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    • 4. 发明申请
    • SULPHONAMIDE DERIVATIVES OF BENZYLAMINE FOR THE TREATMENT OF CNS DISEASES
    • 苯甲酰胺用于治疗CNS疾病的磺酰胺衍生物
    • WO2013140347A1
    • 2013-09-26
    • PCT/IB2013/052204
    • 2013-03-20
    • ADAMED SP. Z O.O.
    • KOŁACZKOWSKI, MarcinMARCINKOWSKA, MonikaBUCKI, AdamŁYSAKOWSKI, TomaszPAWŁOWSKI, Maciej
    • C07C311/21C07D403/12C07D413/14C07D319/18C07D405/12C07D407/12C07D409/12C07D413/12C07D417/12C07D261/20C07D487/04C07D209/08C07D307/79A61K31/18A61P25/00
    • C07D487/04C07C311/21C07D209/08C07D261/20C07D307/79C07D319/18C07D403/12C07D405/12C07D407/12C07D409/12C07D413/12C07D413/14C07D417/12
    • Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted;or 9-or 10-membered bicyclic group, linked to –(O) x - (CH 2 ) y -through one of its aromatic carbon atoms,consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5-or 6-membered non-aromaticheterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C 1 -C 3 - alkyls; D represents a group selected from:phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted;thiophene unsubstituted or substituted;bicyclic group consisting of imidazolering fused with5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2heteroatoms independently selected from the group consisting of N, O and S, unsubstituted or substituted and linked to sulphonamide moiety through one of carbon atoms of benzene ring;and bicyclic group consisting of benzene ring fused with -or 6-membered non-aromatic heterocyclic ring having 1 or 2heteroatoms independently selected from the group consisting of N and O, unsubstituted or substituted, and linked to sulphonamide moiety through one of carbon atoms of benzene ring;R represents H or –CH 3;x is 0 or 1;yis 2 or 3;and pharmaceutically acceptable salts and solvates thereof, with the provisos that if x is 0 and y is 2, then D is naphthyl unsubstituted or substituted with one halogen atom, and if R represents –CH 3, then A is not unsubstituted or substituted phenyl. The compounds can be used in the treatment and/or prophylaxis of central nervous system disorders.
    • 式(I)的苄胺的磺酰胺衍生物,其中A表示未取代或取代的苯基;或与 - (O)x - (CH 2)y连接的9或10元双环,通过其芳族碳原子之一, 由含有1或2个独立地选自N和O的杂原子的含有杂芳环的苯环稠合,其中这样的双环基团是未取代的或取代的,或具有1或2个的5-或6-元非芳族杂环 O原子,其中杂环是未取代的或被一个或多个C 1 -C 3 - 烷基取代; D表示选自以下的基团:未取代或取代的苯基; 未取代或取代的萘基;未取代或取代的噻吩;由5元非芳族碳环稠合的咪唑啉组成的双环; 由与5-元杂芳环稠合的苯环组成的双环基团,具有独立地选自N,O和S的1或2个杂原子,未取代或取代并通过苯环的碳原子连接到磺酰胺部分;和双环 由具有1或2个独立选自N和O的未取代或取代的杂原子的6元非芳香杂环稠合的苯环,和通过苯环的碳原子与磺酰胺部分连接的苯环; R表示H或-CH 3; x为0或1; yis 2或3;及其药学上可接受的盐和溶剂合物,条件是如果x为0且y为2,则D为未取代的或被一个卤素取代的萘基 原子,如果R表示-CH 3,则A不是未取代的或取代的苯基。 所述化合物可用于治疗和/或预防中枢神经系统疾病。