99370-68-0Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS
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, (2017/03/21)
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
IRE-1α INHIBITORS
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Paragraph 1416; 1418; 1419, (2016/10/07)
PROBLEM TO BE SOLVED: To provide compounds which directly inhibit inositol requiring enzyme 1 (IRE-1α activity) in vitro, prodrugs, and pharmaceutically acceptable salts thereof. SOLUTION: The present invention provides a compound represented by formula (A) [R3 and R4 are H or the like; Q5-Q8, together with the benzene ring to which they are attached, form a benzofused ring, where at least one of Q5-Q8 is a heteroatom selected from N, O, and S. COPYRIGHT: (C)2016,JPOandINPIT
Novel Cyclic Phenoxy Compounds and Improved Treatments for Cardiac and Cardiovascular Disease
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, (2015/02/25)
A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wh
NOVEL CYCLIC PHENOXY COMPOUNDS AND IMPROVED TREATMENTS FOR CARDIAC AND CARDIOVASCULAR DISEASE
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, (2013/08/28)
A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: (Formula (I)) wherein either Q1, CR6a and optionally R6b together form a cy
Aromatic amine derivative and use thereof
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Page/Page column 32, (2010/01/31)
The present invention provides a novel SCD inhibitor. An SCD inhibitor containing a compound represented by the formula [I] wherein ring A is an optionally substituted aromatic ring, ring B is an optionally substituted ring, ring C is an optionally substi
BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES
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Page/Page column 18, (2009/02/11)
The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones
Mahboobi, Siavosh,Uecker, Andrea,Cenac, Christophe,Sellmer, Andreas,Eichhorn, Emerich,Elz, Sigurd,Boehmer, Frank-D.,Dove, Stefan
, p. 2187 - 2197 (2008/02/01)
A series of bis(benzo[b]furan-2-yl)methanones was synthesized and tested for inhibition of FLT3 and PDGFR autophosphorylation. Mostly, C-5 substitution leads to PDGFR selectivity, which was strongest in the case of the 5,5′-dimethoxy derivative. The 5,5′-
Novel heterocyclic thyromimetics. Part 2
Haning, Helmut,Mueller, Ulrich,Schmidt, Gunter,Schmeck, Carsten,Voehringer, Verena,Kretschmer, Axel,Bischoff, Hilmar
, p. 3992 - 3996 (2008/02/08)
Novel heterocyclic thyromimetics are presented carrying carboxy-substituted benzofurans or sulfur containing heterocycles, as replacements for the amino acid side chain of T3. Potent agonists were identified in both series. SAR trends are examined and fou
CYSTEINE PROTEASE INHIBITORS
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Page/Page column 79-80, (2010/02/12)
A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O)2 ; where Ra is H, C1-C4 alkyl or CH3C(=O); R5 is independently selected from H or methyl; E is -C(=O)-, -S(=O)m-, -NR5S(=O)m-, -NR5C(=O)-, -OC(=O)-, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
