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Piperidine derivatives as Selective antagonists of receptor subtypes n-methyl-d-aspartate

机译:哌啶衍生物作为受体亚型n-甲基-d-天冬氨酸的选择性拮抗剂

摘要

Refers to piperidine Derivatives of formula I wherein R1 is alkyl, alkoxy, alquilaminoalquilo alquenilo, among others; g is 0 - 3; H is 0 - 1; R2 and R3 are h, Oh, alkoxy, V is N (CH2)MK = o (CH2); n is 1 - 4; M is 0 - 4; b is 1 - aza - 2 - ciclobutanon - 3.4 - dilaurate, dirradical Aromatic heterocycle,No Aromatic or non Aromatic Tetrahydro Dihydro 5 members; dirradical Aromatic heterocycle substituted tetrahydro - oxo 5 members,Dirradical Aromatic heterocycle Aromatic or non Aromatic Tetrahydro not hexahidro 6 membersHeterocycle substituted Aromatic oxo not dirradical hexahidro with 6 members; heterocicleno Atoms which are attached to V and the phenyl Group is (x1) D are carbon Atoms; when BIs a Aromatic heterocycle containing can not understand and S = s or - S - (= o) 2; x1 is alquenilo, alkyl, alkoxy, aralquilo, halogen, Nitro, amino, haloalquilo,Among others; d is 0 - 2; e h o e,; and;And along with the phenylene Ring bicyclic form a condensate of 9 - 10 members; and 2 Atoms of the bicyclic Ring; and is a donor of hydrogen Atom contains a bicyclic ring.Preferred compounds are 6 - [5 - (4 - bencilpiperidin - 1 - methyl isoxazole) - 4,5-dihydro - - 3 - yl] - 3H - benzoxazole - 2 - One; (+) - 6 - (5 - [4 - (4-fluorobenzyl) piperidin-1-ylmethyl) - 4Dihidroisoxazol - 3 - 5 - il} - 3H - benzoxazole - 3-one among others.The compounds are antagonists of n-methyl-d-aspartate (NMDA) and may be useful for the treatment of Stroke, cerebral ischemia, CNS Disorders
机译:指式I的哌啶衍生物,其中R 1是烷基,烷氧基,alquilaminoalquilo alquenilo等。 g为0-3; H为0-1; R2和R3为h,Oh,烷氧基,V为N(CH2)MK = o(CH2); n为1-4; M是0-4; b为1-氮杂-2-环丙泛酸-3.4-二月桂酸酯,顺式芳族杂环,无芳族或非芳族四氢二氢5元;芳基杂环取代的四氢-氧代5元,芳基杂环杂环或非芳族四氢非六氢杂环化合物6元杂环取代的芳族非芳基六氢杂环化合物;连接至V且苯基为(x1)D的杂原子为碳原子;当BI所含的芳香杂环无法理解且S = s或-S-(= o)2时; x1是alquenilo,烷基,烷氧基,alalquilo,卤素,硝基,氨基,卤代alquilo,其他d是0-2; e h o e ;;并且与亚苯基环双环形成9-10元的缩合物;和2个双环原子;且是氢的供体Atom包含一个双环。首选化合物为6-[5-(4--苯并哌啶-1-甲基异恶唑)-4,5-二氢--3-yl]-3H-苯并恶唑-2-1 ; (+)-6-(5-[4-(4-氟苄基)哌啶-1-基甲基)-4Dihidroisoxazol-3-5-il}-3H-苯并恶唑-3-one等。该化合物是n-的拮抗剂天门冬氨酸甲酯(NMDA),可用于治疗中风,脑缺血,中枢神经系统疾病

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