PE107899A1 - PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS - Google Patents

PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS

Info

Publication number
PE107899A1
PE107899A1 PE1998000828A PE00082898A PE107899A1 PE 107899 A1 PE107899 A1 PE 107899A1 PE 1998000828 A PE1998000828 A PE 1998000828A PE 00082898 A PE00082898 A PE 00082898A PE 107899 A1 PE107899 A1 PE 107899A1
Authority
PE
Peru
Prior art keywords
alkyl
compound
pirrolopyrolone
leucocitary
derivatives
Prior art date
Application number
PE1998000828A
Other languages
Spanish (es)
Inventor
Michael Dennis Dowle
Lee Andrew Harrison
Graham George Adam Inglis
Geoffrey Duke Edward Clarke
Harry Finch
Pritom Shah
Martin Redpath Johnson
Simon John Fawcett Macdonald
Robin Andrew Smith
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 GBGB9719189.4A external-priority patent/GB9719189D0/en
Priority claimed from GBGB9719183.7A external-priority patent/GB9719183D0/en
Priority claimed from GBGB9719290.0A external-priority patent/GB9719290D0/en
Priority claimed from GBGB9803611.4A external-priority patent/GB9803611D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE107899A1 publication Critical patent/PE107899A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs 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

SE REFIERE A UN COMPUESTO DE FORMULA I, R1 ES ALQUILO C1-C6; R2 ES ALQUILO C2-C4 o ALQUENILO C2-C4; X ES CO o SO2; HET ES UN MONOCICLO O BICICLO AROMATICO DE 5-10 MIEMBROS OPCIONALMENTE SUSTITUIDO; n ES 0-4; R3 Y R4 SON H, ALQUILO C1-C8, -(CH2)(1-4)CONR5R6, CO(ALQUILO C1-C4), (CH2)(CERO-2)Fen; Fen ES FENILO OPCIONALMENTE SUSTITUIDO; O NR3R4 SON AZETIDINILO, PIRROLIDINILO, PIPERIDINILO,ENTRE OTROS; R5 Y R6 SON H o ALQUILO C1-C4. UN COMPUESTO PREFERIDO ES (3S,3aS,6aR)-3-ISOPROPIL-1-METANSULFONIL-4-(2-PIRROLIDIN-1-ILMETIL-OXAZOL-4-CARBONIL)-HEXAHIDRO-PIRROLO[3,2-b]PIRROL-2-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN INHIBIDOR DE LA ELASTASA NEUTROFILA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE BRONQUITIS CRONICA O ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA, ASMAIT REFERS TO A COMPOUND OF FORMULA I, R1 IS C1-C6 ALKYL; R2 IS C2-C4 ALKYL or C2-C4 ALKYNYL; X IS CO or SO2; HET IS AN OPTIONALLY REPLACED 5-10 MEMBER AROMATIC MONOCYCLE OR BICYCLE; n ES 0-4; R3 and R4 ARE H, C1-C8 ALKYL, - (CH2) (1-4) CONR5R6, CO (C1-C4 ALKYL), (CH2) (ZERO-2) Fen; Fen is optionally substituted phenyl; OR NR3R4 ARE AZETIDINYL, PYRROLIDINYL, PIPERIDINYL, AMONG OTHERS; R5 AND R6 ARE H or C1-C4 ALKYL. A PREFERRED COMPOUND IS (3S, 3aS, 6aR) -3-ISOPROPIL-1-METANSULFONIL-4- (2-PIRROLIDIN-1-ILMETIL-OXAZOL-4-CARBONIL) -HEXAHIDRO-PIRROLO [3,2-b] PIRROL- 2-ONA; AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR PREPARATION. COMPOUND I IS A NEUTROPHILIC ELASTASE INHIBITOR AND MAY BE USEFUL FOR THE TREATMENT OF CHRONIC BRONCHITIS OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE, ASTHMA

PE1998000828A 1997-09-09 1998-09-04 PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS PE107899A1 (en)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
PE107899A1 true PE107899A1 (en) 1999-11-17

Family

ID=27451698

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1998000828A PE107899A1 (en) 1997-09-09 1998-09-04 PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS

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
EP1771432B1 (en) 2004-03-31 2010-12-08 Janssen Pharmaceutica NV Non-imidazole heterocyclic compounds as histamine h3 receptor modulators
DE102004024772A1 (en) * 2004-05-17 2005-12-22 Grünenthal GmbH Substituted 5-aminomethyl-1H-pyrrole-2-carboxamides
TWI355380B (en) * 2004-05-27 2012-01-01 Nihon Nohyaku Co Ltd Substituted pyrazinecarboxanilide derivatives or s
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
GB2418427A (en) 2004-09-02 2006-03-29 Univ Cambridge Tech Ligands for G-protein coupled receptors
CA2590533C (en) 2004-11-23 2010-09-07 Warner-Lambert Company Llc 7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives as hmg co-a reductase inhibitors for the treatment of lipidemia
EP2024367B1 (en) 2006-05-04 2010-09-08 Pulmagen Therapeutics (Inflammation) Limited 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
GB2452696B (en) 2007-08-02 2009-09-23 Cambridge Entpr Ltd 3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one and its use in pharmaceutical compositions
US7662967B2 (en) 2007-08-02 2010-02-16 Cambridge Enterprise Limited Anti-inflammatory compounds and 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
AU2020349353A1 (en) 2019-09-17 2022-04-14 Duke University Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
AU2021256835A1 (en) 2020-04-16 2022-10-13 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
EP4419102A1 (en) 2021-10-20 2024-08-28 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9211783D0 (en) * 1992-06-04 1992-07-15 Ici Plc Amide derivatives
GB9402680D0 (en) * 1994-02-11 1994-04-06 Zeneca Ltd Pyrrolidine derivatives
AP823A (en) * 1996-03-28 2000-04-25 Glaxo Group Ltd Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase.

Also Published As

Publication number Publication date
AU9741298A (en) 1999-03-29
ID24452A (en) 2000-07-20
NO20001198L (en) 2000-05-08
WO1999012933A2 (en) 1999-03-18
CA2303176A1 (en) 1999-03-18
TR200000907T2 (en) 2000-11-21
AP2000001761A0 (en) 2000-03-31
NO20001198D0 (en) 2000-03-08
MA26543A1 (en) 2004-12-20
EA200000204A1 (en) 2000-10-30
AR017072A1 (en) 2001-08-22
NZ503130A (en) 2001-08-31
CO4970719A1 (en) 2000-11-07
IL134791A0 (en) 2001-04-30
KR20010023766A (en) 2001-03-26
HUP0004644A3 (en) 2002-01-28
HUP0004644A2 (en) 2001-09-28
BR9812062A (en) 2000-09-26
CN1278820A (en) 2001-01-03
SK3192000A3 (en) 2001-03-12
WO1999012933A3 (en) 1999-05-27
PL339176A1 (en) 2000-12-04
IS5391A (en) 2000-02-29
EE200000138A (en) 2001-02-15
JP2001515904A (en) 2001-09-25
EP1003748A2 (en) 2000-05-31

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