AU2002333758B2 - Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin K inhibitory activity for the treatment of inflammations and other diseases - Google Patents

Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin K inhibitory activity for the treatment of inflammations and other diseases Download PDF

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Publication number
AU2002333758B2
AU2002333758B2 AU2002333758A AU2002333758A AU2002333758B2 AU 2002333758 B2 AU2002333758 B2 AU 2002333758B2 AU 2002333758 A AU2002333758 A AU 2002333758A AU 2002333758 A AU2002333758 A AU 2002333758A AU 2002333758 B2 AU2002333758 B2 AU 2002333758B2
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AU
Australia
Prior art keywords
lower alkyl
heterocyclyl
phenyl
piperazin
aryl
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Ceased
Application number
AU2002333758A
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English (en)
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AU2002333758A1 (en
Inventor
Eva Altman
Kenji Hayakawa
Genji Iwasaki
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Novartis AG
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Novartis AG
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Priority claimed from GB0121024A external-priority patent/GB0121024D0/en
Priority claimed from GBGB0121026.9A external-priority patent/GB0121026D0/en
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2002333758A1 publication Critical patent/AU2002333758A1/en
Application granted granted Critical
Publication of AU2002333758B2 publication Critical patent/AU2002333758B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2002333758A 2001-08-30 2002-08-29 Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin K inhibitory activity for the treatment of inflammations and other diseases Ceased AU2002333758B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0121026.9 2001-08-30
GB0121024A GB0121024D0 (en) 2001-08-30 2001-08-30 Organic compounds
GBGB0121026.9A GB0121026D0 (en) 2001-08-30 2001-08-30 Organic compounds
GB0121024.4 2001-08-30
PCT/EP2002/009661 WO2003020278A1 (en) 2001-08-30 2002-08-29 Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases

Publications (2)

Publication Number Publication Date
AU2002333758A1 AU2002333758A1 (en) 2003-06-05
AU2002333758B2 true AU2002333758B2 (en) 2006-01-19

Family

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Application Number Title Priority Date Filing Date
AU2002333758A Ceased AU2002333758B2 (en) 2001-08-30 2002-08-29 Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin K inhibitory activity for the treatment of inflammations and other diseases

Country Status (22)

Country Link
US (2) US7112589B2 (enExample)
EP (1) EP1423121B1 (enExample)
JP (1) JP4131701B2 (enExample)
KR (1) KR100629834B1 (enExample)
CN (1) CN1549717B (enExample)
AR (1) AR036375A1 (enExample)
AT (1) ATE345136T1 (enExample)
AU (1) AU2002333758B2 (enExample)
BR (1) BR0212141A (enExample)
CA (1) CA2456127C (enExample)
CO (1) CO5560576A2 (enExample)
DE (1) DE60216122T2 (enExample)
ES (1) ES2275946T3 (enExample)
HU (1) HUP0401431A3 (enExample)
IL (1) IL160295A0 (enExample)
MX (1) MXPA04001930A (enExample)
NZ (1) NZ531287A (enExample)
PE (1) PE20030772A1 (enExample)
PL (1) PL208280B1 (enExample)
PT (1) PT1423121E (enExample)
RU (1) RU2326119C2 (enExample)
WO (1) WO2003020278A1 (enExample)

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SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
GB0220187D0 (en) 2002-08-30 2002-10-09 Novartis Ag Organic compounds
WO2005014006A1 (en) * 2003-07-21 2005-02-17 Novartis Ag Combinations of a cathepsin k inhibitor and a bisphophonate in the treatment of bone metastasis, tumor growth and tumor-induced bone loss
WO2005011703A1 (en) * 2003-08-04 2005-02-10 Akzo Nobel N.V. 2-cyano-1,3,5-triazine-4,6-diamine derivatives
EP1667983A4 (en) * 2003-09-23 2010-07-21 Merck Sharp & Dohme PYRAZOL MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
WO2005049028A1 (en) * 2003-11-19 2005-06-02 Novartis Ag Use of cathepsin k inhibitors in severe bone loss diseases
US20070232586A1 (en) * 2004-04-21 2007-10-04 Kazuyuki Ohmoto Hydrazino-Substituted Heterocyclic Nitrile Compounds and Use Thereof
TW200614993A (en) * 2004-06-11 2006-05-16 Akzo Nobel Nv 4-phenyl-pyrimidine-2-carbonitrile derivatives
WO2006027211A1 (en) * 2004-09-07 2006-03-16 Glaxo Group Limited 2,4-substituted pyrimidines as cysteine protease inhibitors
WO2006040300A1 (en) * 2004-10-12 2006-04-20 N.V. Organon 4-cycloalkyl-pyrimidine-2-carbonitrile derivatives
IL164942A0 (en) * 2004-10-31 2005-12-18 Yeda Res & Dev The use of a protease or a protease inhibitor for the manufacture of medicaments
GB0514684D0 (en) * 2005-07-18 2005-08-24 Novartis Ag Organic compounds
CA2617725C (en) * 2005-08-05 2012-04-03 Hybrigenics Sa Novel cysteine protease inhibitors and their therapeutic applications
WO2007025776A2 (en) * 2005-09-02 2007-03-08 Glaxo Group Limited Cysteine protease inhibitors
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US7932251B2 (en) 2007-07-16 2011-04-26 N.V. Organon 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
EP2489656A1 (en) 2007-12-21 2012-08-22 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
TW201035094A (en) 2009-01-16 2010-10-01 Organon Nv 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
US8026236B2 (en) 2009-01-16 2011-09-27 N.V. Organon 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
EP2316820A1 (en) * 2009-10-28 2011-05-04 Dompe S.p.A. 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them
US9115126B2 (en) 2010-01-15 2015-08-25 Merck Sharp & Dohme B.V. 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives
EP3091085B1 (en) 2010-10-06 2019-02-27 Institució Catalana de Recerca I Estudis Avançats Method of designing a therapy for breast cancer metastasis
US8524710B2 (en) * 2010-11-05 2013-09-03 Hoffmann-La Roche Inc. Pyrrolidine derivatives
EP2650682A1 (en) 2012-04-09 2013-10-16 Fundació Privada Institut de Recerca Biomèdica Method for the prognosis and treatment of cancer metastasis
BR112014030750A2 (pt) 2012-06-06 2017-08-22 Inst Catalana Recerca Estudis Avancats Método para diagnóstico, prognóstico e tratamento da metástase do câncer pulmonar
US10119171B2 (en) 2012-10-12 2018-11-06 Inbiomotion S.L. Method for the diagnosis, prognosis and treatment of prostate cancer metastasis
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CA2906394A1 (en) 2013-03-15 2014-09-18 Fundacio Institut De Recerca Biomedica (Irb Barcelona) Method for the prognosis and treatment of cancer metastasis
US20160032399A1 (en) 2013-03-15 2016-02-04 Inbiomotion S.L. Method for the Prognosis and Treatment of Renal Cell Carcinoma Metastasis
MX362041B (es) 2013-10-09 2019-01-07 Fundacio Inst De Recerca Biomedica Irb Barcelona Método para el pronóstico y tratamiento de cáncer metastásico de los huesos originado de cáncer de mama.
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
CA2967224C (en) 2014-12-11 2023-08-22 Inbiomotion S.L. Binding members for human c-maf
DK3458610T3 (da) 2016-05-25 2021-06-07 Inbiomotion Sl Terapeutisk behandling af brystcancer baseret på c-MAF-status
WO2018138356A1 (en) * 2017-01-27 2018-08-02 Genfit Rorgamma modulators and uses thereof
CN108586356B (zh) * 2017-03-16 2021-02-19 杭州科巢生物科技有限公司 瑞博西尼新中间体及其制备瑞博西尼的合成方法
AU2018372762B2 (en) 2017-11-22 2025-08-21 Inbiomotion S.L. Therapeutic treatment of breast cancer based on c-maf status
CN109467536B (zh) * 2018-12-23 2020-06-05 沧州普瑞东方科技有限公司 2-氯/羟基嘧啶-5-羧酸的合成方法
WO2020201572A1 (en) 2019-04-05 2020-10-08 Université De Bretagne Occidentale Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning
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WO2001083460A1 (en) * 2000-04-28 2001-11-08 Tanabe Seiyaku Co., Ltd. Cyclic compounds

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SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201976D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds

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WO2001083460A1 (en) * 2000-04-28 2001-11-08 Tanabe Seiyaku Co., Ltd. Cyclic compounds

Also Published As

Publication number Publication date
MXPA04001930A (es) 2004-06-15
DE60216122T2 (de) 2007-09-06
ES2275946T3 (es) 2007-06-16
KR20040029101A (ko) 2004-04-03
CO5560576A2 (es) 2005-09-30
CN1549717B (zh) 2011-08-17
CA2456127C (en) 2009-10-20
JP2005505550A (ja) 2005-02-24
WO2003020278A1 (en) 2003-03-13
DE60216122D1 (de) 2006-12-28
AR036375A1 (es) 2004-09-01
PL208280B1 (pl) 2011-04-29
PT1423121E (pt) 2007-02-28
BR0212141A (pt) 2004-08-24
KR100629834B1 (ko) 2006-09-29
US7112589B2 (en) 2006-09-26
NZ531287A (en) 2005-12-23
US20060074092A1 (en) 2006-04-06
PE20030772A1 (es) 2003-10-02
ATE345136T1 (de) 2006-12-15
HUP0401431A2 (hu) 2004-10-28
IL160295A0 (en) 2004-07-25
PL367821A1 (en) 2005-03-07
CA2456127A1 (en) 2003-03-13
EP1423121A1 (en) 2004-06-02
RU2326119C2 (ru) 2008-06-10
RU2004109812A (ru) 2005-10-20
JP4131701B2 (ja) 2008-08-13
US20040249153A1 (en) 2004-12-09
HUP0401431A3 (en) 2004-11-29
EP1423121B1 (en) 2006-11-15
CN1549717A (zh) 2004-11-24

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