Methods for treating or preventing breast cancer or leukemia in subjects in need of such treatment are provided which involve the administration of 6-[3-[1-adamantyl]-4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN), a retinoid which induces G.sub.0 /G.sub.1 arrest and apoptosis. These methods are useful for treatment of breast cancers which express or do not express estrogen receptors.

Centre International de Recherches Dermatologiques Galderma

Method for treating or preventing breast cancer or leukemia using 6-[3-[1-adamantyl]-4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN)

The present invention provides a method of producing an optically active form of a compound represented by the formula (I) having a steroid C.sub.17,20 -lyase inhibitory activity and is useful as an agent for the prophylaxis or treatment of prostatism, tumor such as breast cancer, and the like or a salt thereof, which method includes reacting a mixture of optically active compounds of a naphthalene derivative represented by the formula: ##STR1##wherein R is a nitrogen-containing heterocyclic group, R.sup.1 is a hydrogen atom, a hydrocarbon group or an aromatic heteromonocyclic group, R.sup.2 is a hydrogen atom or a lower alkyl group, * shows the position of an asymmetric carbon, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are each independently a hydrogen atom, a hydrocarbon group, a hydroxy group, a thiol group, an amino group, a carbamoyl group, an acyl group or a halogen atom, and R.sup.7 is bonded with R.sup.6 or R.sup.8 to form, together with a carbon atom on a naphthalene ring, a 5 or 6-membered ring containing an oxygen atom, with an optically active form of a compound represented by the formula: ##STR2##wherein ring A is a benzene ring, R.sup.10 and R.sup.11 are the same or different and each is a hydrogen atom, a hydrocarbon group or a halogen atom, or R.sup.10 and R.sup.11 in combination show an alkylene group, * shows the position of an asymmetric carbon, and ring B and ring C are each an aromatic ring, separating the resulting salt, and isolating the optically active form, and a novel reagent for optical resolution.

Takeda Chemical Industries, Ltd.

Process for producing optically active naphthalene derivative and optical resolver therefor

A class of substituted benzylnaphthylene compounds of the structure ##STR1##where R.sup.1 and R.sup.2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is --(CH.sub.2).sub.1-6 ; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N'-(lower alkyl)ureido; or N, N'-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.5]undecan-3-yl; pyrrolidinon-1-yl; unsubstituted phenyl; or phenyl substituted with acyl of two to four carbon atoms, alkyl of one to four carbon atoms, halo, or alkoxy of one to four carbon atoms; with the proviso that n is not 2 or 3 when Z is 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, N,N-dimethylamino or N,N-diethylamino; are selective estrogen receptor modulators useful in the prophylaxis or treatment of breast cancer.

naphthalene/tumore della mammella

Method for treating or preventing breast cancer or leukemia using 6-[3-[1-adamantyl]-4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN)

Process for producing optically active naphthalene derivative and optical resolver therefor

1-(4-(Substituted alkoxy)benzyl)naphthalene compounds having estrogen inhibitory activity

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