1548332-55-3

Upstream product

• 872-32-2 2-methyl-1H-pyrroline 
• 226409-94-5 4,4-dichloro-5-(trichloromethyl)-3,4-dihydro-2H-pyrrole 
• 226410-00-0 3-chloro-1H-pyrrole-2-carboxylic acid methyl ester 
• 1053658-09-5 3-chloro-1H-pyrrole-2-carboxylic acid 
• 1466565-96-7 3-chloro-N-phenyl-1H-pyrrole-2-carboxamide 
• 1403941-86-5 1-amino-3-chloro-N-phenyl-1H-pyrrole-2-carboxamide 
• 1548942-78-4 (S)-5-chloro-3-phenyl-2-(pyrrolidine-2-yl)pyrrolo[2,1-f][1,2,4]triazine-4(3H)-one 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 1548339-08-7 1-amino-3-chloro-1H-pyrrole-2-carboxamide 
• 87-42-3 6-chloropurine 

Relevant academic research and scientific papers

Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3KδDual Inhibitors

An electronic density model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγand PI3Kδ. Guided by molecular docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a novel cyclic moiety. Further structure-activity relationship optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ-PI3Kδdual inhibitor with favorable drug metabolism and pharmacokinetic properties in preclinical species.

Pyrimido oxazine derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases

The present invention relates to pyrimido oxazine 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. The pyrimido oxazine derivatives according to the present invention 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

NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS

Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune disorders diseases and cancer.

NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS

The invention relates to novel heteroaryl and heterocycle compounds and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3k and for treating inflammatory and autoimmune disorders diseases and cancer.

NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITION AND METHODS THEREOF

Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.