- GLP-1R AGONISTS AND USES THEREOF
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Provided are compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
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Page/Page column 64; 170-171
(2020/06/10)
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- PIPERIDINYL- AND PIPERAZINYL-SUBSTITUTED HETEROAROMATIC CARBOXAMIDES AS MODULATORS OF GPR6
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Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R4, R5, R8, R10, R11, X1, X2, X3, X9, X12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.
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Paragraph 0609
(2018/10/25)
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- Discovery of imigliptin, a novel selective DPP-4 inhibitor for the treatment of type 2 diabetes
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We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.
- Shu, Chutian,Ge, Hu,Song, Michael,Chen, Jyun-Hong,Zhou, Huimin,Qi, Qu,Wang, Feng,Ma, Xifeng,Yang, Xiaolei,Zhang, Genyan,Ding, Yanwei,Zhou, Dapeng,Peng, Peng,Shih, Cheng-Kon,Xu, Jun,Wu, Frank
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supporting information
p. 921 - 926
(2014/09/17)
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- FUSED PYRIDINE DERIVATIVES
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Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
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- FUSED PYRIDINE DERIVATIVES
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Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
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- Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase
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Based upon the activity and X-ray crystallographic studies of tri-substituted benzene derivatives containing carboxylic acid, acetamido and guanidine groups, we investigated the effect of the fourth substituent to fulfill the fourth pocket of neuraminidas
- Chand, Pooran,Kotian, Pravin L.,Morris, Philip E.,Bantia, Shanta,Walsh, David A.,Babu, Yarlagadda S.
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p. 2665 - 2678
(2007/10/03)
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