CA2288868A1 - Inhibiteurs de proteases - Google Patents

Inhibiteurs de proteases Download PDF

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Publication number
CA2288868A1
CA2288868A1 CA002288868A CA2288868A CA2288868A1 CA 2288868 A1 CA2288868 A1 CA 2288868A1 CA 002288868 A CA002288868 A CA 002288868A CA 2288868 A CA2288868 A CA 2288868A CA 2288868 A1 CA2288868 A1 CA 2288868A1
Authority
CA
Canada
Prior art keywords
6alkyl
amino
leucine
tetrahydrofuran
ylcarbonyl
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.)
Abandoned
Application number
CA002288868A
Other languages
English (en)
Inventor
Robert W. Marquis
Ashley Edward Fenwick
Andrew D. Gribble
Jason Witherington
Daniel Frank Veber
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
Individual
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 Individual filed Critical Individual
Publication of CA2288868A1 publication Critical patent/CA2288868A1/fr
Abandoned legal-status Critical Current

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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)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Cette invention se rapporte à des composés de leucine à substitution 3-hydroxy-cyclohétéro et 3-céto-cyclohétéro, qui constituent des inhibiteurs des cystéine-protéases, en particulier la cathépsine K, et qui sont utiles dans le traitement des maladies pour lesquelles l'inhibition de la déperdition osseuse constitue un facteur. La fraction 3-hydroxy ou 3-céto est liée à un cycle tétrahydrothiophène, tétrahydrothiopyranne, tétrahydrofuranne ou tétrahydropyranne.
CA002288868A 1997-05-06 1998-05-06 Inhibiteurs de proteases Abandoned CA2288868A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4575897P 1997-05-06 1997-05-06
US60/045,758 1997-05-06
PCT/US1998/003200 WO1998050533A1 (fr) 1997-05-06 1998-05-06 Inhibiteurs de proteases

Publications (1)

Publication Number Publication Date
CA2288868A1 true CA2288868A1 (fr) 1998-11-12

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002288868A Abandoned CA2288868A1 (fr) 1997-05-06 1998-05-06 Inhibiteurs de proteases

Country Status (19)

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

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150165A1 (es) * 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
DZ3083A1 (fr) * 1999-02-19 2004-06-02 Smithkline Beecham Corp Composés nouveaux inhibiteurs de protéases, procédé pour leur préparation et compositions pharmaceutiques les conentant.
GB9911417D0 (en) * 1999-05-18 1999-07-14 Peptide Therapeutics Ltd Furanone derivatives as inhibitors of cathepsin s
JP2003513971A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
EP1326848A1 (fr) * 2000-10-19 2003-07-16 Naeja Pharmaceutical Inc. Derives de dihydropyrimidine utilises comme inhibiteurs de cysteine protease
IL155958A0 (en) * 2000-11-17 2003-12-23 Medivir Ab Cysteine protease inhibitors
WO2002040462A2 (fr) * 2000-11-17 2002-05-23 Medivir Uk Limited Inhibiteurs de cystéine protéase
IL156776A0 (en) * 2001-01-17 2004-02-08 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
US7132449B2 (en) * 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
JP2004522738A (ja) * 2001-01-17 2004-07-29 アミュラ テラピューティクス リミテッド クルジパインおよび他のシステインプロテアーゼの阻害剤としての環状２−カルボニルアミノケトン
WO2002057270A1 (fr) * 2001-01-17 2002-07-25 Amura Therapeutics Limited Inhibiteurs de la cruzipaine et autres cysteines proteases
CA2463770A1 (fr) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Composes convenant comme inhibiteurs reversibles de proteases de la cysteine
WO2004007501A1 (fr) * 2002-07-16 2004-01-22 Amura Therapeutics Limited Composes a activite biologique
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
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
AR046078A1 (es) 2003-08-06 2005-11-23 Senomyx Inc Nuevos sabores, modificadores de sabores, sustancias gustativas, mejoradores de gusto, sustancias gustativas y/o mejoradoras del gusto umani o dulce y uso de los mismos.
AU2005203972B2 (en) 2004-01-08 2010-11-18 Medivir Ab Cysteine protease inhibitors
MX2008002363A (es) * 2005-08-17 2008-03-18 Schering Corp Ligandos novedosos de cinasa basados en quinolina de alta afinidad.
GB0614042D0 (en) 2006-07-14 2006-08-23 Amura Therapeutics Ltd Compounds
CN101784516B (zh) * 2007-06-13 2014-07-02 百时美施贵宝公司 作为凝血因子抑制剂的二肽类似物
US7893067B2 (en) 2007-06-27 2011-02-22 Medivir Ab Cysteine protease inhibitors
EP2240491B1 (fr) 2008-01-09 2015-07-15 Amura Therapeutics Limited DÉRIVÉS DE TÉTRAHYDROFURO(2,3-b)PYRROL-3-ONE COMME INHIBITEURS DE CYSTÉINE PROTÉINASES
GB0817424D0 (en) * 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
JPH05140063A (ja) * 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
CA2111930A1 (fr) * 1992-12-25 1994-06-26 Ryoichi Ando Derives d'aminocetones
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
JP3599287B2 (ja) * 1993-04-28 2004-12-08 三菱化学株式会社 スルホンアミド誘導体
US5403952A (en) * 1993-10-08 1995-04-04 Merck & Co., Inc. Substituted cyclic derivatives as novel antidegenerative agents
SK48198A3 (en) * 1995-10-30 1998-10-07 Smithkline Beecham Corp Cathepsin k molecule, a peptid being bonded to the hollow of active positon of cathepsin k, a composition, method for identification of inhibiting compound and inhibitors being competitively bonded to the active position of cathepsin k
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 (fr) * 1996-07-29 1998-02-05 Mitsubishi Chemical Corporation Derives heterocycliques oxygenes

Also Published As

Publication number Publication date
NO995434L (no) 1999-11-05
KR20010012256A (ko) 2001-02-15
BR9809306A (pt) 2000-07-04
HUP0002247A2 (hu) 2001-05-28
AU7562598A (en) 1998-11-27
CO4950618A1 (es) 2000-09-01
TR199902766T2 (xx) 2000-02-21
PL336856A1 (en) 2000-07-17
NO995434D0 (no) 1999-11-05
HUP0002247A3 (en) 2003-01-28
EP1003846A1 (fr) 2000-05-31
EP1003846A4 (fr) 2002-11-13
AR013079A1 (es) 2000-12-13
UY25143A1 (es) 1998-11-27
ZA983762B (en) 1998-11-06
JP2001525804A (ja) 2001-12-11
CN1255161A (zh) 2000-05-31
NZ337889A (en) 2001-09-28
PE71599A1 (es) 1999-09-15
WO1998050533A1 (fr) 1998-11-12
IL132088A0 (en) 2001-03-19

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Legal Events

Date Code Title Description
FZDE Discontinued