Compounds of estrogen-related receptor modulators and the uses thereof
AssigneeGuangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
InventorsKe Ding, Chiwai Wong, Lijie Peng, Zhanfang Kang, Xi Zhou
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Abstract
The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.
Claims9
Compounds having Formula lor their pharmaceutical acceptable salts or stereo isomers:
- wherein,
- A, B, D, and E are each independently selected as CH or N;
- n is selected as 0, 1, 2, 3, or 4;
- in the following, a is 0 or 1;
- b is 0 or 1;
- R1 is selected from:
- 1)H;
- 2) halide;
- 3)OH;
- 4) NO2;
- 5)CO2H;
- 6) (C═O)aObC1˜C8 alkyl;
- 7) (C═O)aOb aryl;
- 8) (C═O)aObC2˜C8 alkenyl;
- 9) (C═O)aObC2˜C8 alkynyl;
- 10) ObC1˜C8 fluoroalkyl;
- 11) (C═O)aNR6R5;
- 12) CN;
- 13) (C═O)aObC3˜C8 cycloalkyl;
- 14) (C═O)aOb heterocycle;
- 15) SO2NR6R7;
- 16) SO2C1˜C8 alkyl;
- 17) (C═O)aObC0˜C8-NR6R5;
- the alkyl, aryl, alkenyl, alkynyl, cycloalkyl or heterocycle groups mentioned above can be substituted by 0, 1 or more substituted groups independently selected from R4;
- R2 is selected from:
- 1) H;
- 2) C1˜C8 alkyl;
- 3) aryl;
- 4) C3˜C8 alkenyl;
- 5) C3˜C8 alkynyl;
- 6) C1˜C8 fluoroalkyl;
- 7) C1˜C6 aryl alkyl;
- 8) C3˜C6 cycloalkyl;
- 9) heterocycle;
- the alkyl, aryl, alkenyl, alkynyl, cycloalkyl or heterocycle groups mentioned above can be substituted by 0, 1 or more substituted group independently selected from R4;
- R3 is selected from:
- 1) (C═O)aObC1˜C8 alkyl;
- 2) (C═O)aOb aryl;
- 3) (C═O)aObC2˜C8 alkenyl;
- 4) (C═O)aObC2˜C8 alkynyl;
- 5) ObC1˜C8 fluoroalkyl;
- 6) (C═O)aNR6R5;
- 7) (C═O)aObC3˜C8 cycloalkyl;
- 8) (C═O)aOb heterocycle;
- the alkyl, aryl, alkenyl, alkynyl, cycloalkyl or heterocycle groups mentioned above can be substituted by 0, 1 or more substituted groups independently selected from R4;
- R4 is selected from:
- 1) H;
- 2) halide;
- 3) OH;
- 4) NO2;
- 5) CO2H;
- 6) (C═O)aObC1˜C8 alkyl;
- 7) (C═O)aOb aryl;
- 8) (C═O)aObC2˜C8 alkenyl;
- 9) (C═O)aObC2˜C8 alkynyl;
- 10) ObC1˜C8 fluoroalkyl;
- 11) (C═O)aNR6R5;
- 12) CN;
- 13) (C═O)aObC3˜C8 cycloalkyl;
- 14) (C═O)aOb heterocycle;
- 15) SO2NR6R7;
- 16) SO2C1˜C8 alkyl;
- the alkyl, aryl, alkenyl, alkynyl, cycloalkyl or heterocycle groups mentioned above can be substituted by no more than 3 substituted groups independently selected from R5, OH, (C1˜C6) alkoxy, halide, COOH, CN, O(C═O)C1˜C6 alkyl, or NR5R6groups;
- R5 and R6 are each independently selected from:
- 1) H;
- 2) (C═O)aObC1˜C8 alkyl;
- 3) (C═O)aOb aryl;
- 4) (C═O)aObC2˜C8 alkenyl;
- 5) (C═O)aObC2˜C8 alkynyl;
- 6) ObC1˜C8 fluoroalkyl;
- 7) (C═O)aObC3˜C8 cycloalkyl;
- 8) (C═O)aOb heterocycle;
- 9) (C═O)aObC0˜C8 -NR6R5;
- the alkyl, aryl, alkenyl, alkynyl, cycloalkyl or heterocycle groups mentioned above can be substituted by no more than 3 substituted groups independently selected from R6;
- or R6 and R5 form a 4˜7-atom ring, or a bicyclic ring in which each ring is formed by 4˜7-atoms;
- the ring or bicyclic ring contains 1, 2, or 3 hetero atoms selected from N, O and S atom;
- the ring or bicyclic ring can be substituted by one or more substituted groups independently selected from R5.
Dependencies are inferred from the claim text.