3318-61-4Relevant academic research and scientific papers
NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS
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Paragraph 0276; 0277; 0278; 0280, (2019/05/16)
The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.
Oxone-promoted hydration of electron-deficient allenic esters and ketones into 1,3-dicarbonyl compounds
Yi, Yu-Ping,Zheng, Yan,Nie, Jing,Ma, Jun-An
, p. 4523 - 4526 (2015/06/30)
Abstract A novel and mild protocol for the hydration of electron-deficient allenic esters and ketones into various 1,3-dicarbonyl compounds is described. The hydration of allenes promoted by oxone in DMF afforded the corresponding products in moderate to good yields. This work features the employment of only a catalytic amount of inexpensive and nontoxic solid reagent oxone (2KHSO5·KHSO4·K2SO4), avoiding the utility of toxic metals or traditional Br?nsted acids, in a green version of viewpoint. A possible reaction mechanism for this transformation is also primarily proposed.
Selective access to all four diastereomers of a 1,3-amino alcohol by combination of a keto reductase- and an amine transaminase-catalysed reaction
Kohls, Hannes,Anderson, Mattias,Dickerhoff, Jonathan,Weisz, Klaus,C?rdova, Armando,Berglund, Per,Brundiek, Henrike,Bornscheuer, Uwe T.,H?hne, Matthias
, p. 1808 - 1814 (2015/06/02)
The biocatalytic synthesis of chiral amines has become a valuable addition to the chemists' toolbox. However, the efficient asymmetric synthesis of functionalised amines bearing more than one stereocentre, such as 1,3-amino alcohols, remains challenging. By employing a keto reductase (KRED) and two enantiocomplementary amine transaminases (ATA), we developed a biocatalytic route towards all four diastereomers of 4-amino-1-phenylpentane-2-ol as a representative molecule bearing the 1,3-amino alcohol functionality. Starting from a racemic hydroxy ketone, a kinetic resolution using an (S)-selective KRED provided optically active hydroxy ketone (86% ee) and the corresponding diketone. Further transamination of the hydroxy ketone was performed by either an (R)- or an (S)-selective ATA, yielding the (2R,4R)- and (2R,4S)-1,3-amino alcohol diastereomers. The remaining two diastereomers were accessible in two subsequent asymmetric steps: the diketone was reduced regio- and enantioselectively by the same KRED, which yielded the (S)-configured hydroxy ketone. Eventually, the subsequent transamination of the crude product with (R)- and (S)-selective ATAs yielded the remaining (2S,4R)- and (2S,4S)-diastereomers, respectively.
PRODUCTION METHOD OF PYRIDAZINONE COMPOUNDS
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Paragraph 0202, (2014/09/03)
The present invention provides an industrially advantageous method of producing a pyridazinone compound. The present invention relates to the following method of producing a pyridazinone compound: Formula (II), (IIIa), (IV) or (IV ), Formula (IIIb), (Vb) or (V b), Formula (VI), (I) or (I ). wherein each symbol is as described in the specification.
METHOD OF TREATMENT
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Paragraph 0790, (2014/09/29)
The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
Highly atom-efficient oxidation of electron-deficient internal olefins to ketones using a palladium catalyst
Mitsudome, Takato,Yoshida, Syuhei,Mizugaki, Tomoo,Jitsukawa, Koichiro,Kaneda, Kiyotomi
, p. 5961 - 5964 (2013/06/27)
A 100 % atom-efficient synthesis of ketones from electron-deficient internal olefins was achieved using O2 as a "green" oxidant (see scheme, DMA=N,N-dimethylacetamide, EWG=electron-withdrawing group). Various electron-deficient olefins were oxidized to the corresponding ketones with over 99 % selectivity and without the formation of olefin isomers or their oxidized products. Copyright
AZAINDAZOLES
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Page/Page column 212, (2013/03/28)
Herein are disclosed azaindazoles of formula (I), (I), where the various groups are defined herein, and which are useful for treating cancer.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 61, (2013/12/03)
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
6-N-Linked Heterocycle-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists
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Page/Page column 17, (2008/12/08)
The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: Formula (I) where: R6 is selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification.
