17704-74-4

Upstream product

• 19355-69-2 2-amino-2-cyanopropane 
• 73470-46-9 tert-butyl (1-amino-2-methyl-1-oxopropan-2-yl)carbamate 
• 30992-29-1 Boc-Aib-OH 

Downstream Products

• 16252-90-7 2-amino-2-methylpropanamide 
• 173336-46-4 3-tert-butoxycarbonyl-5(S)-{2(S)-[N-(1-carbamoyl-1-methyl-ethyl)-carbamoyl]-2(S)-isopropyl-ethyl}-4(S)-{2(S)-isopropyl-3-[4-methoxy-3-(3-methoxypropyloxy)-phenyl]-propyl}-2,2-dimethyl-1,3-oxazolidine 
• 1143507-06-5 N-(2-amino-1,1-dimethyl-2-oxoethyl)-3-(4-{[2-({ethyl[(4-fluorophenyl)sulfonyl]amino}methyl)-3,3,3-trifluoro-2-hydroxypropyl]amino}-6-methyl-1H-indazol-1-yl)benzamide 
• 1143502-63-9 N-(2-amino-1,1-dimethyl-2-oxoethyl)-3-{6-methyl-4-[(3,3,3-trifluoro-2-hydroxy-2-{[(1-methylethyl)(2-methylpropanoyl)amino]methyl}propyl)amino]-1H-indazol-1-yl}benzamide 
• 1142945-38-7 N-[2-({[1-(3-{[(2-amino-1,1-dimethyl-2-oxoethyl)amino]carbonyl}phenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-3,3,3-trifluoro-2-hydroxypropyl]-2,6-dichloro-N-ethylbenzamide 
• 1142945-45-6 N-[2-({[1-(3-{[(2-amino-1,1-dimethyl-2-oxoethyl)amino]carbonyl}phenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-3,3,3-trifluoro-2-hydroxypropyl]-2,6-dichloro-N-(1-methylethyl)benzamide 
• 1170700-89-6 2-[5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-yl]-5,5-dimethyl-3,5-dihydroimidazol-4-one 
• 1610954-94-3 N-(1-amino-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide 
• 652997-78-9 N-(2-amino-1,1-dimethyl-2-oxoethyl)-3-[6-(ethylthio)-3,4,8,9-tetrahydro-3,3,8,8-tetramethylfuro[2,3-h]isoquinolin-1-yl]benzamide 
• 62-57-7 2-Aminoisobutyric acid 

Relevant academic research and scientific papers

Imidazol-4-one and Imidazole-4-thione Compounds

Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.

PYRIDINE DERIVATIVES AS SODIUM CHANNEL BLOCKERS

Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein; each of R1 to R4 is independently selected from hydrogen and C1-4 alkyl, and each of rings A and B independently is optionally further substi

QUINAZOLINE DERIVATIVES

A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.

Dipeptide nitriles

N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.

Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors

The specificity of the immune response relies on processing of foreign proteins and presentation of antigenic peptides at the cell surface. Inhibition of antigen presentation, and the subsequent activation of T-cells, should, in theory, modulate the immune response. The cysteine protease Cathepsin S performs a fundamental step in antigen presentation and therefore represents an attractive target for inhibition. Herein, we report a series of potent and reversible Cathepsin S inhibitors based on dipeptide nitriles. These inhibitors show nanomolar inhibition of the target enzyme as well as cellular potency in a human B cell line. The first X-ray crystal structure of a reversible inhibitor cocrystallized with Cathepsin S is also reported.

CONVERSION OF α-AMINONITRILES TO AMIDES BY A NEW PINNER TYPE REACTION

α-Aminonitriles were converted exclusively to the amides by 2-mercaptoethanol in anhydrous THF at -78 deg C by bubbling dry HCl gas.

Hydrolysis of various nitrile compounds to the amides by catalysis of 2-mercaptoethanol in a phosphate buffer

α-Aminonitriles, 4-nitrobenzonitrile and 3,5-dinitrobenzonitrile were hydrolyzed exclusively to amides efficiently when they were stirred with 2-mercaptoethanol in a phosphate buffer (pH 7.0, 50 mM).