88738-86-7Relevant academic research and scientific papers
LSD1 INHIBITORS
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Paragraph 0162-0164, (2017/05/20)
The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical com
NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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, (2015/10/05)
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.
The binding of synthetic retinoids to lipocalin β-lactoglobulins
Riihim?ki-Lampén, Laura H.,Vainio, Mikko J.,Vahermo, Mikko,Pohjala, Leena L.,Heikura, Jonna M. S.,Valkonen, Kaija H.,Virtanen, Vesa T.,Yli-Kauhaluoma, Jari T.,Vuorela, Pia M.
supporting information; experimental part, p. 514 - 518 (2010/05/19)
The binding of therapeutically relevant synthetic retinoid derivatives to bovine and reindeer β-lactoglobulin (βLG) is demonstrated using fluorescence quenching and ultrafiltration/HPLC methods. Furthermore, synthesis of methyl (E)-3-[4-[(E)-2-(2,6,6-trimethylcyclohex-1-enyl)vinyl]phenyl]-acrylate 4 and (E)-3-[4-[(E)-2-(2,6,6-trimethylcyclohex-1-enyl)vinyl]phenyl]acrylic acid 5 is described. All studied compounds bind to both βLG homologues with nanomolar Kd values, and the interaction diminishes the pH-dependent aggregation of retinoids. Thus, βLG may show benefits in improving the bioavailability of retinoid derivatives.
Paracyclophanes: Extending the bridges. Synthesis
Pechlivanidis, Zissis,Hopf, Henning,Ernst, Ludger
experimental part, p. 223 - 237 (2009/06/21)
Preparatively satisfactory routes to [3.2]paracyclophane (10), [4.2]paracyclophane (14), [4.3]paracyclophane (19) as well as several derivatives of these compounds - among others the bromides 25, the ester 31, the diesters 40-43 - are described using well-established methods of cyclophane chemistry (ring-closure reactions leading to thiacyclophanes, ring contraction by sulfone pyrolysis). The parent systems and their derivatives are now available in gram quantities allowing a study of their chemical properties. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.
Syntheses of (rac)3-Substituted 4-Methoxycarbonyl-1,3-thiazolidine-2-thiones via Rearrangement of a Substituted Group from exo-S to N in (rac)2-Substituted Thio-4-methoxycarbonyl-Δ2-1,3-thiazolines
Nagao, Yoshimitsu,Inoue, Keiko,Yamaki, Masae,Takagi, Shuzo,Fujita, Eiichi
, p. 495 - 508 (2007/10/02)
Based on the previously obtained structural information, (rac)3-substituted 4-carboxy-1,3-thiazolidine-2-thiones 10 were designed as new aldose reductase inhibitors which might be helpful in treating the chronic complications of diabetes.After several trials to find efficient reaction conditions for preparation of the precursors 15 of compounds 10, a catalytic thermal rearrangement reaction of 14 proved to be practically available.Thus, various 3-substituted 4-methoxycarbonyl-1,3-thiazolidine-2-thiones 15a and 15d-t were readily synthesized by heating tha corresponding 2-substituted thio-Δ2-1,3-thiazolines 14a and 14d-t at 120 deg C in the presence of 0.1 mol eq of the corresponding halides 13a and 13d-t without any organic solvent (Sykes conditions).A plausible reaction pathway for the catalytic thermal rearrangement reaction of 14a or 14d-t is presented.Keywords - aldose reductase inhibitor; (rac)2-substituted thio-4-methoxycarbonyl-Δ2-1,3-thiazoline; (rac)3-substituted 4-methoxycarbonyl-1,3-thiazolidine-2-thione; Sykes-type reaction; rearrangement; stepwise cationic reaction; concerted bimolecular transition state
Pharmaceutically active phenylcarboxylic acid derivatives
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, (2008/06/13)
Compounds which antagonize the slow-reacting substance of anaphylaxis or components thereof, e.g., leukotrienes, in warm blooded animals as well as intermediates and methods for their preparation, pharmaceutical compositions and methods for their administration. The compounds are diphenyl carboxylic acids with particular linking groups between the individual phenyl rings and the carboxylic acid moiety. Particular utilities are to relieve asthma and inflammation in man.
A 1,10-HOFMANN ELIMINATION. SYNTHESIS OF A PARACYCLOPHANE TETRAENE
Glatzhofer, Daniel T.,Longone, Daniel T.
, p. 4413 - 4416 (2007/10/02)
The synthesis of (E,E,E,E)-paracyclophane-1,5,13,17-tetraene via the cyclodimerization of 7,8-divinyl-p-quinodimethane is described.
Cinnamic acid derivatives, their preparation, and pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the formula (I): STR1 or a pharmaceutically acceptable ester, amide or salt thereof wherein R1 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R2 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl group; R3 is a hydrogen, chlorine or bromine atom or a hydroxyl group; R4 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R5 is a hydrogen atom or a methyl group; R6 is a hydrogen atom or a methyl group; R7 is a hydrogen atom or a methyl or ethyl group; R8 is a hydrogen atom or a methyl or ethyl group; X is an oxygen atom or a bond, and Y is an alkylene group of up to 5 carbon atoms, or a bond has been found to possess anti-obesity and/or anti-hyperglycaemic activity.
