摘要:
The present invention relates to tripartite compounds comprising a modulator moiety for endosomal G protein-coupled receptors like neurokinin-1 receptor, a linker and a lipid anchor suitable for anchoring the tripartite compound into a plasma membrane. The present invention also relates to a prodrug and a pharmaceutical composition comprising the tripartite compound and the use of the tripartite compound for the treatment of a disease or disorder mediated by endosomal G protein-coupled receptors signalling like NK1R signalling.
摘要:
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
摘要:
Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are described
摘要:
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要:
Damage to the skin of the annular cowl (11) of the intake duct of a turbo-fan engine of an aircraft by exhausting on to it of hot air used within the cowl for de-icing its leading edge (10) is avoided by channelling spent air through an exhaust duct (15) to an exhaust aperture (21) in the surface of the cowl, and providing a heat shield (23) in the skin downstream of the exhaust aperture (21).
摘要:
Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译:提供式(I)化合物,其中T是CHO,COR 8或C(OH)R 1 R 2 2; R 1和R 2均为氢,任选取代的低级烷基,CF 3,任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是(CF 3)n烷基,(CF 3 N)N(S) (取代的烷基),(CF 3)n烷基苯基,(CF 3)n烷基(取代的苯基)或(C 3 -C 6)烷基 (F)环烷基; n = 1-3; 当Y-C时,R 5是氢,卤素,CF 3 O,与Y稠合的二烯,或Y-C时与Y稠合的取代的二烯; W,Y和Z是C,CR 6或N,其中W,Y或Z中的至少一个是C; R 6是氢,卤素或任选取代的低级烷基; X是O,S,SO 2或NR 7; R 7是氢,任选取代的低级烷基,任选取代的苄基或任选取代的苯基; 和R 8是低级烷基,CF 3或任选取代的苯基。 还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。
摘要:
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor.
摘要:
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor.
摘要:
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
摘要:
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.