BRPI0518054A - composto ou um sal, estereoisÈmero ou derivado de n-óxido farmaceuticamente aceitáveis do mesmo, composição farmacêutica, e, uso de um composto - Google Patents

composto ou um sal, estereoisÈmero ou derivado de n-óxido farmaceuticamente aceitáveis do mesmo, composição farmacêutica, e, uso de um composto

Info

Publication number
BRPI0518054A
BRPI0518054A BRPI0518054-6A BRPI0518054A BRPI0518054A BR PI0518054 A BRPI0518054 A BR PI0518054A BR PI0518054 A BRPI0518054 A BR PI0518054A BR PI0518054 A BRPI0518054 A BR PI0518054A
Authority
BR
Brazil
Prior art keywords
compound
stereoisomer
derivative
pharmaceutically acceptable
pharmaceutical composition
Prior art date
Application number
BRPI0518054-6A
Other languages
English (en)
Inventor
Jacques Yves Gauthier
Chun Sing Li
Christophe Mellon
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 BRPI0518054A publication Critical patent/BRPI0518054A/pt

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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (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

COMPOSTO OU UM SAL, ESTEREOISÈMERO OU DERIVADO DE NóXIDO FARMACEUTICAMENTE ACEITáVEIS DO MESMO, COMPOSIçãO FARMACêUTICA, E, USO DE UM COMPOSTO. Esta invenção diz respeito a uma nova classe de compostos, esquematizados abaixo, em queR˜,R,R,R¬4¬,R¬5¬,R¬6¬,R¬7¬,Densao nesta definidos, que são inibidores de proteína cisteina, incluindo, mas não limitando a, inibidores de catepsinas K, L, S e B. Estes compostos são úteis para tratar doenças em que a inibição da reabsorção óssea é indicada, tal como a osteoporose.
BRPI0518054-6A 2004-11-23 2005-11-18 composto ou um sal, estereoisÈmero ou derivado de n-óxido farmaceuticamente aceitáveis do mesmo, composição farmacêutica, e, uso de um composto BRPI0518054A (pt)

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 (1)

Publication Number Publication Date
BRPI0518054A true BRPI0518054A (pt) 2008-10-28

Family

ID=36497694

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0518054-6A BRPI0518054A (pt) 2004-11-23 2005-11-18 composto ou um sal, estereoisÈmero ou derivado de n-óxido farmaceuticamente aceitáveis do mesmo, composição farmacêutica, e, uso de um composto

Country Status (24)

Country Link
US (2) US7407959B2 (pt)
EP (1) EP1817276B1 (pt)
JP (1) JP5055488B2 (pt)
KR (1) KR20070085435A (pt)
CN (2) CN102391151A (pt)
AR (1) AR055283A1 (pt)
AU (1) AU2005309267B2 (pt)
BR (1) BRPI0518054A (pt)
CA (1) CA2589085C (pt)
DK (1) DK1817276T3 (pt)
ES (1) ES2394618T3 (pt)
IL (1) IL183308A (pt)
MX (1) MX2007006136A (pt)
MY (1) MY137717A (pt)
NO (1) NO339125B1 (pt)
NZ (1) NZ554872A (pt)
PE (1) PE20061054A1 (pt)
PL (1) PL1817276T3 (pt)
PT (1) PT1817276E (pt)
RU (1) RU2399613C2 (pt)
SI (1) SI1817276T1 (pt)
TW (1) TWI353244B (pt)
WO (1) WO2006056047A1 (pt)
ZA (1) ZA200703530B (pt)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003219953B8 (en) * 2002-03-05 2008-09-25 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
JP4991295B2 (ja) * 2003-09-18 2012-08-01 ビロベイ，インコーポレイティド システイン・プロテアーゼ阻害剤としてのハロアルキルを含む化合物
US8013186B2 (en) * 2004-12-01 2011-09-06 Virobay, Inc. Haloalkyl containing compounds as cysteine protease inhibitors
WO2006060810A1 (en) * 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
WO2006076796A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and obesity
EP2783687A1 (en) * 2005-03-02 2014-10-01 Merck Sharp & Dohme Corp. Composition for inhibition of cathepsin K
BRPI0609695A2 (pt) 2005-03-21 2011-10-18 Applera Corp composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, método para tratar uma doença e uma paciente sofrendo uma terapia
CA2602112A1 (en) * 2005-03-22 2006-09-28 Celera Genomics Sulfonyl containing compounds as cysteine protease inhibitors
EP2077869B1 (en) * 2006-08-28 2015-02-25 Akademia Medyczna Im. Piastow Slaskich We Wroclaw iu A system for the extra-corporeal purification of blood of pathogenic enzymes
US20100048717A1 (en) * 2006-09-25 2010-02-25 MERCK FROSST CANADA LTD, Merk & Co., Inc. Cathepsin b inhibitors
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
WO2008042968A2 (en) * 2006-10-04 2008-04-10 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
WO2010056877A2 (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
US10758559B1 (en) * 2017-09-01 2020-09-01 University Of Wyoming Targeting cathepsin K to facilitate wound healing
US11766467B2 (en) 2017-09-01 2023-09-26 University Of Wyoming Methods of treating wounds using cathepsin K inhibitors
CA3107899A1 (en) * 2018-08-02 2020-02-06 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
AU2019312842A1 (en) 2018-08-02 2021-02-04 Intervet International B.V. Process to make a selective cathepsin cysteine protease inhibitor
EP3946332A1 (en) 2019-04-05 2022-02-09 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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL135508A (en) 1997-11-05 2006-12-10 Novartis Ag Nitriles of dipeptide
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
JP4343690B2 (ja) * 2001-11-13 2009-10-14 メルク フロスト カナダ リミテツド プロテアーゼ阻害薬としてのシアノアルキルアミノ誘導体
AU2003219953B8 (en) * 2002-03-05 2008-09-25 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
WO2004052921A1 (en) * 2002-12-05 2004-06-24 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
JP4991295B2 (ja) * 2003-09-18 2012-08-01 ビロベイ，インコーポレイティド システイン・プロテアーゼ阻害剤としてのハロアルキルを含む化合物
EP2783687A1 (en) * 2005-03-02 2014-10-01 Merck Sharp & Dohme Corp. Composition for inhibition of cathepsin K

Also Published As

Publication number Publication date
CN101061093A (zh) 2007-10-24
IL183308A0 (en) 2007-09-20
SI1817276T1 (sl) 2012-12-31
KR20070085435A (ko) 2007-08-27
CN102391151A (zh) 2012-03-28
CA2589085A1 (en) 2006-06-01
US20070293578A1 (en) 2007-12-20
DK1817276T3 (da) 2012-11-19
PT1817276E (pt) 2012-10-25
NO20073222L (no) 2007-08-03
TW200631576A (en) 2006-09-16
AU2005309267B2 (en) 2011-05-12
US20060111440A1 (en) 2006-05-25
EP1817276A1 (en) 2007-08-15
AR055283A1 (es) 2007-08-15
JP2008520590A (ja) 2008-06-19
CA2589085C (en) 2014-04-29
EP1817276A4 (en) 2009-12-09
ES2394618T3 (es) 2013-02-04
WO2006056047A9 (en) 2007-06-21
NZ554872A (en) 2010-12-24
AU2005309267A1 (en) 2006-06-01
MX2007006136A (es) 2007-07-19
PL1817276T3 (pl) 2012-12-31
EP1817276B1 (en) 2012-08-08
RU2007123611A (ru) 2008-12-27
US7407959B2 (en) 2008-08-05
ZA200703530B (en) 2008-01-08
RU2399613C2 (ru) 2010-09-20
PE20061054A1 (es) 2006-10-20
MY137717A (en) 2009-03-31
IL183308A (en) 2013-05-30
JP5055488B2 (ja) 2012-10-24
WO2006056047A1 (en) 2006-06-01
NO339125B1 (no) 2016-11-14
TWI353244B (en) 2011-12-01

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 10A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2343 DE 01-12-2015 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.