基,氯基,甲基,三氟甲基,氟基,溴甲基或二甲基氨基甲基中的任何一个的对位取代的苯基,R 2a, / SUP>不能是未取代的杂芳基,和(2)当R 1a是4-甲苯基或4-氟苯基时,R 2a不能 为未取代的苯基,4-甲氧基苯基或4-氟苯基,或其药学上可接受的盐。 本发明的异恶唑吡啶酮衍生物或其药学上可接受的盐具有代谢型谷氨酸受体拮抗作用,并且可用于治疗例如焦虑症,心理障碍,强迫性神经症,双相情感障碍,忧郁症,进食障碍 ,精神分裂症,多发性梗塞性痴呆,阿尔茨海默病,癫痫,帕金森病,亨廷顿舞蹈病,疼痛或逆行神经症。