- QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITOR, COMPOSITIONS, METHODS OF MAKING THEM AND THEIR USE
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The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).
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- PHENYLTETRAZOLE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
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Phenyltetrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof are plasma kallikrein inhibitors useful for the treatment of ocular diseases, in particular for the treatment of diabetic macular edema, age-related macular degeneration and choroidal neovascularization.
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Page/Page column 42
(2020/05/19)
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- SERINE/THREONINE KINASE INHIBITORS
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Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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Paragraph 0589
(2015/02/19)
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- Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex- 6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists
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A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described.
- Biagetti, Matteo,Leslie, Colin Philip,Mazzali, Angelica,Seri, Catia,Pizzi, Domenica Antonia,Bentley, Jonathan,Genski, Thorsten,Fabio, Romano Di,Zonzini, Laura,Caberlotto, Laura
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scheme or table
p. 4741 - 4744
(2010/10/04)
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- OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
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The present invention relates to certain substituted phenyl oxazolidinones of the formula h wherein T is a ring and to the processes for the synthesis of the same. The compounds are useful antimicrobial agents, effective against a number of human and v
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