1083326-67-3

Upstream product

• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 73183-34-3 bis(pinacol)diborane 
• 1083168-94-8 2-methoxy-3-nitro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) pyridine 
• 893440-50-1 2-(methyloxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3-pyridinamine 
• 98-09-9 benzenesulfonyl chloride 
• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 
• 884495-39-0 5-bromo-2-(methyloxy)-3-pyridinamine 
• 1086063-47-9 N-(5-bromo-2-methoxypyridin-3-yl)benzenesulphonamide 

Downstream Products

• 1552300-66-9 N-(5-(7-amino-1-cyclopentyl-5-methyl-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-methoxypyridin-3-yl)benzenesulfonamide 
• 1551455-21-0 N-(2-methoxy-5-(4-((trimethylsilyl)ethynyl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide 
• 1416335-63-1 N-[5-{2-amino-1-[4-(4-morpholinyl)phenyl]-1H-benzimidazol-6-yl}-2-(methyloxy)-3-pyridinyl]benzenesulfonamide 

Relevant academic research and scientific papers

Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity

Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymatic and cellular activities. Most compounds displ

Micro-reactor tandem synthesis method of indole anticancer drug molecules

The invention relates to a micro-reactor tandem synthesis method of indole anticancer drug molecules. The method comprises the following steps: a reaction liquid 1 and a reaction liquid 2 are mixed, then are introduced into a first micro-reactor, and are reacted to obtain a first effluent, the first effluent and a reaction liquid 3 are mixed, then are introduced into a second micro-reactor, and are reacted to obtain a second effluent, the second effluent and a reaction liquid 4 are mixed, then are introduced into a third micro-reactor, and are reacted to obtain a final effluent, and the finaleffluent is concentrated and separated to obtain the indole anticancer drug molecules, wherein the reaction liquid 1 is a mixed solution containing 5-bromine-3-amino-2-substituted (R1)-pyridine, the reaction liquid 2 is substituted (R2)-benzenesulfonyl chloride, the reaction liquid 3 is a mixed solution containing bis(pinacolato)diboron, the reaction liquid 4 is a mixed solution containing a 5-bromo-7-azaindole derivative, and the indole anticancer drug molecules are benzenesulfonamidopyridylazaindole compounds. Compared with the prior art, the method of the invention has the advantages of high reaction efficiency, few side reactions and simple production process.

Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR

The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.

Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity

The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at molecular and cellular levels as well as cell proliferation in a panel of human tumor cells.

A urea compound and its salt compounds of synthetic method and application

Belonging to the technical field of antitumor drugs, the invention discloses a 1-alkyl-3-(6-substituted-2-(1, 2, 4-triazolo[1, 5-a]pyridyl)urea compound, a synthesis method and application thereof. The synthesis method comprises the steps of: 1) reacting

PI3 kinase modulators and methods of use thereof, and use thereof

The invention belongs to the field of medicines, concretely relates to a compound for treating cancer, a composition and an application of the composition and particularly relates to a PI3 kinase regulator as well as a use method and application of the PI3 kinase regulator. The invention provides a compound as shown in the formula (I), a pharmaceutically accepted salt of the compound and a pharmaceutical preparation of the compound, wherein the compound is used for regulating the activity of protein kinase and intercellular or intracellular signal response. The invention also relates to a pharmaceutical composition containing the compound and a method for treating high-proliferative diseases of mammals and particularly human beings by using the pharmaceutical composition as shown in the formula (I).

PI3K inhibitor, preparation method and application thereof in pharmacy

The invention belongs to the technical field of pharmaceuticals and particularly relates to a PI3K inhibitor, a preparation method and application thereof in the pharmacy. The PI3K inhibitor is a compound of the structure shown by the general formula I or medically acceptable salt of the inhibitor. After the PI3K inhibitor is tested with a PI3K biochemical activity test method, the compound has excellent inhibitory activity to PI3K alpha and PI3K gamma, wherein the IC50 values of a plurality of compounds to the PI3K alpha and PI3K gamma reach nanomole grades (smaller than 100 nM). The result shows that the compounds can provide the inhibitor with better effectiveness and selectivity for curing PI3K-acted proliferative disease, and further a targeted drug for curing No. I type diabetes mellitus, lung disease, breast cancer, prostatic cancer, solid tumor, lymphoma, cardiovascular disease, rheumatoid arthritis, leukemia and the like can be hopefully developed. (Please see the general formula I in the description.).

Protein Kinase Inhibitors

The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.

PI3 KINASE MODULATORS AND METHODS OF USE

This invention relates to the field of lipid kinases and modulators thereof. In particular, the invention relates to modulators of phosphatidylinositol 3-kinases (PI3 kinases or PBKs) signaling pathways, and methods of their use. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in modulating of PI3K signaling pathways and their related disorders in mammals, especially humans.

AMINOQUINOLINE DERIVATIVES AS ANTIVIRAL AGENTS

Provided are compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).