BR112013030281A2 - espiro-[1,3]-oxazinas e espiro-[1,4]-oxazepinas como inibidores de bace1 e/ou bace2 - Google Patents
espiro-[1,3]-oxazinas e espiro-[1,4]-oxazepinas como inibidores de bace1 e/ou bace2Info
- Publication number
- BR112013030281A2 BR112013030281A2 BR112013030281A BR112013030281A BR112013030281A2 BR 112013030281 A2 BR112013030281 A2 BR 112013030281A2 BR 112013030281 A BR112013030281 A BR 112013030281A BR 112013030281 A BR112013030281 A BR 112013030281A BR 112013030281 A2 BR112013030281 A2 BR 112013030281A2
- Authority
- BR
- Brazil
- Prior art keywords
- spiro
- bace1
- bace2
- oxazepines
- inhibitors
- Prior art date
Links
Classifications
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- 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
- 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
- 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
- C07D498/12—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 three hetero rings
- C07D498/20—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
resumo patente de invenção: "espiro-[1,3]-oxazinas e espiro-[1,4]-oxazepinas como inibidores de bace1 e/ou bace2". a presente invenção refere-se a espiro-[1,3]-oxazinas e espiro-[1,4]-oxazepinas de fórmula i, tendo atividade inibidora de bace1 e/ou bace2, sua fabricação, composições farmacêuticas contendo-as e seu uso como substâncias terapeuticamente ativas. os compostos ativos da presente invenção são úteis no tratamento terapêutico e/ou profilático de, por exemplo, doença de alzheimer e diabetes do tipo 2.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11167835 | 2011-05-27 | ||
PCT/EP2012/059688 WO2012163790A1 (en) | 2011-05-27 | 2012-05-24 | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112013030281A2 true BR112013030281A2 (pt) | 2016-11-29 |
Family
ID=46177417
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112013030281A BR112013030281A2 (pt) | 2011-05-27 | 2012-05-24 | espiro-[1,3]-oxazinas e espiro-[1,4]-oxazepinas como inibidores de bace1 e/ou bace2 |
Country Status (22)
Country | Link |
---|---|
US (1) | US9079919B2 (pt) |
EP (1) | EP2714697B1 (pt) |
JP (1) | JP2014515382A (pt) |
KR (1) | KR20140048137A (pt) |
CN (1) | CN103596961B (pt) |
AU (1) | AU2012264875B2 (pt) |
BR (1) | BR112013030281A2 (pt) |
CA (1) | CA2833813A1 (pt) |
CL (1) | CL2013003372A1 (pt) |
CO (1) | CO6801773A2 (pt) |
CR (1) | CR20130580A (pt) |
EA (1) | EA024286B1 (pt) |
EC (1) | ECSP13013048A (pt) |
ES (1) | ES2600636T3 (pt) |
IL (1) | IL229334A (pt) |
MA (1) | MA35191B1 (pt) |
MX (1) | MX2013013910A (pt) |
PE (1) | PE20141205A1 (pt) |
SG (1) | SG194835A1 (pt) |
UA (1) | UA111847C2 (pt) |
WO (1) | WO2012163790A1 (pt) |
ZA (1) | ZA201308395B (pt) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体 |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2703399A4 (en) | 2011-04-26 | 2014-10-15 | Shionogi & Co | OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF |
EP2747769B1 (en) | 2011-08-22 | 2017-08-02 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
WO2013181202A2 (en) | 2012-05-30 | 2013-12-05 | Astellas Pharma Inc. | Chromane compounds |
EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
EP2961749B1 (en) | 2013-03-01 | 2019-10-09 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | 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過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法 |
EP3043802B1 (en) | 2013-09-13 | 2018-04-18 | Merck Sharp & Dohme Corp. | C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use |
CN106795147B (zh) | 2014-08-08 | 2020-09-22 | 美国安进公司 | 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法 |
UY36347A (es) * | 2014-10-07 | 2016-04-01 | Astrazeneca Ab | Compuestos y su uso como inhibidores de bace |
RU2712272C2 (ru) | 2015-03-20 | 2020-01-28 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы бета-секретазы |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2003220483A1 (en) | 2002-05-09 | 2003-11-11 | Pharmacia Corporation | Substituted pyrazolyl compounds for the treatment of inflammation |
TW200624426A (en) * | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
CN101238124A (zh) * | 2005-07-18 | 2008-08-06 | 默克公司 | 用于治疗阿尔茨海默氏病的螺哌啶β-分泌酶抑制剂 |
RU2416603C9 (ru) * | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
US20100298342A1 (en) | 2006-09-07 | 2010-11-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease |
WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
CN102105475B (zh) * | 2008-07-28 | 2014-04-09 | 卫材R&D管理有限公司 | 螺氨基二氢噻嗪衍生物 |
WO2010021680A2 (en) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
WO2010047372A1 (ja) * | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体 |
WO2010073078A2 (en) | 2008-12-22 | 2010-07-01 | Orchid Research Laboratories Ltd. | Heterocyclic compounds as hdac inhibitors |
US8461160B2 (en) * | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
UY32799A (es) * | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
US8188079B2 (en) * | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
WO2011058763A1 (ja) * | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
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 |
WO2011123674A1 (en) * | 2010-03-31 | 2011-10-06 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
JP2012250933A (ja) * | 2011-06-03 | 2012-12-20 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
-
2012
- 2012-05-21 US US13/476,094 patent/US9079919B2/en not_active Expired - Fee Related
- 2012-05-24 CN CN201280025801.2A patent/CN103596961B/zh not_active Expired - Fee Related
- 2012-05-24 ES ES12724116.4T patent/ES2600636T3/es active Active
- 2012-05-24 WO PCT/EP2012/059688 patent/WO2012163790A1/en active Application Filing
- 2012-05-24 PE PE2013002577A patent/PE20141205A1/es not_active Application Discontinuation
- 2012-05-24 AU AU2012264875A patent/AU2012264875B2/en not_active Expired - Fee Related
- 2012-05-24 KR KR1020137033959A patent/KR20140048137A/ko not_active Application Discontinuation
- 2012-05-24 CA CA2833813A patent/CA2833813A1/en not_active Abandoned
- 2012-05-24 JP JP2014513129A patent/JP2014515382A/ja active Pending
- 2012-05-24 UA UAA201315118A patent/UA111847C2/uk unknown
- 2012-05-24 BR BR112013030281A patent/BR112013030281A2/pt not_active IP Right Cessation
- 2012-05-24 EA EA201391752A patent/EA024286B1/ru not_active IP Right Cessation
- 2012-05-24 MX MX2013013910A patent/MX2013013910A/es unknown
- 2012-05-24 SG SG2013082607A patent/SG194835A1/en unknown
- 2012-05-24 EP EP12724116.4A patent/EP2714697B1/en not_active Not-in-force
-
2013
- 2013-11-07 ZA ZA2013/08395A patent/ZA201308395B/en unknown
- 2013-11-07 IL IL229334A patent/IL229334A/en not_active IP Right Cessation
- 2013-11-07 CR CR20130580A patent/CR20130580A/es unknown
- 2013-11-13 CO CO13267226A patent/CO6801773A2/es not_active Application Discontinuation
- 2013-11-25 CL CL2013003372A patent/CL2013003372A1/es unknown
- 2013-11-25 EC ECSP13013048 patent/ECSP13013048A/es unknown
- 2013-12-18 MA MA36582A patent/MA35191B1/fr unknown
Also Published As
Publication number | Publication date |
---|---|
CR20130580A (es) | 2013-12-09 |
IL229334A (en) | 2017-02-28 |
IL229334A0 (en) | 2014-01-30 |
AU2012264875A1 (en) | 2013-10-31 |
KR20140048137A (ko) | 2014-04-23 |
PE20141205A1 (es) | 2014-09-22 |
AU2012264875B2 (en) | 2017-04-27 |
NZ616817A (en) | 2015-12-24 |
EP2714697A1 (en) | 2014-04-09 |
US9079919B2 (en) | 2015-07-14 |
MX2013013910A (es) | 2014-01-24 |
SG194835A1 (en) | 2013-12-30 |
ES2600636T3 (es) | 2017-02-10 |
JP2014515382A (ja) | 2014-06-30 |
US20120302549A1 (en) | 2012-11-29 |
UA111847C2 (uk) | 2016-06-24 |
EA024286B1 (ru) | 2016-09-30 |
CL2013003372A1 (es) | 2014-07-25 |
MA35191B1 (fr) | 2014-06-02 |
ECSP13013048A (es) | 2014-01-31 |
ZA201308395B (en) | 2014-07-30 |
CO6801773A2 (es) | 2013-11-29 |
WO2012163790A1 (en) | 2012-12-06 |
CN103596961B (zh) | 2016-09-28 |
CN103596961A (zh) | 2014-02-19 |
CA2833813A1 (en) | 2012-12-06 |
EA201391752A1 (ru) | 2014-04-30 |
EP2714697B1 (en) | 2016-08-31 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A ANUIDADE. |
|
B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
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