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Most Cited Patent Families 2000-Chemistry and Related

Following is a CAS database record representing a highly cited patent family.

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CAPLUS COPYRIGHT 2007 ACS

TITLE:	Imidazole derivatives and their use as cytokine inhibitors
INVENTOR(S):	Adams, Jerry Leroy; Gallagher, Timothy Francis; Lee, John C.; White, John Richard
PATENT ASSIGNEE(S):	SmithKline Beecham Corp., USA
SOURCE:	PCT Int. Appl., 70 pp. CODEN: PIXXD2
LANGUAGE:	English

PATENT INFORMATION:

PATENT NO.       KIND  DATE           APPLICATION NO.  DATE
---------------  ----  --------       ---------------  --------
WO 9314081        A1   19930722       WO 1993-US674    19930113
	 RW: AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE,
	     BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, SN, TD, TG
ES 2053401        A1   19940716       ES 1993-33       19930112
ES 2053401        B1   19950301
AU 9335923        A1   19930803       AU 1993-35923    19930113
AU 671271         B2   19960822
ZA 9300213        A    19931118       ZA 1993-213      19930113
CN 1083473        A    19940309       CN 1993-101706   19930113
EP 623126         A1   19941109       EP 1993-904624   19930113
    R:  AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LI, LU, MC, NL, PT, SE
JP 07503017       T2   19950330       JP 1993-512741   19930113
HU 69714          A2   19950928       HU 1994-2092     19930113
BR 9305809        A    19970218       BR 1993-5809     19930113
EP 943616         A1   19990922       EP 1999-201468   19930113
    R:  AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT, IE
NO 9402618        A    19940830       NO 1994-2618     19940712
FI 9403319        A    19940912       FI 1994-3319     19940712
US 5686455        A    19971111       US 1994-256500   19941130

ABSTRACT:
The title compds. I [R1 = 4-pyridyl, pyrimidinyl, quinolyl, isoquinolinyl, (un)substituted 1-imidazolyl or 1-benzimidazolyl; R2 = H, heterocyclyl, heterocyclylalkyl, OH, C1-4 alkoxy, avrialoxy, etc.; R3 = (un)substituted aryl or heteroaryl group, P-contg. substituent, etc.; R4 = PH, (un)substituted 1-naphthyl or 2-naphthyl, etc.], useful as medications for treating cytokine-mediated diseases (no data) and which inhibit the formation of cytokines, are prepd. Thus, 2-(4-cyanophenyl)-1-methyl-4-phenyl-5-(4-pyridyl)imidazole was hydrolyzed in aq. HCl soln. and neutralized, producing Na 4-[1-methyl-4-phenyl-5-(4-pyridyl)imidazol-2-yl]benzoate, which demonstrated 50-65% inhibition of IL-8 proinflammatory cytokine in primary human umbilical cord endothelial cells.

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