157754-77-3

Upstream product

• 147269-67-8 3-(benzyloxycarbonylamino)pyrid-2-one 
• 6332-56-5 3-nitropyridone 
• 33630-99-8 3-amino-2-pyridone 
• 147269-67-8 (2-hydroxypyridin-3-yl)carbamic acid benzyl ester 
• 100-51-6 benzyl alcohol 
• 609-71-2 2-hydroxy-3-carboxypyridine 

Relevant academic research and scientific papers

Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues

The obligate intracellular bacterium Chlamydia trachomatis (C. trachomatis) is responsible for the most common bacterial sexually transmitted infection and is the leading cause of preventable blindness, representing a major global health burden. While C.

SYSTEMIC FORMULATION OF A PYRIDINONE DERIVATE FOR COELIAC DISEASE

The present invention relates to a systemic formulation, in particular an oral formulation, for the prophylaxis and/or treatment of coeliac disease, i.e. for use in the prophylaxis and/or treatment of coeliac disease.

SYSTEMIC FORMULATION OF A PYRIDINONE DERIVATE FOR TG2-RELATED DISEASES

The present invention relates to a formulation in particular an oral formulation for the prophylaxis and treatment of TG2-related disorders like fibrosis in particular diabetic nephropathy and/or diabetic associated non-alcoholic steatohepatitis (NASH) an

Tissue transgutaminase pyridinone deriv. as inhibitor

Pyridinone derivatives (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. Pyridinone derivatives of formula (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. E1, E2 : -CO- or -SO 2; Rc : -NYY1a, -NH-CH 2-COOH, -NH-CH(CH 3)-COOH, -NH-CH (CH 2CH 2SCH 3)-COOH, -NH-CH(CH 2OH)-COOH, -NH-CH(CH 2SH)-COOH, -NH-CH(CH 2CONH 2)-COOH,-NH-CH(CH 2CH 2CONH 2)-COOH, [(1-carboxy-2-methyl-propyl)amino], [(1-carboxy-2-methyl-butyl)amino], [(1-carboxy-3-methyl-butyl)amino], [(1-carboxy-2-hydroxy-propyl)amino], [(1-benzyl-2-hydroxy-2-oxo-ethyl)amino], [[2-hydroxy-2-oxo-1-(p-tolylmethyl)ethyl]amino], [(1-carboxy-3-hydroxy-3-oxo-propyl)amino], [(1-carboxy-4-hydroxy-4-oxo-butyl)amino], piperazin-1-yl, morpholino, 1-piperidyl, (4-phenylpiperazin-1-yl), (4-benzylpiperazin-1-yl), (4-phenylpiperazin-1-yl), (4-methylpiperazin-1-yl), (2-oxo-1-piperidyl), (2,6-dioxo-1-piperidyl), isoindolin-2-yl, azepan-1-yl, azetidin-1-yl, aziridin-1-yl, 4,5-dihydrotriazol-1-yl, (3-methylimidazolidin-1-yl), pyrrolidin-1-yl, (2-oxopyrrolidin-1-yl), or (2,5-dioxopyrrolidin-1-yl); and Z : -CH 3, -C 2H 5, -C 3H 7, -CH(CH 3) 2,-C 4H 9, -C 6H 5, -CH 2-C 6H 5, -OCH 3, -OC 2H 5, -OC 3H 7, -OCH(CH 3) 2, -OC 4H 9, -OC 6H 5, -OCH 2C 6H 5, -OCH=CH 2 or -OCH 2-CH=CH 2. N.B. Rd is not defined. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a pharmaceutical composition comprising (I) and carrier, excipient or solvent; and (2) preparation of (I). [Image] ACTIVITY : Antiinflammatory; Neuroprotective; Anticonvulsant; Nootropic; Antiparkinsonian; Ophthalmological; Antiseborrheic; Dermatological; Antipsoriatic; Thrombolytic. MECHANISM OF ACTION : Transglutaminase 2 inhibitor.

Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis

Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.