Physiologically active substance Tan-931, its derivatives, their

Details Physiologically active substance Tan-931, its derivatives, their Physiologically active substance Tan-931, its derivatives, their

1990-04-13

1991-05-07

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

544 3, 544 8, 544174, 544176, 544391, 546226, 548127, 548128, 548214, 548578, 560 56, 562440, 562441, 562460, 564167, 564169, A61K 3119, C07C 6503, C07C 6519, C07C 6530

Patent

active

050137573

ABSTRACT:
A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.

REFERENCES:
patent: 2853521 (1958-09-01), Hardy et al.
patent: 3049503 (1962-08-01), Milionis et al.
patent: 4235787 (1980-11-01), Schulz et al.
patent: 4323700 (1982-04-01), Kondo et al.
patent: 4935543 (1990-06-01), Kanamaru et al.
Kanamaru et al., "Physiologically active substance Tan-931, etc.", CA 113, 5954a (1990).
Ballantine, J. et al., "The Brosynthesis of Phenol. Part XXI, The Molecular Structure, etc.", J. Chem. Soc., pp. 1175-1182 (1970).
Chemical Abstracts, vol. 87, No. 11, Sep. 12, 1977, p. 564, abstract No. 84687m; Columbus, Ohio; U.S.; & JP-A-77 31 059 (Mitsubishi Gas Chemical Co., Inc.) 09-03-1977.

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