Four kinds of symmetrically branched oligoglyceryl trimeric (BGL003)-paclitaxel conjugates and a corresponding heptameric (BGL007) conjugate were synthesized. Molecular weights of all the compounds were less than two times that of paclitaxel. The anti-tumor activity of the most water-soluble BGL003 conjugate was examined and found to be preserved in spite of the chemical modification that is displacement of the N3'-debenzoyl residue with the BGL003 succinyl residue. (C) 2012 Elsevier Ltd. All rights reserved.
[EN] CARBOHYDRATE CONJUGATED RNA AGENTS AND PROCESS FOR THEIR PREPARATION<br/>[FR] AGENTS D'ARN CONJUGUÉS À DES GLUCIDES ET LEUR PROCÉDÉ DE PRÉPARATION
申请人:ALNYLAM PHARMACEUTICALS INC
公开号:WO2014025805A1
公开(公告)日:2014-02-13
This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.
[EN] 4 -AMINO -7,8- DIHYDROPYRIMIDO [5, 4 - F] [1, 4] OXAZEPIN- 5 ( 6H) - ONE BASED DGAT1 INHIBITORS<br/>[FR] INHIBITEURS DE DGAT1 À BASE DE 4-AMINO-7,8-DIHYDROPYRIMIDO[5,4,F][1,4]OXAZÉPIN-5(6H)-ONE
申请人:ASTRAZENECA AB
公开号:WO2011121350A1
公开(公告)日:2011-10-06
DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro- drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, diabetes and obesity wherein, R1, R2, R3, R4, X2, q, Y1, Y2, n, Q and Z are as defined in the description.
[EN] PROCESS FOR PREPARATION OF LANREOTIDE ACETATE<br/>[FR] PROCÉDÉ DE PRÉPARATION D'ACÉTATE DE LANRÉOTIDE
申请人:EMCURE PHARMACEUTICALS LTD
公开号:WO2019077507A1
公开(公告)日:2019-04-25
The invention relates to an improved method for the solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments wherein the threonine hydroxyl is protected, to give an octapeptide, which on deprotection, oxidation, followed by treatment with acetic acid provides Lanreotide acetate (1) having desired purity.
HIV protease inhibitors useful for the treatment of aids
申请人:MERCK & CO. INC.
公开号:EP0534511A1
公开(公告)日:1993-03-31
Compounds of the form,
A-G-J
wherein A is an amine protecting group or urethane, G a dipeptide isostere and J a small terminal group are described. They are distinguished by tetrahydrofuryl or tetrahydropyranyl substituents, and the like. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
2-aminopyridines containing fused ring substituents
申请人:——
公开号:US20010049379A1
公开(公告)日:2001-12-06
The present invention relates to 2-aminopyridine derivatives of the formula
1
wherein G, R
1
and R
2
are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.