540496-34-2

Upstream product

• 87219-29-2 benzyl (3S)-5-oxotetrahydro-3-furanylcarbamate 
• 100-39-0 benzyl bromide 
• 161745-47-7 benzyl 3(S)-<(tert-butoxycarbonylamino)>-4-p-toluenesulfonyl-1-butyrate 
• 2177-63-1 (S)-2-amino-4-(benzyloxy)-4-oxobutanoic acid 
• 79069-52-6 N-Boc-L-aspartic aldehyde β-benzyl ester 
• 4515-23-5 N-benzyloxycarbonyl-L-aspartic acid anhydride 
• 79069-16-2 benzyl (3S)-3-[(tert-butoxycarbonyl)amino]-4-hydroxybutanoate 
• 7536-58-5 BOC-L-aspartic acid 4-benzyl ester 
• 1152-61-0 N-Cbz-L-Asp 
• 84890-97-1 (S)-3-tert-Butoxycarbonylamino-4-isobutoxycarbonyloxy-4-oxo-butyric acid benzyl ester 

Downstream Products

• 540496-36-4 [(S)-3-((S)-2-tert-Butoxycarbonylamino-3-methyl-butyryl)-2-oxo-oxazolidin-4-yl]-acetic acid benzyl ester 
• 760979-68-8 {(S)-3-[2-((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetyl]-2-oxo-oxazolidin-4-yl}-acetic acid benzyl ester 
• 760979-71-3 [(S)-3-(2-{(S)-3-[2-((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetyl]-2-oxo-oxazolidin-4-yl}-acetyl)-2-oxo-oxazolidin-4-yl]-acetic acid benzyl ester 
• 760979-74-6 ((S)-3-{2-[(S)-3-(2-{(S)-3-[2-((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetyl]-2-oxo-oxazolidin-4-yl}-acetyl)-2-oxo-oxazolidin-4-yl]-acetyl}-2-oxo-oxazolidin-4-yl)-acetic acid benzyl ester 
• 760979-73-5 [(S)-3-(2-{(S)-3-[2-((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetyl]-2-oxo-oxazolidin-4-yl}-acetyl)-2-oxo-oxazolidin-4-yl]-acetic acid pentafluorophenyl ester 
• 760979-70-2 {(S)-3-[2-((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetyl]-2-oxo-oxazolidin-4-yl}-acetic acid pentafluorophenyl ester 
• 760979-67-7 ((S)-3-Acetyl-2-oxo-oxazolidin-4-yl)-acetic acid pentafluorophenyl ester 
• 603142-91-2 (4S)-4-(2-fluoro-2-methylpropyl)-1,3-oxazolidin-2-one 

Relevant academic research and scientific papers

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Cathepsin K inhibitors and use thereof

The invention relates to compounds and pharmaceutical compositions thereof for treatment or prevention of cathepsin dependent diseases; the compounds and the compositions comprising the compounds can be used as bone absorption inhibitors for treatment of related diseases, wherein the cathepsin includes, but is not limited to, cathepsin K.

3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH

The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K

Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors.

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 i

Practical and efficient route to (S)-γ-fluoroleucine

A practical and efficient route to (S)-γ-fluoroleucine was developed via compound 9. Introduction of the fluorine was achieved using N,N-diethylaminosulfur trifluoride (DAST) treatment on a tertiary alcohol 8.

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R1, R2, R3 et R4 are indicated therein, 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.

CATHEPSIN INHIBITORS

This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3 and R4 are indicated therein, 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, osteoarthritis and rheumatoid arthritis.

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.

β-Pseudopeptide foldamers. the homo-oligomers of (4R)-(2-oxo-1,3-oxazolidin-4-yl)-acetic acid (D-Oxac)

A total synthesis in solution and a conformational analysis of the homo-oligomers of (4R)-(2-oxo-1,3-oxazolidin-4-yl)-acetic acid (D-Oxac) to the tetramer level are described. As the D-Oxac building block contains both an oxazolidin-2-one and a β-amino acid group, it may represent a new type of conformationally constrained tool for the construction of β-pseudopeptide foldamers. A conformational investigation using NMR and an extensive, unconstrained analysis with a Monte Carlo search to the octamer level, both in water and in chloroform, showed that these homo-oligomers tend to fold in a regular helical structure in a competitive solvent, such as water. Since aqueous solutions are of major relevance for biological systems, these molecules are good candidates for application to these environments.