- Novel indole derivatives as selective androgen receptor modulators (SARMS)
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The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
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Page/Page column 48
(2008/06/13)
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- NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS)
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The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
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Page/Page column 47
(2008/06/13)
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- Novel indole derivatives as selective androgen receptor modulators (SARMS)
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The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
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Page/Page column 48
(2010/02/14)
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- Highly chemoselective α-diazo carbonyl insertion reactions into N-H and S-H bonds catalysed by [RuCl(η5-C5H5)(PPh3)2]
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Complex [RuCl(η5-C5H5)(PPh3)2], in chloroform at 60 deg C, catalyses the chemoselective insertion of α-diazo carbonyl compounds into N-H and S-H bonds to afford α-keto-amines and α-keto-thioethers.
- Del Zotto, Alessandro,Baratta, Walter,Rigo, Pierluigi
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p. 3079 - 3082
(2007/10/03)
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- Synthesis and reactivity of α-halomethyl ketimines
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The synthesis of N-(1-halo-2-alkylidene)amines, i.e. α-halomethyl ketimines, is described for the first time, utilizing the TiCl4-induced condensation of α-halomethyl ketones with primary amines. The reactivity of these new α-halomethylketimines was studied with respect to nucleophiles such as iodide, cyanide, alcohols, alkoxides, amines and thiolates. α-Halomethyl ketimines are powerful ambident electrophiles which underwent a variety of reactions leading to functionalized imines and heterocycles.
- De Kimpe,De Cock,Stevens
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p. 2739 - 2760
(2007/10/02)
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- Nonsteroidal antiandrogens. Synthesis and structure-activity relationship of 3-substituted derivatives of 2-hydroxypropionanilides
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A series of 3-(substituted thio)-2-hydroxypropionanilides and some corresponding sulfones and sulfoxides of general structure 7, in which R' is methyl or trifluoromethyl, were prepared and tested for antiandrogen activity. Members of the trifluoromethyl series (7,R' = CF3) generally exhibited partial androgen agonist activity whereas the members of the methyl series (7,R' = CH3) were pure antagonists. Lead optimization in the methyl series has led to the discovery of novel, potent antiandrogens, which are peripherally selective. One of these, (RS)-4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'-(trifd luoromethyl)propionanilide, 40 (ICI 176334), is being developed currently for the treatment of androgen-responsive benign and malignant disease.
- Tucker,Crook,Chesterson
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p. 954 - 959
(2007/10/02)
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