阅读说明：本技术 多西紫杉醇共缀物在制备预防或治疗各种免疫疾病的药物中的应用 (Application of docetaxel conjugate in preparation of medicines for preventing or treating various immune diseases ) 是由 刘刚 温晓明 欧颖烨 黄伟鑫 于 2018-09-04 设计创作，主要内容包括：如下所示的式(I)的化合物或其药学上可接受的盐在制备预防或治疗各种免疫疾病的药物中的用途。<Image he="407" wi="544" file="RE-294883DEST_PATH_IMAGE001.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>(The use of a compound of formula (I) as shown below, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention or treatment of various immune disorders.)

The application of the docetaxel conjugate compound shown as the formula I and the pharmaceutically acceptable salt thereof in preparing the medicines for preventing or treating various immune diseases,

wherein m is 0 or 1;

n is 2,3,4,5,6,7,8,9 or 10;

R₁selected from substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl and substituted or unsubstituted alkoxy of C1-C6, wherein the substituted substituent is selected from hydroxyl, sulfydryl, halogen, amino, nitro, cyano, aldehyde group, alkyl of C1-C6, carboxyl, hydroxyamino, alkylene of C2-C6, amido of C1-C4;

R₂is selected from hydrogen, substituted or unsubstituted alkyl of C1-C6, substituted or unsubstituted alkoxy of C1-C6, and the substituted substituent is selected from halogen.

The use according to claim 1, for the treatment of various immune disorders by acting on a signalling pathway and/or factors selected from NF- κ B, p-I κ B α, I κ B a, p-ERK, p-p38, p-JNK, MMP8, MMP9, MMP2, TIMP-1, IL-1 β, IL-6, IL-8, TNF- α, CD11B, Gr-1, Ly-6G, TSP-1, NOD1, NOD2, S100a8, S100a 9.

Use according to claim 1 or 2, characterized in that said immunity essentially comprises tumor growth and metastasis, anti-inflammatory, such as rheumatoid arthritis and systemic lupus erythematosus; myelosuppression, and macrophage, lymphocyte defects.

The use according to claim 1, wherein said aryl is selected from the group consisting of five-ten membered aryl and heteroaryl is selected from the group consisting of five-ten membered heteroaryl.

The use according to claim 4, wherein said five-ten membered aryl group is selected from the group consisting of five membered aryl group, six membered aryl group, nine membered fused ring aryl group, ten membered fused ring aryl group,

the five-membered aryl group is selected fromThe six-membered aryl is selected fromThe nine-membered fused ring aryl is selected fromThe ten-membered fused ring aryl is selected from

The five-ten membered heteroaryl is selected from a five-membered heterocyclic group containing 1-4 heteroatoms selected from N, O or S, a six-membered heterocyclic group containing 1-4 heteroatoms selected from N, O or S, a ten-membered fused heterocyclic group containing 1-4 heteroatoms selected from N, O or S;

the five-membered heterocyclic group containing 1-4 heteroatoms selected from N, O or S is selected from:

the six-membered heterocyclic group containing 1 to 4 heteroatoms selected from N, O or S is selected from:

the ten-membered fused heterocyclic group containing 1 to 4 heteroatoms selected from N, O or S is selected from:

the use according to claim 1, wherein the alkyl group having 1-6 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, cyclopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclobutyl, n-pentyl, cyclopentyl, n-hexyl, cyclohexyl, dimethylpropyl, 2-methylbutyl, 2-dimethylbutyl, and 2, 3-dimethylbutyl; the C1-C6 alkoxy is selected from methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, isopentoxy, n-hexoxy, isohexoxy, methoxyethoxy, ethoxymethoxy, propoxymethoxy and propoxyethoxy.

The use according to claim 1, wherein the halogen is selected from fluorine, chlorine, bromine or iodine; the alkenyl of C2-C6 is ethenyl, propenyl, butenyl, isobutenyl, 2-butenyl, pentenyl, isopentenyl, 2-pentenyl, hexenyl and isohexenyl; the C1-C4 acylamino is acetylamino, propionylamino, butyrylamino or isobutyrylamino.

According to claim1, wherein R is₂Is hydrogen or hydrogen is replaced by metal or nonmetal cation to form pharmaceutically acceptable salt, and the metal or nonmetal cation is selected from Na⁺，K⁺,Ca²⁺,Mg²⁺,Zn²⁺,Al³⁺And NH₄ ⁺。

The use according to claim 1, wherein the compound of formula I includes, but is not limited to, compounds of formula IA:

use according to claim 1, characterized in that said compound is selected from the group consisting of

A pharmaceutical composition for preventing or treating various immune diseases is characterized by comprising a compound shown as a formula I, pharmaceutically acceptable salts thereof and more than one pharmaceutically acceptable carrier, m, n, R₁And R₂As defined above.