69383-71-7Relevant academic research and scientific papers
Structure–Activity Relationships of 1-Benzoylazulenes at the OX1 and OX2 Orexin Receptors
Turku, Ainoleena,Leino, Teppo O.,Karhu, Lasse,Yli-Kauhaluoma, Jari,Kukkonen, Jyrki P.,Wallén, Erik A. A.,Xhaard, Henri
, p. 965 - 981 (2019/04/10)
We previously demonstrated the potential of di- or trisubstituted azulenes as ligands (potentiators, weak agonists, and antagonists) of the orexin receptors. In this study we investigated 27 1-benzoylazulene derivatives, uncovering seven potentiators of t
BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 00738-00740, (2019/06/05)
Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N -[3-[(Benzimidazol-2-yl)amino]propyl]amides
Keurulainen, Leena,Vahermo, Mikko,Puente-Felipe, Margarita,Sandoval-Izquierdo, Elena,Crespo-Fernández, Benigno,Guijarro-López, Laura,Huertas-Valentín, Leticia,De Las Heras-Due?a, Laura,Leino, Teppo O.,Siiskonen, Antti,Ballell-Pages, Lluís,Sanz, Laura M.,Casta?eda-Casado, Pablo,Jiménez-Díaz, M. Belén,Martínez-Martínez, María S.,Viera, Sara,Kiuru, Paula,Calderón, Félix,Yli-Kauhaluoma, Jari
supporting information, p. 4573 - 4580 (2015/06/25)
Malaria continues to be a major global health problem, being particularly devastating in the African population under the age of five. Artemisinin-based combination therapies (ACTs) are the first-line treatment recommended by the WHO to treat Plasmodium falciparum malaria, but clinical resistance against them has already been reported. As a consequence, novel chemotypes are urgently needed. Herein we report a novel, in vivo active, fast-acting antimalarial chemotype based on a benzimidazole core. This discovery is the result of a medicinal chemistry plan focused on improving the developability profile of an antichlamydial chemical class previously reported by our group. (Graph Presented).
Acidity of benzoic acids bearing the (CO)5Cr=CN(CH 3)2 group
Parik, Patrik,Kulhanek, Jiri,Ludwig, Miroslav,Wagner, Roman,Rotrekl, Ivan,Drahonovsky, Dusan,Meca, Ludek,Smidkova, Marketa,Tobrman, Tomas,Dvorak, Dalimil
experimental part, p. 4135 - 4138 (2011/01/03)
Benzoic acids 2a and 2b, bearing the (CO)5Cr=CN(CH 3)2 group in the p- and m-position, and the corresponding benzoic acids 2c and 2d, in which the rotation of the aminocarbene moiety was blocked by the presence of a methyl group, were prepared together with the corresponding N,N-dimethylamido acids 3a-d. The measurement of pKa values in EtOH and DMF revealed that the (CO)5Cr=CN(CH 3)2 group is a very weak electron acceptor (δp = 0; δm = 0.14). The restriction of the rotation of the aminocarbene moiety did not significantly influence its electronic properties. The obtained results are in accordance with earlier findings that the relatively strong acidity of carbene complexes bearing hydrogens at the ±-position to the carbene atom is due to the resonance stabilization of the anion.
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 69, (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.
THIAZOLE DERIVATIVE
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Page/Page column 135, (2010/11/23)
(Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic grou
BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
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Page 71, (2010/02/08)
Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
PHARMACOLOGICALLY ACTIVE AMINOALKYLPHENYL COMPOUNDS AND THEIR USE
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, (2008/06/13)
Compounds of the general formula: STR1 and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR 1 and R 2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group STR2 in which R 4 represents hydrogen or lower alkyl; or R 1 and R 2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions--O--and STR3 R 3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents--O--,--S--or--CH 2--or STR4 where R 5 is hydrogen or lower alkyl; Y represents =S, =O, =NR 6 or =CHR. sub.7 ;in which R 6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R 7 represents nitro, lower alkylsulphonyl or arylsulphonyl; m is an integer from 2 to 4 inclusive; n is zero, 1 or 2; and Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms. The compounds have therapeutic activity.
