Steroid spiro-oxazolidine derivs. - with anti:aldosterone activity free from antiandrogenic side effects
Steroid spirooxazolidines of formula (I) and their stereoisomers are new: In (I) (R1 is 1-4C alkyl, R2 is H, 1-4C alkyl, 1-4C (sic) alkenyl or di(1-3C) alkylphosphinoxymethyl. Z is one of the gps. In A, when R1 is R4, c is a double bond; when R1 is R5 then b only; b and d; a and b; or a, b and d are...
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| creator | SOLYOM SANDOR SZONDY ELEONORA TOLDY LAJOS SCHAFER INGE SZILAGYI KATALIN BORVENDEG JANOS |
| description | Steroid spirooxazolidines of formula (I) and their stereoisomers are new: In (I) (R1 is 1-4C alkyl, R2 is H, 1-4C alkyl, 1-4C (sic) alkenyl or di(1-3C) alkylphosphinoxymethyl. Z is one of the gps. In A, when R1 is R4, c is a double bond; when R1 is R5 then b only; b and d; a and b; or a, b and d are double bonds, all others are single bonds, e and f can be double or single bonds. R3=H or CH3. R4=F, OH, 1-3C acyloxy, 1-4C alkoxycarbonyloxy, oxo, oximino or 1-3C alkoxy-imino. R5=oxo, oximino or 1-3C alkoxy-imino R6=1-3C alkyl). Where Z is (XII); f=single bond) and R1 and R6 are CH3, then R2 is not H or 1-4C alkyl. (I) have powerful anti-aldosterone (diuretic) activity but at therapeutic doses are free from anti-androgenic side effects. Some also have hormonal activity. In an example androsta-5-ene-3 beta-ol-17S-spiro-5'-(2'-oxo-3'-methyloxazolidine) was made from N-ethoxycarbonyl-17 alpha-CH3NHCH2-androsta-5-ene-3 beta, 17 beta-diol. |
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Z is one of the gps. In A, when R1 is R4, c is a double bond; when R1 is R5 then b only; b and d; a and b; or a, b and d are double bonds, all others are single bonds, e and f can be double or single bonds. R3=H or CH3. R4=F, OH, 1-3C acyloxy, 1-4C alkoxycarbonyloxy, oxo, oximino or 1-3C alkoxy-imino. R5=oxo, oximino or 1-3C alkoxy-imino R6=1-3C alkyl). Where Z is (XII); f=single bond) and R1 and R6 are CH3, then R2 is not H or 1-4C alkyl. (I) have powerful anti-aldosterone (diuretic) activity but at therapeutic doses are free from anti-androgenic side effects. Some also have hormonal activity. In an example androsta-5-ene-3 beta-ol-17S-spiro-5'-(2'-oxo-3'-methyloxazolidine) was made from N-ethoxycarbonyl-17 alpha-CH3NHCH2-androsta-5-ene-3 beta, 17 beta-diol.</description><edition>4</edition><language>eng ; ita</language><subject>HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><creationdate>1988</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19880708&DB=EPODOC&CC=IT&NR=1193465B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19880708&DB=EPODOC&CC=IT&NR=1193465B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>SOLYOM SANDOR</creatorcontrib><creatorcontrib>SZONDY ELEONORA</creatorcontrib><creatorcontrib>TOLDY LAJOS</creatorcontrib><creatorcontrib>SCHAFER INGE</creatorcontrib><creatorcontrib>SZILAGYI KATALIN</creatorcontrib><creatorcontrib>BORVENDEG JANOS</creatorcontrib><title>Steroid spiro-oxazolidine derivs. - with anti:aldosterone activity free from antiandrogenic side effects</title><description>Steroid spirooxazolidines of formula (I) and their stereoisomers are new: In (I) (R1 is 1-4C alkyl, R2 is H, 1-4C alkyl, 1-4C (sic) alkenyl or di(1-3C) alkylphosphinoxymethyl. Z is one of the gps. In A, when R1 is R4, c is a double bond; when R1 is R5 then b only; b and d; a and b; or a, b and d are double bonds, all others are single bonds, e and f can be double or single bonds. R3=H or CH3. R4=F, OH, 1-3C acyloxy, 1-4C alkoxycarbonyloxy, oxo, oximino or 1-3C alkoxy-imino. R5=oxo, oximino or 1-3C alkoxy-imino R6=1-3C alkyl). Where Z is (XII); f=single bond) and R1 and R6 are CH3, then R2 is not H or 1-4C alkyl. (I) have powerful anti-aldosterone (diuretic) activity but at therapeutic doses are free from anti-androgenic side effects. Some also have hormonal activity. In an example androsta-5-ene-3 beta-ol-17S-spiro-5'-(2'-oxo-3'-methyloxazolidine) was made from N-ethoxycarbonyl-17 alpha-CH3NHCH2-androsta-5-ene-3 beta, 17 beta-diol.</description><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1988</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFi7sKwkAQRdNYiPoNzg9ECFFBS0XR2vRh2J01A3En7Azx8fVGsbe5pzjnjrPmYpSEPWjHSXJ54Eta9hwJPCXudQE53NkawGi8xdaLfh6DR2fcsz0hJKJh5PZtMPokV4rsQNkTUAjkTKfZKGCrNPtxks2Ph2p_yqmTmrRDR5GsPldFsSmX69Wu_F-8AUVBQBE</recordid><startdate>19880708</startdate><enddate>19880708</enddate><creator>SOLYOM SANDOR</creator><creator>SZONDY ELEONORA</creator><creator>TOLDY LAJOS</creator><creator>SCHAFER INGE</creator><creator>SZILAGYI KATALIN</creator><creator>BORVENDEG JANOS</creator><scope>EVB</scope></search><sort><creationdate>19880708</creationdate><title>Steroid spiro-oxazolidine derivs. - with anti:aldosterone activity free from antiandrogenic side effects</title><author>SOLYOM SANDOR ; SZONDY ELEONORA ; TOLDY LAJOS ; SCHAFER INGE ; SZILAGYI KATALIN ; BORVENDEG JANOS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_IT1193465B3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; ita</language><creationdate>1988</creationdate><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><toplevel>online_resources</toplevel><creatorcontrib>SOLYOM SANDOR</creatorcontrib><creatorcontrib>SZONDY ELEONORA</creatorcontrib><creatorcontrib>TOLDY LAJOS</creatorcontrib><creatorcontrib>SCHAFER INGE</creatorcontrib><creatorcontrib>SZILAGYI KATALIN</creatorcontrib><creatorcontrib>BORVENDEG JANOS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>SOLYOM SANDOR</au><au>SZONDY ELEONORA</au><au>TOLDY LAJOS</au><au>SCHAFER INGE</au><au>SZILAGYI KATALIN</au><au>BORVENDEG JANOS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Steroid spiro-oxazolidine derivs. - with anti:aldosterone activity free from antiandrogenic side effects</title><date>1988-07-08</date><risdate>1988</risdate><abstract>Steroid spirooxazolidines of formula (I) and their stereoisomers are new: In (I) (R1 is 1-4C alkyl, R2 is H, 1-4C alkyl, 1-4C (sic) alkenyl or di(1-3C) alkylphosphinoxymethyl. Z is one of the gps. In A, when R1 is R4, c is a double bond; when R1 is R5 then b only; b and d; a and b; or a, b and d are double bonds, all others are single bonds, e and f can be double or single bonds. R3=H or CH3. R4=F, OH, 1-3C acyloxy, 1-4C alkoxycarbonyloxy, oxo, oximino or 1-3C alkoxy-imino. R5=oxo, oximino or 1-3C alkoxy-imino R6=1-3C alkyl). Where Z is (XII); f=single bond) and R1 and R6 are CH3, then R2 is not H or 1-4C alkyl. (I) have powerful anti-aldosterone (diuretic) activity but at therapeutic doses are free from anti-androgenic side effects. Some also have hormonal activity. In an example androsta-5-ene-3 beta-ol-17S-spiro-5'-(2'-oxo-3'-methyloxazolidine) was made from N-ethoxycarbonyl-17 alpha-CH3NHCH2-androsta-5-ene-3 beta, 17 beta-diol.</abstract><edition>4</edition><oa>free_for_read</oa></addata></record> |
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| title | Steroid spiro-oxazolidine derivs. - with anti:aldosterone activity free from antiandrogenic side effects |
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