387819-41-2Relevant articles and documents
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores
Childress, Elizabeth S.,Wieting, Joshua M.,Felts, Andrew S.,Breiner, Megan M.,Long, Madeline F.,Luscombe, Vincent B.,Rodriguez, Alice L.,Cho, Hyekyung P.,Blobaum, Anna L.,Niswender, Colleen M.,Emmitte, Kyle A.,Conn, P. Jeffrey,Lindsley, Craig W.
, p. 378 - 384 (2019)
A scaffold hopping exercise from a monocyclic mGlu2 NAM with poor rodent PK led to two novel heterobicyclic series of mGlu2 NAMs based on either a functionalized pyrazolo[1,5-a]pyrimidine-5-carboxamide core or a thieno[3,2-b]pyridine-5-carboxamide core. These novel analogues possess enhanced rodent PK, while also maintaining good mGlu2 NAM potency, selectivity (versus mGlu3 and the remaining six mGlu receptors), and high CNS penetration. Interestingly, SAR was divergent between the new 5,6-heterobicyclic systems.
BIOMARKER-BASED THERAPEUTIC COMPOSITION
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, (2021/05/13)
The present invention provides an anticancer agent for treating a patient who is resistant to a protein kinase inhibitor, the anticancer agent comprising, as an active ingredient, a thienopyridine derivative compound or a pharmaceutically acceptable salt thereof. Here, the patient may be a patient carrying active RON. In addition, the patient may be a patient carrying normal KRAS. In addition, the anticancer agent may be applied to a patient who is resistant to an EGFR inhibitor. In particular, the anticancer agent may be usefully used to treat a patient who is resistant to the therapeutic agent cetuximab.
IMPROVED METHODS FOR PREPARING BENZOFUSED HETEROARYL AMIDE DERIVATIVES OF THIENOPYRIDINES
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Page/Page column 18-19, (2010/11/26)
The invention relates to methods for preparing compounds of formulae (I) and (XI): or pharmaceutically acceptable salts or solvates thereof. Compounds of the formula (I) and (XI) Fare useful as anti-angiogenesis agents and as agents for modulating and/or inhibiting the activity of protein kinases, thus providing treatments for cancer or other diseases associated with cellular proliferation mediated by protein kinases.