Vitamin receptor binding drug delivery conjugates

Vitamin receptor binding drug delivery conjugates

  • CN 101,239,190 B
  • Filed: 01/27/2004
  • Issued: 09/25/2013
  • Est. Priority Date: 01/27/2003
  • Status: Active Grant
First Claim
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1. vitamin receptor binding drug delivery conjugates, described conjugate comprises:

  • (a) vitamin receptor bound fraction;

    () Han You –

    SSCH b 2CH 2OC (O)-divalent linker;

    With (c) medicine;

    Wherein said vitamin receptor bound fraction is covalently bound to described divalent linker;

    Described medicine is covalently bound to described divalent linker;

    Described divalent linker comprises chooses any one kind of them or multiple interval connection base or hetero atom connection base;

    AndDescribed medicine is selected from vinblastine, takes off acetyl vinblastine one hydrazides and vincristine, Epothilones and tubulysin.2. the drug delivery conjugates of claim 1, wherein said medicine is selected from vinblastine, takes off acetyl vinblastine one hydrazides and vincristine.3. the vitamin receptor binding drug delivery conjugates of claim 1, wherein said divalent linker Han You –

    SSCH 2CH 2OC (O) NHNH-. 4. each drug delivery conjugates among the claim 1-3, wherein said divalent linker contains peptide.5. each drug delivery conjugates among the claim 1-3, wherein said divalent linker contains aspartic acid.6. each drug delivery conjugates among the claim 1-3, wherein said divalent linker contains naturally occurring aminoacid.7. each drug delivery conjugates among the claim 1-3, wherein said vitamin receptor bound fraction is folic acid, or the analog of folic acid or derivant, its be selected from folinic acid, pteroylglutamic acid, folacin receptor combination tetrahydrochysene pterin, denitrogenation tetrahydrochysene pterin, two denitrogenation tetrahydrochysene pterins, dihydrofoilic acid, denitrogenation dihydrofoilic acid, two denitrogenation dihydrofoilic acid, tetrahydrofolic acid, denitrogenation tetrahydrofolic acid, two denitrogenation tetrahydrofolic acids, 1-denitrogenation folic acid, 3-denitrogenation folic acid, 5-denitrogenation folic acid, 8-denitrogenation folic acid, 10-denitrogenation folic acid, aminopterin, methotrexate, N10-methopterin, 2-deaminizating-hydroxyl folic acid, 1,5-two denitrogenation folic acid, 5,10-two denitrogenation folic acid, 8,10-two denitrogenation folic acid, 5,8-two denitrogenation folic acid, 1-denitrogenation methotrexate, 3-denitrogenation methotrexate and 3'"'"', 5'"'"'-two chloro-4-amino-4-deoxidations- N10-methyl pteroylglutamic acid. 8. the vitamin receptor binding drug delivery conjugates of claim 1, it has following formula;

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