3,4-diarylpyrazoles and their use in the therapy of cancer

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C548S373100, C548S377100

Reexamination Certificate

active

10499030

ABSTRACT:
The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3is independently: a C5-20aryl group, and is optionally substituted; Ar4is independently: a C5-20aryl group, and is optionally substituted; R5is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R<SP>N</SP> is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, such compounds for medical use, such compounds use in the treatment of conditions mediated by HSP90, including, for example, cancer, and use of such compounds in the preparation of medicaments for such treatments.

REFERENCES:
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Ohsumi et al.: “Syntheses and antitumor activity of cisrestricted combretastatins: 5-membered heterocyclic analogs”; Bioorganic & Medicinal Chemistry Letters; vol. 8, No. 22; pp. 3153-3158; XP002235812.
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DATABASE WPI; Section Ch, Week 200312; Derwent Publications Ltd.; AN 2003-129155; XP002235817.
DATABASE CA ′Online!; Chemical Abstracts Service; Khilya et al.: “Synthetic and modified isoflavonoids. XV. Reaction of synthetic isoflavone analogs with hydrazine hydrate derivatives”; retrieved from STN; Database accession No. 124:8437 CA; XP002235816; & Khimiy a Prirodnykh Soedinenii (1994), (5), 629-33, 1994.

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