D-PROLINE DERIVATIVES Russian patent published in 2003 - IPC

Abstract RU 2201937 C2

FIELD: amino acids, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of D-proline of the general formula: or where R means SH, benzyl or phenyl optionally substituted with hydroxy-group or lower alkoxy-group, or group of the formula: ; R1 means hydrogen or halogen atom; X means , -CH-, , benzyl, =CH-, CH2CH-(OH)- or thizole-2,5-diyl; Y means -S-S-, , -O-, -NH-, , -CH=CH-, -NHC(O)NH-, , -N-(alkoxyalkyl)-, -N-(cycloalkylmethyl)-, 2,6-pyridyl, 2,5-furanyl, 2,5-thienyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-naphthyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl or diphenylene, 1,2-phenylene, 1,3-phenylene or 1,4-phenylene where phenylene groups are substituted optionally with substituents taken among group including halogen atom, lower alkyl, lower alkoxy-group, hydroxy-group, carboxy-group, -COO-lower alkyl, nitrile, 5-tetrazole, (2-carboxypyrrolidine-1-yl)-2-oxoethoxy-group, N-hydroxycarbami- -midoyl, 5-oxo-[1,2,4] -oxadiazolyl, 2-oxo-[1,2,3,5]-oxathiadiazolyl, 5-thioxo-[1,2,4]-oxadiazolyl and 5-tert. -butylsulfanyl-[1,2,4] -oxadi- -azolyl; X' means , benzyl, -CH= C(R2), -CH(OH)-CH2 or thiazol- -2,5-diyl; R2 means lower alkyl, lower alkoxy-group or benzyl; n = 0-3, to their pharmaceutically acceptable salts, mono- and diesters with exception for (R)-1-[(R)- and (R)-1-[<S)-3-mercapto-2-methyl- -propionyl]-pyrrolidine-2-carboxylic acids, medicine agents eliciting amyloidosis activity and method of synthesis of these derivatives. EFFECT: valuable medicinal properties of compounds. 15 cl, 1 tbl, 106 ex

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RU 2 201 937 C2

Authors

Khertel' Kornelija

Khoffmann Torshten

Jjakob-Retne Roland

Norkross Roger David

Dates

2003-04-10Published

1998-10-30Filed