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    • 7. 发明授权
    • Aspartyldipeptideamine derivatives and sweetner
    • 天冬氨酰二酰胺衍生物和甜味剂
    • US5795612A
    • 1998-08-18
    • US579976
    • 1995-12-28
    • Tadashi TakemotoYusuke AminoRyoichiro Nakamura
    • Tadashi TakemotoYusuke AminoRyoichiro Nakamura
    • A23L27/30C07K5/062C07K5/072C07K5/075A23L1/236C07C229/00
    • C07K5/06113
    • Novel aspartyldipeptideamide derivatives of formula (I): L--Asp--X--NH--C*HR.sub.1 R.sub.2 and salts thereof, wherein X is a D-.alpha.-amino acid residue or a DL-.alpha.-amino acid residue selected from the group consisting of D-alanine, D-.alpha.-aminobutyric acid, D-norvaline, D-valine, D-norleucine, D-leucine, D-isoleucine, D-alloisoleucine, D-t-leucine, D-serine, D-O-methylserine, D-threonine, D-O-methylthreonine, D-allothreonine, D-O-methylallothreonine, D-phenyl glycine and D- or DL furyl glycine, or X is a cyclic or non-cyclic .alpha., .alpha.-dialkyl amino acid residue having 3 to 6 carbon atoms; R.sub.1 is a linear or branched alkyl group having 1 to 6 carbon atoms or an alkoxymethyl group having 2 to 7 carbon atoms in the alkoxy portion; R.sub.2 is a phenyl group having a substituent in its 2, 3- or 4-position selected from the group consisting of F, Cl, Br, I, a hydroxy group, a linear or branched alkoxy group having 1 to 6 carbon atoms, a cyano group, a nitro group, an acetyl group, an amino group and an acetylamino group, or R.sub.2 is a phenyl group having a methylenedioxy group, a trimethylene group or a tetramethylene group in its 2, 3- or 3, 4- position or R.sub.2 is a 2, 3- or 4-pyridyl group, a 2- or 3-furyl group or a 2- or 3-thienyl group; the configuration of C* in formula (I) is (S) or (RS) when R.sub.1 is a linear or branched alkyl group; (R), (S), or (RS) when R.sub.1 is an alkoxymethyl group; and in formula (I), L-Asp and X are .alpha.-bonded.
    • 式(I)的新型天冬氨酰二肽酰胺衍生物:L-Asp-X-NH-C * HR1R2及其盐,其中X为D-氨基酸残基或DL-α-氨基酸残基,其选自 D-丙氨酸,D-α-氨基丁酸,D-正缬氨酸,D-缬氨酸,D-正亮氨酸,D-亮氨酸,D-异亮氨酸,D-异亮氨酸,D-L-亮氨酸,D-丝氨酸,DO-甲基丝氨酸,D-苏氨酸 ,D-甲基苏氨酸,D-异亮氨酸,DO-甲基缩氨基丁酸,D-苯基甘氨酸和D-或DL呋喃基甘氨酸,或X是具有3至6个碳原子的环状或非环状α,α-二烷基氨基酸残基; R1是烷氧基部分中具有1至6个碳原子的直链或支链烷基或具有2至7个碳原子的烷氧基甲基; R2是在其选自F,Cl,Br,I,羟基,具有1至6个碳原子的直链或支链烷氧基的2,3或4位中具有取代基的苯基, 氰基,硝基,乙酰基,氨基和乙酰氨基,或者R2是在其3-或4-或3-位上具有亚甲二氧基,三亚甲基或四亚甲基的苯基, R2是2,3-或4-吡啶基,2-或3-呋喃基或2-或3-噻吩基; 当R 1为直链或支链烷基时,式(I)中C *的构型为(S)或(RS) (R),(S)或(RS); 在式(I)中,L-Asp和X是α键。