239137-57-6Relevant academic research and scientific papers
5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE AND 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE DERIVATIVES AS C-MYC AND P300/CBP HISTONE ACETYLTRANSFERASE INHIBITORS FOR TREATING CANCER
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Page/Page column 171, (2019/04/10)
The invention is directed to substituted 5-(1H-benzo[d]imidazo-2-yl)- pyridin-2-amine and 5-(3H-imidazo[4,5-b]pyridin-6-yl)-pyridin-2-amine derivatives. Specifically, the invention is directed to compounds according to Formula (lb) wherein R', R2', R3', R4', Rs', R6', R7', and X1' are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention decrease MYC protein (c-MYC) in cells and/or inhibit p300/CBP histone acetyltransferase and can be useful in the treatment of cardiac hypertrophy, diabetes, obesity and nonalcoholic fatty liver disease, HIV, polycystic kidney disease, inflammatory diseases, ankylosing spondylitis, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, cancer and pre-cancerous syndromes, and diseases associated with dysregulation of Myc or inhibition of p300/CBP histone acetyltransferase. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention still further discloses methods of reducing MYC protein (c-MYC) in cells and inhibiting p300/CBP histone acetyltransferase activity, and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
FLAP MODULATORS
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Paragraph 2416, (2015/11/03)
The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention
7-Azaindoles via carbolithiation of vinyl pyridines
Cottineau, Bertrand,O'Shea, Donal F.
, p. 10354 - 10362 (2008/02/13)
The sequential reactions of a pyridine vinylation and alkene carbolithiation constitutes a new route to substituted 7-azaindoles. The methodology involves a reaction sequence of controlled carbolithiation of the vinyl double bond, subsequent trapping of t
New access to oxazolopyridines via hydroxyamidine derivatives; application to quinolines
Garnier, Ethel,Blanchard, Stephanie,Rodriguez, Ivan,Jarry, Christian,Leger, Jean-Michel,Caubere, Paul,Guillaumet, Gerald
, p. 2033 - 2040 (2007/10/03)
Several 2-aryl and 2-heteroaryloxazolo[4,5-b]pyridines were synthesised in high yields from zwitterion or hydroxyamidine derivatives by heating in dimethylacetamide. These intermediates were generated via hetarynic reaction with the complex base NaNH2-t-BuONa (5:2). The same reactions were possible with quinoline derivatives.
5,10-dihydrodipyrido[2,3-b:2,3-e]pyrazin and 5,10-dihydrodipyrido[2,3-b:3,2-e]pyrazin compounds
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, (2008/06/13)
A compound selected from those of formula (I): wherein: X represents N, C or CH, Y represents N when X represents C or CH, or Y represents C or CH when X represents N, R1 represents an optionally substituted alkyl, R2 and R3, which may be identical or different, represent Z or W, as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
Novel synthetic strategy of carbolines via palladium-catalyzed amination and arylation reaction
Iwaki, Takehiko,Yasuhara, Akito,Sakamoto, Takao
, p. 1505 - 1510 (2007/10/03)
Four parent carbolines and the corresponding 5- or 9-methylsulfonyl derivatives were synthesized by the palladium-catalyzed intramolecular arylation reaction of ortho-bromo-substituted anilinopyridines which were prepared by the palladium-catalyzed amination reaction of iodobenzenes with aminopyridines. Carbazole and its 9-methylsulfonyl derivative were also synthesized by the same method.
