248953-91-5

Upstream product

• 1197-18-8 trans-4-aminomethyl-cyclohexyl-carboxylic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 27687-14-5 trans 4-(tert-butyloxycarbonylamino)methylcyclohexanecarboxylic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 

Downstream Products

• 248953-96-0 Boc-Tra-ψ(CH2-NH)-Phe-APAA-OBzl 
• 648882-90-0 [4-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-cyclohexylmethyl]-carbamic acid tert-butyl ester 
• 570360-66-6 trans-tert-butyl [4-(1,8-naphthyridin-2-yl)cyclohexyl]methylcarbamate 
• 648882-89-7 (4-acetyl-cyclohexylmethyl)-carbamic acid tert-butyl ester 
• 180046-90-6 trans 4-(tert-butyloxycarbonylaminoethyl)cyclohexaneacetaldehyde 

Relevant academic research and scientific papers

Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors

In this study, a series of novel hydroxyamidine derivatives were identified as potent and selective IDO1 inhibitors by structure-based drug design. Among them, compounds 13-15 and 18 exhibited favorable enzymatic and cellular activities. Compound 18 showed improved bioavailability in mouse, rat, and dog (F% = 44%, 58.8%, 102.1%, respectively). With reasonable in vivo pharmacokinetic properties, compound 18 was further evaluated in a transgenic MC38 xenograft mouse model. The combination of compound 18 with PD-1 monoclonal antibody showed a synergistic antitumor effect. These data indicated that compound 18 as a potential cancer immunotherapy agent should warrant further investigation.

Halogenated sulfonamide derivatives

This invention is directed to halogenated sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutic

Design and synthesis of 1,5- and 2,5-substituted tetrahydrobenzazepinones as novel potent and selective integrin αVβ3 antagonists

The design and synthesis of novel integrin αVβ3 antagonists based on a 1,5- or 2,5-substituted tetrahydrobenzaezpinone core is described. In vitro activity of respective compounds was determined via αVβ3 binding assay, and selected derivatives were submitted to further characterization in functional cellular assays. SAR was obtained by modification of the benzazepinone core, variation of the spacer linking guanidine moiety and core, and modification of the guanidine mimetic. These efforts led to the identification of novel αVβ3 inhibitors displaying potency in the subnanomolar range, selectivity versus αIIbβ3 and functional efficacy in relevant cellular assays. A method for the preparation of enantiomerically pure derivatives was developed, and respective enantiomers evaluated in vitro. Compounds 31 and 37 were assessed for metabolic stability, resorption in the Caco-2 assay and pharmacokinetics.

Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: The importance of the peptide backbone

Pseudo-peptide analogs of trans-4-aminomethylcyclohexanecarbonyl-L- phenylalanyl-4-aminophenyl acetic acid (PKSI-527, plasma kallikrein selective inhibitor), in which an amide bond (peptide bond) has been replaced by a CH2-NH bond, i.e. trans-4