Patent RU-2345067-C2 (RU)
Inventor: EDVARDS POL DZHON
IPC: C07D213/42
Filed: 2005-02-25
Granted: 2009-01-27
Abstract: FIELD: chemistry, pharmaceutics. 
     SUBSTANCE: claimed invention relates to novel compounds of general formula (I) Z-C(R 1 R 2 )-C(R 3 NH 2 )-C(R 4 R 5 )-X-N(R 6 R 7 ) (I), or its pharmaceutically acceptable salt which is different because Z represents phenyl; where Z can be substituted with one or more R 8 , where R 8  represents halogen; R 1 , R 4  represent H; R 2 , R 5  represent H; R 3  represents H; X is selected from group consisting of S(O) 2  and C(O); R 6 , R 7  are independently selected from group consisting of H, (C(R 29 R 30 )) m -X 1 -Z 1  and (C(R 31 R 32 )) n -X 2 -X 3 -Z 2  and C 1-4 alkyl, which carries substitution with one or more R 29a , where R 29a  is independently selected from group consisting of R 29b  and Z 1 , on condition that R 6  and R 7  are selected in such way that R 6  and R 7  were not simultaneously independently selected from group consisting of H, CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3  and CH(CH 3 ) 2 ; R 29  R 29b , R 30 , R 31 , R 32  are independently selected from group consisting of H, C 1-6 alkyl and N(R 32a )-C 1-6 alkyl; R 32a  represents C 1-6 alkyl; m is 0, 1 or 2; n is 2; X 1  is independently selected from group consisting of covalent bond, -C 1-6 alkyl and -C 1-6 alkyl-N(R 33 )-; X 2  represents -N(R 35 )-; X 3  represents -C(O)-; R 33  represents C 1-6 alkyl; R 35  represents H; Z 1 , Z 2  are independently selected from group consisting of Z 3  and -C(R 37a )Z 3a Z 3b ; R 37a  represents H; Z 3 , Z 3a , Z 3b  are independently selected from group consisting of T 1 , T 2 , C 1-6 alkyl, C 1-6 alkyl-T 1  and C 1-6 alkyl-T 2 ; T 1  represents phenyl; where T 1  is optionally substituted with one or more R 38 ; R 38  being independently selected from group consisting of halogen, CN, R 39 , C(O)NH 2 , S(O) 2 NH 2 , OT 3 , C(O)N(R 40 )T 3  and T 3 , T 2  is selected from group consisting of C 3-7 cycloalkyl, indanyl, tetralinyl, heterocycle and heterobicycle, T 2  optionally carries substitution with one or more R 41 , where R 41  is independently selected from group consisting of halogen, R 42 , OH and T 3 ; R 39  is selected from group consisting of C 1-6 alkyl, O-C 1-6 alkyl, S-C 1-6 alkyl, C(O)N(R 44 )-C 1-6 alkyl, S(O)-C 1-6 alkyl and S(O) 2 -C 1-6 alkyl, where each C 1-6 alkyl optionally carries substitution with one or more R 45 , where R 45  is independently selected from group consisting of F, N(R 46 R 47 ) and T 3 ; R 42  represents C 1-6 alkyl, each C 1-6 alkyl optionally carries substitution with one or more R 45 , where R 45  is independently selected from group consisting of F; R 40 , R 46 , R 47  are independently selected from group consisting of H and C 1-6 alkyl; R 44  represents H; T 3  is selected from group consisting of T 4  and T 5 ; T 4  represents phenyl, where T 4  optionally carries substitution with one or more R 51 , where R 51  is independently selected from group consisting of halogen, OR 52 , S(O) 2 N(R 52 R 53 ), C 1-6 alkyl; R 52 , R 53  are independently selected from group consisting of H and C 1-6 alkyl; T 5  is selected from group consisting of heretocycle C 3-7 cycloalkyl, where T 5  optionally carries substitution with one or more R 54 , where R 54  represents C 1-6 alkyl; where heterocycle represents ring of cyclobutane, cyclopentane, cyclohexane, which can contain double bonds in number up to maximal, or aromatic or non-aromatic ring which is fully or partially saturated or unsaturated, and in which at least one carbon atom, maximally up to four carbon atoms, are substituted with heteroatom, selected from group including oxygen and nitrogen, and where ring is bound with remaining part of molecule through carbon or nitrogen atom; where heterobicycle represents heterocycle as stated above, which is condensed with phenyl or other heterocycle with formation of bicyclic ring system, on condition that the following compound is excluded from claim:3-amino-N-cyclohexyl-4-phenylbutyramide. Invention also relates to pharmaceutical composition based on compound of general formula (I) and to their application for manufacturing medication for treatment and/or prevention of conditions during which it is desirable to inhibit DPP-IV. 
     EFFECT: obtaining novel group of compounds possessing useful biological properties. 
     26 cl, 8 tbl, 193 ex