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Pharmaceutical compositions containing compounds with bridged and unbridged heterocyclic groups, spiro-connected with oxazoline and thiazoline groups, and some new such compounds

机译:药物组合物,其包含具有桥连和未桥连的杂环基,并与恶唑啉和噻唑啉基螺线连接的化合物以及一些新的此类化合物

摘要

Compounds (I) and (II), including enantiomers, racemates and acid addition and quaternary salts, are for treating diseases of the central and peripheral nervous system, CHEM wherein in formula (I) Q is (CH2)m or C(CH3)2 attached to the 1 min ,4 min or 1 min ,5 min positions of the six-membered ring (m = 1, 2 or 3,) and in formula (II) Q is two hydrogen atoms, (CH2)m or C(CH3)2(m = 1, 2 or 3) and n and p are each independently 0, 1, 2 or 3, provided that n + p = 1-3; R DEG is hydrogen, methyl or OH; CHEM R and R min are independently H, NH2, NH-C1-6-alkyl, N(C1-6-alkyl)2, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7- cycloalkyl, C1-6-alkyl substituted by 1-6 halogen atoms, HO- C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, C1-6-alkoxy-C1-6-alkyl, carboxy-C1-6-alkyl, (C1-6-alkoxy)carbonyl-C1-6-alkyl, amino-C1-6-alkyl, mono-(C1-6-alkyl)amino-C1-6-alkyl, di-(C1-6-alkyl)amino-C1-6-alkyl, 2-oxo-pyrrolidin-1-yl-methyl, Ar, di(Ar)methylol, or (Ar)1-2C1-6-alkyl, or R min may be C1-6-alkanoyl or Arcarbonyl; and Ar denotes Ph optionally substituted by 1-3 of halogen, C1-6-alkyl, C1-6-alkoxy and CF3, subject to certain provisos.
机译:化合物(I)和(II),包括对映异构体,外消旋体和酸加成盐和季盐,用于治疗中枢神经系统和周围神经系统疾病,其中式(I)中的Q为(CH2)m或C(附着在六元环的1分钟,4分钟或1分钟,5分钟位置上的CH3)2(m = 1、2或3,),在式(II)中Q是两个氢原子(CH2)m或C(CH3)2(m = 1、2或3),且n和p分别独立为0、1、2或3,前提是n + p = 1-3; R DEG为氢,甲基或OH; R和R min独立地为H,NH 2,NH-C 1-6烷基,N(C 1-6烷基)2,C 1-6烷基,C 2-6烯基,C 2-6炔基,C 3 -7-环烷基,被1-6个卤原子取代的C1-6-烷基,HO-C1-6-烷基,C1-6-烷氧基,C1-6-烷硫基,C1-6-烷氧基-C1-6-烷基,羧基-C1-6-烷基,(C1-6-烷氧基)羰基-C1-6-烷基,氨基-C1-6-烷基,单-(C1-6-烷基)氨基-C1-6-烷基,二- (C 1-6-烷基)氨基-C 1-6-烷基,2-氧代-吡咯烷基-1-基-甲基,Ar,二(Ar)羟甲基或(Ar)1-2 C 1-6-烷基,或R min可以是C 1-6烷酰基或芳羰基;且Ar表示在一定条件下可任选被1-3个卤素,C 1-6烷基,C 1-6烷氧基和CF 3取代的Ph。

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