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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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)

Families Citing this family (33)

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WO2004000821A1 (en) * 2002-06-20 2003-12-31 Pharmacia & Upjohn Company Process for preparing 5-(1, 3-oxazol-2-yl) benzoic acid derivatives
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
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)
BRPI0606636A2 (pt) * 2005-01-13 2009-07-07 Novartis Ag compostos macrocìclicos úteis como inibidores de bace
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
WO2007021793A1 (en) 2005-08-12 2007-02-22 Bristol-Myers Squibb Company Macrocyclic diaminopropanes as beta-secretase inhibitors
WO2007022532A2 (en) * 2005-08-19 2007-02-22 Emisphere Technologies, Inc. Cyclopropyl compounds and compositions for delivering active agents
WO2007050612A1 (en) 2005-10-25 2007-05-03 Janssen Pharmaceutica N.V. 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace)
GB0526614D0 (en) 2005-12-30 2006-02-08 Novartis Ag Organic compounds
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US7932261B2 (en) 2006-02-06 2011-04-26 Janssen Pharmaceutica Nv Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
BRPI0715440A2 (pt) * 2006-07-20 2013-07-23 Novartis Ag compostos macrocÍclicos éteis como inibidores de bace
CA2656869A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams
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
JP5526018B2 (ja) 2007-03-21 2014-06-18 エミスフェアー・テクノロジーズ・インク アリルオキシおよびアルキルオキシ安息香酸送達薬剤
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
CA2713998A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of.beta.-secretase (bace)
CN101970429B (zh) 2008-01-29 2013-05-29 詹森药业有限公司 可用作β-分泌酶(BACE)抑制剂的2-氨基喹啉衍生物
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
ES2649964T3 (es) 2011-02-08 2018-01-16 Merck Patent Gmbh Derivados de aminoestatina para el tratamiento de la artrosis
MX350121B (es) 2011-03-18 2017-08-28 Bayer Ip Gmbh Derivados de n-(3-carbamoilfenil)-1h-pirazol-5-carboxamida y el uso de los mismos para el control de plagas de animales.
ES2673873T3 (es) 2012-07-24 2018-06-26 Merck Patent Gmbh Derivados de hidroxiestatina para el tratamiento de la artrosis
WO2014127881A1 (de) 2013-02-25 2014-08-28 Merck Patent Gmbh 2-amino-3,4-dihydrc-chinazolin derivate und ihre verwendung als cathepsin d inhibitoren
ES2759060T3 (es) 2013-08-06 2020-05-07 Merck Patent Gmbh Administración intraarticular de pepstatina para la artrosis
WO2019075259A1 (en) * 2017-10-11 2019-04-18 Cornell University MACROCYCLIC COMPOUNDS AS PROTEASE INHIBITORS
WO2021044478A1 (ja) * 2019-09-02 2021-03-11 昭和電工マテリアルズ株式会社 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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WO1992018490A1 (en) * 1991-04-17 1992-10-29 F. Hoffmann-La Roche Ag Novel dna gyrase inhibitors, process for their manufacture and pharmaceutical preparations containing same
TW343965B (en) * 1994-03-30 1998-11-01 Hoffmann La Roche Novel mono- and bicyclic DNA gyrase inhibitors
BR0210391A (pt) * 2001-06-12 2004-06-15 Elan Pharm Inc Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto
ATE323084T1 (de) * 2001-06-12 2006-04-15 Elan Pharm Inc Für die behandlung von alzheimer krankheit geeignete makrocyclen
GB0325830D0 (en) * 2003-11-05 2003-12-10 Novartis Ag Organic compounds
BRPI0606636A2 (pt) * 2005-01-13 2009-07-07 Novartis Ag compostos macrocìclicos úteis como inibidores de bace
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
GB0526614D0 (en) * 2005-12-30 2006-02-08 Novartis Ag Organic compounds
BRPI0715440A2 (pt) * 2006-07-20 2013-07-23 Novartis Ag compostos macrocÍclicos éteis como inibidores de bace
CA2656869A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams

Also Published As

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

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Legal Events

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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.