MA35191B1 - Spiro-[1,3]-oxazines et spiro-[1,4]-oxazepines en tant qu'inhibiteurs de baec1 et/ou bace2 - Google Patents
Spiro-[1,3]-oxazines et spiro-[1,4]-oxazepines en tant qu'inhibiteurs de baec1 et/ou bace2Info
- Publication number
- MA35191B1 MA35191B1 MA36582A MA36582A MA35191B1 MA 35191 B1 MA35191 B1 MA 35191B1 MA 36582 A MA36582 A MA 36582A MA 36582 A MA36582 A MA 36582A MA 35191 B1 MA35191 B1 MA 35191B1
- Authority
- MA
- Morocco
- Prior art keywords
- spiro
- oxazepines
- oxazines
- bace2
- baec1
- 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
-
- 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
- C07D498/02—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
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (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
La présente invention concerne des spiro-[1,3]-oxazines et des spiro-[1,4]-oxazépines de formule (i) ayant une activité inhibitrice de bace1 et/ou bace2, leur fabrication, des compositions pharmaceutiques les contenant et leur utilisation en tant que substances thérapeutiquement actives. Les composés actifs de la présente invention sont utiles dans le traitement thérapeutique et/ou prophylactique par exemple de la maladie d'alzheimer et du diabète de type 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11167835 | 2011-05-27 | ||
| PCT/EP2012/059688 WO2012163790A1 (fr) | 2011-05-27 | 2012-05-24 | Spiro-[1,3]-oxazines et spiro-[1,4]-oxazépines en tant qu'inhibiteurs de baec1 et/ou bace2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA35191B1 true MA35191B1 (fr) | 2014-06-02 |
Family
ID=46177417
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA36582A MA35191B1 (fr) | 2011-05-27 | 2013-12-18 | Spiro-[1,3]-oxazines et spiro-[1,4]-oxazepines en tant qu'inhibiteurs de baec1 et/ou bace2 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9079919B2 (fr) |
| EP (1) | EP2714697B1 (fr) |
| JP (1) | JP2014515382A (fr) |
| KR (1) | KR20140048137A (fr) |
| CN (1) | CN103596961B (fr) |
| AU (1) | AU2012264875B2 (fr) |
| BR (1) | BR112013030281A2 (fr) |
| CA (1) | CA2833813A1 (fr) |
| CL (1) | CL2013003372A1 (fr) |
| CO (1) | CO6801773A2 (fr) |
| CR (1) | CR20130580A (fr) |
| EA (1) | EA024286B1 (fr) |
| EC (1) | ECSP13013048A (fr) |
| ES (1) | ES2600636T3 (fr) |
| IL (1) | IL229334A (fr) |
| MA (1) | MA35191B1 (fr) |
| MX (1) | MX2013013910A (fr) |
| PE (1) | PE20141205A1 (fr) |
| PH (1) | PH12013502262A1 (fr) |
| SG (1) | SG194835A1 (fr) |
| UA (1) | UA111847C2 (fr) |
| WO (1) | WO2012163790A1 (fr) |
| ZA (1) | ZA201308395B (fr) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2612854B1 (fr) | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Dérivés d'aminothiazolidine et d'aminotétrahydrothiazepine comme inhibiteurs de BACE 1 |
| TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| WO2008133273A1 (fr) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Composition pharmaceutique pour le traitement de la maladie d'alzheimer |
| WO2009151098A1 (fr) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | DÉRIVÉ HÉTÉROCYCLIQUE CONTENANT DU SOUFRE AYANT UNE ACTIVITÉ INHIBANT LA β-SÉCRÉTASE |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 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 |
| WO2011044185A2 (fr) | 2009-10-08 | 2011-04-14 | Schering Corporation | Composés hétérocycliques iminopentafluorosoufrés en tant qu'inhibiteurs de bace-1, compositions et leur utilisation |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044187A1 (fr) | 2009-10-08 | 2011-04-14 | Schering Corporation | Composés de type dioxyde d'imino-thiadiazine utilisés en tant qu'inhibiteurs de bace, compositions en contenant et leur utilisation |
| WO2011044184A1 (fr) | 2009-10-08 | 2011-04-14 | Schering Corporation | Composés hétérocycliques de type imino-pentafluorosulfure utilisés en tant qu'inhibiteurs de bace1, compositions en contenant et leur utilisation |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| EP2634188A4 (fr) | 2010-10-29 | 2014-05-07 | Shionogi & Co | Dérivé d'aminodihydropyrimidine fusionnée |
| WO2012138734A1 (fr) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Composés de dioxyde de thiadiazine condensés avec des dérivés oxacycliques en c5-c6 comme inhibiteurs de bace, compositions, et utilisation use |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| WO2012147763A1 (fr) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | Dérivé d'oxazine et inhibiteur de bace 1 le contenant |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| HK1208817A1 (en) | 2012-05-30 | 2016-03-18 | Comentis, Inc. | Chromane compounds |
| EP2912035A4 (fr) | 2012-10-24 | 2016-06-15 | Shionogi & Co | Dérivés de dihydrooxazine ou d'oxazépine ayant une activité inhibitrice de bace1 |
| EP2934534B1 (fr) | 2012-12-21 | 2017-12-13 | Merck Sharp & Dohme Corp. | Dioxydes d'iminothiadiazine spiro c5 utilisés en tant qu'inhibiteurs de bace |
| CA2902212C (fr) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Composes perfluores 5,6-dihydro-4h-1,3-oxazine-2-amine substitues en tant qu'inhibiteurs de la beta-secretase et procedes d'utilisation correspondants |
| AU2014225604B2 (en) | 2013-03-08 | 2018-05-17 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US9725468B2 (en) | 2013-09-13 | 2017-08-08 | Merck Sharp & Dohme Corp. | C5-spiro iminothiazine dioxides as BACE inhibitors, compositions, and their use |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US10053453B2 (en) | 2014-10-07 | 2018-08-21 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| AU2016236402B2 (en) | 2015-03-20 | 2019-08-01 | F. Hoffmann-La Roche Ag | BACE1 inhibitors |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA04010952A (es) | 2002-05-09 | 2005-01-25 | Pharmacia Corp | Compuestos de pirazolilo sustituidos para el tratamiento de la inflamacion. |
| TW200624426A (en) * | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
| US8211904B2 (en) * | 2005-07-18 | 2012-07-03 | Merck, Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| EP2612854B1 (fr) * | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Dérivés d'aminothiazolidine et d'aminotétrahydrothiazepine comme inhibiteurs de BACE 1 |
| AU2007293416A1 (en) | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease |
| WO2008133273A1 (fr) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Composition pharmaceutique pour le traitement de la maladie d'alzheimer |
| 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 (fr) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibiteurs de la bêta-sécrétase |
| JPWO2010047372A1 (ja) * | 2008-10-22 | 2012-03-22 | 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 (fr) | 2008-12-22 | 2010-07-01 | Orchid Research Laboratories Ltd. | Composés hétérocycliques comme inhibiteurs de hdac |
| US8461160B2 (en) * | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| AR077328A1 (es) * | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8188079B2 (en) * | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| WO2011058763A1 (fr) * | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | Dérivé d'aminothiazine ou d'aminooxazine contenant un lieur amino |
| 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 |
| AR080865A1 (es) * | 2010-03-31 | 2012-05-16 | Array Biopharma Inc | Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer. |
| 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 SG SG2013082607A patent/SG194835A1/en unknown
- 2012-05-24 CN CN201280025801.2A patent/CN103596961B/zh not_active Expired - Fee Related
- 2012-05-24 BR BR112013030281A patent/BR112013030281A2/pt not_active IP Right Cessation
- 2012-05-24 PH PH1/2013/502262A patent/PH12013502262A1/en unknown
- 2012-05-24 WO PCT/EP2012/059688 patent/WO2012163790A1/fr not_active Ceased
- 2012-05-24 ES ES12724116.4T patent/ES2600636T3/es active Active
- 2012-05-24 PE PE2013002577A patent/PE20141205A1/es not_active Application Discontinuation
- 2012-05-24 CA CA2833813A patent/CA2833813A1/fr not_active Abandoned
- 2012-05-24 AU AU2012264875A patent/AU2012264875B2/en not_active Expired - Fee Related
- 2012-05-24 EP EP12724116.4A patent/EP2714697B1/fr not_active Not-in-force
- 2012-05-24 EA EA201391752A patent/EA024286B1/ru not_active IP Right Cessation
- 2012-05-24 UA UAA201315118A patent/UA111847C2/uk unknown
- 2012-05-24 KR KR1020137033959A patent/KR20140048137A/ko not_active Withdrawn
- 2012-05-24 MX MX2013013910A patent/MX2013013910A/es unknown
- 2012-05-24 JP JP2014513129A patent/JP2014515382A/ja active Pending
-
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 |
|---|---|
| AU2012264875A1 (en) | 2013-10-31 |
| IL229334A0 (en) | 2014-01-30 |
| EA024286B1 (ru) | 2016-09-30 |
| CR20130580A (es) | 2013-12-09 |
| CO6801773A2 (es) | 2013-11-29 |
| CN103596961A (zh) | 2014-02-19 |
| MX2013013910A (es) | 2014-01-24 |
| IL229334A (en) | 2017-02-28 |
| WO2012163790A1 (fr) | 2012-12-06 |
| US9079919B2 (en) | 2015-07-14 |
| NZ616817A (en) | 2015-12-24 |
| EA201391752A1 (ru) | 2014-04-30 |
| ES2600636T3 (es) | 2017-02-10 |
| EP2714697B1 (fr) | 2016-08-31 |
| CL2013003372A1 (es) | 2014-07-25 |
| PE20141205A1 (es) | 2014-09-22 |
| US20120302549A1 (en) | 2012-11-29 |
| KR20140048137A (ko) | 2014-04-23 |
| BR112013030281A2 (pt) | 2016-11-29 |
| CN103596961B (zh) | 2016-09-28 |
| UA111847C2 (uk) | 2016-06-24 |
| EP2714697A1 (fr) | 2014-04-09 |
| ZA201308395B (en) | 2014-07-30 |
| JP2014515382A (ja) | 2014-06-30 |
| SG194835A1 (en) | 2013-12-30 |
| ECSP13013048A (es) | 2014-01-31 |
| CA2833813A1 (fr) | 2012-12-06 |
| PH12013502262A1 (en) | 2016-01-22 |
| AU2012264875B2 (en) | 2017-04-27 |
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