483334-60-7

Upstream product

• 5781-53-3 monomethyl oxalyl chloride 
• 6310-21-0 2-(1,1-dimethylethyl)-benzenamine 

Downstream Products

• 254751-08-1 2-((2-(tert-butyl)phenyl)amino)-2-oxoacetic acid 
• 1307704-41-1 1-(2-tert-butylphenyl)indoline-2,3-dione 
• 409369-33-1 3-{2-[(2-tert-butyl-phenylaminooxalyl)-amino]-3-methyl-butyrylamino}-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid tert-butyl ester 
• 254750-83-9 (3S)-3-[N-(N′-(2-tert-butylphenyl)oxamyl)alaninyl]amino-5-(2′,3′,5′,6′-tetrafluorophenoxy)-4-oxopentanoic acid tert-butyl ester 
• 254750-82-8 (3S)-3-[N-(N′-(2-tert-butylphenyl)oxamyl)alaninyl]amino-5-(2′,3′,5′,6′-tetrafluorophenoxy)-4-hydroxypentanoic acid tert-butyl ester 
• 254750-02-2 Emricasan 
• 868565-89-3 5-bromo-3-{2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino}-4-oxo-pentanoic acid tert-butyl ester 
• 868565-78-0 2-{2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino}-succinic acid 4-tert-butyl ester 

Relevant academic research and scientific papers

CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF

Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.

METHODS OF USING CASPASE INHIBITORS IN TREATMENT OF LIVER DISEASE

Provided herein are methods and compositions for treatment of an elevated MELD score or Child-Pugh score or their components by administering a of a caspase inhibitor alone or in combination with current treatments for liver disease.

Reagent Design and Ligand Evolution for the Development of a Mild Copper-Catalyzed Hydroxylation Reaction

Parallel synthesis and mass-directed purification of a modular ligand library, high-throughput experimentation, and rational ligand evolution have led to a novel copper catalyst for the synthesis of phenols with a traceless hydroxide surrogate. The mild reaction conditions reported here enable the late-stage synthesis of numerous complex, druglike phenols.

TREATMENT OF THE COMPLICATIONS OF CHRONIC LIVER DISEASE

Provided herein are methods and compositions for treatment of a portal hypertension and cirrhosis by administering a of a caspase inhibitor alone or in combination with current treatments for portal hypertension. Also provided are methods and compositions

Synthesis of N -arylisatins by the reaction of arynes with methyl 2-Oxo-2-(arylamino)acetates

N-Arylisatins are efficiently prepared by the reaction of 2-oxo-2-(arylamino)acetates and arynes under mild reaction conditions

Highly enantioselective synthesis of atropisomeric anilide derivatives through catalytic asymmetric N-arylation: Conformational analysis and application to asymmetric enolate chemistry

In the presence of (R)-DTBM-SEGPHOS-Pd(OAc)2 catalyst, N-arylation (aromatic amination) of various o-tert-butylanilides with p-iodonitrobenzene proceeds with high enantioselectivity (88-96% ee) to give atropisomeric N-(p-nitrophenyl)anilides having an N-C chiral axis in good yields. Atropisomeric anilide products highly prefer to exist as the E-rotamer which has trans-disposed o-tert-butylphenyl group and carbonyl oxygen. The application of the present catalytic enantioselective N-arylation to an intramolecular version gives atropisomeric lactam derivatives with high optical purity (92-98% ee). The reaction of the lithium enolate prepared from the atropisomeric anilide and lactam products with various alkyl halides gives α-alkylated products with high diastereoselectivity (diastereomer ratio = 13:1 to 46:1).

First-in-class pan caspase inhibitor developed for the treatment of liver disease

A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in vitro data, inhibitors were selected for study in a murine model of α-Fas-induced liver injury. IDN-6556 (1) was further profiled in additional in vivo models and pharmacokinetic studies. This first-in-class caspase inhibitor is now the subject of two Phase II clinical trials, evaluating its safety and efficacy for use in liver disease.

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke

Structural modifications were made to a previously described acyl dipeptide caspase inhibitor, leading to the oxamyl dipeptide series. Subsequent SAR studies directed toward the warhead, P2, and P4 regions of this novel peptidomimetic are described herein.

C-terminal modified oxamyl dipeptides as inhibitors of the ICE-ced-3 family of cysteine proteases

This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients su