SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-METHYLENE ANALOGS OF CALCITRIOL AND RELATED COMPOUNDS

• Main Authors: DELUCA, HECTOR F, SIBILSKA, IZABELA K, SICINSKI, RAFAL R, PLUM, LORI A
• Format: Patent
• Language: English; French
• Published: 09.02.2017
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Disclosed are 2-methylene analogs of vitamin D3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1a-hydroxy-2-methylene-vitamin D3, (20S)-1a-hydroxy-2-methylene- vitamin D3, and (5E)- 1a,25-dihydroxy-2-methylene- vitamin D3, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders. La présente invention concerne des analogues 2-méthylène de la vitamine D3 et des composés apparentés, leurs activités biologiques, et diverses utilisations pharmaceutiques de ces analogues. En particulier l'invention concerne la 1a-hydroxy-2-méthylène-vitamine D3, la (20S)-1a-hydroxy-2-méthylène-vitamine D3, et la (5E)-1a,25-dihydroxy-2-méthylène-vitamine D3, leurs activités biologiques, et diverses utilisations pharmaceutiques de ces composés y compris des méthodes de traitement et/ou de prévention de maladies osseuses et de troubles osseux.