IE841484L - 13-alpha-alkyl-gonanes - Google Patents

13-alpha-alkyl-gonanes

Info

Publication number
IE841484L
IE841484L IE841484A IE148484A IE841484L IE 841484 L IE841484 L IE 841484L IE 841484 A IE841484 A IE 841484A IE 148484 A IE148484 A IE 148484A IE 841484 L IE841484 L IE 841484L
Authority
IE
Ireland
Prior art keywords
carbon atoms
alkyl
hydrogen
alpha
beta
Prior art date
Application number
IE841484A
Other versions
IE57620B1 (en
Original Assignee
Schering 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
Priority claimed from DE3321826A external-priority patent/DE3321826A1/en
Priority claimed from DE19843413036 external-priority patent/DE3413036A1/en
Application filed by Schering Ag filed Critical Schering Ag
Publication of IE841484L publication Critical patent/IE841484L/en
Publication of IE57620B1 publication Critical patent/IE57620B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

1. Claims for the Contracting States BE, CH, LI, DE, FR, GB, IT, LU, NL, SE 13 alpha-Alkyl gonanes of general formula I see diagramm : EP0129499,P14,F3 wherein R**1 means -N R**II -R**I wherein R**I and R**II are hydrogen or alkyl of 1-4 carbon atoms, or R**I and R**II with inclusion of N mean a saturated 5- or 6-membered ring, wherein the ring can contain, besides N, still another hetero atom, such as O, N, S, as well as the corresponding tertiary N-oxides and the acid addition salts, OR**III wherein R**III means methyl, ethyl, propyl, methoxyphenyl, allyl, or beta-dimethylaminoethyl, R**2 means a hydrogen atom, a methyl group or an ethyl group, R**3 means -(CH2 )n -CH3 with n=0-4, -(CH2 )n -CH2 -O(S)R**IV with n=0-4, and R**IV meaning hydrogen or alkyl of 1-4 carbon atoms, -CH=CH-(CH2 )n -OR**V with n=1-4, and R**V meaning hydrogen, alkyl, or alkanoyl of respectively 1-4 carbon atoms, -C -= C-X wherein X means hydrogen, alkyl of 1-4 carbon atoms, or halogen, -(CH2 )n -CH2 CN with n=0-3 or see diagramm : EP0129499,P14,F4 wherein Y means hydrogen or OR**V , R**4 is hydroxy, alkoxy, or alkanoyloxy of respectively 1-4 carbon atoms or R**3 /R**4 means see diagramm : EP0129499,P14,F2 wherein R**3 is in the alpha-position and R**4 is in the beta-position, or R**3 is in the beta-position and R**4 is in the alpha-position with respect to the steroid skeleton, and R**5 is a hydrogen atom or an alpha- or beta-positioned alkyl group of 1-4 carbon atoms. 1. Claim for the Contracting State AT Process for the preparation of 13 alpha-alkylgonanes of the general formula I see diagramm : EP0129499,P15,F4 wherein R**1 represents -N R**II -R**I , wherein R**I and R**II represent hydrogen or alkyl having from 1 to 4 carbon atoms, or R**I and R**II , with the inclusion of N, represent a saturated 5- or 6-membered ring, wherein the ring can contain, in addition to N, a further hetero atom, such as O, N or S, as well as the corresponding tertiary N-oxides and the acid addition salts, or represents -OR**III , wherein R**III represents methyl, ethyl, propyl, methoxyphenyl, allyl or beta-dimethylaminoethyl, R**2 represents a hydrogen atom, a methyl group or an ethyl group, R**3 represents -(CH2 )n -CH3 , where n=0-4, -(CH2 )n -CH2 -O(S)R**IV , where n=0-4 and R**IV represents hydrogen or alkyl having from 1 to 4 carbon atoms, -CH=CH-(CH2 )n -OR**V , where n=1-4 and R**V represents hydrogen, alkyl or alkanoyl each having from 1 to 4 carbon atoms, -C -= C-X, where X represents hydrogen, alkyl having from 1 to 4 carbon atoms, or halogen, -(CH2 )n -CH2 CN, where n=0-3, or see diagramm : EP0129499,P15,F7 where Y represents hydrogen or OR**V , where R**V has the meanings given above, R**4 represents hydroxy, alkoxy or alkanoyloxy each having from 1 to 4 carbon atoms, or R**3 /R**4 represents see diagramm : EP0129499,P16,F1 wherein R**3 is in the alpha-position and R**4 is in the beta-position, or R**3 is in the beta-position and R**4 is in the alpha-position with respect to the steroid skeleton, and R**5 represents a hydrogen atom or an alkyl group in the alpha- or beta-position having from 1 to 4 carbon atoms, characterised in that a compound of the general formula II see diagramm : EP0129499,P16,F3 wherein R**1 , R**2 and R**5 have the meanings given in formula I and Z is an ethylene or 2,2-dimethylpropylene group, is irradiated with ultraviolet light, and the 13-episteroid, obtained by UV irradiation, of the general formula III see diagramm : EP0129499,P16,F2 wherein R**1 , R**2 , R**5 and Z have the meanings given in formula II, is converted into the compounds of the general formula I in accordance with methods known per se by nucleophilic addition to the 17-ketone, cleavage of the 3-ketal protective group, and splitting off of water from the 4,5-position. [EP0129499A2]
IE1484/84A 1983-06-15 1984-06-14 13alpha-alkylgonanes,their preparation and pharmaceutical preparations containing them IE57620B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3321826A DE3321826A1 (en) 1983-06-15 1983-06-15 13 alpha -Alkylgonanes, the preparation thereof and pharmaceutical products containing these
DE19843413036 DE3413036A1 (en) 1984-04-04 1984-04-04 13a-Alkylgonanes, the preparation thereof and pharmaceutical products containing these

Publications (2)

Publication Number Publication Date
IE841484L true IE841484L (en) 1984-12-15
IE57620B1 IE57620B1 (en) 1993-02-10

Family

ID=25811539

Family Applications (1)

Application Number Title Priority Date Filing Date
IE1484/84A IE57620B1 (en) 1983-06-15 1984-06-14 13alpha-alkylgonanes,their preparation and pharmaceutical preparations containing them

Country Status (16)

Country Link
EP (1) EP0129499B1 (en)
JP (1) JPH02167296A (en)
AU (1) AU572849B2 (en)
CA (1) CA1307784C (en)
DD (1) DD218624A5 (en)
DE (1) DE3468030D1 (en)
DK (1) DK166729B1 (en)
ES (1) ES533260A0 (en)
FI (1) FI78709C (en)
GR (1) GR82210B (en)
HU (1) HU191131B (en)
IE (1) IE57620B1 (en)
IL (1) IL72085A (en)
NO (1) NO160521C (en)
NZ (1) NZ208441A (en)
PT (1) PT78732B (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3446661A1 (en) * 1984-12-18 1986-06-19 Schering AG, 1000 Berlin und 4709 Bergkamen NEW 13 (ALPHA) -ALKYL-17 (BETA) - (3-ACYLOXYPROPYL) GONANA
DE3506785A1 (en) * 1985-02-22 1986-08-28 Schering AG, Berlin und Bergkamen, 1000 Berlin 11SS-N, N-DIMETHYLAMINOPHENYL ESTRADIENE, THE PRODUCTION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM
DE3630030A1 (en) * 1986-09-01 1988-03-03 Schering Ag 13 (ALPHA) -ALKYLGONAN- (DELTA) (UP ARROW) 9 (UP ARROW) (UP ARROW) ((UP ARROW) (UP ARROW) 1 (UP ARROW) 1 (UP ARROW)) (UP ARROW) -5, 10-EPOXIDE
US4774236A (en) * 1986-09-17 1988-09-27 Research Triangle Institute 17α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and pharmaceutical compositions containing them
IE60780B1 (en) * 1987-01-23 1994-08-10 Akzo Nv New 11-aryl steroid derivatives
EP0310542B1 (en) * 1987-10-01 1994-06-08 Schering Aktiengesellschaft Antigestagenic and antioestrogenic compounds for the treatment of hormone-dependent tumours
BE1004905A4 (en) * 1987-12-30 1993-02-23 Roussel Uclaf NOVEL 17BETA-OH 19-NOR DERIVATIVES SUBSTITUTED IN 17ALPHA, THEIR PREPARATION PROCESS, THEIR APPLICATION AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
US4954490A (en) * 1988-06-23 1990-09-04 Research Triangle Institute 11 β-substituted progesterone analogs
DE3822770A1 (en) * 1988-07-01 1990-01-04 Schering Ag 13-ALKYL-11SS-PHENYLGONANE
DE3832303A1 (en) * 1988-09-20 1990-04-12 Schering Ag 11SS-PHENYL-14SSH STEROIDS
US5372996A (en) * 1989-03-10 1994-12-13 Endorecherche, Inc. Method of treatment of androgen-related diseases
US5364847A (en) * 1989-03-10 1994-11-15 Endorecherche Inhibitors of sex steroid biosynthesis and methods for their production and use
AU5856090A (en) * 1989-07-07 1991-02-06 Endorecherche Inc. Androgen derivatives for use in the inhibition of sex steroid activity
ATE230994T1 (en) * 1989-07-07 2003-02-15 Endorech Inc METHOD OF TREATING ANDROGEN-RELATED DISEASES
ATE172469T1 (en) * 1989-08-04 1998-11-15 Schering Ag 11 BETA-ARYL-GONA-4,9-DIENE-3-ONE
FR2654337B1 (en) * 1989-11-15 1994-08-05 Roussel Uclaf NOVEL BIODEGRADABLE INJECTABLE MICROSPHERES PREPARATION METHOD AND INJECTABLE SUSPENSIONS CONTAINING THEM.
DE4008584A1 (en) * 1990-03-15 1991-09-26 Schering Ag METHOD FOR PRODUCING INTERMEDIATE PRODUCTS FOR THE ANTIGESTAGE SYNTHESIS (ONAPRISTONE SYNTHESIS)
US5407928A (en) * 1990-08-15 1995-04-18 Schering Aktiengesellschaft 11β-aryl-gona-4,9-dien-3-ones
US5472854A (en) * 1990-08-18 1995-12-05 Schering Aktiengesellschaft Process for the production of 17-oxosteroids via the fermentative oxidation of 17β-hydroxysteroids by Mycobacterium
ATE152773T1 (en) * 1990-08-18 1997-05-15 Schering Ag METHOD FOR PRODUCING 17-OXOSTEROIDS
MX9301121A (en) * 1992-03-02 1993-09-01 Schering Ag METHOD AND EQUIPMENT FOR ORAL CONTRACEPTION AND REGULATION OF MENSTRUATION WITH ESTROGEN / PROGESTIN / ANIPROGESTIN.
US7704983B1 (en) 1992-03-02 2010-04-27 Eastern Virginia Medical School Antiprogestin method for reducing side effects associated with low dosage HRT and oral contraception
US5439913A (en) 1992-05-12 1995-08-08 Schering Aktiengesellschaft Contraception method using competitive progesterone antagonists and novel compounds useful therein
UA35589C2 (en) * 1992-05-21 2001-04-16 Андорешерш Інк. INHIBITORS OF TESTOSTERONE 5-<font face="Symbol">a</font>-REDUCTASE activity, pharmaceutical composition and a method for inhibiting activity of testosterone 5-<font face="Symbol">a</font>-REDUCTASE
DE4413185A1 (en) * 1994-04-12 1995-10-19 Schering Ag 11beta, 19-bridged 13alpha alkyl steroids
DE4415590A1 (en) * 1994-04-28 1995-11-02 Schering Ag Process for the stereoselective introduction of an alkynyl side chain to 11β-aryl-substituted 13alpha-alkylgonan-17-ones
DE4434488A1 (en) * 1994-09-14 1996-03-21 Schering Ag Steroid esters and amides, processes for their preparation and their pharmaceutical use
ZA9510926B (en) 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
RU2129125C1 (en) * 1995-04-06 1999-04-20 Украинский научно-исследовательский институт фармакотерапии эндокринных заболеваний METHOD OF SYNTHESIS OF 13α-TRIENE-19-NORANDROSTANE-3-OL-17-ONE AND ITS METHYL ESTER
US6900193B1 (en) 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
AU710139B2 (en) 1996-05-01 1999-09-16 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The 21-substituted progesterone derivatives as new antiprogestational agents
US6262042B1 (en) * 1998-05-29 2001-07-17 Research Triangle Institute 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
RU2017112748A (en) 2014-11-17 2018-12-19 Арно Терапьютикс, Инк. ONAPRISTON COMPOSITIONS OF LONG-TERM ACTIONS AND METHODS
CA2998924A1 (en) * 2015-09-25 2017-03-30 Context Biopharma Inc. Methods of making onapristone intermediates
CA3008422A1 (en) * 2015-12-15 2017-06-22 Context Biopharma Inc. Amorphous onapristone compositions and methods of making the same
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2377418A1 (en) * 1977-01-13 1978-08-11 Roussel Uclaf NEW 4,9-DIENIC 11B-SUBSTITUTE STEROID DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICINAL PRODUCTS
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
DE3347126A1 (en) * 1983-12-22 1985-07-11 Schering AG, 1000 Berlin und 4709 Bergkamen 11SS-ARYL-ESTRADIENE, THEIR PRODUCTION AND THE PHARMACEUTICAL PREPARATIONS CONTAINING THEM
CA1304916C (en) * 1984-10-18 1992-07-14 Wilhelm Bannwarth Apparatus for the parallel performance of a plurality of chemical reaction sequences

Also Published As

Publication number Publication date
NO842394L (en) 1984-12-17
NO160521C (en) 1989-04-26
IL72085A (en) 1987-09-16
AU2936184A (en) 1984-12-20
DK288184A (en) 1984-12-16
AU572849B2 (en) 1988-05-19
NZ208441A (en) 1988-01-08
FI78709C (en) 1989-09-11
GR82210B (en) 1984-12-13
NO160521B (en) 1989-01-16
ES8502612A1 (en) 1985-02-01
FI842395A0 (en) 1984-06-13
IL72085A0 (en) 1984-10-31
DD218624A5 (en) 1985-02-13
EP0129499A2 (en) 1984-12-27
PT78732A (en) 1985-01-01
CA1307784C (en) 1992-09-22
EP0129499A3 (en) 1985-10-09
IE57620B1 (en) 1993-02-10
JPH0369919B2 (en) 1991-11-05
FI842395A7 (en) 1984-12-16
HUT36139A (en) 1985-08-28
ES533260A0 (en) 1985-02-01
DK288184D0 (en) 1984-06-12
DK166729B1 (en) 1993-07-05
PT78732B (en) 1986-06-03
EP0129499B1 (en) 1987-12-09
HU191131B (en) 1987-01-28
JPH02167296A (en) 1990-06-27
DE3468030D1 (en) 1988-01-21
FI78709B (en) 1989-05-31

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Legal Events

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MM4A Patent lapsed