125064-54-2

Upstream product

• 78945-91-2 cloruro acido della 2-metil-3-carbossi-4-fenil-1,2-diidro-1-ossiisochinolina 
• 78945-92-3 1,2-dihydro-2-methyl-1-oxo-4-phenyl-3-isoquinolinecarboxylic acid 

Downstream Products

• 1027396-00-4 (2-Methyl-1-oxo-4-phenyl-1,2-dihydro-isoquinolin-3-yl)-acetyl chloride 
• 167756-82-3 1,2-dihydro-2-methyl-1-oxo-4-phenyl-3-isoquinolineacetic acid 
• 167756-81-2 1,2-dihydro-2-methyl-1-oxo-4-phenyl-1(2H)-isoquinolineacetonitrile 
• 1027146-46-8 1,2-dihydro-N,2-dimethyl-1-oxo-4-phenyl-3-isoquinolinemethylamine 
• 159819-94-0 3-<<(methylsulfonyl)oxy>methyl>-2-methyl-4-phenyl-1(2H)-isoquinolinone 

Relevant academic research and scientific papers

Isoquinolinyl compounds which are useful in treating cerebral vascular disorders

Compounds represented by the formula: STR1 wherein the ring A and the ring B each stand for an optionally substituted benzene ring; Ar stands for an optionally substituted aryl group or an optionally substituted heterocyclic group; Q stands for an oxygen atom or a sulfur atom; R stands for a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted amino group; X stands for --O-- or --NR1 -- wherein R1 stands for a hydrogen atom or an optionally substituted hydrocarbon group; Y stands for --O--, --NR2 -- wherein R2 stands for a hydrogen atom or an optionally substituted hydrocarbon group, or a bond; m denotes 1, 2 or 3, and n denotes 0, 1 or 2, and salts thereof which have excellent calcium- or substance P receptor-antagonistic activity, being useful for treating a cerebralvascular disorder in mammals such as cerebralischemia, cerebral edema and neuronal damage, their production and use.

Condensed heterocyclic compounds, their production and use

Novel compound represented by the formula: STR1 such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3-acetamide: STR2 or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.

Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyridopyridine

A series of 4-phenylisoquinolone derivatives were synthesized and evaluated for NK1 (substance P) antagonist activity.Highly potent antagonists, 4-phenyl-3-isoquinolone-N-benzylcarboxamides (11), were discovered from the structure-activity relationship studies on the isoquinolone-urea lead 1a.Optimization of the activity in this series resulted in the development of 5-phenyl-6-pyridopyridine-N-benzylcarboxamides (30) which are highly potent orally active NK1 antagonists.Among the compounds synthesized, N--7,8-dihydro-N,7-dimethyl-8-oxo-5-(substituted phenyl)-6-pyridopyridinecarboxamides (30a,f,g) showed excellent antagonist activities with IC50 values (in vitro inhibition of 125I>BH-SP binding in human IM-9-cells) of 0.21-0.34 nM and ED50 values (in vivo inhibition of capsaicin-induced plasma extravasation in guinea-pig trachea, iv) of 0.017-0.030 mg/kg.These compounds exhibited significantly potent activity upon oral adiministration with ED50 values of 0.068-0.17 mg/kg.Conformational studies on 30g indicated that the two stable conformers of 30g are quite similar to those of CP-99,994.

Isoquinolinones

Therapeutically useful isoquinolinone derivatives of the formula A--X--R3, wherein A represents a group of the formula: STR1 wherein R1 and R2 represents cycloalkyl, alkyl, alkenyl or alkynyl optionally substituted by halo