87325-47-1

Upstream product

• 1070-19-5 N-(tert-butyloxycarbonyl) azide 
• 87392-13-0 (2S)-2-amino-4-methylpent-4-enoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 123-91-1 1,4-dioxane 
• 141-78-6 ethyl acetate 
• 200132-62-3 tert-butyl (S)-2-(diphenylmethyleneamino)-4-methylpent-4-enoate 
• 87325-69-7 tert-butyl (2S)-2-amino-4-methylpent-4-enoate 
• 112741-49-8 tert-butyl (2R,3S)-6-oxo-2,3-diphenylmorpholine-4-carboxylate 
• 87325-65-3 (R,S)-2-acetamido-4-methyl-4-pentenoic acid 

Downstream Products

• 666718-78-1 tert-butyl 1-(hydroxymethyl)-3-methylbut-3-enylcarbamate 

Relevant academic research and scientific papers

Synthesis of [4,5-3H-Leu4]salmon calcitonin

The synthesis of salmon calcitonin, a C-terminal amide dotriacontapeptide, labelled with tritium in the leucine residue at position 4 to a specific activity of 100 Ci mmole-1 is described. The peptide was assembled using the Fmoc-Polyamide soli

AMINOCARBAMOYL COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS

The present invention relates to compounds of formula (II) wherein R1-R5, X and L are as described herein, and pharmaceutically acceptable salts thereof, compositions including the compounds and methods of using the compounds, particularly in the treatment and prophylaxis of coronavirus infection.

ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS

The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

Total synthesis of cyclomarins A, C and D, marine cyclic peptides with interesting anti-tuberculosis and anti-malaria activities

Cyclomarins are cyclic heptapeptides containing four unusual amino acids. New synthetic protocols toward their synthesis have been developed, leading to the synthesis and biological evaluation of three natural occurring cyclomarins. Interestingly, cyclomarins address two completely different targets: Clp C1, a subunit of the caseinolytic protease of Mycobacterium tuberculosis (MTB), as well as PfAp3Ase of Plasmodium falciparum. Therefore, cyclomarins are interesting lead structures for the development of drugs against tuberculosis and malaria.

HIV PROTEASE INHIBITORS

Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.

Cysteinyl protease inhibitors

Amino acid di- and tri-peptide analogs having C-terminal vinylic groups, pharmaceutical compositions containing the analogs and methods of treating diseases using cysteinyl protease inhibitors; particularly neurodegenerative, autoimmune, cognitive disorde

Cathepsin cysteine protease inhibitors

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.