148671-87-8Relevant articles and documents
Low-valent dialkoxytitanium(ii): a useful tool for the synthesis of functionalized seven-membered ring compounds
Bodinier, Florent,Sanogo, Youssouf,Ardisson, Janick,Lannou, Marie-Isabelle,Sorin, Geoffroy
, p. 3603 - 3606 (2021/04/14)
Herein, we describe unprecedented access to all-carbon or heterocyclic seven-membered ring frameworks from 1,8-ene-ynes promoted by inexpensive low-valent titanium(ii) species, readily available from Ti(OiPr)4and Grignard reagent. A broad range of cycloheptane, azepane or oxepane derivatives has been obtained (19 examples) with moderate to good yields and an excellent selectivity (up to 95/5 d.r.).
METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE
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Paragraph 00616; 00772; 00773; 00774; 00775, (2021/08/13)
The present disclosure relates to compounds and methods for modulating the expression of dmpk, and treating diseases and conditions in which dmpk plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence CAG or CTG; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence CAG or CTG; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
Law, Robert P.,Atkinson, Stephen J.,Bamborough, Paul,Chung, Chun-Wa,Demont, Emmanuel H.,Gordon, Laurie J.,Lindon, Matthew,Prinjha, Rab K.,Watson, Allan J. B.,Hirst, David J.
supporting information, p. 4317 - 4334 (2018/05/14)
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains - BRD2, BRD3, BRD4, and BRDT - each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biological function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochemical properties, culminating in potent BET inhibitors with BD2 selectivity.
A palladium-catalyzed alkylation/direct arylation synthesis of nitrogen-containing heterocycles
Blaszykowski, Christophe,Aktoudianakis, Evangelos,Alberico, Dino,Bressy, Cyril,Hulcoop, David G.,Jafarpour, Farnaz,Joushaghani, Arash,Laleu, Benoit,Lautens, Mark
, p. 1888 - 1897 (2008/09/18)
(Chemical Equation Presented) A norbornene-mediated palladium-catalyzed sequence is described in which an alkyl-aryl bond and an aryl-heteroaryl bond are formed in one reaction vessel. The aryl-heteroaryl bond-forming step occurs via a direct arylation re
BENZO-FUSED AZEPINONE AND PIPERIDINONE COMPOUNDS USEFUL IN THE INHIBITION OF ACE AND NEP
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, (2008/06/13)
Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: STR1 wherein: Y 1 and Y 2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy;
THIAZOLO BENZAZEPINE CONTAINING DUAL ACTION INHIBITORS
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, (2008/06/13)
Compounds of the formula STR1 wherein A is STR2 are dual inhibitors of NEP and ACE. Compounds wherein A is STR3 are selective ACE inhibitors.
