CR20130588A - Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace 2 - Google Patents
Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace 2Info
- Publication number
- CR20130588A CR20130588A CR20130588A CR20130588A CR20130588A CR 20130588 A CR20130588 A CR 20130588A CR 20130588 A CR20130588 A CR 20130588A CR 20130588 A CR20130588 A CR 20130588A CR 20130588 A CR20130588 A CR 20130588A
- Authority
- CR
- Costa Rica
- Prior art keywords
- bace1
- oxazinas
- halogenoalquil
- bace
- inhibitors
- 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
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- 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
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- 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
La presente invención proporciona compuestos de la fórmula I:que tienen actividad inhibidora de la BACE1 y/o de la BACE2, su obtención, composiciones farmacéuticas que los contienen y su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención son útiles para el tratamiento terapéutico y/o profiláctico p.ej. de la enfermedad de Alzheimer y de la diabetes de tipo 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11169007 | 2011-06-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
CR20130588A true CR20130588A (es) | 2014-02-18 |
Family
ID=46208521
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20130588A CR20130588A (es) | 2011-06-07 | 2013-11-12 | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace 2 |
Country Status (18)
Country | Link |
---|---|
US (1) | US8987255B2 (es) |
EP (1) | EP2718286A1 (es) |
JP (1) | JP2014516063A (es) |
KR (1) | KR20140041687A (es) |
CN (1) | CN103717592A (es) |
AU (1) | AU2012266544A1 (es) |
BR (1) | BR112013031098A2 (es) |
CA (1) | CA2837252A1 (es) |
CL (1) | CL2013003472A1 (es) |
CO (1) | CO6811854A2 (es) |
CR (1) | CR20130588A (es) |
EA (1) | EA023261B1 (es) |
EC (1) | ECSP13013068A (es) |
IL (1) | IL229686A0 (es) |
MA (1) | MA35193B1 (es) |
MX (1) | MX2013013692A (es) |
PE (1) | PE20140623A1 (es) |
WO (1) | WO2012168164A1 (es) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
BRPI0915500A2 (pt) | 2008-06-13 | 2019-08-27 | Shionogi & Co | derivado heterocíclico contendo enxofre tendo atividade inibitória de beta secretase |
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 |
WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
JPWO2012147763A1 (ja) | 2011-04-26 | 2014-07-28 | 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 |
JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としてのハロゲン−アルキル−1,3オキサジン |
UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
CA2896185A1 (en) * | 2013-01-22 | 2014-07-31 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
MX366855B (es) * | 2013-03-01 | 2019-07-26 | Amgen Inc | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. |
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 |
MA44948A1 (fr) | 2013-04-11 | 2020-06-30 | Hoffmann La Roche | Inhibiteurs de bace 1 |
AU2015220873A1 (en) * | 2014-02-19 | 2016-08-11 | 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 |
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 |
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 |
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 |
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 |
CA2979113A1 (en) | 2015-03-20 | 2016-09-29 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
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 |
CR20180077A (es) | 2015-08-12 | 2018-04-09 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 |
EP3784674B1 (en) | 2018-04-27 | 2023-02-22 | Shionogi & Co., Ltd | Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity |
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 |
ATE424383T1 (de) * | 2003-08-08 | 2009-03-15 | Schering Corp | Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren |
US7598250B2 (en) * | 2003-08-08 | 2009-10-06 | Schering Corporation | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
RU2006142552A (ru) * | 2004-06-16 | 2008-07-27 | Вайет (Us) | Производные амино-5,5-дифенилимидазолона как ингибиторы b-секретазы |
PE20060692A1 (es) * | 2004-09-21 | 2006-07-19 | Lilly Co Eli | Inhibidores bace |
TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
CA2628074C (en) * | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
MX2009011498A (es) * | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
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 |
WO2011071135A1 (ja) * | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
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 |
WO2011154431A1 (en) | 2010-06-09 | 2011-12-15 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful 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 |
JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としてのハロゲン−アルキル−1,3オキサジン |
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2012
- 2012-06-04 JP JP2014514010A patent/JP2014516063A/ja active Pending
- 2012-06-04 MX MX2013013692A patent/MX2013013692A/es not_active Application Discontinuation
- 2012-06-04 EA EA201391786A patent/EA023261B1/ru not_active IP Right Cessation
- 2012-06-04 AU AU2012266544A patent/AU2012266544A1/en not_active Abandoned
- 2012-06-04 KR KR1020147000274A patent/KR20140041687A/ko not_active Application Discontinuation
- 2012-06-04 WO PCT/EP2012/060457 patent/WO2012168164A1/en active Application Filing
- 2012-06-04 PE PE2013002764A patent/PE20140623A1/es not_active Application Discontinuation
- 2012-06-04 CA CA2837252A patent/CA2837252A1/en not_active Abandoned
- 2012-06-04 US US14/116,043 patent/US8987255B2/en not_active Expired - Fee Related
- 2012-06-04 BR BR112013031098A patent/BR112013031098A2/pt not_active IP Right Cessation
- 2012-06-04 CN CN201280027493.7A patent/CN103717592A/zh active Pending
- 2012-06-04 EP EP12725743.4A patent/EP2718286A1/en not_active Withdrawn
-
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 |
---|---|
MA35193B1 (fr) | 2014-06-02 |
CN103717592A (zh) | 2014-04-09 |
EP2718286A1 (en) | 2014-04-16 |
BR112013031098A2 (pt) | 2016-12-06 |
CO6811854A2 (es) | 2013-12-16 |
JP2014516063A (ja) | 2014-07-07 |
NZ617507A (en) | 2015-07-31 |
EA023261B1 (ru) | 2016-05-31 |
CA2837252A1 (en) | 2012-12-13 |
KR20140041687A (ko) | 2014-04-04 |
WO2012168164A1 (en) | 2012-12-13 |
US20140080819A1 (en) | 2014-03-20 |
ECSP13013068A (es) | 2014-01-31 |
PE20140623A1 (es) | 2014-05-30 |
US8987255B2 (en) | 2015-03-24 |
EA201391786A1 (ru) | 2014-04-30 |
AU2012266544A1 (en) | 2013-11-21 |
MX2013013692A (es) | 2014-03-05 |
IL229686A0 (en) | 2014-01-30 |
CL2013003472A1 (es) | 2014-08-18 |
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