BRPI0416276A - lactames macrocìclicos e uso farmacêutico dos mesmos - Google Patents

lactames macrocìclicos e uso farmacêutico dos mesmos

Info

Publication number
BRPI0416276A
BRPI0416276A BRPI0416276-5A BRPI0416276A BRPI0416276A BR PI0416276 A BRPI0416276 A BR PI0416276A BR PI0416276 A BRPI0416276 A BR PI0416276A BR PI0416276 A BRPI0416276 A BR PI0416276A
Authority
BR
Brazil
Prior art keywords
macrocyclic
lactames
pharmaceutical use
pharmaceutical
ring
Prior art date
Application number
BRPI0416276-5A
Other languages
English (en)
Inventor
Yves Auberson
Claudia Betschart
Ralf Glatthar
Kurt Laumen
Rainer Machauer
Marina Tintelnot-Blomley
Thomas J Troxler
Siem Jacob Veenstra
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of BRPI0416276A publication Critical patent/BRPI0416276A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/02—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

"LACTAMES MACROCìCLICOS E USO FARMACêUTICO DOS MESMOS". A presente invenção se refere a novos compostos macrocíclicos da fórmula (I) em que R~ 1~, R~ 2~, R~ 3~, U, W, X, Y, Z e n são conforme definido na especificação, o número de átomos no anel incluído no anel macrocíclico sendo 14, 15, 16 ou 17, na forma de base livre ou na forma de sal de adição de ácido, a seu preparo, a seu uso como produtos farmacêuticos e a composições farmacêuticas compreendendo os mesmos.
BRPI0416276-5A 2003-11-05 2004-11-04 lactames macrocìclicos e uso farmacêutico dos mesmos BRPI0416276A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0325830.8A GB0325830D0 (en) 2003-11-05 2003-11-05 Organic compounds
PCT/EP2004/012497 WO2005049585A1 (en) 2003-11-05 2004-11-04 Macrocyclic lactams and pharmaceutical use thereof

Publications (1)

Publication Number Publication Date
BRPI0416276A true BRPI0416276A (pt) 2007-01-23

Family

ID=29725994

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0416276-5A BRPI0416276A (pt) 2003-11-05 2004-11-04 lactames macrocìclicos e uso farmacêutico dos mesmos

Country Status (15)

Country Link
US (2) US7612055B2 (pt)
EP (1) EP1682521A1 (pt)
JP (1) JP4628366B2 (pt)
KR (1) KR20060110289A (pt)
CN (1) CN1902182A (pt)
AR (1) AR046321A1 (pt)
AU (1) AU2004291276B2 (pt)
BR (1) BRPI0416276A (pt)
CA (1) CA2544751A1 (pt)
GB (1) GB0325830D0 (pt)
MX (1) MXPA06005032A (pt)
PE (1) PE20051006A1 (pt)
RU (1) RU2006119504A (pt)
TW (1) TW200530203A (pt)
WO (1) WO2005049585A1 (pt)

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* Cited by examiner, † Cited by third party
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DE60315664D1 (de) * 2002-06-20 2007-09-27 Pharmacia & Upjohn Co Llc Verfahren zur herstellung von 5-(1,3-oxazol-2-yl)benzoesäurederivaten
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
US8383637B2 (en) 2004-08-06 2013-02-26 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8426429B2 (en) 2004-08-06 2013-04-23 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
GB0500683D0 (en) 2005-01-13 2005-02-23 Novartis Ag Organic compounds
KR20070102514A (ko) * 2005-01-13 2007-10-18 노파르티스 아게 Ｂａｃｅ 억제제로서 유용한 마크로시클릭 화합물
US7338974B2 (en) 2005-08-12 2008-03-04 Bristol-Myers Squibb Company Macrocyclic diaminopropanes as beta-secretase inhibitors
NZ566551A (en) * 2005-08-19 2011-09-30 Emisphere Tech Inc Cyclopropyl compounds and compositions for delivering active agents
ATE502036T1 (de) 2005-10-25 2011-04-15 Janssen Pharmaceutica Nv Als inhibitoren von beta-sekretase (bace) geeignete 2-amino-3,4-dihydropyridoä3,4- düpyrimidinderivate
GB0526614D0 (en) 2005-12-30 2006-02-08 Novartis Ag Organic compounds
WO2007092839A2 (en) * 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
WO2007092846A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US7868022B2 (en) 2006-02-06 2011-01-11 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
MX2009000768A (es) * 2006-07-20 2009-01-28 Novartis Ag Lactamas macrociclicas.
JP2009544599A (ja) * 2006-07-20 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｂａｃｅ阻害剤として有用な大環状化合物
US7678784B2 (en) 2006-11-20 2010-03-16 Bristol-Myers Squibb Company Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors
US7772221B2 (en) 2007-02-09 2010-08-10 Bristol-Meyers Squibb Company Diaminopropane derived macrocycles as inhibitors of β amyloid production
EP2136624A4 (en) * 2007-03-21 2011-11-30 Emisphere Tech Inc DISPENSER FOR ALLYLOXY- AND ALKYLOXYBENZOIC ACID
US7732434B2 (en) 2007-04-20 2010-06-08 Bristol-Myers Squibb Company Macrocyclic acyl guanidines as beta-secretase inhibitors
WO2008135488A1 (en) * 2007-05-04 2008-11-13 Medivir Ab Aspartyl protease inhibitors
NZ586831A (en) 2008-01-28 2012-02-24 Janssen Pharmaceutica Nv 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
EP2240472B1 (en) 2008-01-29 2012-11-21 Janssen Pharmaceutica NV 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
WO2010058577A1 (ja) * 2008-11-20 2010-05-27 株式会社カネカ 不飽和アミノカルボン酸誘導体の製造方法
SG192592A1 (en) 2011-02-08 2013-09-30 Merck Patent Gmbh Amino statin derivatives for the treatment of arthrosis
AU2012230503B2 (en) 2011-03-18 2016-07-07 Bayer Intellectual Property Gmbh N-(3-carbamoylphenyl)-1H-pyrazole-5-carboxamide derivatives and the use thereof for controlling animal pests
CN104507957B (zh) 2012-07-24 2018-12-25 默克专利股份有限公司 用于治疗关节病的羟基他汀衍生物
US9663475B2 (en) 2013-02-25 2017-05-30 Merck Patent Gmbh 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors
ES2759060T3 (es) 2013-08-06 2020-05-07 Merck Patent Gmbh Administración intraarticular de pepstatina para la artrosis
US11834515B2 (en) 2017-10-11 2023-12-05 Cornell University Macrocyclic compounds as proteasome inhibitors
JP7444170B2 (ja) * 2019-09-02 2024-03-06 株式会社レゾナック イオン性化合物、有機エレクトロニクス材料、有機層、有機エレクトロニクス素子、有機エレクトロルミネセンス素子、表示素子、照明装置、及び有機エレクトロニクス素子の製造方法
CN116199702B (zh) * 2021-12-01 2026-01-09 上海交通大学医学院附属仁济医院 一种大环内酰胺类化合物、其制备方法及应用
CN116082181B (zh) * 2022-12-12 2025-03-04 爱斯特（成都）生物制药股份有限公司 一种制备3-氨基-5-乙氧基-苯甲酸的方法

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DK0535192T3 (da) * 1991-04-17 1996-08-05 Hoffmann La Roche Hidtil ukendte DNA-gyraseinhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske præparater indeholdende dem
TW343965B (en) * 1994-03-30 1998-11-01 Hoffmann La Roche Novel mono- and bicyclic DNA gyrase inhibitors
WO2002100399A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
EP1404671B1 (en) * 2001-06-12 2006-04-12 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
KR20070102514A (ko) * 2005-01-13 2007-10-18 노파르티스 아게 Ｂａｃｅ 억제제로서 유용한 마크로시클릭 화합물
GB0526614D0 (en) * 2005-12-30 2006-02-08 Novartis Ag Organic compounds
MX2009000768A (es) * 2006-07-20 2009-01-28 Novartis Ag Lactamas macrociclicas.
JP2009544599A (ja) * 2006-07-20 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｂａｃｅ阻害剤として有用な大環状化合物

Also Published As

Publication number Publication date
US20070072792A1 (en) 2007-03-29
AU2004291276B2 (en) 2009-03-12
MXPA06005032A (es) 2006-07-06
CA2544751A1 (en) 2005-06-02
TW200530203A (en) 2005-09-16
EP1682521A1 (en) 2006-07-26
JP2007510002A (ja) 2007-04-19
US20100022500A1 (en) 2010-01-28
AU2004291276A1 (en) 2005-06-02
KR20060110289A (ko) 2006-10-24
PE20051006A1 (es) 2005-12-28
WO2005049585A1 (en) 2005-06-02
US7612055B2 (en) 2009-11-03
CN1902182A (zh) 2007-01-24
JP4628366B2 (ja) 2011-02-09
GB0325830D0 (en) 2003-12-10
RU2006119504A (ru) 2007-12-27
AR046321A1 (es) 2005-11-30

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application fees: application dismissed [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A 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: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012.