cas 56984-32-8, ETHYL 5-CHLORO-METHYL PYRAZOLE-4-CARBOXYLATE

Articles about 56984-32-8Total 8 be found

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 1327

(2018/04/17)

Amide compound and its preparation method, pharmaceutical composition and use thereof
The present invention relates to amide compounds as shown by structural formula (I). The compounds are low absorbable TGR5 agonists and can be used to treat type II diabetes, obesity, liver or intestine chronic inflammatory diseases.
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Paragraph 0439-0442

(2017/10/28)

Discovery and structure-activity relationship study of 4-phenoxythiazol-5-carboxamides as highly potent TGR5 agonists
A novel therapy that stimulates endogenous glucagon-like peptide-1 (GLP-1) secretion by Takeda G-protein-coupled receptor 5 (TGR5) agonists might be a superior alternative for the treatment of type 2 diabetes mellitus. A series of 4-phenoxythiazol-5-carboxamides were developed as highly potent TGR5 agonists using a bioisosteric replacement strategy based on the scaffold of 4-phenoxynicotinamides. The structure-activity relationship on the bottom phenyl ring and the thiazole ring was extensively studied, and the 2-methylthiazole derivatives 30c and e displayed the best in vitro potency toward human TGR5, with EC50 values of approximately 1 nM. While endowed with excellent in vitro potency, the 2-methyl-thiazoles were flawed with high microsomal clearance.
Chen, Zhixiang,Ning, Mengmeng,Zou, Qingan,Cao, Hua,Ye, Yangliang,Leng, Ying,Shen, Jianhua
p. 326 - 339
(2016/05/19)

HETEROCYCLIC COMPOUND HAVING INHIBITORY ACTIVITY ON 11- -HYDROXYSTEROID DEHYDROGENASE TYPE I
Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: -Y-R5, wherein Y is -O- or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: -C(=O)-Z-R6, wherein Z is -NR7- or -NR7-W-, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is =N- or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.
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Page/Page column 21-22

(2008/12/07)

Adamantyl-pyrazole carboxamides as inhibitors of 11B-hydroxysteroid dehydrogenase
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 18

(2008/06/13)

Synthesis of 5-Chloropyrazoles by Chlorodiazoniation with Sulfur Dioxide
A facile synthesis of 5-chloropyrazoles 4a-e from 5-aminopyrazoles 2a-e via diazotization followed by chlorodediazoniation is described.A new application of sulfur dioxide as a catalyst was demonstrated to be the best for the chlorodediazoniation of diazonium chlorides 3a-e.
Yamamoto, Susumu,Morimoto, Katsushi,Sato, Toshiaki
p. 1545 - 1547
(2007/10/02)

Herbicidal pyrazole sulfonyl Imino-2H-1,2,4-thiadiazolo[2,3-a9 pyrimidines
Novel compounds of the formula: STR1 wherein R1 is a pyrazolyl group which may be substituted; R2 and R3 respectively are a lower alkyl group or a lower alkoxy group; and Z is CH or N, which are useful as herbicides.
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(2008/06/13)

Herbicidal and algicidal 1,5-disubstituted-1H-pyrazole-4-carboxamides
1,5-Disubstituted-1H-pyrazole-4-carboxamide derivatives, useful as herbicides and aquatic algicides.
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(2008/06/13)