64362-32-9Relevant academic research and scientific papers
Benzopyridazinone and pyridopyridazinone compounds
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, (2008/06/13)
Benzo or pyridopyridazinones and pyridazinthiones of the formula STR1 wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur; R1 is hydrogen, lower alkyl, aryl, aralkyl, heterocyclo, heterocyclo lower-alkyl, heteroaryl, or heteroaralkyl; R2, R3, R4, R5 and R6 are independently selected from hydrogen, lower alkyl, halo, carboxy, alkoxycarbonyl, carbamoyl, lower-alkyl carbonyl, halocarbonyl, thiomethyl, trifluoromethyl, cyano or nitro; or a pharmaceutically acceptable ester, ether or salt thereof, have been found to be useful as an anti-inflammatory, antasthmatic, immunosuppressive, anti-allograft rejection, anti-graft-vs-host rejection, autoimmune disease or analgetic agent(s).
Tricyclic thiazole and oxazole derivatives and pharmaceutical agents containing them
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, (2008/06/13)
The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I STR1 in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R1 which can be the same or different, Y represents an oxygen or sulphur atom, or a SO or SO2 group, X can be an oxygen or sulphur atom, R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms, in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.
Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyridopyridine
Natsugari, Hideaki,Ikeura, Yoshinori,Kiyota, Yutaka,Ishichi, Yuji,Ishimaru, Takenori,et al.
, p. 3106 - 3120 (2007/10/02)
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.
Application of Organolithium and Related Reagents in Synthesis, Part VI . A General Study of the Lithiation of Secondary Picoline- and Isonicotine Amides
Epsztajn, Jan,Jozwiak, Andrzej,Czech, Krzysztof,Szczesniak, Aleksandra K.
, p. 909 - 921 (2007/10/02)
The lithiation of secondary picoline- (1) and isonicotine-amides (2) and the subsequent reaction of the corresponding (N- and 3-)lithiated amides (3 and 4) with N,N-dimethylbenzamide towards the synthesis of the C3-benzoylated picoline (12a) an
