DIAMINOPYRIMIDINE DERIVATIVES AND METHODS FOR PRODUCTION THEREOF Russian patent published in 2016 - IPC C07D403/12 C07D403/04 C07D413/14 C07D413/04 C07D401/04 A61K31/506 A61K31/5377 A61P1/12 A61P1/14 A61P1/00 

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to a novel compound of diaminopirimidine formula 1 or its pharmaceutically acceptable salts possessing the properties of 5-HT₄ receptors agonist. 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_1-2alkyl (where C_1-2alkyl optionally substituted with halogen), C_1-5alkoxy, C_1-5alkylthio, C_1-5alkoxycarbonyl and aminokarbonil, or heteroaryl group selected from a group consisting of furanyl, pyrrolyl, tiofenil, hinolinil, hromenonil, indolil, benzimidazole-4-yl, benzimidazole-5-yl, benzimidazole-6-yl, benzimidazole-7-yl and indazolil, herewith the heteroaryl group can be optionally substituted with one or more substitutes selected from a group consisting of C_1-5alkyl (where C_1-5alkyl optionally substituted with halogen) and C_1-5alkoxy, R₂ denotes a nitrogen-containing cyclic group selected from a group consisting of the following formulae from A to D (where * symbol in A-D formulae denotes the position of this group attachment to a compound of formula (1))

R₃ denotes C_1-5alkyl group, optionally substituted by phenyl, R₄ denotes hydrogen, C_1-5alkyl group optionally substituted with a substitute selected from a group consisting of hydroxy, C_1-5alkylamino, pyrrolidinyl and hydroxy-C-_1-5alkylamino; C_1-5alkoxycarbonyl group or amin-carbonyl group, R₅ denotes hydrogen, hydroxyl group; C_1-5alkoxy group; C_1-5alkyl group, optionally substituted with a substitute selected from a group consisting of amino and C_1-5alkoksikarbonilamino; or group selected from a group consisting of the following formulae of E to I (where * symbol in E-I formulae is the position of this group attachment to one of the of A-D formula compounds),

R₆ means hydrogen, hydroxyl group or C_1-5alkyl group optionally substituted with hydroxy, X denotes -CH(R₇)-, -C(=O)-, -N(R₈)- or -O-, R₇ means hydrogen; hydroxyl group; amino-carbonyl group; phenyl group or C_1-5alkyl group optionally substituted with hydroxy, R₄ and R₅, R₅ and R₆, R₄ and R₆ or R₅ and R₇ may be interconnected while forming 5- or 6-element ring; the said ring may be carbocyclic or additionally contain an oxygen atom as a heteroatom, R₈ denotes hydrogen or C_1-5alkyl group. Values of R₉-R₁₂ radicals are given in the patent claim.

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

8 cl, 38 tbl, 355 ex