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NO20073222L - Kathepsincysteinproteaseinhibitorer - Google Patents

Kathepsincysteinproteaseinhibitorer

Info

Publication number
NO20073222L
NO20073222L NO20073222A NO20073222A NO20073222L NO 20073222 L NO20073222 L NO 20073222L NO 20073222 A NO20073222 A NO 20073222A NO 20073222 A NO20073222 A NO 20073222A NO 20073222 L NO20073222 L NO 20073222L
Authority
NO
Norway
Prior art keywords
kathepsincysteinproteaseinhibitorer
compounds
osteoporosis
inhibition
useful
Prior art date
Application number
NO20073222A
Other languages
English (en)
Other versions
NO339125B1 (no
Inventor
Jacques Yves Gauthier
Christphe Mellon
Chun Sing Li
Original Assignee
Merck Frosst Canada Ltd
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 Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of NO20073222L publication Critical patent/NO20073222L/no
Publication of NO339125B1 publication Critical patent/NO339125B1/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/45—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C255/46—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/275—Nitriles; Isonitriles
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Foreliggende oppfinnelse gjelder en ny klasse av forbindelser som er vist skjematisk nedenfor, hvori R1, R2, R3, R4, R5, R6, R7, D og n er definert heri, som er cysteinproteaseinhibitorer, innbefattet, men ikke begrenset til, inhibitorer av kathepsinene K, L, S og B. Disse forbindelsene er anvendbare for behandling av sykdommer i hvilke inhibering av benresorpsjon er indikert, f.eks. osteoporose.
NO20073222A 2004-11-23 2007-06-22 Forbindelser som er kathepsincysteinproteaseinhibitorer, et farmasøytisk akseptabelt salt, en stereoisomer eller et N-oksidderivat derav, et farmasøytisk preparat eller en kombinasjon derav, samt anvendelse derav for fremstilling av et medikament. NO339125B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63040504P 2004-11-23 2004-11-23
PCT/CA2005/001764 WO2006056047A1 (en) 2004-11-23 2005-11-18 Cathepsin cysteine protease inhibitors

Publications (2)

Publication Number Publication Date
NO20073222L true NO20073222L (no) 2007-08-03
NO339125B1 NO339125B1 (no) 2016-11-14

Family

ID=36497694

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20073222A NO339125B1 (no) 2004-11-23 2007-06-22 Forbindelser som er kathepsincysteinproteaseinhibitorer, et farmasøytisk akseptabelt salt, en stereoisomer eller et N-oksidderivat derav, et farmasøytisk preparat eller en kombinasjon derav, samt anvendelse derav for fremstilling av et medikament.

Country Status (24)

Country Link
US (2) US20070293578A1 (no)
EP (1) EP1817276B1 (no)
JP (1) JP5055488B2 (no)
KR (1) KR20070085435A (no)
CN (2) CN101061093A (no)
AR (1) AR055283A1 (no)
AU (1) AU2005309267B2 (no)
BR (1) BRPI0518054A (no)
CA (1) CA2589085C (no)
DK (1) DK1817276T3 (no)
ES (1) ES2394618T3 (no)
IL (1) IL183308A (no)
MX (1) MX2007006136A (no)
MY (1) MY137717A (no)
NO (1) NO339125B1 (no)
NZ (1) NZ554872A (no)
PE (1) PE20061054A1 (no)
PL (1) PL1817276T3 (no)
PT (1) PT1817276E (no)
RU (1) RU2399613C2 (no)
SI (1) SI1817276T1 (no)
TW (1) TWI353244B (no)
WO (1) WO2006056047A1 (no)
ZA (1) ZA200703530B (no)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1482924B1 (en) * 2002-03-05 2008-05-21 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
EA011855B1 (ru) * 2003-09-18 2009-06-30 Вайробей, Инк. Соединения, содержащие галоидалкил, как ингибиторы цистеиновых протеаз
JP4988589B2 (ja) * 2004-12-01 2012-08-01 ビロベイ，インコーポレイティド システインプロテアーゼインヒビターとしてのハロアルキル含有化合物
WO2006060810A1 (en) * 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
EP1841419A4 (en) * 2005-01-19 2009-02-25 Merck Frosst Canada Ltd INHIBITORS OF CATHEPSIN K AND OBESITY
US8722734B2 (en) * 2005-03-02 2014-05-13 Merck Sharp & Dohme Corp. Composition for inhibition of cathepsin K
EA201201550A1 (ru) * 2005-03-21 2013-08-30 Вайробей, Инк. Производные альфа-кетоамидов в качестве ингибиторов цистеинпротеаз
JP5215167B2 (ja) * 2005-03-22 2013-06-19 ビロベイ，インコーポレイティド システインプロテアーゼ阻害剤としてのスルホニル基含有化合物
US20100012588A1 (en) * 2006-08-28 2010-01-21 Maciej Siewinski system and method for the extra-corporeal purification of blood of pathogenic enzymes
WO2008037072A1 (en) 2006-09-25 2008-04-03 Merck Frosst Canada Ltd. Cathepsin b inhibitors
US7893112B2 (en) * 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
NZ576105A (en) * 2006-10-04 2012-01-12 Virobay Inc Di-fluoro containing compounds as cysteine protease inhibitors
WO2009065098A1 (en) * 2007-11-16 2009-05-22 Velcura Therapeutics, Inc. Use of cathepsin k antagonists in the treatment of bone cancer
CA2743749A1 (en) * 2008-11-13 2010-05-20 Virobay, Inc. Haloalkyl containing compounds as cysteine protease inhibitors
US8324417B2 (en) * 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US9586928B2 (en) 2011-05-16 2017-03-07 The Scripps Research Institute Modulators of the nuclear hormone receptor ROR
CN106916091B (zh) * 2015-12-24 2020-10-09 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
US11766467B2 (en) 2017-09-01 2023-09-26 University Of Wyoming Methods of treating wounds using cathepsin K inhibitors
US10758559B1 (en) * 2017-09-01 2020-09-01 University Of Wyoming Targeting cathepsin K to facilitate wound healing
CN112513008A (zh) 2018-08-02 2021-03-16 英特维特国际股份有限公司 选择性组织蛋白酶半胱氨酸蛋白酶抑制剂的制备方法
EP3830075A1 (en) 2018-08-02 2021-06-09 Intervet International B.V. Crystalline forms of n1-(1-cyanocycloproply)-n2-((1s)-1-{4'-[(1r-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl}-2,2,2-trifluoroethyl)-4-fluoro-l-leucinamide
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
CN112438972B (zh) * 2019-08-29 2021-07-30 沈阳药科大学 组织蛋白酶抑制剂的医药用途
CN113462728B (zh) * 2021-07-09 2024-06-07 浙江工业大学 一种利用土星轮头酵母制备(r)-1-(4-溴苯基)-2,2,2-三氟乙醇的方法
CN116462570A (zh) * 2023-03-14 2023-07-21 昆明理工大学 一种α-二氟甲基苯乙烯衍生物及其制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0004400A3 (en) * 1997-11-05 2002-10-28 Novartis Ag Dipeptide nitriles, process for their preparation, pharmaceutical compositions comprising thereof and their use
EP1372655B1 (en) * 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US7302587B2 (en) * 2001-06-08 2007-11-27 Matra Transport International Secure computer system
DE60225316T2 (de) * 2001-11-13 2009-02-26 AXYS Pharmaceuticals, Inc., South San Francisco Cyanoalkylamino-derivate als protease-hemmer
EP1482924B1 (en) * 2002-03-05 2008-05-21 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
WO2004052921A1 (en) * 2002-12-05 2004-06-24 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
EA011855B1 (ru) * 2003-09-18 2009-06-30 Вайробей, Инк. Соединения, содержащие галоидалкил, как ингибиторы цистеиновых протеаз
US8722734B2 (en) * 2005-03-02 2014-05-13 Merck Sharp & Dohme Corp. Composition for inhibition of cathepsin K

Also Published As

Publication number Publication date
AU2005309267B2 (en) 2011-05-12
PT1817276E (pt) 2012-10-25
TW200631576A (en) 2006-09-16
WO2006056047A1 (en) 2006-06-01
KR20070085435A (ko) 2007-08-27
TWI353244B (en) 2011-12-01
AR055283A1 (es) 2007-08-15
MX2007006136A (es) 2007-07-19
PL1817276T3 (pl) 2012-12-31
US7407959B2 (en) 2008-08-05
CA2589085A1 (en) 2006-06-01
CA2589085C (en) 2014-04-29
WO2006056047A9 (en) 2007-06-21
ES2394618T3 (es) 2013-02-04
RU2007123611A (ru) 2008-12-27
EP1817276B1 (en) 2012-08-08
AU2005309267A1 (en) 2006-06-01
CN102391151A (zh) 2012-03-28
EP1817276A1 (en) 2007-08-15
RU2399613C2 (ru) 2010-09-20
EP1817276A4 (en) 2009-12-09
US20070293578A1 (en) 2007-12-20
IL183308A0 (en) 2007-09-20
PE20061054A1 (es) 2006-10-20
MY137717A (en) 2009-03-31
CN101061093A (zh) 2007-10-24
IL183308A (en) 2013-05-30
ZA200703530B (en) 2008-01-08
SI1817276T1 (sl) 2012-12-31
NZ554872A (en) 2010-12-24
BRPI0518054A (pt) 2008-10-28
JP2008520590A (ja) 2008-06-19
JP5055488B2 (ja) 2012-10-24
DK1817276T3 (da) 2012-11-19
NO339125B1 (no) 2016-11-14
US20060111440A1 (en) 2006-05-25

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