62471-40-3

Upstream product

• 124-68-5 2-Amino-2-methyl-1-propanol 
• 501-53-1 benzyl chloroformate 
• 150391-25-6 ethyl 2-(((benzyloxy)carbonyl)amino)-2-methylpropanoate 
• 13139-17-8 N-(Benzyloxycarbonyloxy)succinimide 
• 88282-48-8 2,5-dioxopyrrolidin-1-yl 2-(((benzyloxy)carbonyl)amino)-2-methylpropanoate 
• 15030-72-5 Z-Aib-OH 

Downstream Products

• 114856-91-6 benzyl (2-methyl-1-oxopropan-2-yl)carbamate 
• 62471-43-6 2-carbobenzoxyamino-2-methyl-1-propyl acetate 
• 1032764-10-5 2-(benzyloxycarbonyl)amino-2-methylpropyl thioacetate 
• 1037832-93-1 3-(2-(benzyloxycarbonylamino)-2-methylpropoxy)-2,2-dimethyl-3-oxopropane-1-sulfonic acid 
• 1037832-92-0 2-(benzyloxycarbonylamino)-2-methylpropyl 3-(acetylthio)-2,2-dimethylpropanoate 
• 1037833-02-5 S-2-(2-(benzyloxycarbonylamino)-2-methylpropylthio)ethyl ethanethioate 
• 1037833-13-8 benzyl 1-(N-acetylsulfamoyl)-2-methylpropan-2-ylcarbamate 
• 1032764-16-1 2-(benzyloxycarbonyl)amino-2-methylpropanesulfonic acid 
• 1037833-03-6 2-(2-(benzyloxycarbonylamino)-2-methylpropylsulfonyl)ethanesulfonic acid 
• 1258834-19-3 2-(benzyloxycarbonylamino)-1-(tert-butoxycarbonyl-3-hydroxypropylamino)-2-methylpropane 
• 1037832-91-9 2-(benzyloxycarbonylamino)-2-methylpropyl 3-chloro-2,2-dimethylpropanoate 
• 150391-26-7 (S)-2-((S)-2-{(2-Benzyloxycarbonylamino-2-methyl-propyl)-[2-(9H-fluoren-9-ylmethoxycarbonylamino)-acetyl]-amino}-3-phenyl-propionylamino)-4-methyl-pentanoic acid methyl ester 
• 150391-13-2 (S)-2-{(S)-2-[(2-Amino-acetyl)-(2-benzyloxycarbonylamino-2-methyl-propyl)-amino]-3-phenyl-propionylamino}-4-methyl-pentanoic acid methyl ester 
• 150391-11-0 (S)-2-[(S)-2-(2-Benzyloxycarbonylamino-2-methyl-propylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid methyl ester 

Relevant academic research and scientific papers

CHEMICAL COMPOUNDS

A compound of formula (I), wherein Ar1, R21, R23, R24, R25, R26, R27, A, X, Y and W are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS

The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 and A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.

2-(1-HETEROARYLPIPERAZIN-4-YL)METHYL-1,4-BENZODIOXANE DERIVATIVES AS ALPHA2C ANTAGONISTS

Compounds of formula I (formula I), wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2 or 3 N, O or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

DERIVATIVES OF 6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZIN-5- AMINE

The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Efficient access to enantiopure γ4-amino acids with proteinogenic side-chains and structural investigation of γ4- asn and γ4-ser in hybrid peptide helices

Hybrid peptides composed of α- and β-amino acids have recently emerged as new class of peptide foldamers. Comparatively, γ- and hybrid γ-peptides composed of γ4-amino acids are less studied than their β-counterparts. However, recent investigations reveal that γ4-amino acids have a higher propensity to fold into ordered helical structures. As amino acid side-chain functional groups play a crucial role in the biological context, the objective of this study was to investigate efficient synthesis of γ4-residues with functional proteinogenic side-chains and their structural analysis in hybrid-peptide sequences. Here, the efficient and enantiopure synthesis of various N- and C-terminal free-γ4-residues, starting from the benzyl esters (COOBzl) of N-Cbz-protected (E)-α,β-unsaturated γ-amino acids through multiple hydrogenolysis and double-bond reduction in a single-pot catalytic hydrogenation is reported. The crystal conformations of eight unprotected γ4-amino acids (γ4-Val, γ4-Leu, γ4-Ile, γ4-Thr(OtBu), γ4-Tyr, γ4-Asp(OtBu), γ4- Glu(OtBu), and γ-Aib) reveals that these amino acids adopted a helix favoring gauche conformations along the central Cγi￡ Cβ bond. To study the behavior of γ4- residues with functional side chains in peptide sequences, two short hybrid γ-peptides P1 (Ac-Aib-γ4-Asn-Aib-γ4-Leu- Aib-γ4-Leu-CONH2) and P2 (Ac-Aib- γ4-Ser-Aib-γ4-Val-Aib-γ4-Val- CONH2) were designed, synthesized on solid phase, and their 12-helical conformation in single crystals were studied. Remarkably, the γ4-Asn residue in P1 facilitates the tetrameric helical aggregations through interhelical H bonding between the side-chain amide groups. Furthermore, the hydroxyl side-chain of γ4-Ser in P2 is involved in the interhelical H bonding with the backbone amide group. In addition, the analysis of 87 γ4-residues in peptide single-crystals reveal that the γ4-residues in 12-helices are more ordered as compared with the 10/12- and 12/14-helices. Copyright

SUBSTITUTED ISOQUINOLINE DERIVATIVE

The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the

Synthesis of N-vinyloxazolidinones and morpholines from amino alcohols and vinylsulfonium salts: Analysis of the outcome's dependence on the N-protecting group by nanospray mass spectrometry

The effect of the nature of the N-protecting group on 1,2-amino alcohols in annulation reactions with diphenylvinylsulfonium triflate has been investigated. Although tosyl and sulfinamide groups give morpholines in high yields, the use of N-Cbz leads to a high-yielding synthesis of N-vinyloxazolidinones. The reactions were monitored by nanospray MS/MS, which revealed why reactions are successful and the fate of reactive intermediates in the unsuccessful reactions.

Dihydroxyacetone phosphate aldolase catalyzed synthesis of structurally diverse polyhydroxylated pyrrolidine derivatives and evaluation of their glycosidase inhibitory properties

The chemoenzymatic synthesis of a collection of pyrrolidine-type iminosugars generated by the aldol addition of dihydroxyacetone phosphate (DHAP) to C-α-substituted N-Cbz-2-aminoaldehydes derivatives, catalyzed by DHAP aldolases is reported. L-Fuculose-1-phosphate aldolase (FucA) and L-rhamnulose-1-phosphate aldolase (RhuA) from E. coli were used as biocatalysts to generate configurational diversity on the iminosugars. Alkyl linear substitutions at C-α were well tolerated by FucA catalyst (i.e., 40-70% conversions to aldol adduct), whereas no product was observed with C-α-alkyl branched substitutions, except for dimethyl and benzyl substitutions (20%). RhuA was the most versatile biocatalyst: C-α-alkyl linear groups gave the highest conversions to aldol adducts (60-99%), while the C-α-alkyl branched ones gave moderate to good conversions (50-80%), with the exception of dimethyl and benzyl substituents (20%). FucA was the most stereoselective biocatalyst (90-100% anti (3R,4R) adduct). RhuA was highly stereoselective with (S)-N-Cbz-2-aminoaldehydes (90-100% syn (i.e., 3R,4S) adduct), whereas those with R configuration gave mixtures of antilsyn adducts. For iPr and iBu substituents, RhuA furnished the anti adduct (i.e., FucA stereochemistry) with high stereoselectivity. Molecular models of aldol products with iPr and iBu sub-stituents and as complexes with the RhuA active site suggest that the and adducts could be kinetically preferred, while the syn adducts would be the equilibrium products. The polyhydroxylated pyrrolidines generated were tested as inhibitors against seven glycosidases. Among them, good inhibitors of a-L-fucosidase (IC50 = 1-20 μM), moderate of α-L-rhamnosidase (IC50=7-150 μM), and weak of α-D-mannosidase (IC50 = 80-400 μM) were identified. The apparent inhibition constant values (Ki) were calculated for the most relevant inhibitors and computational docking studies were performed to understand both their binding capacity and the mode of interaction with the glycosidases.

Versatile synthesis of free and N-benzyloxycarbonyl-protected 2,2-disubstituted taurines

An effective and versatile method was developed to synthesize N-benzyloxycarbonyl-protected and free 2,2-disubstituted taurines. Several novel 2,2-disubstituted taurines, including aliphatic/aromatic and cyclic/acyclic derivatives, were obtained, which demonstrates the generality of this method. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.

Thiazolidine and oxazolidine derivatives, their preparation and their medical use

Compounds of formula (I): STR1 and salts, esters and solyates thereof and pro-drugs therefor are useful for the treatment and/or prophylaxis of a variety of disorders, including one or more of: hyperlipemia, hyperglycemia, obesity, glucose tolerance insufficiency, insulin resistance and diabetic complications.