Direct Lactonization of Alkenols via Osmium Tetroxide-Mediated Oxidative Cleavage
摘要:
A highly efficient, mild, and simple protocol is presented for the tandem OsO4-mediated oxidative cleavage/oxidative lactonization of alkenols to lactones. The protocol couples the OsO4-catalyzed oxidative cleavage of olefins with Oxone as the co-oxidant with the direct oxidation of aldehydes in alcoholic solvents to their corresponding esters.
[EN] MACROCYCLIC COMPOUNDS FOR MODULATING IL-17<br/>[FR] COMPOSÉS MACROCYCLIQUES POUR UNE MODULATION D'IL-17
申请人:ENSEMBLE THERAPEUTICS CORP
公开号:WO2013116682A1
公开(公告)日:2013-08-08
The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.
[EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
申请人:ASCENDIS PHARMA AS
公开号:WO2013024048A1
公开(公告)日:2013-02-21
The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.
[EN] PROTEIN CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À UN EXCIPIENT PROTÉIQUE
申请人:ASCENDIS PHARMA AS
公开号:WO2013024049A1
公开(公告)日:2013-02-21
The present invention relates to water-soluble protein carrier- linked prodrugs wherein the protein carrier comprises an amino acid sequence consisting of at least 100 amino acid residues forming random coil conformation and comprising alanine, serine and proline residues. It further relates to pharmaceutical compositions comprising said water-soluble protein carrier- linked prodrugs, their use as a medicament as well as methods of treatment and administration.
[EN] SUSTAINED RELEASE COMPOSITION OF PROSTACYCLIN<br/>[FR] COMPOSITION À LIBÉRATION PROLONGÉE DE PROSTACYCLINE
申请人:ASCENDIS PHARMA AS
公开号:WO2013024051A1
公开(公告)日:2013-02-21
The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
本发明涉及前列环素的缓释组合物,以及其用途,特别是用于预防和/或治疗肺动脉高压。
[EN] CARRIER-LINKED TREPROSTINIL PRODRUGS<br/>[FR] PROMÉDICAMENTS À BASE DE TRÉPROSTINIL LIÉ À UN EXCIPIENT
申请人:ASCENDIS PHARMA AS
公开号:WO2013024052A1
公开(公告)日:2013-02-21
The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).