Roussel Uclaf

Other

Hoechst Marion Roussel

Aventis Pharma S.a.

Roussel-ulcaf

Daniel Philibert

Lucien Nedelec

Jean-Georges Teutsch

Roger Deraedt

Francois Nique

Jean G Teutsch

Germain Costerousse

Vesperto Torelli

Andre Claussner

Martine Moguilewsky

Armelle Bonfils

Patrick Van De Velde

Jacques Leclaire

Alain Jouquey

Martine Gaillard-Kelly

Francois Goubet

Yamina Bouali

Marie-Madeleine Bouton

Jean-Noel Veltz

Francis Petit

Nick Goeders

Jean-Francois Gourvest

Dominique Lesuisse

Andre Pierdet

Michel Klich

Jean Paul Vevert

Genevieve Azadian

Fran&ccedil;ois Nique

Francois Nioue

Andr&egrave; Claussner

Roland Bardoneschi

19-Nor-steroids

The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid activity sufficient to treat narcotic withdrawal symptoms.

Use of antimineralocorticoid compounds against narcotic withdrawal syndrome

20-substituted steroids

Use of antimineralocorticoid compounds against drug withdrawal syndrome

A method of treating menopause or perimenopause without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification sufficient to treat menopause or perimenopause symptoms without estrogenic activity at the uterine level.

Method of treating menopause or perimenopause

A method of treating cholesterol without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification without estrogenic activity at the uterine level.

A method of controlling male fertility in warm-blooded animals comprising vaginally administering to female warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl or taken together with the nitrogen form a saturated 5 to 6 ring heterocycle optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.-methyl, n is an integer from 2 to 10; R.sub.4 and R.sub.5 together are =0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from hydrogen, --OH, acyloxy of an organic acid of up to 12 carbon atoms and alkyl, alkenyl and, alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are =0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to bind to the sigma receptor sites and inhibit the influx of calcium into the spermatozoid.

Method of controlling male fertility

A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##

19-nor-steroids

A method of treating male sterility linked to insufficient fertilizing power of the spermatozoa in warm-blooded animals comprising administering to warm-blooded animals an amount of a compound of formula I or its acid addition salts sufficient to increase the fertilizing power of spermatozoa.

Method of treating male sterility

The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts.

Method of controlling fertility in males with 20-substitute of steroids

A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are taken together with the nitrogen to form a saturated 5 to 6 ring heterocycle, optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.-methyl, n is an integer from 2 to 10, R.sub.4 and R.sub.5 together are .dbd.0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from the group consisting of hydrogen, --OH, acyloxy of an organic carboxylic acid of up to 12 carbon atoms and alkyl, alkenyl and alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are .dbd.0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically, acceptable acid addition salts in an amount sufficient to control male fertility.

A method of controlling male fertility in warm-blooded animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl, R.sub.3 is .alpha.- or .beta.- methyl, n is an integer from 2 to 10, either R.sub.4 and R.sub.5 together are .dbd.O and R.sub.6 and R.sub.7 are hydrogen, or R.sub.6 and R.sub.7 together are .dbd.O and R.sub.4 and R.sub.3 are hydrogen or R.sub.4 and R.sub.7 are .dbd.O and R.sub.6 and R.sub.5 are .dbd.O and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

A compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --NO.sub.2 and halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is selected from the group consisting of ##STR2## X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted with a member of the group consisting of halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted with at least one member of the group consisting of oxygen, nitrogen and sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A--B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.

Phenylimidazolidines having antiandrogenic activity

A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl, R.sub.3 is a .alpha.- or .beta.-methyl, n is an integer from 2 to 10, R.sub.4 is hydrogen, R.sub.5 is hydrogen, R.sub.6 and R.sub.7 are hydrogen, and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl or taken together with the nitrogen form a saturated 5 to 6 ring heterocycle optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.- methyl, n is an integer from 2 to 10, R.sub.4 and R.sub.5 together are .dbd.0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from the group consisting of hydrogen, --OH, acyloxy of an organic carboxylic acid of up to 12 carbon atoms and alkyl, alkenyl and alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are .dbd.0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

Growing community of inventors

La Varenne Saint Hilaire, France

Daniel Philibert