FI83225B - Foerfarande foer framstaellning av terapeutiskt verkande 9 ,11 -epoxisteroider. - Google Patents

Foerfarande foer framstaellning av terapeutiskt verkande 9 ,11 -epoxisteroider. Download PDF

Info

Publication number
FI83225B
FI83225B FI852430A FI852430A FI83225B FI 83225 B FI83225 B FI 83225B FI 852430 A FI852430 A FI 852430A FI 852430 A FI852430 A FI 852430A FI 83225 B FI83225 B FI 83225B
Authority
FI
Finland
Prior art keywords
acid
solution
water
methylene
formula
Prior art date
Application number
FI852430A
Other languages
English (en)
Finnish (fi)
Other versions
FI83225C (sv
FI852430A0 (fi
FI852430L (fi
Inventor
Michel Biollaz
Original Assignee
Ciba Geigy Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ciba Geigy Ag filed Critical Ciba Geigy Ag
Publication of FI852430A0 publication Critical patent/FI852430A0/fi
Publication of FI852430L publication Critical patent/FI852430L/fi
Publication of FI83225B publication Critical patent/FI83225B/fi
Application granted granted Critical
Publication of FI83225C publication Critical patent/FI83225C/sv

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C07J53/008—3 membered carbocyclic rings in position 15/16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C07J71/0015—Oxiranes at position 9(11)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (4)

1. Förfarande för framställning av terapeutiskt verkande : 9a,lla-epoxisteroider med formeln I V.; ? /xf‘ <y —......ta (1) y: m > 1 * ...· / \l/ \ / V/* ... · ♦ · Δ III ;;; /Vv'vr 30 8 3 2 2 5 i vilken R är l&galkanoyl och -A-A- är en etylen- eller cyk-lopropylengrupp, kännetecknat därav, att a) till en motsvarande, 6,7-omättad 9α,lla-epoxiförening med formeln II <·-εΛϊ ?>? !··° i i / \|/ \ / i I A i vilken -A-A- betecknar detsanuna som ovan, fogas tili 6,7-dubbelbindningen en lägalkantiosyra med formeln R-SH (III), i vilken R betecknar detsamma som ovan, eller b) i den motsvarande 9(ll)-omättade föreningen med formeln IV . f> cAaii / M_J......k av) . M S ! I / Ψ Y V ✓ vv -s-R i vilken R och -A-A- betecknar detsamma som ovan, epoxide-ras 9(ll)-dubbelbindningen.
2. Förfarande enligt patentkravet 1, kännetecknat därav, att man framställer en förening med formeln I, i vilken R är acetyl.
3. Förfarande enligt patentkravet 1, kännetecknat därav, att man framställer 7a-acetyltio-9a,lla-epoxi-20-spirox-4-en-3,21-dion. 31 83225
4. Förfarande enligt patentkravet 1, känneteck-n a t därav, att man framställer 7a-acetyltio-9a,lla-epoxi-15β,160-metylen-2O-spirox-4-en-3,21-dion.
FI852430A 1984-06-21 1985-06-19 Förfarande för framställning av terapeutiskt verkande 9 ,11 -epoxist eroider FI83225C (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CH300984 1984-06-21
CH300984 1984-06-21
CH464684 1984-09-28
CH464684 1984-09-28

Publications (4)

Publication Number Publication Date
FI852430A0 FI852430A0 (fi) 1985-06-19
FI852430L FI852430L (fi) 1985-12-22
FI83225B true FI83225B (fi) 1991-02-28
FI83225C FI83225C (sv) 1991-06-10

Family

ID=25691934

Family Applications (1)

Application Number Title Priority Date Filing Date
FI852430A FI83225C (sv) 1984-06-21 1985-06-19 Förfarande för framställning av terapeutiskt verkande 9 ,11 -epoxist eroider

Country Status (16)

Country Link
US (1) US4670551A (sv)
EP (1) EP0165902B1 (sv)
AR (2) AR242036A1 (sv)
AU (1) AU582754B2 (sv)
CA (1) CA1239388A (sv)
DE (1) DE3569540D1 (sv)
DK (1) DK173854B1 (sv)
ES (2) ES8704967A1 (sv)
FI (1) FI83225C (sv)
GR (1) GR851499B (sv)
HU (1) HU192232B (sv)
IE (1) IE58050B1 (sv)
IL (1) IL75569A (sv)
NO (1) NO165496C (sv)
NZ (1) NZ212492A (sv)
PT (1) PT80663B (sv)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69637140T2 (de) * 1995-12-11 2008-04-10 G.D. Searle Llc, Chicago Verfahren zur herstellung einer epoxy-verbindung
US6887991B1 (en) 1996-12-11 2005-05-03 G. D. Searle & Company Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein
EP1223174A3 (en) * 1996-12-11 2005-03-16 G.D. Searle & Co. Processes for preparation of 3-keto-7alpha-alkoxycarbonyl-delta-4,5- steroids and intermediates useful therein
BR9714510A (pt) 1996-12-11 2000-11-28 Searle & Co Processo e preparo de esteróides de 9,11-époxi e intermediários úteis dos mesmos
ATE473759T1 (de) 1998-05-22 2010-07-15 Univ Leland Stanford Junior Bifunktionelle moleküle sowie darauf basierende therapien.
MXPA04005674A (es) 2001-12-12 2004-10-15 Pharmacia Corp Metodo para tratar trastornos oftalmicos con antagonistas epoxi-esteroidales del receptor de aldosterona.
US7235655B2 (en) 2002-03-22 2007-06-26 Pharmacia & Upjohn Company Processes to prepare eplerenone
EP2392258B1 (en) 2005-04-28 2014-10-08 Proteus Digital Health, Inc. Pharma-informatics system
WO2007025780A2 (en) * 2005-09-02 2007-03-08 Recordati Ireland Limited Aldosterone receptor antagonists
US9062126B2 (en) 2005-09-16 2015-06-23 Raptor Pharmaceuticals Inc. Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
AU2010216512B2 (en) 2009-02-20 2016-06-30 2-Bbb Medicines B.V. Glutathione-based drug delivery system
WO2010129819A2 (en) 2009-05-06 2010-11-11 Laboratory Skin Care, Inc. Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3013012A (en) * 1960-12-22 1961-12-12 Searle & Co Alkanoylthio-17alpha-carboxyethyl-17beta-hydroxyandrosten-3-one lactones
US3095412A (en) * 1961-12-19 1963-06-25 Searle & Co 9alpha, 11alpha-epoxy and 11beta-chloro-9alpha-hydroxy 17alpha-(2-carboxyethyl)-17beta-hydroxyandrost-4-en-3-one gamma-lactones and delta1 and delta6 analogs
GB1041534A (en) * 1963-04-24 1966-09-07 Merck & Co Inc 20-spiroxane compounds
DE2652761C2 (de) * 1976-11-16 1985-11-21 Schering AG, 1000 Berlin und 4709 Bergkamen 15,16-Methylen-Spirolactone, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
US4559332A (en) * 1983-04-13 1985-12-17 Ciba Geigy Corporation 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
EP0134529B1 (de) * 1983-08-17 1990-03-21 Schering Aktiengesellschaft 7-alpha-Substituierte 3-Oxo-17alpha-pregn-4-en-21.17-carbolactone, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Präparate

Also Published As

Publication number Publication date
AR245731A1 (es) 1994-02-28
EP0165902A2 (de) 1985-12-27
GR851499B (sv) 1985-11-25
DE3569540D1 (en) 1989-05-24
DK280085D0 (da) 1985-06-20
IL75569A (en) 1989-03-31
US4670551A (en) 1987-06-02
HU192232B (en) 1987-05-28
NO852501L (no) 1985-12-23
ES557112A0 (es) 1987-08-16
NZ212492A (en) 1989-02-24
DK173854B1 (da) 2001-12-27
NO165496B (no) 1990-11-12
PT80663A (en) 1985-07-01
FI83225C (sv) 1991-06-10
ES8704967A1 (es) 1987-04-16
IE851535L (en) 1985-12-21
ES8707737A1 (es) 1987-08-16
AR242036A1 (es) 1993-02-26
EP0165902B1 (de) 1989-04-19
ES544387A0 (es) 1987-04-16
IE58050B1 (en) 1993-06-16
CA1239388A (en) 1988-07-19
PT80663B (en) 1987-05-08
DK280085A (da) 1985-12-22
AU582754B2 (en) 1989-04-13
FI852430A0 (fi) 1985-06-19
HUT38367A (en) 1986-05-28
IL75569A0 (en) 1985-10-31
EP0165902A3 (en) 1986-10-22
FI852430L (fi) 1985-12-22
AU4397185A (en) 1986-01-02
NO165496C (no) 1991-02-20

Similar Documents

Publication Publication Date Title
FI77669B (fi) 20-spiroxaner och analoger, som innehaoller en oeppen ring e, foerfarande foer deras framstaellning samt dessa innehaollande farmaceutiska preparat.
CELLA et al. Steroidal aldosterone blockers. II1
FI83225B (fi) Foerfarande foer framstaellning av terapeutiskt verkande 9 ,11 -epoxisteroider.
US8492570B2 (en) 2-substituted estra-1,3,5(10)-triene-3-yl sulfamate with an anti-tumor action
US20100120736A1 (en) Mineralocorticoid Receptor Antagonists
JPH02243698A (ja) 性ステロイド活性を抑制するために用いるエストロゲン核誘導体の薬学組成物
US4502989A (en) Aldosterone-antagonistic steroids
US4789668A (en) 1α,7α-dithio-substituted spirolactones, processes for their preparation, and their use as medicines
HU188923B (en) Process for preparing 19-mercapto-androstane derivatives
FI58779C (fi) Foerfarande foer framstaellning av terapeutiskt anvaendbara aldosteron-antagonistiska steroidfoereningar av spiroxanserien med en syrehaltig grupp i 19-staellningen
KR20000005546A (ko) 알파-17치환제가없는신규의프레그난유도체,이들의의약용도,제조방법,및이의중간체및관련화합물1
EP0207375B1 (en) Steroido [3,2-c] pyrazoles useful as antiandrogenic agents and preparation thereof
Nickisch et al. Aldosterone antagonists. 2. New 7. alpha.-(acetylthio)-15, 16-methylene spirolactones
EP0538312A1 (de) Antiandrogene [3,2-d]Triazolsteroide
US4331663A (en) 4α,5α-Epoxy-3,20-dioxopregnane-2α,16α-dicarbonitrile and intermediates and process for preparation, method of use and compositions thereof
IL41454A (en) 3-keto-7(alpha,bela)-loweralkyl-delta5-androstanes and process for preparing same
JPS59205400A (ja) ２０−スピロキサン系ステロイド及びその製造方法並びに該ステロイドを含有する医薬
JPS6126557B2 (sv)
FI114799B (sv) Ny 7-substituerad oxasteroidförening
US4868166A (en) 2,2:6,6-diethylen-3-oxo-17alpha-pregn-4-ene-21,17alpha-carbolactones, process for their production &amp; pharmaceutical preparations containing them
HU179980B (en) Process for preparing substituted steroid-spiro-oxazolidinone derivatives
JPH0212480B2 (sv)
US4002614A (en) Halogenated 19-norsteroids
USRE39862E1 (en) Unsaturated 14, 15-cyclopropanoandrostanes, a method for their production and pharmaceutical compositions containing these compounds
DE4337416A1 (de) 10,11beta-C¶2¶-überbrückte Steroide

Legal Events

Date Code Title Description
PC Transfer of assignment of patent

Owner name: NOVARTIS AG

MM Patent lapsed

Owner name: NOVARTIS AG