5-HT RECEPTOR MODULATORS AND METHODS FOR USING THEM

FIELD: medicine, pharmaceutics.SUBSTANCE: in general formula, fragment A is specified in a group consisting of,or, R, R, Rand Rmean hydrogen or alkyl; each of Rand Rrepresents hydrogen; Grepresents aryl or heteroaryl, which can by unsubstituted or substituted by 1, 2, 3, 4 or 5 substitutes specified...

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Hauptverfasser: SHEKKHAR SHASHANK, AKRITOPOULOU-ZANZE IRINI, UEHLCH DENNI S, TOMPSON KRISTINA M, LI KHUAN'TSJU, BRAJE VIL'FRID, GANDARILLA KHORKHE, UILSON NOEHL' S, D'JURIK STIVEN V, TERNER SHON K, GASIKI ALAN F, CHZHAN MIN, CHZHAO KHUNJUJ, KRUDZHER AL'BERT V, RELO ANA-LJUSIJA
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: medicine, pharmaceutics.SUBSTANCE: in general formula, fragment A is specified in a group consisting of,or, R, R, Rand Rmean hydrogen or alkyl; each of Rand Rrepresents hydrogen; Grepresents aryl or heteroaryl, which can by unsubstituted or substituted by 1, 2, 3, 4 or 5 substitutes specified in a group consisting of alkyl, halogen, cyano, -OR, -S(O)R, -C(O)R, -C(O)OR, -OC(O)N(R)(R), -(CRR)-OR, -C(OH)[(CRR)-R], and halogenalkyl; Gmeans cycloalkyl, cycloalkenyl or heterocycle unsubstituted or substituted by 1, 2, 3, 4 or 5 substitutes specified in a group consisting of alkyl; Rrepresents hydrogen or alkyl; Rand Rrepresents hydrogen, alkyl or halogenalkyl; Rrepresents alkyl; Rand Rrepresents hydrogen, halogen, alkyl or halogenalkyl; m represents 1, 2, 3, 4 or 5; Ris specified in a group consisting of hydrogen, alkyl, -(CRR)-Gand -S(O)R, Rrepresents G, Xmeans N or CR; Xmeans N or CR; Xmeans CR; Xmeans N or CR; provided one fragment of X, Xor Xcan represent N; each of R, R, R, R, Rand Rindependently represents hydrogen, alkyl, alkenyl, halogen, -G, -G, -OR, -C(O)G, -C(O)OR, -C(O)N(R)(R), -N(R)(R), -(CRR)-G, -CR=CR-G, -(CRR)-G, -CR=C(R), halogenalkyl and fragment; Rand Rrepresents hydrogen, alkyl, haloalkyl, G, -(CRR)-G, Gor -(CRR)-G; Ris alkyl or halogenalkyl; Rrepresents hydrogen, alkyl or helogenalkyl; Grepresents heterocycle attached to an adjoining carbonyl fragment through a nitrogen atom being a part of heterocycle; or Rand Ror Rand Rtogether with carbon atoms which they are attached to, form unsubstituted phenyl or cycloalkyl; Ymeans NR, CRR, C(O), S(O)or O; Ymeans NR, CRRor C(O); Ymeans NR, CRRor C(O); or Yand Ytogether represent CR=CR, n means 2; Rrepresents hydrogen; Rand Rrepresents hydrogen; and Ris specified in a group consisting of hydrogen, alkyl and -S(O)-G.EFFECT: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts possessing the properties of a 5-HTand/or 5-HTreceptor modulator, to a based pharmaceutical composition and to methods for preparing them.33 cl, 7 tbl, 20 dwg, 278 ex Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солям, обладающим свойствами модулятора рецептора 5-HTи/или 5-НТ, фармацевтической композиции на их основе и способам их получения. В общей формуле (I) фрагмент А выбран из группы, состоящей из (i), (ii) или (iii), R, R, Rи Rозначают водород или алкил; каждый из Rи Rпредставляет собой водород; Gпредставляет собой арил или гетероарил, который может