Sri International

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Stanford Research Institute

Richard H Peters

Masato Tanabe

Wan-Ru Chao

Ling Jong

Eric Wuhl

Kazuhiko Shigeno

Jyanwei Liu

Peter D Hobbs

David F Crowe

John G Johansson

Kenneth J Ryan

Keith R Laderoute

George Detre

Khalid Amin

Joy M Calaoagan

Syntheses of steroids such as 3-hydroxy-7&#x3b1;-methyl-21-[2'-methoxy-4&#x2032;-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate ('SR 16234') and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.

Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one

Syntheses of steroids such as 3-hydroxy-7&agr;-methyl-21-&lsqb;2&prime;-methoxy-4&prime;-(diethylaminomethyl)-phenoxy&rsqb;-19-norpregna-1,3,5(10)triene citrate (&ldquo;SR 16234&rdquo;) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.

Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use

Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5(10)-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5(10)-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Anti-estrogenic steroids, and associated pharmaceutical compositions and

Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.

Estrone sulfamate inhibitors of estrone sulfatase, and associated

Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) ##STR1## wherein X and Y, or Y and Z, form an oxathiazine dioxide ring or a dihydro-oxathiazine dioxide ring, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.

Steroid inhibitors of estrone sulfatase and associated pharmaceutical

Steriod inhibitors of estrone sulfatase and associated pharmaceutical

The invention is drawn to 17-oxo-15,16-seco-19-nor steroids which are useful as intermediates in the production of various 15,16-seco-19-nor progestins. These progestins display elevated progestational activity with a minimum of ancillary hormonal activity and are thus useful in the suppression of ovulation in the human female.

15,16-seco-19-nor progestins

15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.

This invention relates to a stereoisomerically pure .DELTA..sup.2 compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen or --(C.dbd.O)--R.sup.2, wherein:

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San Jose, CA, United States of America

Richard H Peters