1932593-75-3

Upstream product

• 149152-68-1 (2S,4S)-1-tert-butyl 2-methyl 4-(((benzyloxy)carbonyl)amino)pyrrolidine-1,2-dicarboxylate 
• 501-53-1 benzyl chloroformate 
• 1018667-18-9 1-tert-butyl 2-methyl (2R,4R)-4-aminopyrrolidine-1,2-dicarboxylate 
• 1279038-50-4 (2S,4R)-tert-butyl 4-amino-2-(hydroxymethyl)pyrrolidine-1-carboxylate hydrochloride 

Downstream Products

• 1194057-65-2 ethyl 7-((2S,4R)-4-benzyloxycarbonylamino-2-(hydroxymethyl)pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-8-hydroxymethyl-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 1194057-67-4 ethyl (3aS,5R)-5-benzyloxycarbonylamino-13-cyclopropyl-8-fluoro-10-oxo-3a,4,5,6,10,13-hexahydro-1H,3H-pyrrolo[2',1':3,4][1,4]oxazepino[5,6-h]quinoline-11-carboxylate 
• 1194057-64-1 ethyl 7-((2S,4R)-4-benzyloxycarbonylamino-2-(hydroxymethyl)pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-8-fomyl-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 1460305-27-4 benzyl N-[(15R,16aS)-10-methyl-9,12-dioxo-9,10,11,12,15,16,16a,17-octahydro-14H-dibenzo[i,k ]pyrrolo[2,1-c][1,4,7]oxadiazacyclododecin-15-yl]carbamate 

Relevant academic research and scientific papers

ROR [gamma]t inhibitor, preparation method and application thereof

The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.

INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR AND USE THEREOF

Provided are an irreversible inhibitor of a fibroblast growth factor receptor (FGFR) as indicated by formula I, a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical preparation, a pharmaceutical composition and an application thereof. R1, R2, R3, R4, ring A, Ar, ring B and warhead are as defined in the specification. The compound has high-efficiency and high-selectivity inhibition of a fibroblast growth factor receptor and can be applied to treatment of abnormal FGF/FGFR-mediated diseases, in particular the treatment of cancers.

SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.

CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS

The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate (TBTU): A new reagent for the cleavage of tetrahydropyranyl, silyl and 4,4'- dimethoxytrityl ethers

A new reagent for the cleavage of tetrahydropyranyl, silyl and 4,4'- dimethoxytrityl ethers is described.

A simple and convenient method for the deprotection of tetrahydropyranyl ether using iodine in methanol

A simple and efficient method for the deprotection of tetrahydropyranyl and 4,4'-dimethoxytrityl ethers using iodine in methanol is described.