A kind of isosulfocyanate compound preparation

A kind of isosulfocyanate compound preparation

  • CN 105,358,130 B
  • Filed: 05/27/2014
  • Issued: 11/19/2019
  • Est. Priority Date: 05/27/2013
  • Status: Active Grant
First Claim
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1. a kind of preparation of isosulfocyanate compound or derivatives thereof, which is characterized in that the preparation is sustained release preparation, andThe sustained release preparation includes:

  • (a) active constituent of therapeutically effective amount, the active constituent are isosulfocyanate compound or derivatives thereof;

    With(b) pharmaceutically acceptable carrier;

    The sustained release preparation includes slow controlled-release material selected from the group below;

    beeswax, microwax, Brazil wax, paraffin, hydrogenation are bigSoya-bean oil, rilanit special, ethyl cellulose, carbomer, or combinations thereof;

    And the dosage of the slow controlled-release material accounts for the 5-90wt% of total preparation;

    And the isosulfocyanate compound is as shown in the formula (I), derivative is as shown in the formula (II);

    A-NCS (I)In Formulas I;

    NCS is isothiocyanate group;

    A is-XR1Or-CR2R3R4, whereinX is-(CH2)n, n is the integer of 0-6;

    R1For methyl, tert-butyl, isopropyl, methyl mercapto, methoxyl group, allyl, methylallyl, cyclohexyl, methyl thionylBase, naphthalene, methylcyclohexyl, morpholinyl, diethylamino, benzoyl, ethoxy carbonyl, t-octyl, chlorine atom, trimethylSilicon substrate, substituted or unsubstituted phenyl;

    Wherein, " substitution " refers to that one or more H is replaced substituent group selected from the group below in group;

    halogen atom, firstBase, bromomethyl, ethyl, methoxyl group, nitro, azido, trifluoromethyl, difluoro-methoxy, methyl mercapto, cyano, trifluoromethoxy,Trifluoromethylthio, tert-butoxycarbonyl, ethoxy carbonyl;



    R4It is each independently H, phenyl or C1-3Alkyl;

    (II)In Formula II;

    A is as defined in Formulas I;

    R5For hydrogen or by sulphur atom withCarbon atom connection the group derived from following compound;

    half Guang of N- acetylPropylhomoserin, glutathione, cysteine (C1-6Alkyl) ester, cysteinyl amino acid and cysteinyl amino acid (C1-6Alkyl) ester.

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