1060802-23-4Relevant articles and documents
Synthesis of the GPR40 partial agonist MK-8666 through a kinetically controlled dynamic enzymatic ketone reduction
Hyde, Alan M.,Liu, Zhijian,Kosjek, Birgit,Tan, Lushi,Klapars, Artis,Ashley, Eric R.,Zhong, Yong-Li,Alvizo, Oscar,Agard, Nicholas J.,Liu, Guiquan,Gu, Xiuyan,Yasuda, Nobuyoshi,Limanto, John,Huffman, Mark A.,Tschaen, David M.
, p. 5888 - 5891 (2016)
A scalable and efficient synthesis of the GPR40 agonist MK-8666 was developed from a simple pyridine building block. The key step to set the stereochemistry at two centers relied on an enzymatic dynamic kinetic reduction of an unactivated ketone. Directed
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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Paragraph 0669; 0671, (2021/02/25)
The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
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Paragraph 0230-0233, (2019/09/16)
Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.
CHROMENOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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Paragraph 0422, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I); where A1, A2, G, R1, R2, R3, R4, and W are described herein.
PYRAZOLE DERIVATIVE
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Paragraph 0123; 0124, (2016/03/05)
Provided are a compound expressed by formula (I) or a pharmacologically permissible salt thereof, as well as a drug or drug composition that contains this compound as an active ingredient, having a xanthine oxidase inhibiting effect that is very useful fo
PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES
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Page/Page column 92, (2016/01/01)
Pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts are disclosed, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha- synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, the compounds are used as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. Futher, the compounds are useful for measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.