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    • 10. 发明授权
    • Alpha-amino acid sulphonyl compounds
    • α-氨基酸磺酰基化合物
    • US06716843B2
    • 2004-04-06
    • US10109407
    • 2002-03-28
    • Guillaume De NanteuilBernard PortevinAlain BenoistNigel LevensOlivier NosjeanBernadette Husson-Robert
    • Guillaume De NanteuilBernard PortevinAlain BenoistNigel LevensOlivier NosjeanBernadette Husson-Robert
    • A61K3140
    • C07D277/04C07D207/16C07D231/04C07D233/06C07D277/06C07D277/10Y02P20/55
    • Compound of formula (I): wherein:  represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.
    • 式(I)化合物:其中:表示任选取代的5元含氮杂环,R 1表示氢,烷基,酰基,脯氨酰基,丙氨酰,组氨酰脯氨酰基或苯丙氨酰脯氨酰基,Ak表示亚烷基或杂亚烷基链,X表示 单键或任选取代的亚苯基,R 2表示任选取代的烷基,(C 3 -C 10)环烷基或-NR 2 a R 2b,其中可以相同或不同的R 2a和R 2b各自代表氢或烷基,或与携带它们的氮原子一起 ,形成含氮杂环,Y表示R 3表示氢或选自烷基,(C 3 -C 7)环烷基和芳基的基团,R 4,R 5和R 6可以相同或不同,各自表示氢或烷基,或R 4 和R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环,其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。