Compounds and methods for treating tumors, cancer and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

Reexamination Certificate

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C560S156000, C514S625000, C564S199000

Reexamination Certificate

active

10705483

ABSTRACT:
The present invention relates to novel compounds, pharmaceutical compositions and methods for treating tumors, cancer and hyperproliferative diseases including psoriasis, genital warts and hyperproliferative cell growth diseases, including hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus. These compounds are described according to the chemical structure:where R1is H, OH, F, Cl, Br, I, a C1-C6optionally substituted alkyl or alkenyl group, an optionally substituted aryl group or a group;Rais a H, OH, C1-C10, optionally substituted alkyl or alkenyl group, an optionally substituted O—(C1-C7alkyl group) or O-aryl group, an amine group which is optionally substituted with at least one C1-C10alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group;R2is a group;Rbis a H, OH, C1-C10, optionally substituted alkyl or alkenyl group, an optionally substituted O—(C1-C7alkyl group) or O-aryl group, an amine group which is optionally substituted with at least one C1-C10alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group;R3and R6are each independently selected from H, OH, F, Cl, Br, I, a C1-C6optionally substituted alkyl or alkenyl group, an optionally substituted aryl group, a carbamate, alkylene carbamate, urethane or alkylene urethane;R4is a group, wherein Rbis as described above; andR5is a group, wherein Rbis as described above,with the proviso that at least one of R1and R2or R4and R5contains an Raor Rbgroup which is an amine group which is optionally substituted with at least one C1-C10alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group;or a stereoisomer, pharmaceutically acceptable salt, solvate, and polymorph thereof.

REFERENCES:
Kathawala, FG ‘Pharmaceutical secondary amides o f2-alkynic acids’ CA 93:94825 (1980).
Miller, LA ‘Derivatives of propiolanilide’ CA 65:38326.

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