CR20130580A - Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores de bace1 y/o bace2 - Google Patents
Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores de bace1 y/o bace2Info
- Publication number
- CR20130580A CR20130580A CR20130580A CR20130580A CR20130580A CR 20130580 A CR20130580 A CR 20130580A CR 20130580 A CR20130580 A CR 20130580A CR 20130580 A CR20130580 A CR 20130580A CR 20130580 A CR20130580 A CR 20130580A
- Authority
- CR
- Costa Rica
- Prior art keywords
- spiro
- oxacepins
- bace2
- bace1
- oxacines
- 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)
- 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
La presente invención proporciona spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas de fórmula I: que presentan actividad inhibidora de BACE1 y/o de BACE2, su preparación, composiciones farmacéuticas que las contienen y su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención resultan útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, la enfermedad de Alzheimer y de la diabetes de tipo 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11167835 | 2011-05-27 |
Publications (1)
Publication Number | Publication Date |
---|---|
CR20130580A true CR20130580A (es) | 2013-12-09 |
Family
ID=46177417
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20130580A CR20130580A (es) | 2011-05-27 | 2013-11-07 | Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores de bace1 y/o bace2 |
Country Status (22)
Country | Link |
---|---|
US (1) | US9079919B2 (es) |
EP (1) | EP2714697B1 (es) |
JP (1) | JP2014515382A (es) |
KR (1) | KR20140048137A (es) |
CN (1) | CN103596961B (es) |
AU (1) | AU2012264875B2 (es) |
BR (1) | BR112013030281A2 (es) |
CA (1) | CA2833813A1 (es) |
CL (1) | CL2013003372A1 (es) |
CO (1) | CO6801773A2 (es) |
CR (1) | CR20130580A (es) |
EA (1) | EA024286B1 (es) |
EC (1) | ECSP13013048A (es) |
ES (1) | ES2600636T3 (es) |
IL (1) | IL229334A (es) |
MA (1) | MA35191B1 (es) |
MX (1) | MX2013013910A (es) |
PE (1) | PE20141205A1 (es) |
SG (1) | SG194835A1 (es) |
UA (1) | UA111847C2 (es) |
WO (1) | WO2012163790A1 (es) |
ZA (1) | ZA201308395B (es) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
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 |
EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | 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 |
WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
EP2854797A4 (en) | 2012-05-30 | 2016-01-13 | Comentis Inc | CHROMANE COMPOUNDS |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
WO2014134341A1 (en) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
EP2964644B1 (en) | 2013-03-08 | 2018-12-26 | Amgen, Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
WO2015038446A1 (en) | 2013-09-13 | 2015-03-19 | Merck Sharp & Dohme Corp. | C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use |
WO2016022724A1 (en) | 2014-08-08 | 2016-02-11 | 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 |
SG11201707050VA (en) | 2015-03-20 | 2017-10-30 | Hoffmann La Roche | 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. |
PE20060692A1 (es) * | 2004-09-21 | 2006-07-19 | Lilly Co Eli | Inhibidores bace |
JP2009502786A (ja) * | 2005-07-18 | 2009-01-29 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病を治療するためのスピロピペリジンβ−セクレターゼ阻害剤 |
ES2537898T3 (es) * | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
WO2008030412A2 (en) | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
US8501733B2 (en) * | 2008-07-28 | 2013-08-06 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
US8450308B2 (en) | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
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 (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 |
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 |
US20120238557A1 (en) * | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
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 MX MX2013013910A patent/MX2013013910A/es unknown
- 2012-05-24 SG SG2013082607A patent/SG194835A1/en unknown
- 2012-05-24 AU AU2012264875A patent/AU2012264875B2/en not_active Expired - Fee Related
- 2012-05-24 EA EA201391752A patent/EA024286B1/ru not_active IP Right Cessation
- 2012-05-24 CN CN201280025801.2A patent/CN103596961B/zh not_active Expired - Fee Related
- 2012-05-24 EP EP12724116.4A patent/EP2714697B1/en not_active Not-in-force
- 2012-05-24 WO PCT/EP2012/059688 patent/WO2012163790A1/en active Application Filing
- 2012-05-24 BR BR112013030281A patent/BR112013030281A2/pt not_active IP Right Cessation
- 2012-05-24 JP JP2014513129A patent/JP2014515382A/ja active Pending
- 2012-05-24 PE PE2013002577A patent/PE20141205A1/es not_active Application Discontinuation
- 2012-05-24 ES ES12724116.4T patent/ES2600636T3/es active Active
- 2012-05-24 UA UAA201315118A patent/UA111847C2/uk unknown
- 2012-05-24 CA CA2833813A patent/CA2833813A1/en not_active Abandoned
- 2012-05-24 KR KR1020137033959A patent/KR20140048137A/ko not_active Application Discontinuation
-
2013
- 2013-11-07 ZA ZA2013/08395A patent/ZA201308395B/en unknown
- 2013-11-07 CR CR20130580A patent/CR20130580A/es unknown
- 2013-11-07 IL IL229334A patent/IL229334A/en not_active IP Right Cessation
- 2013-11-13 CO CO13267226A patent/CO6801773A2/es not_active Application Discontinuation
- 2013-11-25 EC ECSP13013048 patent/ECSP13013048A/es unknown
- 2013-11-25 CL CL2013003372A patent/CL2013003372A1/es unknown
- 2013-12-18 MA MA36582A patent/MA35191B1/fr unknown
Also Published As
Publication number | Publication date |
---|---|
KR20140048137A (ko) | 2014-04-23 |
ZA201308395B (en) | 2014-07-30 |
UA111847C2 (uk) | 2016-06-24 |
US9079919B2 (en) | 2015-07-14 |
EP2714697B1 (en) | 2016-08-31 |
MX2013013910A (es) | 2014-01-24 |
CA2833813A1 (en) | 2012-12-06 |
PE20141205A1 (es) | 2014-09-22 |
EA024286B1 (ru) | 2016-09-30 |
US20120302549A1 (en) | 2012-11-29 |
JP2014515382A (ja) | 2014-06-30 |
AU2012264875A1 (en) | 2013-10-31 |
MA35191B1 (fr) | 2014-06-02 |
AU2012264875B2 (en) | 2017-04-27 |
EA201391752A1 (ru) | 2014-04-30 |
CN103596961B (zh) | 2016-09-28 |
SG194835A1 (en) | 2013-12-30 |
CL2013003372A1 (es) | 2014-07-25 |
NZ616817A (en) | 2015-12-24 |
ECSP13013048A (es) | 2014-01-31 |
WO2012163790A1 (en) | 2012-12-06 |
IL229334A0 (en) | 2014-01-30 |
IL229334A (en) | 2017-02-28 |
CN103596961A (zh) | 2014-02-19 |
EP2714697A1 (en) | 2014-04-09 |
CO6801773A2 (es) | 2013-11-29 |
ES2600636T3 (es) | 2017-02-10 |
BR112013030281A2 (pt) | 2016-11-29 |
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