189030-78-2

Upstream product

• 189030-77-1 2R-isobutyl-succinic acid 1-benzyl ester 4-tert-butyl ester 
• 646-07-1 4-Methylpentanoic acid 
• 77509-00-3 phenylmethyl 4-methylpentanoate 
• 100-51-6 benzyl alcohol 
• 129739-13-5 tert-butyl 3-(R)-benzyloxycarbonyl-5-methylhexanoate 

Downstream Products

• 189030-79-3 2-[2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl]-4-methyl-pentanoic acid benzyl ester 
• 153427-82-8 2,2,2-trichloroethyl 3-(R)-benzyloxycarbonyl-5-methylhexanoate 
• 189030-84-0 (R)-2-[2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl]-4-methyl-pentanoic acid ((S)-1-hydroxymethyl-2-phenyl-ethyl)-amide 
• 189030-86-2 (S)-2-[2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl]-4-methyl-pentanoic acid ((S)-1-hydroxymethyl-2-phenyl-ethyl)-amide 

Relevant academic research and scientific papers

Metalloproteinase inhibitors

Compounds of general formula (II) wherein X is a hydroxamic or carboxylic acid group, Y is carbonyl or sulphonyl and R1 and R2 are as defined in the claims, are matrix metalloproteinase inhibitors. STR1

Exploration of the importance of the P2-P3-NHCO-moiety in a potent di- or tripeptide inhibitor of calpain I: insights into the development of nonpeptidic inhibitors of calpain I.

Calpain I, an intracellular cysteine protease, has been implicated in the neurodegeneration following an episode of cerebral ischemia. In this paper, we report on a series of peptidomimetic ketomethylene and carbamethylene inhibitors of recombinant human calpain I (rh calpain I). Our study reveals that the -NHCO-moiety (possible hydrogen-bonding site) at the P2-P3 region of a potent tripeptide or a dipeptide inhibitor of calpain I is not a strict requirement for enzyme recognition. Compounds 7d ((R)-2-isobutyl-4-oxo-4-(9-xanthenyl)butanoic acid ((S)-1-formyl-3-methyl)butyl amide), 31 ((R)-2-isobutyl-4-(2-sulfonylnaphthyl)butyric acid ((S)1-formyl-3-methyl)butyl amide) and 34 ((R)-2-isobutyl-4-(2-sulfoxylnaphthyl)butyric acid ((S)-1-formyl-3-methyl)butyl amide) which exhibited good activity in the enzyme assay, also inhibited calpain I in a human cell line.

COLLAGENASE INHIBITOR

Compounds having inhibitory activity against inhibitory activity against type IV collagenase and are useful as angiogenesis, cancer infiltration or cancer metastasis inhibitors. The compounds have the formula: STR1 in which R 1 represents a group of formula:--OR. sup.3 (wherein R 3 represents a hydrogen atom or an alkyl group), --NR 4 R 5 (wherein R 4 and R 5 each represents a hydrogen atom, an alkyl or alkoxy group),--NHCH(R 6 COR 7 (wherein R 6 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, and R 7 represents an alkyl group),--NHCH(R 6)COOR. sup.8 (wherein R 8 represents an alkyl group) or--NHCH(R 6)CONR 9 R 10 (wherein R 9 and R 10 each represents a hydrogen atom or an alkyl group, or NR 9 R 10 together represent a heterocyclic ring group); andR 2 represents a hydrogen atom, an alkyl or aralkyl group.