EA201391786A1 - Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и/или bace2 - Google Patents
Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и/или bace2Info
- Publication number
- EA201391786A1 EA201391786A1 EA201391786A EA201391786A EA201391786A1 EA 201391786 A1 EA201391786 A1 EA 201391786A1 EA 201391786 A EA201391786 A EA 201391786A EA 201391786 A EA201391786 A EA 201391786A EA 201391786 A1 EA201391786 A1 EA 201391786A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- bace1
- oxazins
- halogen
- alkyl
- bace2
- Prior art date
Links
Classifications
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
Настоящее изобретение предлагает соединения формулы Iобладающие ингибиторной активностью по отношению к ВАСЕ1 и/или ВАСЕ2, их получение, их содержащие фармацевтические композиции и их применение в качестве терапевтически активных веществ. Действующие вещества по настоящему изобретению полезны в терапевтическом и/или профилактическом лечении, например, болезни Альцгеймера и диабета 2 типа.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11169007 | 2011-06-07 | ||
PCT/EP2012/060457 WO2012168164A1 (en) | 2011-06-07 | 2012-06-04 | Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201391786A1 true EA201391786A1 (ru) | 2014-04-30 |
EA023261B1 EA023261B1 (ru) | 2016-05-31 |
Family
ID=46208521
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201391786A EA023261B1 (ru) | 2011-06-07 | 2012-06-04 | Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2 |
Country Status (18)
Country | Link |
---|---|
US (1) | US8987255B2 (ru) |
EP (1) | EP2718286A1 (ru) |
JP (1) | JP2014516063A (ru) |
KR (1) | KR20140041687A (ru) |
CN (1) | CN103717592A (ru) |
AU (1) | AU2012266544A1 (ru) |
BR (1) | BR112013031098A2 (ru) |
CA (1) | CA2837252A1 (ru) |
CL (1) | CL2013003472A1 (ru) |
CO (1) | CO6811854A2 (ru) |
CR (1) | CR20130588A (ru) |
EA (1) | EA023261B1 (ru) |
EC (1) | ECSP13013068A (ru) |
IL (1) | IL229686A0 (ru) |
MA (1) | MA35193B1 (ru) |
MX (1) | MX2013013692A (ru) |
PE (1) | PE20140623A1 (ru) |
WO (1) | WO2012168164A1 (ru) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2572263T3 (es) | 2005-10-25 | 2016-05-31 | Shionogi & Co | Derivados de dihidrooxazina y tetrahidropirimidina 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 |
ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
CN102119161B (zh) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | 具有β分泌酶抑制作用的含硫杂环衍生物 |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | 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 |
UA110467C2 (ru) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Производные оксазина |
WO2012057248A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
BR112013031098A2 (pt) * | 2011-06-07 | 2016-12-06 | Hoffmann La Roche | halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2 |
UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
CA2896185A1 (en) * | 2013-01-22 | 2014-07-31 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | 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 |
EP2984086A1 (en) | 2013-04-11 | 2016-02-17 | F. Hoffmann-La Roche AG | Bace1 inhibitors |
EP3107897A1 (en) | 2014-02-19 | 2016-12-28 | H. Lundbeck A/S | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
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 |
WO2016001266A1 (en) | 2014-07-04 | 2016-01-07 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
EP3177618A1 (en) | 2014-08-08 | 2017-06-14 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
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 |
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 |
JP6674960B2 (ja) | 2015-03-20 | 2020-04-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤 |
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 |
MX2018001699A (es) | 2015-08-12 | 2018-05-07 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1. |
MX2020011382A (es) | 2018-04-27 | 2020-11-24 | Shionogi & Co | Derivados de tetrahidropiranoxazina que tienen actividad inhibidora de beta-secretasa 1 (bace1) selectiva. |
Family Cites Families (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU7688398A (en) | 1997-06-16 | 1999-01-04 | American Home Products Corporation | Elevation of hdl cholesterol by 2-{(aminothioxomethyl)-hydrazono}-2-arylethyl carbamates |
CN1863770B (zh) * | 2003-08-08 | 2011-05-25 | 先灵公司 | 具有杂环取代基的环胺base-1抑制剂 |
CN1863797A (zh) * | 2003-08-08 | 2006-11-15 | 先灵公司 | 具有苯甲酰胺取代基的环胺bace-1抑制剂 |
TW200602045A (en) * | 2004-06-16 | 2006-01-16 | Wyeth Corp | Amino-5, 5-diphenylimidazolone derivatives for the inhibition of β-secretase |
TW200624426A (en) * | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
ES2572263T3 (es) | 2005-10-25 | 2016-05-31 | Shionogi & Co | Derivados de dihidrooxazina y tetrahidropirimidina como inhibidores de BACE 1 |
ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
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 |
US7964594B1 (en) * | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
UA103272C2 (ru) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-амино-5,5-дифтор-5,6-дигидро-4h-оксазины как ингибиторы bace1 и/или bace2 |
UA110467C2 (ru) * | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Производные оксазина |
DK2580200T3 (en) | 2010-06-09 | 2017-01-09 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H- [1,4] oxazin-3-YLAMINDERIVATER THAT COULD BE USED AS INHIBITORS OF BETA-secretase (BACE) |
US9861114B2 (en) * | 2010-08-05 | 2018-01-09 | Nestec S.A. | Frozen confectionery product with a natural stabiliser |
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 |
BR112013031098A2 (pt) * | 2011-06-07 | 2016-12-06 | Hoffmann La Roche | halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2 |
-
2012
- 2012-06-04 BR BR112013031098A patent/BR112013031098A2/pt not_active IP Right Cessation
- 2012-06-04 WO PCT/EP2012/060457 patent/WO2012168164A1/en active Application Filing
- 2012-06-04 JP JP2014514010A patent/JP2014516063A/ja active Pending
- 2012-06-04 EA EA201391786A patent/EA023261B1/ru not_active IP Right Cessation
- 2012-06-04 CA CA2837252A patent/CA2837252A1/en not_active Abandoned
- 2012-06-04 KR KR1020147000274A patent/KR20140041687A/ko not_active Application Discontinuation
- 2012-06-04 CN CN201280027493.7A patent/CN103717592A/zh active Pending
- 2012-06-04 AU AU2012266544A patent/AU2012266544A1/en not_active Abandoned
- 2012-06-04 EP EP12725743.4A patent/EP2718286A1/en not_active Withdrawn
- 2012-06-04 PE PE2013002764A patent/PE20140623A1/es not_active Application Discontinuation
- 2012-06-04 MX MX2013013692A patent/MX2013013692A/es not_active Application Discontinuation
- 2012-06-04 US US14/116,043 patent/US8987255B2/en not_active Expired - Fee Related
-
2013
- 2013-11-12 CR CR20130588A patent/CR20130588A/es unknown
- 2013-11-20 CO CO13273106A patent/CO6811854A2/es active IP Right Grant
- 2013-11-28 IL IL229686A patent/IL229686A0/en unknown
- 2013-12-04 EC ECSP13013068 patent/ECSP13013068A/es unknown
- 2013-12-04 CL CL2013003472A patent/CL2013003472A1/es unknown
- 2013-12-18 MA MA36584A patent/MA35193B1/fr unknown
Also Published As
Publication number | Publication date |
---|---|
CR20130588A (es) | 2014-02-18 |
ECSP13013068A (es) | 2014-01-31 |
JP2014516063A (ja) | 2014-07-07 |
US20140080819A1 (en) | 2014-03-20 |
PE20140623A1 (es) | 2014-05-30 |
AU2012266544A1 (en) | 2013-11-21 |
IL229686A0 (en) | 2014-01-30 |
EP2718286A1 (en) | 2014-04-16 |
KR20140041687A (ko) | 2014-04-04 |
BR112013031098A2 (pt) | 2016-12-06 |
CN103717592A (zh) | 2014-04-09 |
CL2013003472A1 (es) | 2014-08-18 |
CO6811854A2 (es) | 2013-12-16 |
WO2012168164A1 (en) | 2012-12-13 |
EA023261B1 (ru) | 2016-05-31 |
MX2013013692A (es) | 2014-03-05 |
MA35193B1 (fr) | 2014-06-02 |
CA2837252A1 (en) | 2012-12-13 |
NZ617507A (en) | 2015-07-31 |
US8987255B2 (en) | 2015-03-24 |
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Legal Events
Date | Code | Title | Description |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM RU |