4-6-diphenyl pyridine derivatives as antiinflammatory agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S290000, C546S304000, C514S344000, C514S345000

Reexamination Certificate

active

07410986

ABSTRACT:
4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.

REFERENCES:
patent: 0224651 (2002-03-01), None
patent: WO 02/24651 (2002-03-01), None
CAPLUS Accession No. 1927:3281, abstract of Dilthey et al, “Pyrylium compounds. XVII. Arylated pyridines,” Journal fuer Praktische Chemie (Leipsig), 1926, vol. 114, pp. 153-178.
Database Chemcats Online!, Chem, Abstract Service, retrived from STN: XP002197384 and “Ambinter: Screening Collection,” 2001.
Database Chemcats Online!, Chem, Abstract Service, retrived from STN: XP002197385 and “AsInEx Compound Collection,” 2001.
Database Chemcats Online!, Chem, Abstract Service, retrived from STN: XP002197386 and “Chem.Folio.”
Ankhiwala, M.D., “Synthesis and Biological Studies of Some 2-Amino-3-Cyano-4-Aryl-6-(2′-Hydroxy-4′-N-Butoxy-5′-H/Nitrophenyl)pyridines,” J. Ind. Chem. Soc. 69(3), pp. 166-167 (1992).
Manna, F. et al, “Anti-inflammatory, Analgesis, and Antipyretic 4,6-disubstituted 3-cyano-2-aminopyridines,” Eur. J. Med. Chem., vol. 34, pp. 245-254 (1999).
Database Chemcats ′Online!, Chemical Abstracts Service, Columbus, Ohio, US, retrieved from STN; XP002197384 & “Ambinter: Screening Collection”, May 31, 2001, Ambinter, 75016 Paris, France.
Database Chemcats ′Online!, Chemical Abstracts Service, Columbus, Ohio, US, retrieved from STN; XP002197385 & “AsInEx Compound Collection”, May 10, 2001, Asinex, 123182 Moscow, Russia.
Database Chemcats ′Online!, Chemical Abstracts Service, Columbus, Ohio, US, retrieved from STN; XP002197386, order No. TRG08000#09403-D; TRG08000#13126-D; TRG08000#13131-D; TRG08000#13124-D; TRG08000#01963-D; TRG08000#00603-D; TRG08000#13135-D; TRG08000#13121-D; TRG08000#13122-D & “Chem.Folio”, Lion BioScience AG, 69027 Heidelberg, Germany.
Ankhiwala, M. D.; “Synthesis and Biological Studies of Some 2-Amino-3-Cyano-4-Aryl-6-(2′-Hydroxy-4′-N-Butoxy-5′-H/Nitrophenyl)pyridines”, J. Indian Chem. Soc., 69(3): 166-167 (1992).
Kumar, N., Singh, G., and Yadav, A. K., “Synthesis of some 2-thioxopyrido [2,3-d]pyrimidine ribofuranosides and their antimicrobial activity”, Phosphorus, Sulfur and Silicon, 175: 217-225 (2001).
Manna, F., Chimenti, F., Bolasco, A. Filippelli, A., Palla, A., Filippelli, W., Lampa, E. and Mercantini, R., “Anti-inflammatory, Analgesic and Antipyretic 4,6-Disubstituted 3-Cyanopyridine-2-ones and 3-Cyano-2-Aminopyridines”, Eur. J. Med. Chem., 27: 627-632 (1992).
Manna, F., Chimenti, F., Bolasco, A., Bizzarri, B., Filippelli, W., Filippelli, A., and Gagliardi, L., “Anti-inflammatory, Analgesic and Antipyretic 4,6-Disubstituted 3-Cyano-2-Aminopyridines”, Eur. J. Med. Chem., 34: 245-254 (1999).
Lewis, A. J. and Manning, A. M., “New Targets for Anti-Inflammatory Drugs”, Current Opinion in Chemical Biology, 3: 489-494 (1999).

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