186743-06-6

Upstream product

• 106539-14-4 (S)-methyl 3-(tert-butyloxycarbonylamino)butyrate 
• 210533-61-2 tert-butyl (S)-(4-(methoxy(methyl)amino)-4-oxobutan-2-yl)carbamate 
• 172695-22-6 (2-cyano-1(S)-methylethyl)carbamic acid, 1,1-dimethylethyl ester 
• 166194-56-5 (S)-ethyl 3-((tert-butoxycarbonyl)amino)butanoate 
• 15761-38-3 L-N-Boc-Ala 
• 631914-55-1 Boc-L-Ala-Cl 
• 842103-83-7 (R)-tert-butyl 4-(methoxy(methyl)amino)-4-oxobutan-2-ylcarbamate 
• 167216-17-3 (-)-tert-butyl [(R)-3-hydroxy-1-methylpropyl]carbamate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 159991-23-8 (R)-3-((tert-butoxycarbonyl)amino)butanoic acid 
• 3744-87-4 Boc-(R)-Ala 
• 954143-61-4 (R)-2-tert-butoxycarbonylaminopropionyl chloride 
• 186521-98-2 N-[(1R)-3-diazo-1-methyl-2-oxopropyl]carbamic acid tert-butyl ester 
• 159877-47-1 methyl 3-(R)-[N-(tert-butoxycarbonyl)amino]-propanoate 

Downstream Products

• 842103-85-9 C₂₁H₃₂N₂O₆ 

Relevant academic research and scientific papers

Modulation of the Passive Permeability of Semipeptidic Macrocycles: N- And C-Methylations Fine-Tune Conformation and Properties

Incorporating small modifications to peptidic macrocycles can have a major influence on their properties. For instance, N-methylation has been shown to impact permeability. A better understanding of the relationship between permeability and structure is of key importance as peptidic drugs are often associated with unfavorable pharmacokinetic profiles. Starting from a semipeptidic macrocycle backbone composed of a tripeptide tethered head-to-tail with an alkyl linker, we investigated two small changes: peptide-to-peptoid substitution and various methyl placements on the nonpeptidic linker. Implementing these changes in parallel, we created a collection of 36 compounds. Their permeability was then assessed in parallel artificial membrane permeability assay (PAMPA) and Caco-2 assays. Our results show a systematic improvement in permeability associated with one peptoid position in the cycle, while the influence of methyl substitution varies on a case-by-case basis. Using a combination of molecular dynamics simulations and NMR measurements, we offer hypotheses to explain such behavior.

Enzymatic Polyketide Chain Branching to Give Substituted Lactone, Lactam, and Glutarimide Heterocycles

Polyketides typically result from head-to-tail condensation of acyl thioesters to produce highly functionalized linear chains. The biosynthesis of the phytotoxin rhizoxin, however, involves a polyketide synthase (PKS) module that introduces a δ-lactone ch

SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1 C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.

Peptide analogues comprising at least one type of aminoacylaza-γ(b)3and the use thereof, in particular for therapy

The object of the present invention is analogues of peptides or parent proteins, these peptide analogues, comprising at least one aza-β3 aminoacyl residue, and also their uses in pharmaceutical compositions or for the diagnosis of pathologies w

Syntheses of aza-analogues of macrosphelides via RCM strategy and their biological evaluation

Syntheses of 16-membered macrolactams, which were aza-analogues of macrosphelides, could be established effectively by a ring-closing metathesis (RCM) strategy. Novel 19 analogues and six aza-macrosphelide-epothilone hybrids were furnished according to si

A configurational switch based on iridium-catalyzed allylic cyclization: Application in asymmetric total syntheses of prosopis, dendrobate, and spruce alkaloids

A method for the stereoselective synthesis of 2,6-disubstituted piperidines has been developed that is based on the use of an intramolecular iridium-catalyzed allylic substitution as a configurational switch. The procedure allows the preparation of 2-viny

Stereoselective synthesis of 2,6-disubstituted piperidines using the iridium-catalyzed allylic cyclization as configurational switch: Asymmetric total synthesis of (+)-241 D and related piperidine alkaloids

Total stereoselective synthesis of the dendrobate alkaloid (+)-241D, its C6-epimer, and a spruce alkaloid, was presented. The configurational switch allows preparation of each of the eight stereoisomers with high selectivity, due to availability of enanti

SUBSTITUTED PYRAZOLE AND TRIAZOLE COMPOUNDS AS KSP INHIBITORS

Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis

Conformational analysis of trans-1,2-disubstituted cyclohexane CCR3 antagonist 2 revealed that the cyclohexane linker could be replaced by an acyclic syn-α-methyl-β-hydroxypropyl linker. Synthesis and biological evaluation of mono- and disubstituted propyl linkers support this conformational correlation. It was also found that the α-methyl group to the urea lowered protein binding and that the β-hydroxyl group lowered affinity for CYP2D6. Ab initio calculations show that the α-methyl group governs the spatial orientation of three key functionalities within the molecule. α-Methyl-β-hydroxypropyl urea 31 with a chemotaxis IC50 = 38 pM for eosinophils was chosen to enter clinical development for the treatment of asthma.

Substituted imidazole compounds as KSP inhibitors

The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds. The compounds of the invention have the following general formula: