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2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations

a technology of 2-phenyl-1-benzyl and estrogen, which is applied in the direction of drug compositions, biocide, heterocyclic compound active ingredients, etc., can solve the problems of increasing the risk of endometriosis and/or endometrial cancer

Inactive Publication Date: 2007-06-14
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides pharmaceutical formulations and methods of using compounds of formulas (I) and (II) in combination with estrogens to alleviate symptoms of post-menopausal syndrome in women. The compounds are estrogen agonists / antagonists that can show little uterine stimulation and can minimize the amount of estrogen needed. The use of these compounds in combination with estrogens can also help reduce the side effects of estrogen treatment. The patent also includes methods of using the compounds alone or in combination with other pharmaceutical carriers or excipients.

Problems solved by technology

This proliferation is associated with increased risk for endometriosis and / or endometrial cancer.
However, it is also a partial agonist in the uterus and this is cause for some concern.

Method used

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  • 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
  • 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
  • 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations

Examples

Experimental program
Comparison scheme
Effect test

example no.1 2

Example No. 1 2-Phenyl-3-methyl-1H-indole

[0068] Mp=90-94° C.; 1H NMR (DMSO) 11.13 (s, 1H), 7.68-7.64 (m, 2H), 7.54-7.46 (m, 3H), 7.37-7.32 (m, 2H), 7.12-7.06 (m, 1H), 7.03-6.97 (m, 1H), 2.40 (s, 3H); MS eI m / z 207 (M+).

Example No. 1a 5-Flouro-2-(4-benzyloxy-phenyl)-3-methyl-1H-indole Mp=143-146° C.

example no.2 2

Example No. 2 2-(4-Benzyloxy-phenyl)-3-methyl-1H-indole

[0069] Mp=118-120° C.; 1H NMR (DMSO) 11.03 (s, 1H), 7.57 (dd, 2H, J=2.0 Hz, 6.6 Hz), 7.48-7.46 (m, 3H), 7.44-7.28 (m, 4H), 7.18-7.11 (m, 2H), 7.08-7.03 (m, 1H), 7.0-6.95 (m, 1H), 5.16 (s, 2H), 2.36 (s, 3H); MS eI m / z 313 (M+).

example no.3 5

Example No. 3 5-Benzyloxy-2-phenyl-3-methyl-1H-indole

[0070] Mp=141-144° C.; 1H NMR(DMSO) 10.98 (s, 1H), 7.65-7.61 (m, 2H), 7.51-7.44 (m, 4H), 7.42-7.28 (m, 4H), 7.23 (d, 1H, J=8.8 Hz), 7.10 (d, 1H, J=2.5 Hz), 6.80 (d, 1H, J=6.0 Hz), 5.10 (s, 2H), 2.36 (s, 3H); MS eI m / z 313 (M+).

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Abstract

The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:

Description

[0001] This application claims the benefit of U.S. Provisional Application No. 60 / 109,809, which was converted from U.S. patent application Ser. No. 09 / 079,561, filed May 15, 1998, pursuant to a petition filed under 37 C.F.R. 1.53(c)(2)(i).[0002] The present invention relates to the use of new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, in conjunction with estrogens, as well as pharmaceutical compositions and methods of treatment utilizing these compounds. BACKGROUND OF THE INVENTION [0003] The use of hormone replacement therapy for bone loss prevention in post-menopausal women is well precedented. The normal protocol calls for estrogen supplementation using such formulations containing estrone, estriol, ethynyl estradiol, 17β-estradiol, esterified estrogens, or conjugated estrogens isolated from natural sources (i.e. Premarin® conjugated estrogens from Wyeth-Ayerst) or synthetic estrogens. In some patients, therapy may be contraindi...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/56A61K31/55A61K31/155A61K31/405A61K31/565
CPCA61K31/155A61K31/405A61K31/55A61K31/56A61K31/565A61K31/566A61K2300/00A61P5/30
Inventor PICKAR, JAMES HARRISONKOMM, BARRY SAMUEL
Owner WYETH LLC