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EA199800484A1 - Лактоновые производные 17.бета.-карбокси, карботио и амид андростанов - Google Patents

Лактоновые производные 17.бета.-карбокси, карботио и амид андростанов

Info

Publication number
EA199800484A1
EA199800484A1 EA199800484A EA199800484A EA199800484A1 EA 199800484 A1 EA199800484 A1 EA 199800484A1 EA 199800484 A EA199800484 A EA 199800484A EA 199800484 A EA199800484 A EA 199800484A EA 199800484 A1 EA199800484 A1 EA 199800484A1
Authority
EA
Eurasian Patent Office
Prior art keywords
carbotio
androstanov
amid
carboxy
beta
Prior art date
Application number
EA199800484A
Other languages
English (en)
Other versions
EA001401B1 (ru
Inventor
Кейт Биггедайк
Панайиотис Александроу Прокопиоу
Original Assignee
Глаксо Груп Лимитед
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 GBGB9526651.6A external-priority patent/GB9526651D0/en
Priority claimed from GBGB9613121.4A external-priority patent/GB9613121D0/en
Application filed by Глаксо Груп Лимитед filed Critical Глаксо Груп Лимитед
Publication of EA199800484A1 publication Critical patent/EA199800484A1/ru
Publication of EA001401B1 publication Critical patent/EA001401B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Описаны соединения андростановой серии, имеющие общую формулу (I), и их сольваты, в которых Rпредставляет собой О, S или NH; Rотдельно представляет ОС(=O)Салкил; Rотдельно представляет собой водород, метил (который может быть либо в конфигурации α, либо в конфигурации β) или метилен; Rи Rвместе представляют собой (а), где Rи Rявляются одинаковыми или различными и каждый представляет собой водород или Cалкил; Rи Rявляются одинаковыми или различными и каждый представляет собой водород или галоген; и (б) представляет собой простую или двойную связь. Соединения формулы (I) и их сольваты находят применение в медицине в качестве противовоспалительных и противоаллергических агентов.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800484A 1995-12-29 1996-12-19 ЛАКТОНОВЫЕ ПРОИЗВОДНЫЕ 17β-КАРБОКСИ, КАРБОТИО И АМИД АНДРОСТАНОВ EA001401B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9526651.6A GB9526651D0 (en) 1995-12-29 1995-12-29 Compounds
GBGB9613121.4A GB9613121D0 (en) 1996-06-21 1996-06-21 Compounds
PCT/GB1996/003140 WO1997024365A1 (en) 1995-12-29 1996-12-19 Lactone derivatives of 17.beta.-carboxy, carbothio and amide androstane derivatives

Publications (2)

Publication Number Publication Date
EA199800484A1 true EA199800484A1 (ru) 1999-02-25
EA001401B1 EA001401B1 (ru) 2001-02-26

Family

ID=26308402

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800484A EA001401B1 (ru) 1995-12-29 1996-12-19 ЛАКТОНОВЫЕ ПРОИЗВОДНЫЕ 17β-КАРБОКСИ, КАРБОТИО И АМИД АНДРОСТАНОВ

Country Status (33)

Country Link
US (1) US6197761B1 (ru)
EP (1) EP0876392B1 (ru)
JP (1) JP2947944B2 (ru)
KR (1) KR19990076859A (ru)
CN (1) CN1133643C (ru)
AP (1) AP9801274A0 (ru)
AT (1) ATE194356T1 (ru)
AU (1) AU721865B2 (ru)
BG (1) BG102625A (ru)
BR (1) BR9612309A (ru)
CA (1) CA2241728A1 (ru)
CZ (1) CZ207498A3 (ru)
DE (1) DE69609199T2 (ru)
DK (1) DK0876392T3 (ru)
EA (1) EA001401B1 (ru)
EE (1) EE9800227A (ru)
ES (1) ES2150150T3 (ru)
GR (1) GR3034564T3 (ru)
HU (1) HUP9903707A3 (ru)
IL (1) IL124938A0 (ru)
IS (1) IS4781A (ru)
MX (1) MX9805181A (ru)
NO (1) NO311022B1 (ru)
NZ (1) NZ324373A (ru)
OA (1) OA10701A (ru)
PE (1) PE87598A1 (ru)
PL (1) PL327629A1 (ru)
PT (1) PT876392E (ru)
SI (1) SI0876392T1 (ru)
SK (1) SK89198A3 (ru)
TR (1) TR199801247T2 (ru)
TW (1) TW498072B (ru)
WO (1) WO1997024365A1 (ru)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
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JP2000513380A (ja) * 1997-06-30 2000-10-10 グラクソ、グループ、リミテッド 化合物
GB9909229D0 (en) * 1999-04-23 1999-06-16 Glaxo Group Ltd Enantiomers of mercapto lactones and processes for their synthesis
GB0017988D0 (en) * 2000-07-21 2000-09-13 Glaxo Group Ltd Novel process
US6787532B2 (en) 2000-08-05 2004-09-07 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivatives
US6777399B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6858596B2 (en) * 2000-08-05 2005-02-22 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivative
US6777400B2 (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
US6750210B2 (en) 2000-08-05 2004-06-15 Smithkline Beecham Corporation Formulation containing novel anti-inflammatory androstane derivative
US6759398B2 (en) 2000-08-05 2004-07-06 Smithkline Beecham Corporation Anti-inflammatory androstane derivative
GB0019172D0 (en) * 2000-08-05 2000-09-27 Glaxo Group Ltd Novel compounds
IL154175A0 (en) * 2000-08-05 2003-07-31 Glaxo Group Ltd 17. beta.-carbothioate 17. alpha-arylcarbonyloxyloxy androstane derivatives as anti-inflammatory agents
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
MXPA03009940A (es) * 2001-04-30 2004-01-29 Glaxo Group Ltd DERIVADOS ANTI-INFLAMATORIOS DE 17. BETA-CARBOTIOATO ESTER DE ANDROSTANO CON UN GRUPO DE ESTER CICLICO EN LA POSICIoN 17.ALFA.
US20040248867A1 (en) * 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
WO2003018575A1 (en) * 2001-08-24 2003-03-06 Wyeth Holdings Corporation 5-substituted-3(2h)-furanones useful for inhibition of farnesyl-protein transferase
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
GB0127160D0 (en) * 2001-11-12 2002-01-02 Glaxo Group Ltd Novel compounds
WO2003042229A1 (en) * 2001-11-12 2003-05-22 Glaxo Group Limited Non-aromatic heterocyclic esters of furan-2-one-esters of 17.beta.-carboxyl or 17.beta.-carbothio glucocorticoids
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
WO2004087731A1 (en) * 2003-04-04 2004-10-14 Alpharma Aps Process for the preparation of steroidal carbothioic acid derivatives and intermediates
EP1466920A1 (en) * 2003-04-04 2004-10-13 Alpharma APS Process for the preparation of steroidal 17 beta-carbothioates
CN100558362C (zh) * 2004-04-01 2009-11-11 霍夫曼-拉罗奇有限公司 三氧嘧啶治疗和预防支气管炎症疾病的应用
PT103202B (pt) 2004-10-19 2011-01-27 Hovione Farmaciencia S A Processo para a esterificação de um ácido carbotiótico
GB0507165D0 (en) * 2005-04-08 2005-05-18 Glaxo Group Ltd Novel crystalline pharmaceutical product
TWI374147B (en) * 2006-01-27 2012-10-11 Sun Pharma Advance Res Company Ltd Novel 11β-hydroxyandrosta-4-ene-3-ones
GB0615108D0 (en) * 2006-07-28 2006-09-06 Glaxo Group Ltd Novel formulations
CN103087137A (zh) * 2011-11-07 2013-05-08 天津金耀集团有限公司 一种21位为硫代烃基的糖皮质激素
US20250296918A1 (en) 2022-04-28 2025-09-25 Resonac Corporation Method for producing mercapto heterocyclic compound and method for testing the same
CN120344545A (zh) * 2022-12-16 2025-07-18 津药生物科技（天津）有限公司 新型糖皮质激素、其制备方法及用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4188385A (en) 1978-04-05 1980-02-12 Syntex (U.S.A.) Inc. Thioetianic acid derivatives
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
IL78144A0 (en) 1985-04-04 1986-07-31 Draco Ab Novel androstane-17beta-carboxylic acid esters
US5767113A (en) * 1995-05-10 1998-06-16 The Salk Institute For Biological Studies Compounds useful for concurrently activating glucocorticoid-induced response and reducing multidrug resistance

Also Published As

Publication number Publication date
NO311022B1 (no) 2001-10-01
ES2150150T3 (es) 2000-11-16
DE69609199T2 (de) 2001-03-01
BG102625A (en) 1999-04-30
EP0876392B1 (en) 2000-07-05
PT876392E (pt) 2000-12-29
CA2241728A1 (en) 1997-07-10
CN1209135A (zh) 1999-02-24
BR9612309A (pt) 1999-07-13
GR3034564T3 (en) 2001-01-31
ATE194356T1 (de) 2000-07-15
JPH11501675A (ja) 1999-02-09
SI0876392T1 (en) 2000-12-31
JP2947944B2 (ja) 1999-09-13
US6197761B1 (en) 2001-03-06
NO983004L (no) 1998-08-26
AU721865B2 (en) 2000-07-13
MX9805181A (es) 1998-10-31
HUP9903707A2 (hu) 2000-03-28
HK1012193A1 (en) 1999-07-30
PE87598A1 (es) 1999-01-15
IL124938A0 (en) 1999-01-26
EE9800227A (et) 1998-12-15
CN1133643C (zh) 2004-01-07
TW498072B (en) 2002-08-11
WO1997024365A1 (en) 1997-07-10
CZ207498A3 (cs) 1998-11-11
SK89198A3 (en) 1999-03-12
NZ324373A (en) 1999-10-28
AP9801274A0 (en) 1998-06-30
HUP9903707A3 (en) 2000-04-28
DK0876392T3 (da) 2000-11-06
KR19990076859A (ko) 1999-10-25
OA10701A (en) 2002-05-21
AU1140997A (en) 1997-07-28
EA001401B1 (ru) 2001-02-26
PL327629A1 (en) 1998-12-21
IS4781A (is) 1998-06-23
EP0876392A1 (en) 1998-11-11
DE69609199D1 (de) 2000-08-10
NO983004D0 (no) 1998-06-26
TR199801247T2 (xx) 1998-11-23

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU