BR112014023384A2 - inibidores de bace de di-hidro-tiazina e di-hidro-oxazina espirocíclicos, e composições e usos dos mesmos - Google Patents

inibidores de bace de di-hidro-tiazina e di-hidro-oxazina espirocíclicos, e composições e usos dos mesmos

Info

Publication number
BR112014023384A2
BR112014023384A2 BR112014023384A BR112014023384A BR112014023384A2 BR 112014023384 A2 BR112014023384 A2 BR 112014023384A2 BR 112014023384 A BR112014023384 A BR 112014023384A BR 112014023384 A BR112014023384 A BR 112014023384A BR 112014023384 A2 BR112014023384 A2 BR 112014023384A2
Authority
BR
Brazil
Prior art keywords
dihydro
compositions
compounds
spirocyclic
thiazine
Prior art date
Application number
BR112014023384A
Other languages
English (en)
Other versions
BR112014023384A8 (pt
Inventor
R Artis Dean
L Sham Hing
K Hom Roy
Yuan Shendong
Bowers Simeon
Xu Ying-Zi
Original Assignee
R Artis Dean
Elan Pharm Inc
L Sham Hing
K Hom Roy
Yuan Shendong
Bowers Simeon
Ying Zi Xu
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 R Artis Dean, Elan Pharm Inc, L Sham Hing, K Hom Roy, Yuan Shendong, Bowers Simeon, Ying Zi Xu filed Critical R Artis Dean
Publication of BR112014023384A2 publication Critical patent/BR112014023384A2/pt
Publication of BR112014023384A8 publication Critical patent/BR112014023384A8/pt

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Classifications

    • 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
    • C07D513/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

Abstract

abstract compounds are provided having a structure according to formula i: i wherein a1, a2, a3, y, r1, r2, r3, r4, r5, r6, m, n and p are defined herein. further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as alzheimer’s disease. tradução do resumo resumo patente de invenção: “inibidores de bace de di-hidro-tiazina e di-hidro-oxazina espirocíclicos, e composições e usos dos mesmos”. os compostos são fornecidos tendo uma estrutura de acordo com a fórmula (i): em que a1, a2, a3, y, r1, r2, r3, r4, r5, r6, m, n e p são definidos aqui. ainda fornecidas são composições farmacêuticas incluindo os compostos fornecidos e métodos de fazer e usar os compostos e composições assim fornecidos, por exemplo, no tratamento e prevenção de vários distúrbios, tais como doença de alzheimer.
BR112014023384A 2012-03-20 2013-03-20 inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos. BR112014023384A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261613377P 2012-03-20 2012-03-20
US201261727248P 2012-11-16 2012-11-16
PCT/US2013/033177 WO2013142613A1 (en) 2012-03-20 2013-03-20 Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof

Publications (2)

Publication Number Publication Date
BR112014023384A2 true BR112014023384A2 (pt) 2017-07-11
BR112014023384A8 BR112014023384A8 (pt) 2018-01-16

Family

ID=49223329

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014023384A BR112014023384A8 (pt) 2012-03-20 2013-03-20 inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos.

Country Status (8)

Country Link
US (4) US9493485B2 (pt)
EP (1) EP2827857A4 (pt)
JP (1) JP2015514073A (pt)
AU (1) AU2013235117A1 (pt)
BR (1) BR112014023384A8 (pt)
CA (1) CA2867851A1 (pt)
HK (1) HK1206597A1 (pt)
WO (1) WO2013142613A1 (pt)

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NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
CA2783958A1 (en) 2009-12-11 2011-06-16 Shionogi & Co., Ltd. Oxazine derivative
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
AU2014223334C1 (en) * 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN105164121A (zh) 2013-03-08 2015-12-16 美国安进公司 作为β分泌酶抑制剂的全氟化环丙基稠合的1,3-噁嗪-2-胺化合物以及其使用方法
EA031132B1 (ru) 2014-02-19 2018-11-30 Х. Лундбекк А/С 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
WO2016001266A1 (en) 2014-07-04 2016-01-07 F. Hoffmann-La Roche Ag Fluoro-[1,3]oxazines as bace1 inhibitors
MX2017001794A (es) 2014-08-08 2017-06-29 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
US10011596B2 (en) 2015-08-12 2018-07-03 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
JP7177773B2 (ja) * 2016-12-15 2022-11-24 アムジエン・インコーポレーテツド β－セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
CN109776295B (zh) * 2019-02-18 2021-10-01 浙江师范大学 一种邻位含二氟亚甲基的芳基碘化合物及制备方法

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US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
WO1996040885A2 (en) 1995-06-07 1996-12-19 Athena Neurosciences, Inc. β-SECRETASE, ANTIBODIES TO β-SECRETASE, AND ASSAYS FOR DETECTING β-SECRETASE INHIBITION
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BRPI0617852A2 (pt) 2005-10-25 2011-08-09 Shionogi & Co compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos
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UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2

Also Published As

Publication number Publication date
CA2867851A1 (en) 2013-09-26
BR112014023384A8 (pt) 2018-01-16
EP2827857A1 (en) 2015-01-28
JP2015514073A (ja) 2015-05-18
US20150087826A1 (en) 2015-03-26
US20160272654A1 (en) 2016-09-22
US20150307518A1 (en) 2015-10-29
AU2013235117A1 (en) 2014-10-16
WO2013142613A1 (en) 2013-09-26
US9493485B2 (en) 2016-11-15
EP2827857A4 (en) 2016-03-30
US20150087825A1 (en) 2015-03-26
HK1206597A1 (en) 2016-01-15

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Legal Events

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B07D Technical examination (opinion) related to article 229 of industrial property law
B06F Objections, documents and/or translations needed after an examination request according art. 34 industrial property law
B07E Notice of approval relating to section 229 industrial property law

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06U Preliminary requirement: requests with searches performed by other patent offices: suspension of the patent application procedure
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements