Tetrahydrobenzfluorene derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen in the nitrogen containing substituent

Reexamination Certificate

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C544S154000, C544S358000, C546S184000, C546S248000, C548S400000, C548S528000

Reexamination Certificate

active

10499956

ABSTRACT:
A compound having the formula Iwhereinthe O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position;n is 2-4Reand ′Reare OH, optionally independently etherified or esterified;R1and R2are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1and R2together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor β selective medical treatments.

REFERENCES:
patent: 5147880 (1992-09-01), Jones
patent: 0 524 742 (1993-01-01), None
patent: WO 01/72713 (2001-10-01), None
Tedesco, R. et al, “Synthesis and Evaluation of hexahydrochrysene and Tetrahydrobenzofluorence Ligands for the Estrogen Receptor” Bioorganic & Medicinal Chemistry Letters (2001), 11(10), 1281-1284, May 21, 2001 XP001053388 cited in the application p. 1282.

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