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CS209916B2 - Method of making the esters of 4-halogen-9-fluor-3-oxoandrost-4en and 4-halogen-9-fluor-3-oxoandrosta-1,4-dien-17 beta-thiocarboxyl acid - Google Patents

Method of making the esters of 4-halogen-9-fluor-3-oxoandrost-4en and 4-halogen-9-fluor-3-oxoandrosta-1,4-dien-17 beta-thiocarboxyl acid Download PDF

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Publication number
CS209916B2
CS209916B2 CS792306A CS230679A CS209916B2 CS 209916 B2 CS209916 B2 CS 209916B2 CS 792306 A CS792306 A CS 792306A CS 230679 A CS230679 A CS 230679A CS 209916 B2 CS209916 B2 CS 209916B2
Authority
CS
Czechoslovakia
Prior art keywords
methyl
diene
formula
compound
hydroxy
Prior art date
Application number
CS792306A
Other languages
Czech (cs)
English (en)
Inventor
Francisco S Alvarez
Original Assignee
Syntex Inc
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 Syntex Inc filed Critical Syntex Inc
Publication of CS209916B2 publication Critical patent/CS209916B2/cs

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal 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
    • C07J5/0046Normal 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
    • C07J5/0061Normal 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 substituted in position 16
    • C07J5/0069Normal 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 substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076Normal 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 substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • C07J71/0026Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031Oxygen-containing hetero ring cyclic ketals at positions 16, 17

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pain & Pain Management (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CS792306A 1978-04-05 1979-04-04 Method of making the esters of 4-halogen-9-fluor-3-oxoandrost-4en and 4-halogen-9-fluor-3-oxoandrosta-1,4-dien-17 beta-thiocarboxyl acid CS209916B2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US05/893,390 US4198403A (en) 1978-04-05 1978-04-05 17 Beta-thiocarboxylic acid esters of 4-halo-3-oxoandrost-4-enes

Publications (1)

Publication Number Publication Date
CS209916B2 true CS209916B2 (en) 1981-12-31

Family

ID=25401489

Family Applications (2)

Application Number Title Priority Date Filing Date
CS792306A CS209916B2 (en) 1978-04-05 1979-04-04 Method of making the esters of 4-halogen-9-fluor-3-oxoandrost-4en and 4-halogen-9-fluor-3-oxoandrosta-1,4-dien-17 beta-thiocarboxyl acid
CS797273A CS209919B2 (en) 1978-04-05 1979-04-04 Method of making the esters of the 4-halogen-9-fluor-3-oxo-androst-4-en and 4-halogen-9-fluor-3-oxoandrosta -1,4-dien-17beta-thiocarboxyl acid

Family Applications After (1)

Application Number Title Priority Date Filing Date
CS797273A CS209919B2 (en) 1978-04-05 1979-04-04 Method of making the esters of the 4-halogen-9-fluor-3-oxo-androst-4-en and 4-halogen-9-fluor-3-oxoandrosta -1,4-dien-17beta-thiocarboxyl acid

Country Status (17)

Country Link
US (1) US4198403A (no)
EP (1) EP0004773B1 (no)
JP (1) JPS54135761A (no)
AT (1) ATA251879A (no)
AU (1) AU4575279A (no)
CS (2) CS209916B2 (no)
DE (1) DE2960292D1 (no)
DK (1) DK136479A (no)
ES (1) ES479272A1 (no)
FI (1) FI791088A (no)
GR (1) GR67274B (no)
IL (1) IL56991A (no)
IT (1) IT7967709A0 (no)
NO (1) NO791141L (no)
PL (2) PL121569B1 (no)
PT (1) PT69412A (no)
ZA (1) ZA791638B (no)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4310466A (en) * 1979-08-31 1982-01-12 Syntex (U.S.A.) Inc. Thio etianic acid derivatives
SE8004580L (sv) * 1980-06-19 1981-12-20 Draco Ab Farmaceutisk beredning
US4340538A (en) * 1980-07-21 1982-07-20 The Upjohn Company Process for producing 6α-fluoro-Δ1,4 -3-keto steroids
SE8306370D0 (sv) * 1983-11-18 1983-11-18 Draco Ab Novel androstane-17beta-carboxylic acid esters, a process and intermediates for their preparation, compositions and method for the treatment of inflammatory conditions
US4599331A (en) * 1984-12-24 1986-07-08 Syntex (U.S.A.) Inc. Etianic acids as antiangiogenics
US5646136A (en) * 1994-01-04 1997-07-08 Duke University Methods of inhibiting angiogenesis and tumor growth, and treating ophthalmologic conditions with angiostatic and therapeutic steroids
EP0754701B1 (en) * 1994-04-04 1998-08-12 Meiji Milk Products Company Limited Novel progesterone compound and use thereof
US5981517A (en) * 1996-05-09 1999-11-09 Soft Drugs, Inc. Androstene derivatives
US20020133032A1 (en) * 2000-02-25 2002-09-19 Jufang Barkalow Method for the preparation of fluticasone and related 17beta-carbothioic esters using a novel carbothioic acid synthesis and novel purification methods
US20030085387A1 (en) * 2000-05-31 2003-05-08 Takahiro Fujiyama Optical materials and optical part each containing aromatic sulfide compound and aromatic sulfide compound
US6750210B2 (en) * 2000-08-05 2004-06-15 Smithkline Beecham Corporation Formulation containing novel anti-inflammatory androstane derivative
GB0019172D0 (en) * 2000-08-05 2000-09-27 Glaxo Group Ltd Novel compounds
US6777400B2 (en) * 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6777399B2 (en) * 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6858593B2 (en) * 2000-08-05 2005-02-22 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6759398B2 (en) 2000-08-05 2004-07-06 Smithkline Beecham Corporation Anti-inflammatory androstane derivative
SK287576B6 (sk) * 2000-08-05 2011-03-04 Glaxo Group Limited S-fluórmetylester kyseliny 6alfa, 9alfa-difluór-17alfa-[(2- furanylkarboxyl)oxy]-11beta-hydroxy-16alfa-metyl-3-oxo-androsta- 1,4-dién-17beta-karbotiovej, spôsob jeho prípravy, farmaceutický prostriedok s jeho obsahom, jeho použitie a medziprodukty
US6787532B2 (en) * 2000-08-05 2004-09-07 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivatives
US6858596B2 (en) * 2000-08-05 2005-02-22 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivative
UA77656C2 (en) * 2001-04-07 2007-01-15 Glaxo Group Ltd S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent
IL158222A0 (en) * 2001-04-30 2004-05-12 Glaxo Group Ltd Anti-inflammatory 17. beta-carbothioate ester derivatives of androstane with a cyclic ester group in position 17. alpha
US20050175545A1 (en) * 2002-02-04 2005-08-11 Keith Biggadike Formulation for inhalation comprising a glucocorticoid and a beta 2-adrenoreceptor agonist
GB0202635D0 (en) * 2002-02-05 2002-03-20 Glaxo Wellcome Mfg Pte Ltd Formulation containing novel anti-inflammatory androstane derivative
GB2389530B (en) 2002-06-14 2007-01-10 Cipla Ltd Pharmaceutical compositions
CA2530680A1 (en) * 2003-04-04 2004-10-14 Alpharma Aps Process for the preparation of steroidal carbothioic acid derivatives and intermediates
GB0507165D0 (en) * 2005-04-08 2005-05-18 Glaxo Group Ltd Novel crystalline pharmaceutical product
GB0615108D0 (en) * 2006-07-28 2006-09-06 Glaxo Group Ltd Novel formulations
AU2010260177A1 (en) 2009-06-16 2011-12-15 Merck Sharp & Dohme Corp. Novel [3,2-c] heteroaryl steroids as glucocorticoid receptor agonists, compositions and uses thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3989686A (en) * 1972-06-15 1976-11-02 Glaxo Laboratories Limited Anaesthetic steroids of the androstane series and process for preparing same
US4093721A (en) * 1974-08-30 1978-06-06 Glaxo Laboratories Limited Pharmaceutical compositions of 6α,9α-difluoro-androst-4-ene-17β-carboxylates and derivatives thereof
CH628355A5 (de) * 1976-02-24 1982-02-26 Ciba Geigy Ag Verfahren zur herstellung neuer androstadien-17beta-carbonsaeuren und ihrer ester und salze.

Also Published As

Publication number Publication date
DK136479A (da) 1979-10-06
ATA251879A (de) 1982-04-15
EP0004773B1 (en) 1981-04-29
JPS54135761A (en) 1979-10-22
ES479272A1 (es) 1980-01-16
IT7967709A0 (it) 1979-04-04
ZA791638B (en) 1980-11-26
US4198403A (en) 1980-04-15
PL214675A1 (no) 1980-07-28
PL222926A1 (no) 1981-01-02
DE2960292D1 (en) 1981-08-06
NO791141L (no) 1979-10-08
IL56991A (en) 1982-01-31
GR67274B (no) 1981-06-26
AU4575279A (en) 1979-10-11
IL56991A0 (en) 1979-07-25
EP0004773A2 (en) 1979-10-17
PT69412A (en) 1979-04-01
FI791088A (fi) 1979-10-06
PL118567B1 (en) 1981-10-31
EP0004773A3 (en) 1979-10-31
CS209919B2 (en) 1981-12-31
PL121569B1 (en) 1982-05-31

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