HUP0002247A2 - Proteáz inhibitorok - Google Patents

Proteáz inhibitorok

Info

Publication number
HUP0002247A2
HUP0002247A2 HU0002247A HUP0002247A HUP0002247A2 HU P0002247 A2 HUP0002247 A2 HU P0002247A2 HU 0002247 A HU0002247 A HU 0002247A HU P0002247 A HUP0002247 A HU P0002247A HU P0002247 A2 HUP0002247 A2 HU P0002247A2
Authority
HU
Hungary
Prior art keywords
alkyl group
group
compounds
het
hydrogen atom
Prior art date
Application number
HU0002247A
Other languages
English (en)
Inventor
Ashley Edward Fenwick
Andrew D. Gribble
Robert W. Marquis
Daniel F. Veber
Jason Witherington
Original Assignee
Smithkline Beecham Corp.
Smithkline Beecham Plc.
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 Corp., Smithkline Beecham Plc. filed Critical Smithkline Beecham Corp.
Publication of HUP0002247A2 publication Critical patent/HUP0002247A2/hu
Publication of HUP0002247A3 publication Critical patent/HUP0002247A3/hu

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

Abstract

A találmány tárgyát (I) általános képletű vegyületek -amelyek képletében R1 jelentése R", R"C(O)-, R"C (S)-, R"SO2-,R"OC(O)-, R"R'NC(O)- vagy R"OC(O)NR'CH(R6)C(O)- általános képletűcsoport; R2 jelentése hidrogénatom, alkilcsoport, alkenilcsoport, Ar-alkil-csoport vagy Het-alkil-csoport; R3 jelentése hidrogénatom,alkilcsoport, alkenilcsoport, alkinilcsoport, cikloalkil-csoport, Ar-alkil-csoport vagy Het-alkil-csoport; R4 jelentése hidrogénatom,alkilcsport, alkenilcsoport, Ar-alkil-csoport vagy Het-alkil-csoport;R5 mindegyikének jelentése egymástól függetlenül hidrogénatom,alkilcsoport, alkenilcsoport, Ar-alkil-csoport vagy Het-alkil-csoport;X jelentése oxigén- vagy kénatom; és n értéke 1, 2 vagy 3 - ésgyógyászatilag elfogadható sóik képezik. A találmány magában foglaljaa hatóanyagként (I) általános képletű vegyületeket tartalmazógyógyszerkészítményeket és a vegyületek gyógyszerkészítményekelőállítására történő alkalmazását is, valamint eljárást a fentivegyületek előállítására. A találmány szerinti vegyületek ésgyógyszerkészítmények különösen jól alkalmazhatók az olyan betegségekkezelésére, amelyekben jelentős szerepet játszanak cisztein proteázok,különösen az excesszív csont- és porcvesztéses betegségek, példáu1 azosteoporosis, a periodontitis és az arthritis kezelésére. Ó
HU0002247A 1997-05-06 1998-05-06 Protease inhibitors HUP0002247A3 (en)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
HUP0002247A2 true HUP0002247A2 (hu) 2001-05-28
HUP0002247A3 HUP0002247A3 (en) 2003-01-28

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0002247A HUP0002247A3 (en) 1997-05-06 1998-05-06 Protease inhibitors

Country Status (19)

Country Link
EP (1) EP1003846A4 (hu)
JP (1) JP2001525804A (hu)
KR (1) KR20010012256A (hu)
CN (1) CN1255161A (hu)
AR (1) AR013079A1 (hu)
AU (1) AU7562598A (hu)
BR (1) BR9809306A (hu)
CA (1) CA2288868A1 (hu)
CO (1) CO4950618A1 (hu)
HU (1) HUP0002247A3 (hu)
IL (1) IL132088A0 (hu)
NO (1) NO995434L (hu)
NZ (1) NZ337889A (hu)
PE (1) PE71599A1 (hu)
PL (1) PL336856A1 (hu)
TR (1) TR199902766T2 (hu)
UY (1) UY25143A1 (hu)
WO (1) WO1998050533A1 (hu)
ZA (1) ZA983762B (hu)

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
EP1232155A4 (en) * 1999-11-10 2002-11-20 Smithkline Beecham Corp PROTEASE INHIBITORS
WO2002032879A1 (en) * 2000-10-19 2002-04-25 Naeja Pharmaceutical Inc. Dihydropyrimidine derivatives as cysteine protease inhibitors
WO2002088106A2 (en) * 2000-11-17 2002-11-07 Medivir Ab Cysteine protease inhibitors
EP1345931A2 (en) * 2000-11-17 2003-09-24 Medivir UK Ltd Cysteine protease inhibitors
IL156775A0 (en) * 2001-01-17 2004-02-08 Amura Therapeutics Ltd Cyclic 2-carbonylaminoketones as 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
US6958358B2 (en) 2001-01-17 2005-10-25 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
ATE356130T1 (de) * 2001-01-17 2007-03-15 Amura Therapeutics Ltd Inhibitoren von cruzipain und anderen cysteinproteasen
CA2463770A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
DE60326473D1 (en) * 2002-07-16 2009-04-16 Amura Therapeutics Ltd Pyrrolderivate als hemmstoffe von cystein proteasen
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
SG153714A1 (en) 2003-08-06 2009-07-29 Senomyx Inc T1r hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds
CA2552739A1 (en) * 2004-01-08 2005-07-21 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 (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

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 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
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
CN1255161A (zh) 2000-05-31
BR9809306A (pt) 2000-07-04
PE71599A1 (es) 1999-09-15
CO4950618A1 (es) 2000-09-01
TR199902766T2 (xx) 2000-02-21
UY25143A1 (es) 1998-11-27
ZA983762B (en) 1998-11-06
NO995434D0 (no) 1999-11-05
WO1998050533A1 (en) 1998-11-12
AR013079A1 (es) 2000-12-13
IL132088A0 (en) 2001-03-19
EP1003846A4 (en) 2002-11-13
EP1003846A1 (en) 2000-05-31
CA2288868A1 (en) 1998-11-12
NO995434L (no) 1999-11-05
KR20010012256A (ko) 2001-02-15
HUP0002247A3 (en) 2003-01-28
PL336856A1 (en) 2000-07-17
NZ337889A (en) 2001-09-28
AU7562598A (en) 1998-11-27
JP2001525804A (ja) 2001-12-11

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