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    • 6. 发明申请
    • HIV PRODRUGS CLEAVABLE BY CD26
    • WO2004099135A3
    • 2005-02-17
    • PCT/EP2004050753
    • 2004-05-10
    • TIBOTEC PHARM LTDDE KOCK HERMAN AUGUSTINUSWIGERINCK PIET TOM BERT PAULBALZARINI JAN
    • DE KOCK HERMAN AUGUSTINUSWIGERINCK PIET TOM BERT PAULBALZARINI JAN
    • A61K38/00A61K47/48C07D493/04C07H15/252C07K5/06C07K5/062C07K5/065C07K5/068C07K5/072C07K5/083C07K5/103C07K5/11C07K5/113C07K7/06C07K9/00C07D473/00
    • C07D493/04A61K38/00A61K47/64C07H15/252C07K5/06052C07K5/06113C07K5/0808C07K5/1008C07K5/101C07K5/1019C07K5/1021C07K7/06C07K9/003
    • The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present prodrugs have the formula (I), the stereoisomeric forms and salts thereof, wherein n is I to 5; Y is proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine; X is selected from any amino acid in the D- or L-configuration; X and Y in each repeat of [Y-X] are chosen independently from one another and independently from other repeats; Z is a direct bond or a bivalent straight or branched saturated hydrocarbon group having from 1 to 4 carbon atoms; R is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4akloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R is arylC1-4alkyl; R is C1-10alkyl, C2-6alkenyl or C3-7cycloalkyIC1-4alkyl; R is hydrogen or C1-4alkyl. The present invention furthermore provides the use of said prodrugs as medicines as well as a method of producing said prodrugs.
    • 本发明提供了新的前体药物,其是治疗化合物和肽的缀合物,其中缀合物可被二肽基肽酶切割,更优选通过CD26,也称为DPPIV(二肽基氨基二肽酶IV))。 本发明的前药具有式(I),其立体异构形式及其盐,其中n为1至5; Y是脯氨酸,丙氨酸,羟脯氨酸,二羟脯氨酸,噻唑烷羧酸(硫脯氨酸),脱氢脯氨酸,哌可酸(L-高脯氨酸),氮杂环丁烷羧酸,氮丙啶羧酸,甘氨酸,丝氨酸,缬氨酸,亮氨酸,异亮氨酸和苏氨酸; X选自D-或L-构型中的任何氨基酸; [Y-X]的每个重复中的X和Y彼此独立地独立地选自其它重复; Z是直接键或具有1至4个碳原子的二价直链或支链饱和烃基; R 1是芳基,杂芳基,芳氧基,杂芳氧基,芳氧基C 1-4烷基,杂环烷氧基,杂环烷基C 1-4烷氧基,杂芳氧基C 1-4烷基,杂芳基C 1-4烷氧基; R 2是芳基C 1-4烷基; R 3是C 1-10烷基,C 2-6烯基或C 3-7环烷基C 1-4烷基; R 4是氢或C 1-4烷基。 本发明还提供所述前体药物作为药物的用途以及制备所述前体药物的方法。