53478-05-0Relevant articles and documents
COMPOUNDS, IN PARTICULAR FOR USE IN THE TREATMENT OF A DISEASE OR CONDITION FOR WHICH A BROMODOMAIN INHIBITOR IS INDICATED
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Page/Page column 50, (2016/01/25)
The invention relates to a compound for use in the treatment of a disease or condition for which a bromodomain inhibitor is indicated characterized by a general formula (1) and a compound according to formula (3).
(3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING
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Page/Page column 108, (2009/05/29)
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. (Formula)
De novo Design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosine kinase inhibitors
Uno, Masaharu,Ban, Hyun Seung,Nabeyama, Wataru,Nakamura, Hiroyuki
scheme or table, p. 979 - 981 (2009/02/05)
N-Benzylanilines were designed and synthesized as vascular endothelial growth factor (VEGF)-2 inhibitors using de novo drug design systems based on the X-ray structure of VEGFR-2 kinase domain. Among compounds synthesized, compound 3 showed the most potent inhibitory activity toward VEGFR-2 (KDR) tyrosine kinase and its IC50 value was 0.57 μM.
RENIN INHIBITORS
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Page/Page column 22, (2008/12/05)
The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.
BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)
Clarke, Brian,Demont, Emmanuel,Dingwall, Colin,Dunsdon, Rachel,Faller, Andrew,Hawkins, Julie,Hussain, Ishrut,MacPherson, David,Maile, Graham,Matico, Rosalie,Milner, Peter,Mosley, Julie,Naylor, Alan,O'Brien, Alistair,Redshaw, Sally,Riddell, David,Rowland, Paul,Soleil, Virginie,Smith, Kathrine J.,Stanway, Steven,Stemp, Geoffrey,Sweitzer, Sharon,Theobald, Pam,Vesey, David,Walter, Daryl S.,Ward, John,Wayne, Gareth
, p. 1011 - 1016 (2008/12/20)
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of pot
QUINOXALINES AS B RAF INHIBITORS
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Page/Page column 63-64, (2010/11/08)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 66, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
MACROCYCLIC TERTIARY AMINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 71, (2010/11/08)
The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 29, (2010/02/07)
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.