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filingDate 1997-11-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2002-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b54c8b18bea5eaebdf9517bad3826c27
publicationDate 2002-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2180901-C2
titleOfInvention N-substituted 2-cyanopyrrolidines
abstract FIELD: biologically active compounds. SUBSTANCE: invention provides N-(N'-substituted glycyl)-2- cyanopyrrolidine of formula I: (I), wherein R denotes (i) R 1 R 1a N(CH 2 ) m -, in which R 1 is pyridinyl or pyrimidinyl moiety optionally independently mono- or disubstituted by halogen, trifluoromethyl, cyano, or nitro; R 1a denotes hydrogen or C1-C8-alkyl; and m = 2 or 3; (ii) C3-C12-cycloalkyl optionally substituted by hydroxy- C1-C3-alkyl in position 1; (iii) R 2 (CH 2 ) n -, in which either R 2 is phenyl optionally independently mono-, di- or trisubstituted by C1-C4-alkoxy, halogen, or phenylthio group, in turn optionally substituted by hydroxymethyl in benzene ring; or R 2 is C1-C8- alkyl, [3.1.1]bycyclo-carbocyclic moiety optionally mono- or multisubstituted by C1-C8-alkyl, and further pyridyl, naphthyl, cyclohexenyl, or adamantyl; and n = 1-3; or R 2 is phenoxy group and n = 2; (iv) (R 3 ) 2 CH(CH 2 ) 2 -, in which each R 3 independently denotes phenyl; (v) R 4 -(CH 2 ) p -, in which R 4 is 2-oxopyrrolidinyl or C2- C4-alkoxy and p = 2-4; (vi) isopropyl optionally substituted by C1-C3- hydroxyalkyl in position 1; (vii) R 5 , which denotes indanyl-piperidinyl moiety optionally substituted by benzyl, [2.2.1]- or [3.1.1]bycyclo-carbocyclic moiety optionally mono- or multisubstituted by C1-C8-alkyl, adamantyl, or C1-C8-alkyl in turn optionally mono- or multisubstituted independently by hydroxy, hydroxymethyl, or phenyl in turn optionally mono- or disubstituted by C1-C4- alkyl, C1-C4-alkoxy, or halogen; in free form or in the form of acid addition salt. Compounds I can be used in pharmaceutical composition inhibiting DPP-1y, in particular for treatment of diabetes mellitus, insulin-independent diabetes, and conditions caused by decreased tolerance to glucose. EFFECT: increased choice of antidiabetics. 6 cl, 2 tbl, 2 ex
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priorityDate 1996-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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