1020174-04-2Relevant articles and documents
TYK-2 INHIBITOR
-
Paragraph 0635-0637, (2022/01/05)
Disclosed herein is a compound of Formula (I) for inhibiting TYK2 and treating a disease associated with the undesirable tyk-2 activity (tyk-2 related diseases), a method of using the compounds disclosed herein for treating inflammatory or autoimmune disease, and a pharmaceutical composition comprising the same.
INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
-
Paragraph 684, (2018/02/28)
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
Synthetic method of 1-methyl-1H-pyrazole-3-boronic acid pinacol ester
-
Paragraph 0037; 0038; 0039; 0040, (2016/10/27)
The invention discloses a synthetic method of 1-methyl-1H-pyrazole-3-boronic acid pinacol ester. The method comprises the following steps: step 1, 3-iodine-1-methyl-1H-pyrazole is synthesized from N-methyl-3-aminopyrazole through a diazotization reaction; step 2, 3-iodine-1-methyl-1H-pyrazole prepared in the step 1 is taken as a raw material of reaction, n-butyllithium is taken as a base, isopropoxyboronic acid pinacol ester is taken as a boronizing reagent, and 1-methyl-1H-pyrazole-3-boronic acid pinacol ester is obtained through synthesis. 1-methyl-1H-pyrazole-3-boronic acid pinacol ester with high purity is prepared with a simpler process, lower cost and higher yield. After deep analysis of a target product, N-methyl-3-aminopyrazole is taken as the raw material, iodine with higher activity is prepared through direct diazotization, and production of isomers during methyl introduction in the prior art is avoided, so that the yield is increased greatly and the purification difficulty is reduced greatly.
KETONE DERIVATIVES OF IMIDAZOLES, PHARMACEUTICAL COMBINATIONS AND USES THEREOF
-
Paragraph 0394; 0395, (2016/10/06)
This application relates to ketone compounds of imidazoles, pharmaceutically acceptable salts, solvents, polymorphs or prodrugs thereof, and further relates to pharmaceutical combinations comprising the foregoing substances and uses for preventing and treating protein kinase related diseases such as cancer, metabolic diseases, and cardiovascular diseases.
HETEROCYCLIC COMPOUND
-
Paragraph 0578, (2015/01/18)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
HETARYLAMINONAPHTHYRIDINES
-
Page/Page column 71, (2013/02/27)
Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS
-
Page/Page column 137, (2010/07/09)
The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.