167643-21-2Relevant academic research and scientific papers
QUINOLINE DERIVATIVES USEFUL AS TYROSINE KINASE INHIBITORS
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Paragraph 0148-0149, (2019/12/25)
Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, X, Y1, Y2, Y3 and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.
BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
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Page/Page column 44, (2010/04/03)
Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed
POLYCYCLIC ARYL SUBSTITUTED TRIAZOLES AND POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
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Page/Page column 49; 52, (2009/05/29)
Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
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Page/Page column 132, (2008/12/07)
Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
Synthesis of Perhydro-1,4-ethano-1,5-naphthyridine and Perhydro-4,7-ethanopyrrolopyridine Derivatives: Potential NK1-receptor Antagonists. X-Ray Molecular Structures of (4aR*,8S*,8aR*)-6-Oxo-8-phenylperhydro-1,4-ethano-1,5-naphthyridine and (4aR*,7R*,8R*,8aR*)-7,8-Diphenylper...
Besidsky, Yevgeny,Luthman, Kristina,Claesson, Alf,Fowler, Christopher J.,Csoeregh, Ingeborg,Hacksell, Uli
, p. 465 - 474 (2007/10/02)
Derivatives of perhydro-1,4-ethano-1,5-naphthyridine and 4,7-ethanopyrrolopyridine were designed and synthesized as conformationally constrained analogues of the potent NK1-receptor antagonist CP-96,345. 2-Benzylidenequinuclidin-3-one 1 was used as the common starting material: (i) heterocyclizations of compound 1 with N-(carbamoylmethyl)pyridinium chloride gave unsaturated pyridone derivatives which, after catalytic hydrogenation, afforded 1,5-naphthyridines, and (ii) functionalization of compound 1 by nucleophilic 1,4-addition reactions, followed by reductive cyclizations, gave quinuclidine derivatives with fused five- or six-membered rings.The cyclization reactions proceeded stereoselectively and the relative stereochemistries were determined by a combination of molecular mechanics calculations, X-ray crystallography, and NMR spectroscopy.The biological activities of the synthesized derivatives were evaluated by binding studies to human NK1-receptors in UC11MG cells.The compounds had low to moderate affinity for the NK1-receptor.
