BRPI0614566A2 - derivados de 2-oxo azepan subtituìdos por fluoro - Google Patents

derivados de 2-oxo azepan subtituìdos por fluoro

Info

Publication number
BRPI0614566A2
BRPI0614566A2 BRPI0614566-3A BRPI0614566A BRPI0614566A2 BR PI0614566 A2 BRPI0614566 A2 BR PI0614566A2 BR PI0614566 A BRPI0614566 A BR PI0614566A BR PI0614566 A2 BRPI0614566 A2 BR PI0614566A2
Authority
BR
Brazil
Prior art keywords
substituted
fluoro
halogen
lower alkyl
heteroaryl
Prior art date
Application number
BRPI0614566-3A
Other languages
English (en)
Inventor
Alexandre Flohr
Guido Galley
Roland Jakob-Roetne
Eric Argirios Kitas
Wolfgang Wostl
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BRPI0614566A2 publication Critical patent/BRPI0614566A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

DERIVADOS DE 2-OXO AZEPAN SUBTITUìDOS POR FLUORO. Trata-se de compostos da fórmula geral (I), onde R^ 1^ é alquila inferior substituida por halogênio, ou é arila ou heteroarila, não-substituida ou substituida por halogênio; R^ 2^ é heterocicloalquila, arila ou heteroarila, que são não-substituidas ou substituidas por um ou mais substituintes, selecionados do grupo que consiste em halogênio, alquilóxi interior, alquila inferior substituida por halogênio, O-alquila inferior substituida por halogênio ou são substituidas por C(O)NR"2, (CR2 22)2 m2C(O)R', heteroarila ou S(O)2 22-alquila inferior; R^ 3^/R^ 3'^, R^ 4^/R^ 4^ e R^ 5^/R^ 5^ são independentemente um do outro hidrogênio ou fluoro, onde pelo menos um entre R^ 4^/R^ 4'^ ou sempre é fluoro; R' é arila ou hidróxi; R" é hidrogênio, cicloalquila ou é heterocicloalquila; R é hidrogênio ou alquila inferior; m é 0,1, 2 ou 3; e de sais de adição de ácido farmaceuticamente aceitáveis, enantiómeros opticamente puros, racematos ou misturas diastereoméricas destes. Foi verificado que os compostos da fórmula geral (1) são inibidores de y-secretase e os compostos relacionados podem ser úteis no tratamento de doença de Alzheimer ou cânceres comuns que incluem, porém sem caráter limitativo, carcinomas cervicais e carcinomas de mama e malignidades do sistema hematopoiético.
BRPI0614566-3A 2005-08-12 2006-08-02 derivados de 2-oxo azepan subtituìdos por fluoro BRPI0614566A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05107455 2005-08-12
PCT/EP2006/064935 WO2007020190A1 (en) 2005-08-12 2006-08-02 Fluoro substituted 2-oxo azepan derivatives

Publications (1)

Publication Number Publication Date
BRPI0614566A2 true BRPI0614566A2 (pt) 2009-08-04

Family

ID=37102441

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0614566-3A BRPI0614566A2 (pt) 2005-08-12 2006-08-02 derivados de 2-oxo azepan subtituìdos por fluoro

Country Status (19)

Country Link
US (1) US7501406B2 (pt)
EP (1) EP1915345B1 (pt)
JP (1) JP4885958B2 (pt)
KR (1) KR101020397B1 (pt)
CN (1) CN101238106B (pt)
AR (1) AR055370A1 (pt)
AT (1) ATE492536T1 (pt)
AU (1) AU2006281493A1 (pt)
BR (1) BRPI0614566A2 (pt)
CA (1) CA2619223A1 (pt)
DE (1) DE602006019103D1 (pt)
ES (1) ES2355581T3 (pt)
IL (1) IL189026A0 (pt)
MX (1) MX2008001833A (pt)
NO (1) NO20080498L (pt)
RU (1) RU2419611C2 (pt)
TW (1) TWI325421B (pt)
WO (1) WO2007020190A1 (pt)
ZA (1) ZA200800930B (pt)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010509235A (ja) * 2006-11-03 2010-03-25 ノースウェスタン ユニバーシティ 多発性硬化症の治療
FR2913886B1 (fr) 2007-03-22 2012-03-02 Guerbet Sa Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer
GB201009603D0 (en) 2010-06-08 2010-07-21 Cambridge Entpr Ltd Anti-inflammatory agent
WO2012014127A1 (en) 2010-07-30 2012-02-02 Ranbaxy Laboratories Limited 5-lipoxygenase inhibitors
AR097279A1 (es) 2013-08-09 2016-03-02 Actelion Pharmaceuticals Ltd Derivados de benzimidazolil-metil urea como agonistas del receptor de alx
CN117447298A (zh) * 2023-08-29 2024-01-26 上海泰坦科技股份有限公司 一种卤代甲基二氟甲基苯的合成方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2793246B1 (fr) * 1999-05-03 2001-06-29 Adir Nouveaux derives de 1-aza-2-alkyl-6-aryl-cycloalcanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP1268434A1 (en) * 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta protein production
ZA200507806B (en) * 2003-03-24 2007-03-28 Actimis Pharmaceuticals Inc 2-phenoxy- and 2-enysulfomamide derivatives with CCR3 antagonistic acitivity for the treatment of asthma and other inflammatory or immunolgical disorders
EP1680406A1 (en) * 2003-10-29 2006-07-19 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
RU2378258C2 (ru) * 2004-07-13 2010-01-10 Ф. Хоффманн-Ля Рош Аг Производные сульфонамида

Also Published As

Publication number Publication date
CA2619223A1 (en) 2007-02-22
AR055370A1 (es) 2007-08-22
KR101020397B1 (ko) 2011-03-08
CN101238106A (zh) 2008-08-06
IL189026A0 (en) 2008-08-07
CN101238106B (zh) 2011-02-16
WO2007020190A1 (en) 2007-02-22
ES2355581T3 (es) 2011-03-29
KR20080027936A (ko) 2008-03-28
DE602006019103D1 (de) 2011-02-03
ZA200800930B (en) 2009-02-25
ATE492536T1 (de) 2011-01-15
JP2009504600A (ja) 2009-02-05
US7501406B2 (en) 2009-03-10
US20070037789A1 (en) 2007-02-15
RU2419611C2 (ru) 2011-05-27
EP1915345B1 (en) 2010-12-22
EP1915345A1 (en) 2008-04-30
MX2008001833A (es) 2008-04-09
TWI325421B (en) 2010-06-01
NO20080498L (no) 2008-03-07
TW200734308A (en) 2007-09-16
AU2006281493A1 (en) 2007-02-22
JP4885958B2 (ja) 2012-02-29
RU2008103452A (ru) 2009-09-20

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Legal Events

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

Free format text: REFERENTE A 7A ANUI DADE.

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 2214 DE 11/06/2013.