137225-47-9Relevant academic research and scientific papers
Dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases
-
Paragraph 0256; 0257; 0261; 0262, (2017/09/12)
The present invention relates to dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. According to the present invention, the dihydropteridin-one derivatives have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017
PI3K PROTEIN KINASE INHIBITORS, PARTICULARLY DELTA AND/OR GAMMA INHIBITORS
-
Paragraph 143, (2015/01/16)
The present disclosure provides novel compounds (I) useful as PI3K protein kinase modulators, in particular as PI3K delta (8) and/or gamma (y) protein kinase modulators. The present disclosure also provides methods for preparing PI3K protein kinase modulators, pharmaceutical compositions containing them, and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.
Synthesis and some reactions of 2-(1-chloroethyl)-3,1-benzoxazin-4(H)-one
Sayed, M A,El-Kafrawy, A F,Soliman, A Y,El-Bassiouny, F A
, p. 980 - 983 (2007/10/02)
2-(1-Chloroethyl)-3,1-benzoxazin-4(H)-one (II) reacts with ammonia to give the corresponding quinazolone (III) which on alkylation provides 3-N-alkyl quinazolones (IVa,b).Quinazolone III undergoes Mannich reaction with formaldehyde to give the Mannich base (V).It also reacts with P2S5 to give quinazole-4-thione (VI).The benzoxazinone II also reacts with hydrazines to give 3-aminoquinazolones (VIIa,b) which undergo condensation with p-chlorobenzaldehyde to afford the schiff base (VIII).Amonolysis of II gives the anilides (XIa,b) which undergo ring closure with Ac2O to give the quinazolone IVb.Reaction of II with P2S5 gives the benzothiazinone (XII) which reacts with benzylamine to give IVb.Reaction of II with hydrocarbons under Friedel Crafts conditions furnishes the phenyl aryl ketone derivatives (XIIIa,b).
