Patent RU-2587493-C2 (RU)
Inventor: LEE HYUN-JOO
IPC: C07D405/14
Filed: 2012-02-24
Granted: 2016-06-20
Abstract: FIELD: pharmaceutics. 
     SUBSTANCE: present invention relates to a novel diaminopyrimidine derivative formula 1 or pharmaceutically acceptable salts thereof possessing properties of agonist of 5-HT 4  receptors. In formula 1 
        (Formula 1) 
     R 1  denotes a phenyl group substituted with one or more substitutes selected from a group consisting of hydroxy, amino, halogen, cyano, nitro, C 1-5 alkyl (where C 1-5 alkyl is optionally substituted with halogen), C 1-5 alkoxy, C 1-5 alkylthio, C 1-5 alkoxycarbonyl, 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 1-5 alkyl (where C 1-5 alkyl is optionally substituted with halogen) and acetyl, R 2  denotes hydrogen; C 1-5 alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, C 1-5 alkoxy, benzylamino (where benzylamino is optionally substituted by halogen), phenylamino, C 1-5 alkylamino, C 3-6 cycloalkylamino and hydroxy-C 1-5 alkylamino; C 1-5 alkoxycarbonyl group or formyl group, R 3  denotes hydrogen, hydroxyl group; C 1-5 alkyl group, optionally substituted with a substitute selected from a group consisting of C 1-5 alkoxycarbonylamino and di-C 1-5 alkylamino, 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), 
     
       
     
     R 4  denotes hydrogen, R 5  denotes C 1-5 alkyl group, optionally substituted phenyl or C 2-6 alkenyl group, optionally substituted phenyl or C 3-6 cycloalkyl, R 6  denotes C 1-10 alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, halogen, C 1-5 alkoxy, amino, C 1-5 alkoxycarbonylamino, benzyloxycarbonylamino, di-C 1-5 alkylamino, C 1-5 alkoxy-C 1-5 alkyloxy, phenoxy, benzyloxy, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, amino and C 1-5 alkoxy), thiophenyl, pyridinyl, piperidinyl, piperazinyl (where piperazinyl is optionally substituted with benzyl) and acetyl; C 3-6 cycloalkyl group; piperidinyl group; C 1-10 alkenyl group, optionally substituted phenyl; trifluoromethyl group, trifluoroethyl group or a phenyl group optionally substituted with halogen, R 7  denotes hydrogen, R 8  and R 9  each independently denote hydrogen; C 1-10 alkyl group, optionally substituted with substitute selected from a group consisting of amino, C 1-5 alkoxycarbonylamino, hydroxy, C 1-5 alkylthio, C 3-10 cycloalkyl, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of hydroxy, C 1-5 alkyl, mono-or di-C 1-5 alkylamino, trifluoromethyl, halogen, C 1-5 alkoxy C 1-5 alkylcarbonyloxy), thiophenyl, pyrrolyl, furanyl (where furanyl is optionally substituted with mono-or di-C 1-5 alkyl), pyridinyl and benzyloxy; piperidinyl group, optionally substituted benzyl, benzoyl, C 1-5 alkyl or C 1-5 alkylcarbonyl; azetidinyl group, optionally substituted C 1-5 alkoxycarbonyl; C 1-5 alkylsulphonyl group or C 3-10 cycloalkyl 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