Preparation ofl-Threoninol and Its Bisoxazoline Derivative
摘要:
(R,R)-Threoninol was prepared in one step from L-threonine in 86% isolated yield. The product was regioselectively transformed into 2,2-bis[(4R,5R)-4-(hydroxymethyl)-5-methyl-1,3-oxazolin-2-yl]propane in 42% isolated yield.
[EN] INHIBITORS OF APOL1 AND USE OF THE SAME<br/>[FR] INHIBITEURS D'APOL1 ET LEUR UTILISATION
申请人:VERTEX PHARMA
公开号:WO2021252859A1
公开(公告)日:2021-12-16
The disclosure provides at least one compound, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of formula (I), deuterated derivatives thereof, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of making and using the same, including use in treating APOL1 mediated kidney disease.
Through a series of linkers, 9-amino-2-methoxy-6-nitroacridine and 9-amino-6-chloro-2-methoxyacridine were tethered to the middle of oligonucleotide, and the abilities of these conjugates for site-selective activation of RNA (inducing site-selective scission by Lu(III)) were compared. The RNA-activating ability was strongly dependent on the structures of both acridine and linker. By tethering 9-ami
[EN] PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES<br/>[FR] INHIBITEURS DE JAK3 DE TYPE PYRROLOPYRIDAZINE ET LEUR UTILISATION POUR TRAITER LES MALADIES INFLAMMATOIRES ET AUTO-IMMUNES
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012125887A1
公开(公告)日:2012-09-20
Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
molecular Ni catalysis driven by light, which enables stereoretentive C-N coupling of opticallyactive amines, amino alcohols, and amino acid esters with aryl bromides, with no need for any external photosensitizer. The method is effective for a wide variety of coupling partners, including those bearing functional groups sensitive to bases and nucleophiles, thus providing a viable alternative to accessing
[EN] PROCESS FOR PREPARATION OF OCTREOTIDE ACETATE<br/>[FR] PROCÉDÉ DE PRÉPARATION D'ACÉTATE D'OCTRÉOTIDE
申请人:EMCURE PHARMACEUTICALS LTD
公开号:WO2017175107A1
公开(公告)日:2017-10-12
Disclosed herein is an improved 4+4 solution phase synthesis of octreotide acetate. The process comprises coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, and treatment with acetic acid provides octreotide acetate having desired purify.