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US 10,745,350 B2Granted
Compounds and pharmaceutical composition associated with ubiquitination-proteasome system
AssigneeCalgent Biotechnology Co., Ltd.
InventorsYun Yen, Jing-ping Liou, Shiow-lin Pan
Life of this patent
Estimating the term…
Abstract
The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.
Claims17
A compound having the following Formula (I):
- wherein
- R1 is halogen, alkyl, alkenyl, alkynyl, NH2, NO2, OH or CN;
- each R2 is the same or different, representing H, alkyl, C2-10 alkenyl, alkynyl, NH2, NO2, C1-10 alkyloxy, alkylthio, alkylamino, alkyloxyalkyl, OH or CN, aryl or heterocyclic having 1 to 3 heteroatoms selected from the group consisting of N, O and S;
- R3 is H, alkyl, alkenyl, alkynyl, NH2, NO2, OH or CN;
- R4 is H, alkyl, alkenyl, alkynyl, NH2, NO2, OH or CN, or R4 together with nitrogen atom attached therefrom and R5 form a fused bicyclic ring having 0 to 3 heteroatoms selected from O;
- N and S;
- R5 is alkylene-R6 wherein R6 is OH, NO2, CN, alkyl, alkenyl, alkynyl, NRaRb, cycloalkyl, aryl, heterocyclic ring having 0 to 3 heteroatoms selected from O;
- N and S or fused heterocyclic ring having 0 to 3 heteroatoms selected from O, N and S, each of cycloalkyl, aryl, heterocyclic ring and fused heterocyclic ring is unsubstituted or substituted with one to three of OH;
- halogen;
- NH2;
- NO2, CN, alkyl;
- alkenyl;
- alkynyl;
- alkyloxy;
- heteroaryl having 1 to 3 heteroatoms selected from the group consisting of N, O and S, unsubstituted or substituted with alkyl, alkenyl, alkynyl, OH, halogen, CN, NH2 or NO2;
- and
- Ra and Rb are the same or different, independently representing H;
- OH;
- alkyl;
- alkenyl;
- alkynyl;
- alkyloxy;
- cycloalkyl;
- heterocyclyl;
- alkyleneamino;
- alkylene-N-(alkyl)2;
- aryl unsubstituted or substituted with OH, halogen, CN, NH2, NO2, alkyl, alkenyl, alkynyl, alkyloxy or heteroaryl, heteroaryl unsubstituted or substituted with OH, halogen, CN, NH2, NO2, alkyl, alkenyl, alkynyl or alkyloxy;
- alkylene-heteroaryl;
- or alkylene-heterocyclyl unsubstituted or substituted with alkyl;
- X is —C(O), —S(O)2— or —NH—C(O)—;
- m is an integer of 0-3;
- and
- n is an integer of 1-7;
- or a tautomer or stereoisomer thereof, or a solvate, prodrug or a pharmaceutically acceptable salt thereof.
31 more elements
Dependencies are inferred from the claim text.