- NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS
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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.
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Paragraph 0276; 0277; 0278; 0280
(2019/05/16)
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- Oxone-promoted hydration of electron-deficient allenic esters and ketones into 1,3-dicarbonyl compounds
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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.
- Yi, Yu-Ping,Zheng, Yan,Nie, Jing,Ma, Jun-An
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p. 4523 - 4526
(2015/06/30)
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- Selective access to all four diastereomers of a 1,3-amino alcohol by combination of a keto reductase- and an amine transaminase-catalysed reaction
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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.
- Kohls, Hannes,Anderson, Mattias,Dickerhoff, Jonathan,Weisz, Klaus,C?rdova, Armando,Berglund, Per,Brundiek, Henrike,Bornscheuer, Uwe T.,H?hne, Matthias
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p. 1808 - 1814
(2015/06/02)
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- METHOD OF TREATMENT
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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.
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Paragraph 0790
(2014/09/29)
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- PRODUCTION METHOD OF PYRIDAZINONE COMPOUNDS
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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.
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Paragraph 0202
(2014/09/03)
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- AZAINDAZOLES
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Herein are disclosed azaindazoles of formula (I), (I), where the various groups are defined herein, and which are useful for treating cancer.
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Page/Page column 212
(2013/03/28)
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- ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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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.
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Page/Page column 61
(2013/12/03)
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- Highly atom-efficient oxidation of electron-deficient internal olefins to ketones using a palladium catalyst
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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
- Mitsudome, Takato,Yoshida, Syuhei,Mizugaki, Tomoo,Jitsukawa, Koichiro,Kaneda, Kiyotomi
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p. 5961 - 5964
(2013/06/27)
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- INDAZOLES
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Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
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Page/Page column 148-149
(2011/11/30)
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- 6-N-Linked Heterocycle-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists
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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.
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Page/Page column 17
(2008/12/08)
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- Photosensitive compound
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Photosensitive compounds having preferably a functional group such as --SO2 Cl, --SO3 H, --SO3 R, STR1 (R, R', R" being alkyl) on a terminal benzene or naphthalene ring connected via a methylene group and STR2 moiety are improved in sensitivity to light and thermal stability, and thus useful in a photo resist.
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- An Improved Two-step Route for the Preparation of β-Diketones from Aldehydes and its Application to the Synthesis of β-Damascone
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α-Diazo-β-hydroxyketones, obtained by condensation of aldehydes with 1-diazo-1-lithioacetone, are efficiently transformed into the corresponding β-diketones by exposure to rhodium(II) acetate, The sequence is applied to a new synthesis of β-damascone (10).
- Pellicciari, Roberto,Fringuelli, Renata,Sisani, Ettore,Curini, Massimo
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p. 2566 - 2569
(2007/10/02)
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