[EN] SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS [FR] COMPOSÉS DE SPIROHYDANTOÏNE ET LEUR UTILISATION COMME MODULATEURS SÉLECTIFS DES RÉCEPTEURS DES ANDROGÈNES
[EN] SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS [FR] COMPOSÉS DE SPIROHYDANTOÏNE ET LEUR UTILISATION COMME MODULATEURS SÉLECTIFS DES RÉCEPTEURS DES ANDROGÈNES
Spirohydantoin compounds and their use as selective androgen receptor modulators
申请人:NOVARTIS AG
公开号:US20150299120A1
公开(公告)日:2015-10-22
The present invention relates to a compound of formula (I-1) in free form or in pharmaceutically acceptable salt form
in which the substituents are as defined in the specification; to its preparation, to its use as a medicament and to medicaments comprising it. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
The Horner-Wadsworth-Emmons reactions of 2-fluoro-2-diethylphosphonoacetic acid with 241(triisopropylsilyl)oxy]methyl)cyclopentanone (2-TOM-cyclopentanone) using methylrnagnesium chloride furnished the corresponding tetra-substituted fluoroolefin in a Z-selective manner (E/Z = 9:91). A facile synthesis of rac-N-Cbz-Gly-Psi[(Z)-CF=C]-Pro-OH as a dipeptide isostere was achieved based on the Z-selective Horner-Wadsworth-Emmons reaction. (C) 2014 Elsevier Ltd. All rights reserved.
SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS