Eli Lilly and Company

C David Jones

Tulio Suarez

Arvind L Thakkar

Philip J Burck

Ronald E Zimmerman

John S Ward

Kenneth S Hirsch

Eriks V Krumkalns

Donald G Saunders

Certain 5-phenyl-5H-indeno[1,2-d]pyrimidines, their pharmaceutical formulations, and their use in methods for inhibiting aromatase and treating or preventing estrogen-dependent diseases.

Indenopyrimidine aromatase inhibitors

2-Fluoro-17.beta.-estradiol is synthesized by mercurating a 17.beta.-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.

Method of preparing 2-fluoro-17.beta.-estradiol

Long chain alkyl and alkenyl sulfonates, sulfates and sulfoalkyl alkanoate salts, administered intravaginally for contraception.

Contraceptive methods

Derivatives of 3-phenyl-4-aroyl-1,2-dihydronaphthalenes and 1-aroyl-2-phenylnaphthalenes are useful as antifertility agents.

3-Phenyl-4-benzoyl-1,2-dihydronaphthalenes

Antifertility compounds

Introduction of a pharmaceutically acceptable non-toxic cation salt of a straight-chain or branched chain alkyl sulfonate having from 11 to 16 carbon atoms into the uterine lumen or vaginal cavity prevents conception. Sodium tetradecyl sulfonate is preferred.

Contraceptive methods and compositions

Introduction of a pharmaceutically acceptable non-toxic cation salt of a sulfoalkyl alkanoate, for example, sodium sulfopropyl dodecanoate, into the uterine lumen or vaginal cavity prevents conception.

Introduction of a compound of the formula:

Derivatives of 3-phenyl-4-aroyl-1,2-dihydronaphthalenes and 1-aroyl-2-phenylnaphthalenes are useful both as antifertility agents and in suppressing the growth of mammary tumors.

Derivatives of 2-phenyl-3-aroylbenzothiophenes and 2-phenyl-3-aroylbenzothiophene-1-oxides are useful as antifertility agents. Certain of these compounds also are useful in suppressing the growth of mammary tumors.

2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents

Derivatives of 2-aroyl-3-phenylbenzothiophenes and 2-aroyl-3-phenylbenzothiophene-1-oxides are useful as antifertility agents.

Derivatives of 2-aroyl-3-phenylindenes, 3-aroyl-4-phenyl-1,2-dihydronaphthalenes, and 1-phenyl-2-aroyl-naphthalenes are useful as antifertility agents.

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Indianapolis, IN, United States of America

C David Jones