[go: up one dir, main page]

WO2001034566A3 - Protease inhibitors - Google Patents

Protease inhibitors Download PDF

Info

Publication number
WO2001034566A3
WO2001034566A3 PCT/US2000/030682 US0030682W WO0134566A3 WO 2001034566 A3 WO2001034566 A3 WO 2001034566A3 US 0030682 W US0030682 W US 0030682W WO 0134566 A3 WO0134566 A3 WO 0134566A3
Authority
WO
WIPO (PCT)
Prior art keywords
protease inhibitors
solvate
hydrate
inhibition
inhibitor
Prior art date
Application number
PCT/US2000/030682
Other languages
French (fr)
Other versions
WO2001034566A2 (en
Inventor
Robert W Marquis Jr
Daniel Frank Veber
Original Assignee
Smithkline Beecham Corp
Robert W Marquis Jr
Daniel Frank Veber
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, Robert W Marquis Jr, Daniel Frank Veber filed Critical Smithkline Beecham Corp
Priority to JP2001536515A priority Critical patent/JP2003533432A/en
Priority to EP00977056A priority patent/EP1351930A4/en
Priority to AU14747/01A priority patent/AU1474701A/en
Publication of WO2001034566A2 publication Critical patent/WO2001034566A2/en
Publication of WO2001034566A3 publication Critical patent/WO2001034566A3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • A61P33/12Schistosomicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.
PCT/US2000/030682 1999-11-10 2000-11-08 Protease inhibitors WO2001034566A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2001536515A JP2003533432A (en) 1999-11-10 2000-11-08 Protease inhibitor
EP00977056A EP1351930A4 (en) 1999-11-10 2000-11-08 Protease inhibitors
AU14747/01A AU1474701A (en) 1999-11-10 2000-11-08 Protease inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16456199P 1999-11-10 1999-11-10
US60/164,561 1999-11-10

Publications (2)

Publication Number Publication Date
WO2001034566A2 WO2001034566A2 (en) 2001-05-17
WO2001034566A3 true WO2001034566A3 (en) 2003-07-31

Family

ID=22595065

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/030682 WO2001034566A2 (en) 1999-11-10 2000-11-08 Protease inhibitors

Country Status (4)

Country Link
EP (1) EP1351930A4 (en)
JP (1) JP2003533432A (en)
AU (1) AU1474701A (en)
WO (1) WO2001034566A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002533397A (en) * 1998-12-23 2002-10-08 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
US6534498B1 (en) 1999-11-10 2003-03-18 Smithkline Beecham Corporation Protease inhibitors
JP2003513971A (en) 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 Protease inhibitor
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp Protease inhibitors
AU4344101A (en) 2000-03-21 2001-10-03 Smithkline Beecham Corp Protease inhibitors
CO5280093A1 (en) * 2000-04-18 2003-05-30 Smithkline Beecham Corp TREATMENT METHODS
CN105288305A (en) * 2015-11-30 2016-02-03 延欣虹 Pharmaceutical composition for curing oral excessive inflammation and gingival pain and swelling and preparation method of pharmaceutical composition

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000038687A1 (en) * 1998-12-23 2000-07-06 Smithkline Beecham Corporation Protease inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DZ2285A1 (en) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Cysteine protease inhibitors.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000038687A1 (en) * 1998-12-23 2000-07-06 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
WO2001034566A2 (en) 2001-05-17
JP2003533432A (en) 2003-11-11
EP1351930A2 (en) 2003-10-15
AU1474701A (en) 2001-06-06
EP1351930A4 (en) 2004-09-15

Similar Documents

Publication Publication Date Title
WO2002069901A3 (en) Cathepsin cysteine protease inhibitors
WO2003075836A3 (en) Cathepsin cysteine protease inhibitors
MXPA04001930A (en) Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases.
CA2458684A1 (en) Pyrrolo pyrimidines as agents for the inhibition of cystein proteases
AU2003243095A1 (en) New use of pyrimidine - or triazine- 2-carbonitiles for treating diseases associated with cysteine protease activity and novel pyrimidine-2-carbonitile derivatives
IL165262A (en) Kinase inhibitors and pharmaceutical compositions containing them
PL361404A1 (en) Synergistic combinations comprising a renin inhibitor for cardiovascular diseases
GEP20074098B (en) Lactam-containing compounds and derivatives thereof as factor xa inhibitors
WO2001034565A3 (en) Protease inhibitors
MXPA03006224A (en) Inhibitors of cruzipain and other cysteine proteases.
WO2004031145A3 (en) Lactam-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor xa inhibitors
WO2001034566A3 (en) Protease inhibitors
AR021241A1 (en) PROTEASE INHIBITORS
AU2002348473A1 (en) Nitrogen heterocycle inhibitors of aspartyl protease
AU8039501A (en) New amidino derivatives and their use as thrombin inhibitors
WO2004108892A3 (en) 1,1-DISUBSTITUTEDCYCLOALKYL-, GLYCINAMIDYL-, SULFONYL-AMIDINO-, AND TETRAHYDROPYRIMIDINYL-CONTAINING DIAMINOALKYL, β-AMINOACIDS, α-AMINOACIDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
WO2002070517A3 (en) Cathepsin cysteine protease inhibitors
MY132033A (en) New mandelic acid derivatives and their use as thrombin inhibitors
IL160068A0 (en) Mew mandelic acid derivatives and their use as thrombin inhibitors
WO2001079162A3 (en) INHIBITORS OF THE ICE/ced-3 FAMILY OF CYSTEINE PROTEASES
AU2002346812A1 (en) Use of 1-phenyl-oxazolidine-2-one compounds as protease m inhibitors
ECSP993018A (en) NEW PROTEASE INHIBITORS, PARTICULARLY CYSTEINE AND SERINE PROTEASE INHIBITORS
AU2002348212A8 (en) Protease inhibitors of the coagulation cascade isolated from dysidea sponges
MY139221A (en) Cathepsin cysteine protease inhibitors
UY25369A1 (en) PROCEDURE FOR PREPARING PROTEASE INHIBITORS

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AU CA JP US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR

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)
ENP Entry into the national phase

Ref country code: JP

Ref document number: 2001 536515

Kind code of ref document: A

Format of ref document f/p: F

WWE Wipo information: entry into national phase

Ref document number: 10129648

Country of ref document: US

WWE Wipo information: entry into national phase

Ref document number: 2000977056

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2000977056

Country of ref document: EP

WWW Wipo information: withdrawn in national office

Ref document number: 2000977056

Country of ref document: EP