LIGANDS FOR H-HISTAMINE RECEPTOR Russian patent published in 2003 - IPC

Abstract RU 2214406 C2

FIELD: organic chemistry, medicine, pharmacology. SUBSTANCE: invention relates to compounds of the formula (I): where A is ; m = from 1 to 3; B is ; n = from 1 to 3; x = from 0 to 2; R1 is taken among hydroxy- group, C1-C9-alkoxy-group optionally substituted with halogen atom, C1-C9-cycloalkyloxy-group wherein cycloalkyl group is optionally substituted with C1-C4-alkyl or halogen atom and alkoxyl group is optionally substituted with halogen atom, arylalkoxy-group wherein aryl group is optionally substituted with C1-C4-alkyl, C1-C3-alkoxy-group or halogen atom and alkoxy-group is optionally substituted with halogen atom and C1-C9- alkylamino-group wherein alkyl group is optionally substituted with halogen atom; R2 is taken among hydrogen atom, alkyl, aryl, arylalkyl, cycloalkyl and cycloalkylalkyl wherein alkyl groups are optionally substituted with halogen atom and aryl group optionally substituted with C1-C4-alkyl, C1-C4-alkoxy-group or halogen atom; R3 is hydrogen atom, C1-C7-alkyl or benzyl when Y-Z-R2 is not added to W; R3 is absent when Y-Z-R2 is added to W; W is nitrogen atom; X is or ; R4 is hydrogen atom or C1-C3-alkyl; Y substitutes hydrogen atom in any among A, B, W and X and means C2-C10-alkylene wherein one terminal carbon atom can be substituted with oxygen atom; Z means ; ; ; ; or ; R5 and R7 are taken independently among hydrogen atom, aryl-(C1-C3)-alkyl and cycloalkyl-(C1-C3)-alkyl and they are optionally substituted with halogen atom; Q means hydrogen atom or methyl or Q is bound with R5 or R7 to form five-membered ring; or Q is bound with R2 to form six-membered ring under condition that when Z means then at least one of R5 and R7 means aryl-(C1-C3)-alkyl or cycloalkyl-(C1-C3)-alkyl optionally substituted with halogen atom; or to its pharmaceutically acceptable salt and to pharmaceutical composition eliciting ability to bind with H3-histamine receptors and comprising effective amount of compound of the general formula (I). Proposed compounds relate to class of low-toxic drugs and can be used in therapy as sedative agents, sleep regulating agents, anticonvulsive agents, regulating agents of hypothalamus-hypophysis secretion, antidepressants, modulating agents of cerebral circulation, in asthma and irritable bowel syndrome treatment. EFFECT: valuable medicinal properties of compounds. 11 cl, 1 tbl, 17 dwg, 143 ex

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RU 2 214 406 C2

Authors

Kalindzhan Sarkis Behrret

Bak Ildiko Marija

Linni Jan Dunkan

Vatt Dzhillian Fehrful

Kharper Ehlejn Anne

Shehnkli Najdzhel Pol

Dates

2003-10-20Published

1999-02-15Filed