BR112014023384A8 - inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos. - Google Patents
inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos.Info
- Publication number
- BR112014023384A8 BR112014023384A8 BR112014023384A BR112014023384A BR112014023384A8 BR 112014023384 A8 BR112014023384 A8 BR 112014023384A8 BR 112014023384 A BR112014023384 A BR 112014023384A BR 112014023384 A BR112014023384 A BR 112014023384A BR 112014023384 A8 BR112014023384 A8 BR 112014023384A8
- Authority
- BR
- Brazil
- Prior art keywords
- dihydro
- compositions
- compounds
- spirocyclic
- thiazine
- Prior art date
Links
Classifications
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- 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
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- 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.
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 BR112014023384A2 (pt) | 2017-07-11 |
BR112014023384A8 true 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) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
EP2511268B2 (en) | 2009-12-11 | 2021-02-17 | Shionogi & Co., Ltd. | Oxazine derivative |
US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
JP6389830B2 (ja) * | 2013-03-01 | 2018-09-12 | アムジエン・インコーポレーテツド | ベータ−セクレターゼ阻害剤としてのパーフルオロ化5,6−ジヒドロ−4h−1,3−オキサジン−2−アミン化合物および使用方法 |
US9085576B2 (en) | 2013-03-08 | 2015-07-21 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
CN106029639B (zh) | 2014-02-19 | 2019-01-08 | H.隆德贝克有限公司 | 治疗阿尔茨海默病的bace1抑制剂的2-氨基-3,5,5-三氟-3,4,5,6-四氢吡啶 |
WO2016001266A1 (en) | 2014-07-04 | 2016-01-07 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
WO2016022724A1 (en) | 2014-08-08 | 2016-02-11 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
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 |
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 |
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 |
US20180244645A1 (en) | 2015-08-12 | 2018-08-30 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
WO2018112086A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
MX2019007104A (es) | 2016-12-15 | 2019-11-05 | Amgen Inc | Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. |
CA3047288A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
MA52722A (fr) * | 2016-12-15 | 2021-04-14 | Amgen Inc | Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
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 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5744346A (en) | 1995-06-07 | 1998-04-28 | Athena Neurosciences, Inc. | β-secretase |
JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
EP1937638A1 (en) | 2005-10-12 | 2008-07-02 | Elan Pharmaceuticals Inc. | Methods of treating amyloidosis using aryl-cyclopropyl derivative aspartyl protease inhibitors |
KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
US7745484B2 (en) | 2005-11-21 | 2010-06-29 | Amgen Inc. | Beta-secretase modulators and methods of use |
JP5274258B2 (ja) * | 2005-11-21 | 2013-08-28 | アムジエン・インコーポレーテツド | β−セクレターゼ調節物質及び使用方法 |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
EP2324032B1 (en) * | 2008-08-19 | 2014-10-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
US7964594B1 (en) * | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
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 |
-
2013
- 2013-03-20 WO PCT/US2013/033177 patent/WO2013142613A1/en active Application Filing
- 2013-03-20 EP EP13764741.8A patent/EP2827857A4/en not_active Withdrawn
- 2013-03-20 US US14/386,722 patent/US9493485B2/en not_active Expired - Fee Related
- 2013-03-20 BR BR112014023384A patent/BR112014023384A8/pt not_active Application Discontinuation
- 2013-03-20 CA CA2867851A patent/CA2867851A1/en not_active Abandoned
- 2013-03-20 JP JP2015501888A patent/JP2015514073A/ja active Pending
- 2013-03-20 AU AU2013235117A patent/AU2013235117A1/en not_active Abandoned
-
2014
- 2014-12-01 US US14/556,895 patent/US20150087825A1/en not_active Abandoned
- 2014-12-01 US US14/556,914 patent/US20150087826A1/en not_active Abandoned
-
2015
- 2015-07-23 HK HK15107058.7A patent/HK1206597A1/xx unknown
-
2016
- 2016-06-01 US US15/169,978 patent/US20160272654A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US20150307518A1 (en) | 2015-10-29 |
US20150087826A1 (en) | 2015-03-26 |
BR112014023384A2 (pt) | 2017-07-11 |
HK1206597A1 (en) | 2016-01-15 |
JP2015514073A (ja) | 2015-05-18 |
WO2013142613A1 (en) | 2013-09-26 |
EP2827857A4 (en) | 2016-03-30 |
US20150087825A1 (en) | 2015-03-26 |
CA2867851A1 (en) | 2013-09-26 |
AU2013235117A1 (en) | 2014-10-16 |
US9493485B2 (en) | 2016-11-15 |
US20160272654A1 (en) | 2016-09-22 |
EP2827857A1 (en) | 2015-01-28 |
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Legal Events
Date | Code | Title | Description |
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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 |