Research Triangle Institute

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Research Triangle Research North Carolina

John A Kepler

C Edgar Cook

Gary S Bartley

Rupa S Shetty

Yue-Wei Lee

Mansukh C Wani

Scott P Runyon

Hernan A Navarro

Michael A Rogawski

David Yue-wei Lee

Matthew Orr

Rafal Kaminski

Edgar Cook

Jill M O'Reilly

C Ray Tallent

David Y-w Lee

Ping-sheng Zhang

Hernan Navarro

Edgar (deceased) Cook

Edgar C Cook

Ray C Tallent

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage. 

Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties

Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.

The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

17&#x3b2;-amino and hydroxylamino-11 &#x3b2;-arylsteroids and their derivatives having agonist or antagonist hormonal properties

An androgenic steroid compound of the formula:wherein:

Androgenic steroid compounds and a method of making and using the same

The invention is directed to a novel class of 17&bgr;-acyl-17&agr;-propynyl steroids which exhibit potent antiprogestational activity.

17&bgr;-acyl-17&agr;-propynyl-11&bgr;-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties

17&bgr;-amino and hydroxylamino-11&bgr;-arylsteroids and their derivatives having agonist or antagonist hormonal properties

The invention is directed to a novel class of 17&bgr;-acyl-17&bgr;-propynyl steroids which exhibit potent antiprogestational activity.

17&bgr;-acyl-17&agr;-propynyl-11&bgr;-arylsteroids and their derivatives having agonist or antagonist hormonal properties

17.beta.-nitro-11.beta.-arylsteroids and their derivatives having

The invention is directed to 11.beta.-aryl-17,17-spirothiolane substituted steroid compounds of formula (I) exhibiting binding to the progestin receptor. ##STR1## Also disclosed are methods of using and process of making the compounds.

11.beta.-aryl-17, 17-spirothiolane-substituted steroids

The invention is directed to 20-keto-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.9, R.sup.12 and X are as defined by the specification. The compounds exhibit progestational and antiprogestational activities.

20-keto-11.beta.-arylsteroids and their derivatives having agonist or

The invention is directed to 11.beta.-arylsteroids of formula II: ##STR1## wherein R.sup.1, R.sup.6, R.sup.8, R.sup.12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment of fibroids, endometriosis, cervical ripening prior to delivery, hormone replacement therapy and in the control of fertility.

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Raleigh, NC, United States of America

John A Kepler