DIAMINOPYRIMIDINE DERIVATIVES AND METHODS FOR PRODUCTION THEREOF Russian patent published in 2016 - IPC C07D405/14 C07D403/14 C07D403/12 C07D403/04 C07D401/04 A61K31/506 A61P1/00 A61P1/12 A61P1/14 

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to a novel diaminopyrimidine derivative formula 1 or pharmaceutically acceptable salts thereof possessing properties of agonist of 5-HT₄ receptors. In formula 1

(Formula 1)

R₁ denotes a phenyl group substituted with one or more substitutes selected from a group consisting of hydroxy, amino, halogen, cyano, nitro, C_1-5alkyl (where C_1-5alkyl is optionally substituted with halogen), C_1-5alkoxy, C_1-5alkylthio, C_1-5alkoxycarbonyl, aminosulphonyl and benzyloxycarbonylamino; or heteroaryl group selected from a group comprising pyridinyl, quinolinyl, chromenonyl, indolyl, indolinyl and benzimidazolyl, wherein heteroaryl group can be optionally substituted with one or more substitutes selected from a group consisting of C_1-5alkyl (where C_1-5alkyl is optionally substituted with halogen) and acetyl, R₂ denotes hydrogen; C_1-5alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, C_1-5alkoxy, benzylamino (where benzylamino is optionally substituted by halogen), phenylamino, C_1-5alkylamino, C_3-6cycloalkylamino and hydroxy-C_1-5alkylamino; C_1-5alkoxycarbonyl group or formyl group, R₃ denotes hydrogen, hydroxyl group; C_1-5alkyl group, optionally substituted with a substitute selected from a group consisting of C_1-5alkoxycarbonylamino and di-C_1-5alkylamino, or group selected from a group consisting of following formulae A, B, D and E (where symbol * in formulae A, B, D and E denotes position of attachment of said group of compounds of formula 1),

R₄ denotes hydrogen, R₅ denotes C_1-5alkyl group, optionally substituted phenyl or C_2-6alkenyl group, optionally substituted phenyl or C_3-6cycloalkyl, R₆ denotes C_1-10alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, halogen, C_1-5alkoxy, amino, C_1-5alkoxycarbonylamino, benzyloxycarbonylamino, di-C_1-5alkylamino, C_1-5alkoxy-C_1-5alkyloxy, phenoxy, benzyloxy, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, amino and C_1-5alkoxy), thiophenyl, pyridinyl, piperidinyl, piperazinyl (where piperazinyl is optionally substituted with benzyl) and acetyl; C_3-6cycloalkyl group; piperidinyl group; C_1-10alkenyl group, optionally substituted phenyl; trifluoromethyl group, trifluoroethyl group or a phenyl group optionally substituted with halogen, R₇ denotes hydrogen, R₈ and R₉ each independently denote hydrogen; C_1-10alkyl group, optionally substituted with substitute selected from a group consisting of amino, C_1-5alkoxycarbonylamino, hydroxy, C_1-5alkylthio, C_3-10cycloalkyl, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of hydroxy, C_1-5alkyl, mono-or di-C_1-5alkylamino, trifluoromethyl, halogen, C_1-5alkoxy C_1-5alkylcarbonyloxy), thiophenyl, pyrrolyl, furanyl (where furanyl is optionally substituted with mono-or di-C_1-5alkyl), pyridinyl and benzyloxy; piperidinyl group, optionally substituted benzyl, benzoyl, C_1-5alkyl or C_1-5alkylcarbonyl; azetidinyl group, optionally substituted C_1-5alkoxycarbonyl; C_1-5alkylsulphonyl group or C_3-10cycloalkyl group.

EFFECT: invention relates to use of formula 1 or its pharmaceutically acceptable salt for preparing a drug for preventing or treating gastrointestinal motility dysfunction; gastrointestinal motor dysfunction is gastroesophageal reflux disease (GERD), lock (constipation), irritable bowel syndrome (IBS), dyspepsia, postoperative intestinal obstruction, prolonged gastric emptying, gastroparesis, intestinal pseudo-obstruction,drug-induced delayed transit content over colon or diabetic gastroparesis.

9 cl, 54 tbl, 495 ex