1240568-16-4Relevant articles and documents
FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
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Paragraph 0208, (2021/04/02)
The present disclosure relates to a class of fused pyrimidine compounds of Formula I, their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to a process of preparation of these fused pyrimidine compounds, and to pharmaceutical compositions containing them.
Synthetic method of JAK inhibitor
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Paragraph 0030-0032; 0034, (2020/11/26)
The invention discloses a synthesis method of a JAK inhibitor, which is characterized in that: 4-nitro pyrazole and 3-oxetanone are adopted as initial raw materials; a Chan-Lam coupling reaction is performed on the initial raw material 4-nitro pyrazole an
SULFONYLUREA DERIVATIVES AND USES THEREOF
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Paragraph 01449-01450, (2020/12/30)
The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Paragraph 00497, (2020/07/07)
Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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Paragraph 0165, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
INDOLINONE COMPOUNDS FOR USE AS MAP4K1 INHIBITORS
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Page/Page column 71-72, (2020/05/15)
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring C, X1, X2, L1, R1, R2, R3, R4, R5, R6, R7, m and n are as defined herein, which are useful as MAP4K1 inhibitors, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by MAP4K1.
2-substituted parazoleamino-4-substituted amino-5-pyrimidine formamide compound, composition and application thereof
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Paragraph 0102-0105, (2019/04/10)
The invention relates to a series of new compounds as a JAK inhibitor, as well as compositions and applications thereof, and particularly provides a series of compounds (I) that have a strong JAK inhibiting activity, or stereisomers, geometrical isomers, tautomers, pharmaceutically acceptable salts, prodrugs, metabolites, isotope derivatives, and solvates, as well as medicine compositions comprising such compounds. The invention also discloses applications of the compounds or the medicine compositions in preparation of a medicine, which is used for treatment of autoimmune diseases or cancer.
SULPHONYL UREA DERIVATIVES AS NLRP3 INFLAMMASOME MODULATORS
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Paragraph 0911, (2019/07/13)
The present disclosure relates to compounds of Formula (I): (I) and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors
Kawahata, Wataru,Asami, Tokiko,Irie, Takayuki,Sawa, Masaaki
, p. 145 - 151 (2017/12/06)
BTK is a promising target for the treatment of multiple diseases such as B cell malignances, asthma, and rheumatoid arthritis. Here, we report the discovery of a series of novel pyrimidine analogs as potent, highly selective, non-covalent inhibitors of BTK. Compound 25d demonstrated higher affinity to an unactivated conformation of BTK that resulted in an excellent kinase selectivity. Compound 25d showed a good oral bioavailability in mice, and significantly inhibits the PCA reaction in mice.
Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof
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Paragraph 0470; 0471, (2015/12/07)
A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.