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(19)

RU

(11)

2 286 986

(13)

C2

(51)

IPC

C07D209/52(2006-01-01)

C07D403/12(2006-01-01)

A61K31/403(2006-01-01)

A61P3/04(2006-01-01)

A61P3/06(2006-01-01)

A61P3/10(2006-01-01)

(21) (22)

Application

2002125491/04, 2001-03-05

(24)

Start date

2001-03-05

(22)

Actual filing date

2001-03-05

(45)

Published

2006-11-10

(72)

Inventor

Robl Dzheffri A.Salski Richard B.Odzheri Dehvid Dzh.Mehgnin Dehvid R.Khehmehnn Lourens G.Betebenner Dehvid A.

(73)

Holder

Bristol-Maers Skvibb Ko.

DIPEPTIDYL PEPTIDASE IV INHIBITORS BASED ON CONDENSED CYCLOPROPYLPYRROLIDINES AND METHOD FOR THEIR USING Russian patent published in 2006 - IPC C07D209/52 C07D403/12 A61K31/403 A61P3/04 A61P3/06 A61P3/10 

Abstract RU 2286986 C2

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel condensed cyclopropylpyrrolidines of the formula: wherein x means 0 or 1 and y means 0 or 1 under condition that x means 1 when y means 0, and x means 0 when y means 1; and wherein n means 0 or 1; X means hydrogen atom (H) of group -CN; R1, R2, R3 and R4 are similar or different and chosen independently from H, (C1-C10)-alkyl, (C2-C12)-alkenyl, saturated (C3-C10)-cycloalkyl, saturated (C3-C10)-cycloalkyl-(C1-C10)-alkyl, saturated (C3-C10)-bicycloalkyl, saturated (C3-C10)-tricycloalkyl, hydroxyl-(C1-C10)-alkyl-saturated (C3-C10)-cycloalkyl, (C1-C10)-alkylthio-(C1-C10)-alkyl, (C6-C10)-aryl-(C1-C10)-alkylthio-(C1-C10)-alkyl, (C6-C10)-aryl-(C1-C10)-alkyl, 5- or 6-membered heteroaryl comprising one nitrogen atom (N) or one oxygen atom (O), 5- or 6-membered heteroaryl comprising one atom N condensed with (C6-C10)-aryl ring, 5- or 6-membered heteroaryl comprising one atom N or one atom O, (C1-C10)-alkyl, cycloheteroalkyl that represents (C5-C8)-saturated ring comprising one heteroatom, such as N or O; if necessary, all compounds comprise 1, 2, 3, 4 or 5 groups of substitutes at corresponding carbon atom chosen from halogen atom, (C1-C10)-alkyl, (C2-C12)-alkenyl, hydroxy-group, hydroxy-(C1-C10)-alkyl or cyano-group; R1 and R4 can form in common, if necessary, the group -(CR5R6)m- wherein m means 2-6, and R5 and R6 are similar or different and chosen independently from hydroxy-group, H or (C1-C10)-alkyl including all their stereoisomers; and their pharmaceutically acceptable salt, or prodrug esters and all their stereoisomers. These compound inhibit activity of dipeptidyl peptidase IV that allows their using in pharmaceutical compositions used in treatment of diabetes mellitus of type-2.

EFFECT: valuable medicinal properties of compounds.

20 cl, 6 tbl, 113 ex

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RU 2 286 986 C2

Authors

Robl Dzheffri A.

Salski Richard B.

Odzheri Dehvid Dzh.

Mehgnin Dehvid R.

Khehmehnn Lourens G.

Betebenner Dehvid A.

Dates

2006-11-10—Published

2001-03-05—Filed

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