作者:R. Soundararajan、S. Krishnamurthy、Vilanoor S. Srinivasan、T.R. Balasubramanian
DOI:10.1016/s0022-328x(00)99321-5
日期:1983.10
Some representative N-halo compounds like N-bromosuccinimide, N-iodosuccinimide, N-bromophthalimide, N-iodophthalmide, N-iodobenzimidazole and N-iodobenzeotriazole have been synthesised in good yields and neutral and mild conditions via an intermediate formed from the parent NH species and bis(tri-n-butyltin) oxide. The tin oxide is recovered as recyclable tri-n-butyltin halide.
[EN] COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY<br/>[FR] COMPOSÉS INHIBANT L'ACTIVITÉ ENZYMATIQUE DE LA KINASE À RÉPÉTITIONS RICHES EN LEUCINE
申请人:MERCK SHARP & DOHME
公开号:WO2015026683A1
公开(公告)日:2015-02-26
The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
METHOD FOR OBTAINING 5-AMINO-2,3-DIHYDROPHTHALAZINE-1,4-DIONE ALKALI METAL SALTS AND THEIR USE IN MEDICINE
申请人:ABIDOPHARMA PL SP. Z.O.O.
公开号:US20140113902A1
公开(公告)日:2014-04-24
A method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salts with alkali metals of the formula II, pharmaceutical compositions including such salts, and their application in medicine. The sodium salt may be used for treatment of heart diseases, pancreas diseases and diabetes as well as optionally in combination with lithium salt for treatment of the nervous system diseases.
where M represents Li, Na, K
The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Amphiphilic Block Copolymer And Preparation Method Thereof And Micellar Drug-Loading System Formed By Same With Antitumor Drug
申请人:LIU Ke
公开号:US20150283246A1
公开(公告)日:2015-10-08
The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided. Said micelles are more effective in restricting the drug molecules inside the micellar core and preventing the drug from dissolved out of the micelles. Therefore, a drug-loaded micelle with high stability is obtained.