Abstract:
The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
Abstract:
Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X− is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.
Abstract:
The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
Abstract:
Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X− is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.