Granted Patent B2

US 8,933,130 · App. 12/308,640 · Granted Jan 13, 2015

Abstract

Claims (17)

1. A method of treating vasomotor symptoms in a patient in need thereof comprising administering to said patient an effective amount of a selective estrogen receptor modulator represented by the following formula:

wherein

R a ′ and R b ′ independently are a hydrogen atom, a C 1 -C 8 alkyl group which may have a substituent, or when R a ′ and R b ′ are bonded together, they may form, together with the nitrogen atom that is adjacent to R a ′ and R b ′, a 4- to 8 membered ring which may have a an additional heteroatom, and

R c is a hydrogen atom or a C 1 -C 6 alkyl group; or a salt thereof, or a hydrate thereof.

2. The method of claim 1 wherein each of R a and R b represents a hydrogen atom, a methyl group, an ethyl group, a n-propyl group, an iso-propyl group, a n-butyl group, tent-butyl group, or a cyclohexyl group.

3. The method of claim 1 wherein the selective estrogen receptor modulator is a compound selected from the group consisting of:

(a) (R)-6-{2-{Ethyl[4-(2-ethylaminoethyl)benzyl]amino }4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol;

(b) (R)-6-{2-{Ethyl[4-(2-methylaminoethyl)benzyl]amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol;

(c) (R)-6-{2-{Ethyl[4-(2-propylaminoethyl)benzyl]amino }-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol;

(d) (R)-6-{2-{[4-(2-Butylaminoethyl)benzyl]ethylamino}-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol;

(e) (R)-6-{2-Ethyl [4-(2-isopropylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol;

(f) (R)-6-{2-{[4-(2-tert-Butylaminoethyl)benzyl]ethylamino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol; and

(g) (R)-6- {2-{[4-(2-Cyclohexylaminoethyl)benzyl]ethylamino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol or a salt of any of the foregoing.

4. A method of treating vasomotor symptoms in a patient in need thereof comprising administering to said patient an effective amount of (R)-6-{2-{Ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol or a salt thereof.

5. A method of treating hot flashes in a female patient in need thereof comprising administering to said patient an effective amount of (R)-6-{2-{Ethyl[4-(2-ethylaminoethyl)benzyl]amino }-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol or a salt thereof.

6. The method of claim 4 , wherein the vasomotor symptom is hot flashes or night sweats.

7. The method of claim 4 or claim 6 , where the patient is a female.

Assignments (11)