213382-45-7Relevant academic research and scientific papers
QUINAZOLINYL COMPOUNDS AND METHODS OF USE
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Paragraph 0376-0377, (2020/12/30)
Provided herein are compounds and pharmaceutically acceptable salts thereof useful in the treatment of IRE1-related diseases and disorders described herein.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00920; 001311-001313, (2021/01/23)
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
INHIBITORS OF HISTONE DEACETYLASE USEFUL FOR THE TREATMENT OR PREVENTION OF HIV INFECTION
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Page/Page column 73, (2020/06/01)
The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4 and A are as defined herein. The present invention also relates to compos
BICYCLIC HETEROCYCLE DERIVATIVES AS BROMODOMAIN INHIBITORS
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Page/Page column 38, (2017/01/23)
The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1,Cy2, R1,R2 and L have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are usefulas bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors
Close, Adam J.,Jones, Rhiannon N.,Ocasio, Cory A.,Kemmitt, Paul,Roe, S. Mark,Spencer, John
, p. 8246 - 8252 (2016/09/09)
Nitration of three regioisomers of bromo-fluorobenzaldehyde proceeds regioselectively, notably with H2SO4/HNO3 at 0 °C. The thereby synthesized tetrasubstituted aromatics, endowed with orthogonal substituents, can be elabo
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Paragraph 0431; 0432; 0433, (2015/05/05)
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
SELECTIVE HDAC1 AND HDAC2 INHIBITORS
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Paragraph 0252; 0253; 0254; 0295; 0296, (2014/05/20)
Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 74, (2011/08/08)
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
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Page/Page column 45-46, (2009/09/05)
The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and / or dementia. The compounds of the present invention are inhibitors of β-secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.
