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TREATING DIABETES MELITUS USING INSULIN INJECTIONS WITH LESS THAN DAILY INJECTION FREQUENCY

  • US 20110230402A1
  • Filed: 10/29/2009
  • Published: 09/22/2011
  • Est. Priority Date: 10/30/2008
  • Status: Active Grant
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Assignment
First Claim
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1. A method of treating a condition or disease where administration of insulin will be of benefit comprising administering an effective amount of an insulin derivative to a patient in need thereof, wherein said insulin derivative is administered at intervals longer than 24 hours, and wherein the insulin derivative has a side chain attached to the α

  • -amino group of the N-terminal amino acid residue of the B chain or to the ε

    -amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula;


    —

    W—

    X—

    Y—

    Zwherein W is;

    an α

    -amino acid residue having a carboxylic acid group in the side chain which residue forms, with one of its carboxylic acid groups, an amide group together with the α

    -amino group of the N-terminal amino acid residue of the B chain or together with the ε

    -amino group of a Lys residue present in the B chain of the parent insulin;

    a chain composed of two, three or four α

    -amino acid residues linked together via amide bonds, which chain—

    via an amide bond—

    is linked to the α

    -amino group of the N-terminal amino acid residue of the B chain or to the ε

    -amino group of a Lys residue present in the B chain of the parent insulin, the amino acid residues of W being selected from the group of amino acid residues having a neutral side chain and amino acid residues having a carboxylic acid group in the side chain so that W has at least one amino acid residue which has a carboxylic acid group in the side chain;

    ora covalent bond from X to the α

    -amino group of the N-terminal amino acid residue of the B chain or to the ε

    -amino group of a Lys residue present in the B chain of the parent insulin;

    X is;

    —

    CO—

    ;

    —

    COCH(COOH)CO—

    ;

    —

    CON(CH2COOH)CH2CO—

    ;

    —

    CON(CH2COOH)CH2CON(CH2COOH)CH2CO—

    ;

    —

    CON(CH2CH2COOH)CH2CH2CO—

    ;

    —

    CON(CH2CH2COOH)CH2CH2CON(CH2CH2COOH)CH2CH2CO—

    ;

    —

    CONHCH(COOH)(CH2)4NHCO—

    ;

    —

    CON(CH2CH2COOH)CH2CO—

    ;

    or—

    CON(CH2COOH)CH2CH2CO—

    thata) when W is an amino acid residue or a chain of amino acid residues, via a bond from the underscored carbonyl carbon forms an amide bond with an amino group in W, orb) when W is a covalent bond, via a bond from the underscored carbonyl carbon forms an amide bond with the N-terminal α

    -amino group in the B chain or with the ε

    -amino group of a Lys residue present in the B chain of the parent insulin;

    Y is;

    —

    (CH2)m—

    where m is an integer in the range of 6 to 32;

    a divalent hydrocarbon chain comprising 1, 2 or 3 —

    CH═

    CH—

    groups and a number of —

    CH2—

    groups sufficient to give a total number of carbon atoms in the chain in the range of 10 to 32;

    a divalent hydrocarbon chain of the formula —

    (CH2)vC6H4(CH2)W—

    wherein v and w are integers or one of them is zero so that the sum of v and w is in the range of 6 to 30; and

    Z is;

    —

    COOH;

    —

    CO-Asp;

    —

    CO-Glu;

    —

    CO-Gly;

    —

    CO-Sar;

    —

    CH(COOH)2;

    —

    N(CH2COOH)2;

    —

    SO3H;

    or—

    PO3H;

    and any Zn2+ complexes thereof, provided that when W is a covalent bond and X is —

    CO—

    , then Z is different from —

    COOH.

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