WO1999012933A3 - Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase - Google Patents

Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase Download PDF

Info

Publication number
WO1999012933A3
WO1999012933A3 PCT/EP1998/005609 EP9805609W WO9912933A3 WO 1999012933 A3 WO1999012933 A3 WO 1999012933A3 EP 9805609 W EP9805609 W EP 9805609W WO 9912933 A3 WO9912933 A3 WO 9912933A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
neutrophil elastase
pyrrolopyrrolone
derivatives
pyrrolopyrrolone derivatives
Prior art date
Application number
PCT/EP1998/005609
Other languages
French (fr)
Other versions
WO1999012933A2 (en
Inventor
Geoffrey Duke Edward Clarke
Michael Dennis Dowle
Harry Finch
Lee Andrew Harrison
Graham George Adam Inglis
Martin Redpath Johnson
Simon John Fawcett Macdonald
Pritom Shah
Robin Andrew Smith
Original Assignee
Glaxo Group Ltd
Geoffrey Duke Edward Clarke
Michael Dennis Dowle
Harry Finch
Lee Andrew Harrison
Graham George Adam Inglis
Martin Redpath Johnson
Simon John Fawcett Macdonald
Pritom Shah
Robin Andrew Smith
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 GBGB9719183.7A external-priority patent/GB9719183D0/en
Priority claimed from GBGB9719189.4A external-priority patent/GB9719189D0/en
Priority claimed from GBGB9719290.0A external-priority patent/GB9719290D0/en
Priority claimed from GBGB9803611.4A external-priority patent/GB9803611D0/en
Priority to EA200000204A priority Critical patent/EA200000204A1/en
Priority to JP2000510740A priority patent/JP2001515904A/en
Priority to KR1020007002422A priority patent/KR20010023766A/en
Priority to NZ503130A priority patent/NZ503130A/en
Priority to APAP/P/2000/001761A priority patent/AP2000001761A0/en
Priority to EEP200000138A priority patent/EE200000138A/en
Application filed by Glaxo Group Ltd, Geoffrey Duke Edward Clarke, Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Adam Inglis, Martin Redpath Johnson, Simon John Fawcett Macdonald, Pritom Shah, Robin Andrew Smith filed Critical Glaxo Group Ltd
Priority to EP98951348A priority patent/EP1003748A2/en
Priority to BR9812062-0A priority patent/BR9812062A/en
Priority to HU0004644A priority patent/HUP0004644A3/en
Priority to AU97412/98A priority patent/AU9741298A/en
Priority to CA002303176A priority patent/CA2303176A1/en
Priority to IL13479198A priority patent/IL134791A0/en
Priority to PL98339176A priority patent/PL339176A1/en
Priority to SK319-2000A priority patent/SK3192000A3/en
Publication of WO1999012933A2 publication Critical patent/WO1999012933A2/en
Publication of WO1999012933A3 publication Critical patent/WO1999012933A3/en
Priority to IS5391A priority patent/IS5391A/en
Priority to NO20001198A priority patent/NO20001198L/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

There are provided according to the invention compounds of formula (I) wherein R?1, R2 and R3¿ are as defined in the specification. Compounds of formula (I) are useful, inter alia, in the treatment of inflammatory disorders of the respiratory tract.
PCT/EP1998/005609 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase WO1999012933A2 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
CA002303176A CA2303176A1 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
IL13479198A IL134791A0 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
PL98339176A PL339176A1 (en) 1997-09-09 1998-09-07 Derivatives of pyrrolopyrrolone as inhibitors of neutrophilic elastase
SK319-2000A SK3192000A3 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
HU0004644A HUP0004644A3 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase and pharmaceutical compositions containing them
KR1020007002422A KR20010023766A (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
NZ503130A NZ503130A (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
APAP/P/2000/001761A AP2000001761A0 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase.
EEP200000138A EE200000138A (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
EA200000204A EA200000204A1 (en) 1997-09-09 1998-09-07 Pyrrolopyrlonone derivatives as ELASTASIS INHIBITORS NEUTROPHILS
EP98951348A EP1003748A2 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
BR9812062-0A BR9812062A (en) 1997-09-09 1998-09-07 Compound, use of this, process for preparing it, purified single enantiomer, pharmaceutical composition, and, processes for the treatment of chronic bronchitis or chronic obstructive pulmonary disease in a human or animal individual, and for treatment of asthma in a human or animal individual
JP2000510740A JP2001515904A (en) 1997-09-09 1998-09-07 Pyrrolopyrrolones as neutrophil elastase
AU97412/98A AU9741298A (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
IS5391A IS5391A (en) 1997-09-09 2000-02-29 Pyrrolopyrrolone derivatives that inhibit the elastase neutralization
NO20001198A NO20001198L (en) 1997-09-09 2000-03-08 Pyrrolopyrrole subunits as inhibitors of neutrophil elastase

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
GB9719183.7 1997-09-09
GBGB9719183.7A GB9719183D0 (en) 1997-09-09 1997-09-09 Compounds
GB9719189.4 1997-09-09
GBGB9719189.4A GB9719189D0 (en) 1997-09-09 1997-09-09 New therapeutic method
GBGB9719290.0A GB9719290D0 (en) 1997-09-10 1997-09-10 Compounds
GB9719290.0 1997-09-10
GB9803611.4 1998-02-21
GBGB9803611.4A GB9803611D0 (en) 1998-02-21 1998-02-21 Compounds

Publications (2)

Publication Number Publication Date
WO1999012933A2 WO1999012933A2 (en) 1999-03-18
WO1999012933A3 true WO1999012933A3 (en) 1999-05-27

Family

ID=27451698

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1998/005609 WO1999012933A2 (en) 1997-09-09 1998-09-07 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase

Country Status (24)

Country Link
EP (1) EP1003748A2 (en)
JP (1) JP2001515904A (en)
KR (1) KR20010023766A (en)
CN (1) CN1278820A (en)
AP (1) AP2000001761A0 (en)
AR (1) AR017072A1 (en)
AU (1) AU9741298A (en)
BR (1) BR9812062A (en)
CA (1) CA2303176A1 (en)
CO (1) CO4970719A1 (en)
EA (1) EA200000204A1 (en)
EE (1) EE200000138A (en)
HU (1) HUP0004644A3 (en)
ID (1) ID24452A (en)
IL (1) IL134791A0 (en)
IS (1) IS5391A (en)
MA (1) MA26543A1 (en)
NO (1) NO20001198L (en)
NZ (1) NZ503130A (en)
PE (1) PE107899A1 (en)
PL (1) PL339176A1 (en)
SK (1) SK3192000A3 (en)
TR (1) TR200000907T2 (en)
WO (1) WO1999012933A2 (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9905418D0 (en) * 1999-03-09 1999-05-05 Glaxo Group Ltd Process
MXPA06011410A (en) 2004-03-31 2007-04-20 Johnson & Johnson Non-imidazole heterocyclic compounds.
DE102004024772A1 (en) * 2004-05-17 2005-12-22 Grünenthal GmbH Substituted 5-aminomethyl-1H-pyrrole-2-carboxamides
JP4853759B2 (en) * 2004-05-27 2012-01-11 日本農薬株式会社 Substituted pyrazinecarboxylic acid anilide derivatives or salts thereof, intermediates thereof, agricultural and horticultural agents, and methods of use thereof
TWI355380B (en) * 2004-05-27 2012-01-01 Nihon Nohyaku Co Ltd Substituted pyrazinecarboxanilide derivatives or s
GB2418427A (en) 2004-09-02 2006-03-29 Univ Cambridge Tech Ligands for G-protein coupled receptors
KR20070084455A (en) 2004-11-23 2007-08-24 워너-램버트 캄파니 엘엘씨 7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives as hmg co-a reductase inhibitors for the treatment of lipidemia
NZ572250A (en) 2006-05-04 2011-10-28 Pulmagen Therapeutics Inflammation Ltd Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
US7662967B2 (en) 2007-08-02 2010-02-16 Cambridge Enterprise Limited Anti-inflammatory compounds and compositions
GB2452696B (en) 2007-08-02 2009-09-23 Cambridge Entpr Ltd 3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one and its use in pharmaceutical compositions
WO2009060206A1 (en) * 2007-11-07 2009-05-14 Argenta Discovery Limited 3,4,6,7-tetrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-diones and their therapeutic use
US20110212181A1 (en) * 2010-02-26 2011-09-01 The University Of Hong Kong Compositions and methods for treating chronic respiratory inflammation
BR112022004861A2 (en) 2019-09-17 2022-06-07 Univ Duke Alvestat for use in the treatment of transplant rejection, bronchiolitis obliterans syndrome and transplant versus host disease
IL297211A (en) 2020-04-16 2022-12-01 Mereo Biopharma 4 Ltd Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
TW202325294A (en) 2021-10-20 2023-07-01 英商梅瑞奧生物製藥４有限公司 Neutrophil elastase inhibitors for use in the treatment of fibrosis

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993024519A1 (en) * 1992-06-04 1993-12-09 Zeneca Limited Lactam dipeptides having hle inhibiting activity
WO1995021855A1 (en) * 1994-02-11 1995-08-17 Zeneca Limited Diastereomeric pure trifluoromethyl ketone peptide derivatives as inhibitors of human leukocyte elastase
WO1997036903A1 (en) * 1996-03-28 1997-10-09 Glaxo Group Limited Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993024519A1 (en) * 1992-06-04 1993-12-09 Zeneca Limited Lactam dipeptides having hle inhibiting activity
WO1995021855A1 (en) * 1994-02-11 1995-08-17 Zeneca Limited Diastereomeric pure trifluoromethyl ketone peptide derivatives as inhibitors of human leukocyte elastase
WO1997036903A1 (en) * 1996-03-28 1997-10-09 Glaxo Group Limited Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase

Also Published As

Publication number Publication date
AP2000001761A0 (en) 2000-03-31
EA200000204A1 (en) 2000-10-30
BR9812062A (en) 2000-09-26
CN1278820A (en) 2001-01-03
AU9741298A (en) 1999-03-29
NO20001198D0 (en) 2000-03-08
WO1999012933A2 (en) 1999-03-18
JP2001515904A (en) 2001-09-25
AR017072A1 (en) 2001-08-22
HUP0004644A3 (en) 2002-01-28
IS5391A (en) 2000-02-29
CO4970719A1 (en) 2000-11-07
NO20001198L (en) 2000-05-08
SK3192000A3 (en) 2001-03-12
TR200000907T2 (en) 2000-11-21
EP1003748A2 (en) 2000-05-31
IL134791A0 (en) 2001-04-30
HUP0004644A2 (en) 2001-09-28
NZ503130A (en) 2001-08-31
CA2303176A1 (en) 1999-03-18
KR20010023766A (en) 2001-03-26
EE200000138A (en) 2001-02-15
PL339176A1 (en) 2000-12-04
MA26543A1 (en) 2004-12-20
PE107899A1 (en) 1999-11-17
ID24452A (en) 2000-07-20

Similar Documents

Publication Publication Date Title
CA2343236A1 (en) 4,4-biarylpiperidine derivatives
WO2001066564A3 (en) Gamma-secretase inhibitors
CA2274464A1 (en) Ketobenzamides as calpain inhibitors
WO2001072728A3 (en) Novel piperazine derivatives
WO1999012933A3 (en) Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
AU1617901A (en) Urea derivatives as anti-inflammatory agents
JO2311B1 (en) Alkyne-aryl phosphodiesterase-4 inhibitors
CA2289851A1 (en) Compounds and methods for the inhibition of the expression of vcam-1
CA2210258A1 (en) Substituted oxazolidine calpain and/or cathepsin b inhibitors
CA2205198A1 (en) Human neutrophil elastase inhibitors
CA2276455A1 (en) Phthalazinones
WO2002096905A8 (en) Thiazole compounds useful as inhibitors of protein kinases
AU6645998A (en) Oxygen or sulfur containing heteroaromatics as factor xa inhibitors
CA2356380A1 (en) Immunosuppressive effects of pteridine derivatives
WO2003053359A3 (en) 1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders
BG103310A (en) Benzonaphthyridins as bronchial therapeutical means
WO2001055066A3 (en) 3-phenoxy-1-phenyl acetylene derivatives and their use as herbicides
WO2002085906A3 (en) Phthalazinones derivatives useful as pde4/7 inhibitors
WO2001038311A3 (en) Pyrimidine derivatives as selective inhibitors of cox-2
WO2000039083A3 (en) Pyrazole compounds and uses thereof
NO984470L (en) Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
YU87202A (en) Arylmethylamine derivatives for use as tryptase inhibitors
WO2002094020A8 (en) Use of triazolopyrimidine derivatives as microbicides in the protection of materials
WO2002032901A3 (en) Bridged piperazine derivatives
WO2003053971A8 (en) Pyridoquinoxaline antivirals

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 134791

Country of ref document: IL

Ref document number: 98810954.9

Country of ref document: CN

AK Designated states

Kind code of ref document: A2

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GE GH GM HR HU ID IL IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GE GH GM HR HU ID IL IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 503130

Country of ref document: NZ

Ref document number: 97412/98

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 1998951348

Country of ref document: EP

ENP Entry into the national phase

Ref document number: 2303176

Country of ref document: CA

Ref document number: 2303176

Country of ref document: CA

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 3192000

Country of ref document: SK

Ref document number: PA/a/2000/002325

Country of ref document: MX

Ref document number: 200000204

Country of ref document: EA

WWE Wipo information: entry into national phase

Ref document number: 1020007002422

Country of ref document: KR

Ref document number: P-143/00

Country of ref document: YU

WWE Wipo information: entry into national phase

Ref document number: P20000135A

Country of ref document: HR

Ref document number: PV2000-877

Country of ref document: CZ

WWE Wipo information: entry into national phase

Ref document number: 2000/00907

Country of ref document: TR

WWE Wipo information: entry into national phase

Ref document number: 09508313

Country of ref document: US

WWP Wipo information: published in national office

Ref document number: 1998951348

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: PV2000-877

Country of ref document: CZ

WWP Wipo information: published in national office

Ref document number: 1020007002422

Country of ref document: KR

WWR Wipo information: refused in national office

Ref document number: PV2000-877

Country of ref document: CZ

WWW Wipo information: withdrawn in national office

Ref document number: 1998951348

Country of ref document: EP

WWW Wipo information: withdrawn in national office

Ref document number: 1020007002422

Country of ref document: KR