Synthesis of indole analogs of...

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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C548S469000, C548S490000

Reexamination Certificate

active

11274436

ABSTRACT:
The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole (YC-1), and their anti-platelet activity.

REFERENCES:
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Coutoure, A, Deniau, E, Gimbert, Y, Grandclaudon, P. An expeditious synthesis of 3-alkyl, aryl-, and heteroaryl-indoles by way of an intramolecular Horner-Wittig reaction. J. Chem. Soc. Perkin Trans. I, 1993, 20, 2463-2466.
Abarca, B, Ballesteros, R. Indoles and annulated indoles I. The preparation of some 2-substituted-3-(2′-thienyl)indoles. Anales de Quimica, 1983, 79, 23-26.
Abarca, et al., “Indoles and annulated indoles I. The preparation of some 2-substituted-3-(2′-thienyl)indoles,” 1983, vol. 79, p. 23-26.
Chauder B, Larkin A, Snieckus V. Rapid route to 3,4-substituted indoles via a directed ortho metalation-retro-Mannich sequence. Org Lett. Mar. 7, 2002;4(5):815-7.
Chun YS, Yeo EJ, Park JW. Versatile pharmacological actions of YC-1: anti-platelet to anticancer. Cancer Lett. Apr. 15, 2004;207(1):1-7.
Ko FN, Wu CC, Kuo SC, Lee FY, Teng CM. YC-1, a novel activator of platelet guanylate cyclase. Blood. Dec. 15, 1994;84(12):4226-33.
Lee FY, Lien JC, Huang LJ, Huang TM, Tsai SC, Teng CM, Wu CC, Cheng FC, Kuo SC. Synthesis of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole analogues as novel antiplatelet agents. J Med Chem. Oct. 25, 2001;44(22):3746-9.
Wu CC, Ko FN, Kuo SC, Lee FY, Teng CM. YC-1 inhibited human platelet aggregation through NO-independent activation of solube guanylate cyclase. Br J Pharmacol. Oct. 1995;116(3):1973-8.

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