BR112014029742A2 - diflúor-hexa-hidrociclopentaoxazinilas e diflúor-hexa-benzo-oxazinilas como inibidores da bace1 - Google Patents
diflúor-hexa-hidrociclopentaoxazinilas e diflúor-hexa-benzo-oxazinilas como inibidores da bace1Info
- Publication number
- BR112014029742A2 BR112014029742A2 BR112014029742A BR112014029742A BR112014029742A2 BR 112014029742 A2 BR112014029742 A2 BR 112014029742A2 BR 112014029742 A BR112014029742 A BR 112014029742A BR 112014029742 A BR112014029742 A BR 112014029742A BR 112014029742 A2 BR112014029742 A2 BR 112014029742A2
- Authority
- BR
- Brazil
- Prior art keywords
- alzheimer
- beta
- bace1
- disease
- amyloid
- 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
- C07D413/12—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
-
- 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
- A61K31/536—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 ortho- or peri-condensed with carbocyclic 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
resumo patente de invenção: "diflúor-hexa-hidrociclopentaoxazinilas e diflúor-hexa-benzo-oxazinilas como inibidores da bace1". a presente invenção fornece diflúor-ciclopentaoxazinilas e difluorenzo-oxazinilas de fórmula i i com atividade inibidora da bace1, sua fabricação, composições farmacêuticas contendo os mesmos e sua utilização como substâncias terapeuticamente ativas. os compostos ativos da presente invenção são úteis no tratamento terapêutico e/ou profilático, por exemplo, da doença de alzheimer. i hardy et al., the amyloid hypothesis of alzheimer's disease: progress and problems on the road to therapeutics, science. 19 de julho de 2002; 297(5580): 353-6, ii selkoe, cell biology of the amyloid beta-protein precursor and the mechanism of alzheimer's disease, annu rev cell biol. 1994;10:373-403 iii vassar et al., beta-secretase cleavage of alzheimer's amyloid precursor protein by the transmembrane aspartic protease bace, science. 22 de outubro de 1999; 286 (5440): 735 iv luo et al., mice deficient in bace1, the alzheimer's beta-secretase, have normal phenotype and abolished beta-amyloid generation, nat neurosci. março de 2001; 4(3): 231-2 v roberds et al., bace knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for alzheimer's disease therapeutics, hum mol genet. 1º de junho de 2001;10(12): 1317-24 vi mcconlogue et al., partial reduction of bace1 has dramatic effects on alzheimer plaque and synaptic pathology in app transgenic mice. j biol chem. 7 de setembro de 2007;282(36):26326 vii wo 2011071135 viii biochem. pharmacol. (1973) 22:3099 ix compendium of chemical terminology, 2ª edição, a. d. mcnaught & a. wilkinson (eds). blackwell scientific publications, oxford (1997) x brockhaus et al., neuroreport 9, 1481-1486; 1998 xi r.l.walsky e r.s.obach, drug metabolism and disposition 32: 647-660, 2004. e s.fowler e h.zhang, the aaps journal, vol.10, no. 2, 410-424, 2008 xii guo l, guthrie h, automated electrophysiology in the preclinical evaluation of drugs for potential qt prolongation. journal of pharmacological & toxicological methods, (2005) 52(1):123-35 xiii c.m.dieckhaus et al. em in chem.res.toxicol. 2005, 18, 630-638 xiv wo2010047372) xv wo2011009898)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12173690 | 2012-06-26 | ||
| PCT/EP2013/063086 WO2014001228A1 (en) | 2012-06-26 | 2013-06-24 | Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112014029742A2 true BR112014029742A2 (pt) | 2017-06-27 |
Family
ID=48672630
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112014029742A BR112014029742A2 (pt) | 2012-06-26 | 2013-06-24 | diflúor-hexa-hidrociclopentaoxazinilas e diflúor-hexa-benzo-oxazinilas como inibidores da bace1 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9181232B2 (pt) |
| EP (1) | EP2864324B1 (pt) |
| JP (1) | JP6251257B2 (pt) |
| KR (1) | KR20150023450A (pt) |
| CN (1) | CN104470915B (pt) |
| AU (1) | AU2013283524B2 (pt) |
| BR (1) | BR112014029742A2 (pt) |
| CA (1) | CA2872181A1 (pt) |
| CL (1) | CL2014003325A1 (pt) |
| CO (1) | CO7151509A2 (pt) |
| CR (1) | CR20140528A (pt) |
| EA (1) | EA025273B1 (pt) |
| HK (1) | HK1206344A1 (pt) |
| IL (1) | IL236138A (pt) |
| MA (1) | MA37763B1 (pt) |
| MX (1) | MX2014014937A (pt) |
| NZ (1) | NZ702253A (pt) |
| PE (1) | PE20142450A1 (pt) |
| PH (1) | PH12014502623B1 (pt) |
| SG (1) | SG11201407576YA (pt) |
| UA (1) | UA113309C2 (pt) |
| WO (1) | WO2014001228A1 (pt) |
Families Citing this family (9)
| 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 |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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 |
| CA2903215C (en) | 2013-03-08 | 2021-07-20 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物 |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| RU2712272C2 (ru) | 2015-03-20 | 2020-01-28 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы бета-секретазы |
| AU2019258575A1 (en) | 2018-04-27 | 2020-10-29 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| 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
- 2013-06-24 CN CN201380033783.7A patent/CN104470915B/zh not_active Expired - Fee Related
- 2013-06-24 JP JP2015519008A patent/JP6251257B2/ja not_active Expired - Fee Related
- 2013-06-24 US US14/406,289 patent/US9181232B2/en not_active Expired - Fee Related
- 2013-06-24 BR BR112014029742A patent/BR112014029742A2/pt not_active IP Right Cessation
- 2013-06-24 EA EA201590066A patent/EA025273B1/ru not_active IP Right Cessation
- 2013-06-24 PE PE2014002406A patent/PE20142450A1/es not_active Application Discontinuation
- 2013-06-24 NZ NZ702253A patent/NZ702253A/en not_active IP Right Cessation
- 2013-06-24 MA MA37763A patent/MA37763B1/fr unknown
- 2013-06-24 CA CA2872181A patent/CA2872181A1/en not_active Abandoned
- 2013-06-24 KR KR20147036016A patent/KR20150023450A/ko not_active Application Discontinuation
- 2013-06-24 SG SG11201407576YA patent/SG11201407576YA/en unknown
- 2013-06-24 EP EP13730887.0A patent/EP2864324B1/en not_active Not-in-force
- 2013-06-24 WO PCT/EP2013/063086 patent/WO2014001228A1/en active Application Filing
- 2013-06-24 MX MX2014014937A patent/MX2014014937A/es unknown
- 2013-06-24 UA UAA201500578A patent/UA113309C2/uk unknown
- 2013-06-24 AU AU2013283524A patent/AU2013283524B2/en not_active Expired - Fee Related
-
2014
- 2014-11-18 CR CR20140528A patent/CR20140528A/es unknown
- 2014-11-24 PH PH12014502623A patent/PH12014502623B1/en unknown
- 2014-12-05 CL CL2014003325A patent/CL2014003325A1/es unknown
- 2014-12-08 IL IL236138A patent/IL236138A/en not_active IP Right Cessation
- 2014-12-10 CO CO14271199A patent/CO7151509A2/es unknown
-
2015
- 2015-07-21 HK HK15106931.2A patent/HK1206344A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| MX2014014937A (es) | 2015-03-09 |
| KR20150023450A (ko) | 2015-03-05 |
| PE20142450A1 (es) | 2015-01-28 |
| EP2864324A1 (en) | 2015-04-29 |
| MA37763B1 (fr) | 2017-05-31 |
| US20150133440A1 (en) | 2015-05-14 |
| US9181232B2 (en) | 2015-11-10 |
| JP6251257B2 (ja) | 2017-12-20 |
| CN104470915A (zh) | 2015-03-25 |
| AU2013283524A1 (en) | 2014-11-13 |
| HK1206344A1 (en) | 2016-01-08 |
| PH12014502623A1 (en) | 2015-01-21 |
| EA025273B1 (ru) | 2016-12-30 |
| IL236138A (en) | 2016-10-31 |
| JP2015521640A (ja) | 2015-07-30 |
| MA37763A1 (fr) | 2016-08-31 |
| NZ702253A (en) | 2016-06-24 |
| IL236138A0 (en) | 2015-02-01 |
| CO7151509A2 (es) | 2014-12-29 |
| CA2872181A1 (en) | 2014-01-03 |
| CL2014003325A1 (es) | 2015-04-24 |
| EP2864324B1 (en) | 2018-03-28 |
| AU2013283524B2 (en) | 2017-03-30 |
| UA113309C2 (xx) | 2017-01-10 |
| SG11201407576YA (en) | 2015-03-30 |
| CR20140528A (es) | 2015-01-12 |
| WO2014001228A1 (en) | 2014-01-03 |
| EA201590066A1 (ru) | 2015-04-30 |
| CN104470915B (zh) | 2019-07-26 |
| PH12014502623B1 (en) | 2015-01-21 |
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Legal Events
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 6A ANUIDADE. |
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| 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: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2519 DE 16-04-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |