[EN] POLYCONJUGATES FOR DELIVERY OF RNAI TRIGGERS TO TUMOR CELLS IN VIVO<br/>[FR] POLYCONJUGUÉS POUR L'ADMINISTRATION DE DÉCLENCHEURS D'ARNI À DES CELLULES TUMORALES IN VIVO
申请人:ARROWHEAD RES CORP
公开号:WO2015021092A1
公开(公告)日:2015-02-12
The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand- targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.
HERBICIDAL AND FUNGICIDAL 5-OXY-SUBSTITUTED 3-PHENYLISOXAZOLINE-5-CARBOXAMIDES AND 5-OXY-SUBSTITUTED 3-PHENYLISOXAZOLINE-5-THIOAMIDES
申请人:BAYER CROPSCIENCE AG
公开号:US20150245616A1
公开(公告)日:2015-09-03
Herbicidally and fungicidally active 5-oxy-substituted 3-phenylisoxazoline-5-carboxamides and 5-oxy-substituted 3-phenylisoxazoline-5-thioamides of the formula (I) are described.
In this formula (I), X, X
2
to X
6
, R
1
to R
4
are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.
The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.
Intramolecular 4+3 cycloadditions. Vinylthionium ions from allylic alcohols
作者:Michael Harmata、Darin E. Jones
DOI:10.1016/0040-4039(95)02391-7
日期:1996.2
Aldehyde 9 can be prepared from ethyl pyruvate in several steps. Treatment of 1 with various diene-containing Grignard reagents results in the formation of the corresponding allylic alcohol in good yield. Exposure of these alcohols to triflic anhydride results in the formation of 4+3 cycloadducts in good to excellent yields. Furan and simple butadiene trap the intermediate allylic cation efficiently in