1312784-89-6Relevant academic research and scientific papers
SUBSTITUTED PHENYLPROPENYL PYRIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL APPLICATIONS
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Paragraph 0446-0447, (2021/12/29)
Disclosed are a substituted phenylpropenylpyridine derivative, a preparation method therefor and the use thereof as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.
PYRIDO[3,2-D]PYRIMIDINE COMPOUNDS AS IMMUNOMODULATORS
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Paragraph 0194; 0197-0198, (2021/04/02)
The present disclosure is directed to compounds of Formula (I): which modulate PD-1/PD-L1 protein/protein interaction, compositions, and methods of treating various diseases, including infectious diseases and cancer.
SALTS AND CRYSTALLINE FORMS OF A PD-1/PD-L1 INHIBITOR
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Paragraph 0404-0405, (2021/05/14)
This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4′-(((((2,2′-dichloro-[1,1′-biphenyl]-3,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer.
Method for synthesizing methyl 1-methyl-imidazolyl-2-formate derivative
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Paragraph 0028; 0031-0032; 0037; 0040-0041, (2020/04/17)
The invention provides a method for synthesizing a methyl 1-methyl-imidazolyl-2-formate derivative, and particularly relates to the technical field of medicines. The method comprises the following steps: S1, taking 3-methylhistamine dihydrochloride shown in the formula (II) as an initial raw material, carrying out a cyclization reaction process on the raw material and formaldehyde, and carrying out aftertreatment to obtain a compound 1-methyl-4, 5, 6, 7-tetrahydro-1H-imidazo[4, 5-c]pyridine shown in the formula (III), S2, enabling the N-5 site of the compound shown in the formula (III) to react with di-tert-butyl dicarbonate to generate a compound tert-butyl 1-methyl-6, 7-dihydro-1H-imidazo[4, 5-C]pyridin-5-(4H)-carboxylate shown in the formula (IV), S3, making active hydrogen at the C-2 site of the compound (IV) react with butyl lithium to generate a lithium salt, and then making the lithium salt react with carbon dioxide to generate a compound tert-butyl 1-methyl-6, 7-dihydro-1H-imidazo[4, 5-C]pyridin-5-(4H)-carboxylate-2-carboxylic acid shown in the formula (V), and S4, carrying out a condensation reaction process on the compound shown in the formula (V) and methanol to obtain the target compound shown in the formula (I). The method has the advantages of cheap and accessible raw materials, high reaction yield and low production cost, and can easily implement industrialization.
Fused ring derivative inhibitor as well as preparation method and application thereof
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Paragraph 0180; 0183-0186, (2020/11/25)
The invention relates to a fused ring derivative inhibitor as well as a preparation method and application thereof. Particularly, the invention relates to a compound shown as a general formula (I), apreparation method thereof, a pharmaceutical composition containing the compound and application of the compound serving as an inhibitor in treatment of cancers, infectious diseases and autoimmune diseases, and substituent groups in the general formula (I) are the same as definitions in the specification.
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
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Paragraph 0331; 0332, (2019/11/22)
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
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Paragraph 0427; 0428, (2018/01/18)
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
PRMT5 INHIBITORS AND USES THEREOF
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, (2016/04/20)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof:wherein Y1 is of formula (?) or formula (y):Ring Y is a 5- to 6-membered heteroaryl ring; and V4, V5, Rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
