Facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers and uses thereof

Facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers and uses thereof

  • CN 1,922,133 A
  • Filed: 01/21/2005
  • Published: 02/28/2007
  • Est. Priority Date: 01/23/2004
  • Status: Active Application
First Claim
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1. treat the method for infected by microbes in the animal of needs, described method comprises uses the oligopolymer that comprises formula I of significant quantity or the pharmaceutical composition of its acceptable salt or solvate and drug acceptable carrier or thinner to animal:

  • R 1-[-A 1-s-A 2-s-] m-R 2 (I),

    Wherein;

    A 1And A 2Be optional arylidene that replaces or the optional heteroarylidene that replaces independently, wherein;

    (i) A 1And A 2The optional independently combination with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups replaces;

    Or (ii) A 1Or A 2One of them as above defines, and optional combination replacement with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups;

    And A 1Or A 2Wherein another is group-C ≡

    C (CH 2) pC ≡

    C-, wherein p is 0 to 8, and-(CH 2) p-alkylidene chain is optional to be replaced with one or more amino or hydroxyl;

    S does not exist, perhaps representative-CH 2-,-CH 2-CH 2-,-CH=CH-or-C ≡

    C-;

    R 1Be (i) hydrogen, polar group (PL) or non-polar group (NPL), and R 2Be-A 1-R 1, A wherein 1As above definition, and optional combination replacement with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups;

    Or (ii) hydrogen, polar group (PL) or non-polar group (NPL), and R 2Be-A 1-s-A 2-R 1, A wherein 1And A 2Each as above defines, and optional combination replacement with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups;

    Or (iii) A '"'"'-s-, and R 2Be-A 1-s-A '"'"', wherein A '"'"' is aryl or heteroaryl, and the two any optional combination with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups replaces;

    Or (iv) A '"'"'-s-, and R 2Be-A '"'"', wherein A '"'"' is aryl or heteroaryl, and the two any optional combination with one or more polarity (PL) group, one or more nonpolar (NPL) groups or one or more polarity (PL) group and one or more nonpolar (NPL) groups replaces;

    Or (v) R 1And R 2Form singly-bound together;

    NPL independently is selected from-B (OR 4) 2Or-(NR 3 '"'"') Q1NPL-U NPL-(CH 2) PNPL-(NR 3 ") Q2NPL-R 4Non-polar group, wherein;

    R 3, R 3 '"'"', and R 3 "Be independently selected from down group;

    hydrogen, alkyl and alkoxyl group;

    R 4Be selected from down group;

    hydrogen, alkyl, thiazolinyl, alkynyl, cycloalkyl, aryl and heteroaryl, wherein any is optional with one or more alkyl or halogen replacement;

    U NPLDo not exist, or be selected from down group;

    O, S, S (=O), S (=O) 2, NR 3,-(C=O)-,-(C=O)-N=N-NR 3-,-(C=O)-NR 3-N=N-,-N=N-NR 3-,-C (=N-N (R 3) 2)-,-C (=NR 3)-,-C (=O) O-,-C (=O) S-,-C (=S)-,-O-P (=O) 2O-,-R 3O-,-R 3S-,-S-C=N-and-(C=O)-NR 3-O-, the group that wherein has two chemical non-equivalence ends can be taked two kinds of possible orientations;

    -(CH 2) PNPL-alkylidene chain is optional to be replaced with one or more amino or hydroxyl, and perhaps alkylidene chain is undersaturated;

    PNPL is 0 to 8;

    Q1NPL and q2NPL are 0 to 2 independently;

    PL is the polar group that is selected from down group;

    halogen, '"'"'-hydroxyethoxy ylmethyl, methoxy ethoxy methyl, polyoxyethylene and-(NR 5 '"'"') Q1PL-U PL-(CH 2) PPL-(NR 5 '"'"') Q2PL-V, wherein;

    R 5, R 5 '"'"', and R 5 "Be independently selected from down group;

    hydrogen, alkyl and alkoxyl group;

    U PLDo not exist, or be selected from down group;

    O, S, S (=O), S (=O) 2, NR 5,-(C=O)-,-(C=O)-N=N-NR 5-,-(C=O)-NR 5-N=N-,-N=N-NR 5-,-C (=N-N (R 5) 2)-,-C (=NR 5)-,-C (=O) O-,-C (=O) S-,-C (=S)-,-O-P (=O) 2O-,-R 5O-,-R 5S-,-S-C=N-and-(C=O)-NR 5-O-, the group that wherein has two chemical non-equivalence ends can be taked two kinds of possible orientations;

    V is selected from down group;

    nitro, cyano group, amino, hydroxyl, alkoxyl group, alkylthio, alkylamino, dialkyl amido ,-NH (CH 2) pNH 2,-N (CH 2CH 2NH 2) 2, diazoamino, amidino groups, guanidine radicals, amidino groups, semicarbazone, aryl, heterocycle and heteroaryl, wherein any optional with one or more amino, halogen, cyano group, nitro, hydroxyl ,-NH (CH 2) pNH 2,-N (CH 2CH 2NH 2) 2, amidino groups, guanidine radicals, amidino groups, amino-sulfonyl, aminoalkoxy, amino alkylthio, lower acyl amino or benzyloxycarbonyl replace;

    -(CH 2) PPLOptional usefulness-individual or a plurality of amino of-alkylidene chain or hydroxyl replace, and perhaps alkylidene chain is undersaturated;

    PPL is 0 to 8;

    Q1PL and q2PL are 0 to 2 independently;

    AndM is 1 to about 25;

    Condition is if A 1And A 2Be thiophene, polar group can not be 3-(propionic acid) or methoxyl group (diethoxy) ethyl so, and non-polar group can not be a dodecyl.

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