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WO2003062259A3 - Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents - Google Patents

Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents Download PDF

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Publication number
WO2003062259A3
WO2003062259A3 PCT/GB2003/000234 GB0300234W WO03062259A3 WO 2003062259 A3 WO2003062259 A3 WO 2003062259A3 GB 0300234 W GB0300234 W GB 0300234W WO 03062259 A3 WO03062259 A3 WO 03062259A3
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WO
WIPO (PCT)
Prior art keywords
esters
aromatic
androstane
beta
alpha
Prior art date
Application number
PCT/GB2003/000234
Other languages
French (fr)
Other versions
WO2003062259A2 (en
Inventor
Keith Biggadike
Gillian Elizabeth Morton
Original Assignee
Glaxo Group Ltd
Keith Biggadike
Gillian Elizabeth Morton
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 GB0201357A external-priority patent/GB0201357D0/en
Priority claimed from GB0224608A external-priority patent/GB0224608D0/en
Application filed by Glaxo Group Ltd, Keith Biggadike, Gillian Elizabeth Morton filed Critical Glaxo Group Ltd
Priority to AU2003201693A priority Critical patent/AU2003201693A1/en
Publication of WO2003062259A2 publication Critical patent/WO2003062259A2/en
Publication of WO2003062259A3 publication Critical patent/WO2003062259A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J17/00Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

A compound of formula (I); wherein R1 represents represents C1-6 alkyl or C1-6 haloalkyl; R2 represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with one or more methyl or halogen groups; R3 represents methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represent hydrogen or halogen; and formula (II) represents a single or a double bond;and salt and solvates thereof.
PCT/GB2003/000234 2002-01-21 2003-01-20 Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents WO2003062259A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003201693A AU2003201693A1 (en) 2002-01-21 2003-01-20 Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0201357.1 2002-01-21
GB0201357A GB0201357D0 (en) 2002-01-21 2002-01-21 Novel compounds
GB0224608A GB0224608D0 (en) 2002-10-23 2002-10-23 Novel compounds
GB0224608.0 2002-10-23

Publications (2)

Publication Number Publication Date
WO2003062259A2 WO2003062259A2 (en) 2003-07-31
WO2003062259A3 true WO2003062259A3 (en) 2003-08-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2003/000234 WO2003062259A2 (en) 2002-01-21 2003-01-20 Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents

Country Status (2)

Country Link
AU (1) AU2003201693A1 (en)
WO (1) WO2003062259A2 (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7291608B2 (en) 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
US7531528B2 (en) 2000-08-05 2009-05-12 Glaxo Group Limited Formulation containing anti-inflammatory androstane derivatives
US7541350B2 (en) 2000-08-05 2009-06-02 Glaxo Group Limited Formulation containing anti-inflammatory androstane derivative
US7592329B2 (en) 2002-02-04 2009-09-22 Glaxo Group Limited Crystalline complexes of fluticasone-2-furoate

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* Cited by examiner, † Cited by third party
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EP1305330B1 (en) 2000-08-05 2008-12-03 Glaxo Group Limited 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivatives as anti-inflammatory agents
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US8236786B2 (en) 2008-08-07 2012-08-07 Pulmagen Therapeutics (Inflammation) Limited Respiratory disease treatment
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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3828080A (en) * 1972-01-20 1974-08-06 Glaxo Lab Ltd Androstane-17beta-carboxylic acids and processes for the preparation thereof
US3856828A (en) * 1972-07-19 1974-12-24 Glaxo Lab Ltd Anti-inflammatory steroids of the androstane series having a halo-substituted c{11 {14 c{11 {11 alkoxy carbonyl group at the 17{62 {0 position
GB1514476A (en) * 1974-08-30 1978-06-14 Glaxo Lab Ltd Alkyl and haloalkyl androst-4-ene and androsta-1,4-diene-17beta-carboxylates
WO2002000679A2 (en) * 2000-06-28 2002-01-03 Novartis Ag 9.alpha.-chloro-6.alpha.-fluoro-17.alpha.-hydroxy-16-methyl-17-beta-methoxycarbonyl-androst-1,4-dienes esterified in position 17.alpha. by a cyclic acyl group

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3828080A (en) * 1972-01-20 1974-08-06 Glaxo Lab Ltd Androstane-17beta-carboxylic acids and processes for the preparation thereof
US3856828A (en) * 1972-07-19 1974-12-24 Glaxo Lab Ltd Anti-inflammatory steroids of the androstane series having a halo-substituted c{11 {14 c{11 {11 alkoxy carbonyl group at the 17{62 {0 position
GB1514476A (en) * 1974-08-30 1978-06-14 Glaxo Lab Ltd Alkyl and haloalkyl androst-4-ene and androsta-1,4-diene-17beta-carboxylates
WO2002000679A2 (en) * 2000-06-28 2002-01-03 Novartis Ag 9.alpha.-chloro-6.alpha.-fluoro-17.alpha.-hydroxy-16-methyl-17-beta-methoxycarbonyl-androst-1,4-dienes esterified in position 17.alpha. by a cyclic acyl group

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ISOGAI M ET AL: "BINDING AFFINITIES OF MOMETASONE FUROATE AND RELATED COMPOUNDS INCLUDING ITS METABOLITES FOR THE GLUCOCORTICOID RECEPTOR OF RAT SKIN TISSUE", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, ELSEVIER SCIENCE LTD., OXFORD, GB, vol. 44, no. 2, 1993, pages 141 - 145, XP001040943, ISSN: 0960-0760 *
KNOBIL K ET AL: "ADDING SALMETEROL IS MORE EFFECTIVE THAN INCREASING THE DOSE OF FLUTICASONE FOR PATIENTS WITH ASTHMA WHO ARE SYMPTOMATIC ON LOW DOSE FLUTICASONE", EUROPEAN RESPIRATORY REVIEW, COPENHAGEN, DK, vol. 12, no. SUPPL 29, December 1998 (1998-12-01), pages 19S - 20S, XP000992769 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7531528B2 (en) 2000-08-05 2009-05-12 Glaxo Group Limited Formulation containing anti-inflammatory androstane derivatives
US7541350B2 (en) 2000-08-05 2009-06-02 Glaxo Group Limited Formulation containing anti-inflammatory androstane derivative
US7629335B2 (en) 2000-08-05 2009-12-08 Glaxo Group Limited Anti-inflammatory androstane derivative
US7291608B2 (en) 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
US7592329B2 (en) 2002-02-04 2009-09-22 Glaxo Group Limited Crystalline complexes of fluticasone-2-furoate

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AU2003201693A1 (en) 2003-09-02
WO2003062259A2 (en) 2003-07-31

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