PE87598A1 - Derivados de lactona de 17�-carboxi, carbotio y amida androstano - Google Patents

Derivados de lactona de 17�-carboxi, carbotio y amida androstano

Info

Publication number
PE87598A1
PE87598A1 PE1997000549A PE00054997A PE87598A1 PE 87598 A1 PE87598 A1 PE 87598A1 PE 1997000549 A PE1997000549 A PE 1997000549A PE 00054997 A PE00054997 A PE 00054997A PE 87598 A1 PE87598 A1 PE 87598A1
Authority
PE
Peru
Prior art keywords
formula
compound
alkyl
methyl
carbothium
Prior art date
Application number
PE1997000549A
Other languages
English (en)
Inventor
Keith Biggadike
Panayiotis Alexandrou Procopiou
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE87598A1 publication Critical patent/PE87598A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • 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
    • C07J41/0066Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • 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
    • 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
    • C07J41/00Normal 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I), EN DONDE: R1 ES O, S o NH; R2 ES OC(=O)ALQUILO C1-C6, DE PREFERENCIA DICHO ALQUILO ES METILO, ETILO O N-PROPILO; R3 ES H, METILO (EL CUAL PUEDE ESTAR EN LA CONFIGURACION O o �) O ES METILENO; O R2 Y R3 JUNTOS REPRESENTAN (-O)(-O)CR6R7, EN DONDE R6 Y R7 SON H O ALQUILO C1-C6, DE PREFERENCIA SON H, METILO o N-PROPILO; R4 Y R5 SON H o HALOGENO, DE PREFERENCIA DICHO HALOGENO ES F; LAS LINEAS PUNTEADAS SON UN DOBLE ENLACE OPCIONAL. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE (I), QUE COMPRENDE: (A) TRATAR UN COMPUESTO DE FORMULA (II), EN DONDE "X" ES OH O UN DERIVADO ACTIVO DEL MISMO, CON UN COMPUESTO DE FORMULA (III), EN DONDE "Z" ES OH, NH2 O SH; O (B) TRATAR UN COMPUESTO DE FORMULA (II), EN DONDE "X" ES OH O SH, CON UN COMPUESTO DE FORMULA (VI), EN DONDE "Q" ES UN GRUPO DE SEPARACION TAL COMO Cl, Br o OSO2A, SIENDO "A" POR EJEMPLO CH3, CF3 o p-CH3C6H4, O CON UN COMPUESTO DE FORMULA (VII). LOS COMPUESTOS OBTENIDOS ACTUAN COMO AGONISTAS DEL ADRENORRECEPTOR �2, QUE POSEEN LA VENTAJA DE PRESENTAR POCO O NINGUN EFECTO SISTEMICO, SIENDO UTILES EN EL TRATAMIENTO INFLAMATORIO Y ALERGICO
PE1997000549A 1995-12-29 1997-06-27 Derivados de lactona de 17�-carboxi, carbotio y amida androstano PE87598A1 (es)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
PE87598A1 true PE87598A1 (es) 1999-01-15

Family

ID=26308402

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000549A PE87598A1 (es) 1995-12-29 1997-06-27 Derivados de lactona de 17�-carboxi, carbotio y amida androstano

Country Status (34)

Country Link
US (1) US6197761B1 (es)
EP (1) EP0876392B1 (es)
JP (1) JP2947944B2 (es)
KR (1) KR19990076859A (es)
CN (1) CN1133643C (es)
AP (1) AP9801274A0 (es)
AT (1) ATE194356T1 (es)
AU (1) AU721865B2 (es)
BG (1) BG102625A (es)
BR (1) BR9612309A (es)
CA (1) CA2241728A1 (es)
CZ (1) CZ207498A3 (es)
DE (1) DE69609199T2 (es)
DK (1) DK0876392T3 (es)
EA (1) EA001401B1 (es)
EE (1) EE9800227A (es)
ES (1) ES2150150T3 (es)
GR (1) GR3034564T3 (es)
HK (1) HK1012193A1 (es)
HU (1) HUP9903707A3 (es)
IL (1) IL124938A0 (es)
IS (1) IS4781A (es)
MX (1) MX9805181A (es)
NO (1) NO311022B1 (es)
NZ (1) NZ324373A (es)
OA (1) OA10701A (es)
PE (1) PE87598A1 (es)
PL (1) PL327629A1 (es)
PT (1) PT876392E (es)
SI (1) SI0876392T1 (es)
SK (1) SK89198A3 (es)
TR (1) TR199801247T2 (es)
TW (1) TW498072B (es)
WO (1) WO1997024365A1 (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2215310T3 (es) * 1997-06-30 2004-10-01 Glaxo Group Limited Procedimiento para identificar compuestos que tienen una actividad sistemica reducida.
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
US6858596B2 (en) * 2000-08-05 2005-02-22 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivative
US6750210B2 (en) 2000-08-05 2004-06-15 Smithkline Beecham Corporation Formulation containing novel anti-inflammatory androstane derivative
US6777399B2 (en) * 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6759398B2 (en) 2000-08-05 2004-07-06 Smithkline Beecham Corporation Anti-inflammatory androstane derivative
US6787532B2 (en) 2000-08-05 2004-09-07 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivatives
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
EA005992B1 (ru) * 2000-08-05 2005-08-25 Глаксо Груп Лимитед S-ФТОРМЕТИЛОВЫЙ ЭФИР 6α,9α-ДИФТОР-17α-[(2-ФУРАНИЛКАРБОНИЛ)ОКСИ]-11β-ГИДРОКСИ-16α-МЕТИЛ-3-ОКСОАНДРОСТА-1,4-ДИЕН-17β-КАРБОТИОКИСЛОТЫ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНОГО АГЕНТА
GB0019172D0 (en) 2000-08-05 2000-09-27 Glaxo Group Ltd Novel compounds
US6858593B2 (en) 2000-08-05 2005-02-22 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
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
AU2002253342B2 (en) * 2001-04-30 2007-01-04 Glaxo Group Limited Novel anti-inflammatory androstane derivatives
ES2307751T3 (es) * 2001-06-12 2008-12-01 Glaxo Group Limited Nuevos esteres heterociclicos centi-inflamatorios 17 alfa de derivados 17 beta de carbotioato de androstano.
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
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
GB0127160D0 (en) * 2001-11-12 2002-01-02 Glaxo Group Ltd Novel compounds
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
AU2004226318B2 (en) * 2003-04-04 2008-06-05 Xellia Pharmaceuticals 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
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
AR059216A1 (es) * 2006-01-27 2008-03-19 Sun Pharmaceutical Ind Ltd 11b-hidroxiandrosta-4-eno-3-onas
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

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
BG102625A (en) 1999-04-30
CZ207498A3 (cs) 1998-11-11
DE69609199D1 (de) 2000-08-10
EA199800484A1 (ru) 1999-02-25
HK1012193A1 (en) 1999-07-30
SI0876392T1 (en) 2000-12-31
NO311022B1 (no) 2001-10-01
JP2947944B2 (ja) 1999-09-13
AU721865B2 (en) 2000-07-13
HUP9903707A2 (hu) 2000-03-28
NO983004D0 (no) 1998-06-26
HUP9903707A3 (en) 2000-04-28
EA001401B1 (ru) 2001-02-26
BR9612309A (pt) 1999-07-13
NZ324373A (en) 1999-10-28
SK89198A3 (en) 1999-03-12
WO1997024365A1 (en) 1997-07-10
CA2241728A1 (en) 1997-07-10
CN1133643C (zh) 2004-01-07
GR3034564T3 (en) 2001-01-31
US6197761B1 (en) 2001-03-06
EP0876392A1 (en) 1998-11-11
CN1209135A (zh) 1999-02-24
DE69609199T2 (de) 2001-03-01
OA10701A (en) 2002-05-21
ATE194356T1 (de) 2000-07-15
TW498072B (en) 2002-08-11
IS4781A (is) 1998-06-23
PL327629A1 (en) 1998-12-21
EP0876392B1 (en) 2000-07-05
EE9800227A (et) 1998-12-15
TR199801247T2 (xx) 1998-11-23
AU1140997A (en) 1997-07-28
JPH11501675A (ja) 1999-02-09
MX9805181A (es) 1998-10-31
PT876392E (pt) 2000-12-29
AP9801274A0 (en) 1998-06-30
KR19990076859A (ko) 1999-10-25
NO983004L (no) 1998-08-26
IL124938A0 (en) 1999-01-26
DK0876392T3 (da) 2000-11-06
ES2150150T3 (es) 2000-11-16

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Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed