cas 33643-94-6, 4-HYDROXY-2-PHENYLPYRIMIDINE

Articles about 33643-94-6Total 9 be found

Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead
Oncogenic activation of RET kinase has been found in several neoplastic diseases, like medullary thyroid carcinoma, multiple endocrine neoplasia, papillary thyroid carcinoma, and non-small-cell lung cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Hence, novel compounds able to inhibit both wild-type RET (wtRET) and its mutants (e.g., V804MRET) are needed. Herein we present the development and the preliminary evaluation of a new sub-micromolar wtRET/V804MRET inhibitor, N-(2-fluoro-5-trifluoromethylphenyl)-N′-{4′-[(2′′-benzamido)pyridin-4′′-ylamino]phenyl}urea (69), endowed with a 4-anilinopyridine structure, starting from our previously identified 4-anilinopyrimidine hit compound. Profiling against a panel of kinases indicated 69 as a multi cKIT/wtRET/V804MRET inhibitor.
Mologni, Luca,Dalla Via, Martina,Chilin, Adriana,Palumbo, Manlio,Marzaro, Giovanni
supporting information
p. 1390 - 1398
(2017/09/01)

Synthesis of mono- and diaza-'pyridones' via stille coupling of alkoxystannanes
Various alkoxy-substituted heterocyclic stannanes provide access to the corresponding substituted 'pyridone' moieties via Stille cross-coupling. Both pyridyl and a series of diazinyl stannanes are prepared, and options for unmasking (via demethylation or debenzylation) of the pyridone unit are evaluated. Georg Thieme Verlag Stuttgart. New York.
Smith, Charlotte L.,Hirschh?user, Christoph,Malcolm, Georgia K.,Nasrallah, Daniel J.,Gallagher, Timothy
p. 1904 - 1908
(2014/08/18)

PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS
The present invention relates to compounds II useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.
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Page/Page column 109

(2011/02/24)

Desulfitative cross-coupling of protecting group-free 2-thiouracil derivatives with organostannanes
We here report a unique and efficient copper bromide mediated pallado-catalyzed coupling of protecting group-free 2-thiouracil derivatives with organostannanes. The nature of the copper appears to be crucial for successful cross coupling.
Sun, Qi,Suzenet, Franck,Guillaumet, Gerald
supporting information; experimental part
p. 3473 - 3476
(2010/08/06)

A convenient synthesis of 5- and 6-substituted 2-phenyl-3H-pyrimidin-4-ones
A simple and convenient one-pot procedure for the synthesis of 5- and 6-substituted 2-phenyl-3H-pyrimidin-4-ones by the condensation of 4-alkoxy-1,1,1-trichloroalk-3-en-2-ones with benzamidine hydrochloride is described. Georg Thieme Verlag Stuttgart.
Zanatta, Nilo,Fantinel, Leonardo,Lourega, Rogerio V.,Bonacorso, Helio G.,Martins, Marcos A. P.
p. 358 - 362
(2008/09/20)

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic beta cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
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Page/Page column 14

(2010/10/20)

PYRIMIDINES USEFUL AS MODULATORS OF VOLTAGE-GATED ION CHANNELS
The present invention relates to compounds useful as inhibitors of voltage-gated ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Page 130

(2010/02/10)

2-AMINO-1-CYANOETHENYLTRIPHENYLPHOSPHONIUM IODIDE, A NEW REAGENT FOR HETEROCYCLIZATIONS
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Smolii, O. B.,Panchishin, S. Ya.,Drach, B. S.
p. 827 - 828
(2007/10/02)

A Facile Method for the Preparation of 2-Substituted Pyrimidin-4(3H)-ones by a Retro-Diels-Alder Reaction
diexo-3-Aza-4-oxotricyclo2.5>non-7-ene (1) reacted with carboximidic esters by ring expansion to yield tricyclic 5,6-dihydropyrimidin-4(3H)-ones 3; when the latter were refluxed in chlorobenzene solution, cyclopentadiene split off to gi
Stajer, Geza,Szabo, Angela E.,Bernath, Gabor,Sohar, Pal
p. 290 - 292
(2007/10/02)