EP1003846A4 - Protease inhibitors - Google Patents

Protease inhibitors

Info

Publication number
EP1003846A4
EP1003846A4 EP98923299A EP98923299A EP1003846A4 EP 1003846 A4 EP1003846 A4 EP 1003846A4 EP 98923299 A EP98923299 A EP 98923299A EP 98923299 A EP98923299 A EP 98923299A EP 1003846 A4 EP1003846 A4 EP 1003846A4
Authority
EP
European Patent Office
Prior art keywords
protease inhibitors
protease
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP98923299A
Other languages
German (de)
French (fr)
Other versions
EP1003846A1 (en
Inventor
Andrew D Gribble
Ashley Edward Fenwick
Robert W Marquis
Daniel F Veber
Jason Witherington
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Ltd
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Ltd
SmithKline Beecham Corp
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
Application filed by SmithKline Beecham Ltd, SmithKline Beecham Corp filed Critical SmithKline Beecham Ltd
Publication of EP1003846A1 publication Critical patent/EP1003846A1/en
Publication of EP1003846A4 publication Critical patent/EP1003846A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/32—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/99—Enzyme inactivation by chemical treatment
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06—Anabolic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/83—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/86—Benzo [b] furans; Hydrogenated benzo [b] furans with an oxygen atom directly attached in position 7
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Microbiology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
EP98923299A 1997-05-06 1998-05-06 Protease inhibitors Withdrawn EP1003846A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4575897P 1997-05-06 1997-05-06
US45758P 1997-05-06
PCT/US1998/003200 WO1998050533A1 (en) 1997-05-06 1998-05-06 Protease inhibitors

Publications (2)

Publication Number Publication Date
EP1003846A1 EP1003846A1 (en) 2000-05-31
EP1003846A4 true EP1003846A4 (en) 2002-11-13

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98923299A Withdrawn EP1003846A4 (en) 1997-05-06 1998-05-06 Protease inhibitors

Country Status (19)

Country Link
EP (1) EP1003846A4 (en)
JP (1) JP2001525804A (en)
KR (1) KR20010012256A (en)
CN (1) CN1255161A (en)
AR (1) AR013079A1 (en)
AU (1) AU7562598A (en)
BR (1) BR9809306A (en)
CA (1) CA2288868A1 (en)
CO (1) CO4950618A1 (en)
HU (1) HUP0002247A3 (en)
IL (1) IL132088A0 (en)
NO (1) NO995434D0 (en)
NZ (1) NZ337889A (en)
PE (1) PE71599A1 (en)
PL (1) PL336856A1 (en)
TR (1) TR199902766T2 (en)
UY (1) UY25143A1 (en)
WO (1) WO1998050533A1 (en)
ZA (1) ZA983762B (en)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150165A1 (en) * 1998-11-13 2002-04-29 Smithkline Beecham Plc PROTEASE INHIBITORS: KATEPSIN K TYPE
DZ3083A1 (en) * 1999-02-19 2004-06-02 Smithkline Beecham Corp New protease inhibitor compounds, process for their preparation and pharmaceutical compositions containing them
GB9911417D0 (en) * 1999-05-18 1999-07-14 Peptide Therapeutics Ltd Furanone derivatives as inhibitors of cathepsin s
EP1232155A4 (en) * 1999-11-10 2002-11-20 Smithkline Beecham Corp Protease inhibitors
CA2426271A1 (en) * 2000-10-19 2002-04-25 Naeja Pharmaceutical Inc. Dihydropyrimidine derivatives as cysteine protease inhibitors
JP2004513942A (en) * 2000-11-17 2004-05-13 メディヴァー　ユーケイ　リミテッド Cysteine protease inhibitor
EP1358183B1 (en) * 2000-11-17 2006-04-12 Medivir Ab Cysteine protease inhibitors
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
CA2434068A1 (en) 2001-01-17 2002-07-25 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
DE60218633T2 (en) * 2001-01-17 2008-02-21 Amura Therapeutics Ltd. INHIBITORS OF CRUCIPAIN AND OTHER CYSTONE PROTEASES
WO2002057249A1 (en) * 2001-01-17 2002-07-25 Amura Therapeutics Limited Cyclic 2-carbonylaminoketones as inhibitors of cruzipain and other cysteine proteases
WO2003037892A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
ATE424401T1 (en) * 2002-07-16 2009-03-15 Amura Therapeutics Ltd PYRROL DERIVATIVES AS INHIBITORS OF CYSTEIN PROTEASES
KR100962972B1 (en) 2002-07-26 2010-06-09 주식회사유한양행 1-phenylpiperidin-3-one derivatives and processes for the preparation thereof
EP1660859A4 (en) 2003-08-06 2012-10-10 Senomyx Inc T1r hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds
AU2016206281B2 (en) * 2003-08-06 2017-11-30 Senomyx, Inc. Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
DE602005019971D1 (en) 2004-01-08 2010-04-29 Medivir Ab INHIBITORS OF CYSTONE PROTEASE
CA2619706A1 (en) * 2005-08-17 2007-02-22 Schering Corporation Novel high affinity quinoline-based kinase ligands
GB0614042D0 (en) 2006-07-14 2006-08-23 Amura Therapeutics Ltd Compounds
US8367709B2 (en) * 2007-06-13 2013-02-05 Bristol-Myers Squibb Company Dipeptide analogs as coagulation factor inhibitors
US7893067B2 (en) 2007-06-27 2011-02-22 Medivir Ab Cysteine protease inhibitors
EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-b)PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES
GB0817424D0 (en) 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0525420A1 (en) * 1991-07-01 1993-02-03 Mitsubishi Chemical Corporation Pseudopeptides and dipeptides characterised by a substituted methyl ketone moiety at the C-terminus as thiol protease inhibitors
EP0543310A2 (en) * 1991-11-19 1993-05-26 Suntory Limited Dipeptide derivative and prophylactic and therapeutic agent for bone diseases containing the same
EP0603873A1 (en) * 1992-12-25 1994-06-29 Mitsubishi Chemical Corporation Aminoketone derivatives
EP0611756A2 (en) * 1993-02-19 1994-08-24 Takeda Chemical Industries, Ltd. Alcohol or aldehyde derivatives as cathepsin L inhibitor and bone resorption inhibitor
EP0623627A1 (en) * 1993-04-28 1994-11-09 Mitsubishi Chemical Corporation Sulfonamide derivatives
WO1997016177A1 (en) * 1995-10-30 1997-05-09 Smithkline Beecham Corporation Method of inhibiting cathepsin k

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5403952A (en) * 1993-10-08 1995-04-04 Merck & Co., Inc. Substituted cyclic derivatives as novel antidegenerative agents
TW448172B (en) * 1996-03-08 2001-08-01 Pharmacia & Upjohn Co Llc Novel hydroxamic acid derivatives useful for the treatment of diseases related to connective tissue degradation
WO1998004539A1 (en) * 1996-07-29 1998-02-05 Mitsubishi Chemical Corporation Oxygenic heterocyclic derivatives

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0525420A1 (en) * 1991-07-01 1993-02-03 Mitsubishi Chemical Corporation Pseudopeptides and dipeptides characterised by a substituted methyl ketone moiety at the C-terminus as thiol protease inhibitors
EP0543310A2 (en) * 1991-11-19 1993-05-26 Suntory Limited Dipeptide derivative and prophylactic and therapeutic agent for bone diseases containing the same
EP0603873A1 (en) * 1992-12-25 1994-06-29 Mitsubishi Chemical Corporation Aminoketone derivatives
EP0611756A2 (en) * 1993-02-19 1994-08-24 Takeda Chemical Industries, Ltd. Alcohol or aldehyde derivatives as cathepsin L inhibitor and bone resorption inhibitor
EP0623627A1 (en) * 1993-04-28 1994-11-09 Mitsubishi Chemical Corporation Sulfonamide derivatives
WO1997016177A1 (en) * 1995-10-30 1997-05-09 Smithkline Beecham Corporation Method of inhibiting cathepsin k

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
J. L. CONROY: "Synthesis of cyclohexanone-based Cathepsin B inhibitors that interact with both the S and S' binding sites", TETRAHEDRON LETTERS, vol. 39, 5 November 1998 (1998-11-05), pages 8253 - 8256, XP002211176 *
J. L. CONROY: "Using the electrostatic field effect to design a new class of inhibitors for cysteine proteases", J. AM. CHEM. SOC., vol. 119, 7 May 1997 (1997-05-07), pages 4285 - 4291, XP002211175 *
R. W. MARQUIS ET AL.: "Cyclic ketone inhibitors of the cysteine protease Cathepsin K", J. MED. CHEM., vol. 44, 2001, pages 725 - 736, XP002211174 *
See also references of WO9850533A1 *

Also Published As

Publication number Publication date
UY25143A1 (en) 1998-11-27
PE71599A1 (en) 1999-09-15
CO4950618A1 (en) 2000-09-01
HUP0002247A3 (en) 2003-01-28
TR199902766T2 (en) 2000-02-21
NZ337889A (en) 2001-09-28
NO995434L (en) 1999-11-05
KR20010012256A (en) 2001-02-15
WO1998050533A1 (en) 1998-11-12
AU7562598A (en) 1998-11-27
ZA983762B (en) 1998-11-06
AR013079A1 (en) 2000-12-13
BR9809306A (en) 2000-07-04
JP2001525804A (en) 2001-12-11
EP1003846A1 (en) 2000-05-31
PL336856A1 (en) 2000-07-17
IL132088A0 (en) 2001-03-19
CN1255161A (en) 2000-05-31
NO995434D0 (en) 1999-11-05
HUP0002247A2 (en) 2001-05-28
CA2288868A1 (en) 1998-11-12

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