FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to derivatives of adamantine of the formula (I): wherein D represents -CH2 or -CH2-CH2; E represents -C(O)NH or -NHC(O); each R1 and R2 represents independently hydrogen atom or halogen atom but R1 and R2 can't mean hydrogen atom simultaneously; R3 represents group of the formula: -R4-X-R5 (II) wherein R4 represents (C1-C6)-alkyl group; X represents oxygen or sulfur atom or the group NR13; R5 represents (C1-C6)-alkyl or (C2-C6)-alkenyl and each of them can be optionally substituted with at least one substitute taken among halogen atom, hydroxyl, di-(C1-C6)-alkylamino-group, -Y-R6, , and 5- or 6-membered heteroaromatic ring comprising 1-4 heteroatoms taken independently among nitrogen atom wherein heteroaromatic ring can be optionally substituted with at least one (C1-C6)-alkyl; Y represents oxygen or sulfur atom or the group -NH; R6 represents the group -R7Z wherein R7 represents (C2-C6)-alkyl group and Z represents -OH; when Y represents oxygen or sulfur atom or the group -NH then R6 represents additionally hydrogen atom, (C1-C6)-alkyl, (C1-C6)-alkylcarbonyl; R13 represents hydrogen atom, (C3-C8)-cycloalkyl, (C3-C8)-cycloalkylmethyl; or R13 represents (C1-C6)-alkyl group optionally substituted with at least one hydroxyl, or to its pharmaceutically acceptable salts or solvates. These compounds are effective antagonists of P2X7 receptors and can be used in treatment of rheumatic arthritis or lung chronic obstructive disease. Also, invention describes methods for preparing these compounds, pharmaceutical composition comprising indicated compounds, method for preparing pharmaceutical composition and their using in therapy.
EFFECT: improved preparing and treatment methods, valuable medicinal properties of compounds and composition.
19 cl, 1 tbl, 77 ex
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Authors
Dates
2006-03-20—Published
2000-12-12—Filed