PE20151748A1 - Inhibidores de bace1 - Google Patents
Inhibidores de bace1Info
- Publication number
- PE20151748A1 PE20151748A1 PE2015002129A PE2015002129A PE20151748A1 PE 20151748 A1 PE20151748 A1 PE 20151748A1 PE 2015002129 A PE2015002129 A PE 2015002129A PE 2015002129 A PE2015002129 A PE 2015002129A PE 20151748 A1 PE20151748 A1 PE 20151748A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- cyanopicolinamide
- fluoropyridin
- oxazin
- dihydro
- Prior art date
Links
- 229940125759 BACE1 protease inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- ONDYYYPIGRXDRW-JDFRZJQESA-N n-[6-[(4r,5r,6s)-2-amino-5-fluoro-4-methyl-6-(trifluoromethyl)-5,6-dihydro-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide Chemical compound N=1C(NC(=O)C=2N=CC(=CC=2)C#N)=CC=C(F)C=1[C@@]1(C)N=C(N)O[C@H](C(F)(F)F)[C@@H]1F ONDYYYPIGRXDRW-JDFRZJQESA-N 0.000 abstract 1
- JDFWETJUGPKDKZ-SJCJKPOMSA-N n-[6-[(4s,6s)-2-amino-4-methyl-6-(trifluoromethyl)-5,6-dihydro-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide Chemical compound N=1C(NC(=O)C=2N=CC(=CC=2)C#N)=CC=C(F)C=1[C@]1(C)C[C@@H](C(F)(F)F)OC(N)=N1 JDFWETJUGPKDKZ-SJCJKPOMSA-N 0.000 abstract 1
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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- 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
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Se refiere a compuestos de Formula I, donde R1, R2, R3, R4, R5 son tal como se definen en la descripcion. Son compuestos preferidos: N-(6-((4R, 5R, 6S)-2-amino-5-fluoro-4-metil-6-(trifluorometil)-5,6-dihidro-4H-1,3-oxazin-4-il)-5-fluoropiridin-2-il)-5-cianopicolinamida; N-(6-((4S, 6S)-2-amino-4-metil-6-(trifluorometil)-5,6-dihidro-4H-1,3-oxazin-4-il)-5-fluoropiridin-2-il)-5-cianopicolinamida; entre otros. Tambien se refiere procedimientos para su fabricacion y a composiciones que los contienen. Dichos compuestos inhiben la actividad de BACE1, siendo utiles para el tratamiento de la enfermedad de Alzheimer
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13163430 | 2013-04-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151748A1 true PE20151748A1 (es) | 2015-12-02 |
Family
ID=48050604
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002129A PE20151748A1 (es) | 2013-04-11 | 2014-04-08 | Inhibidores de bace1 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US11447478B2 (es) |
| EP (1) | EP2984086A1 (es) |
| JP (2) | JP6574756B2 (es) |
| KR (1) | KR102247765B1 (es) |
| CN (1) | CN105431430B (es) |
| AU (1) | AU2014253275B2 (es) |
| BR (1) | BR112015019412A8 (es) |
| CA (1) | CA2900433C (es) |
| CL (1) | CL2015002897A1 (es) |
| EA (1) | EA027860B1 (es) |
| HK (1) | HK1216533A1 (es) |
| IL (2) | IL240263A0 (es) |
| MA (2) | MA44948A1 (es) |
| MX (1) | MX2015014083A (es) |
| MY (1) | MY174747A (es) |
| PE (1) | PE20151748A1 (es) |
| PH (1) | PH12015502365B1 (es) |
| SG (1) | SG11201508412XA (es) |
| UA (1) | UA119141C2 (es) |
| WO (1) | WO2014166906A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| UA110467C2 (uk) † | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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 |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | アムジエン・インコーポレーテツド | β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法 |
| 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 |
| EP3177618A1 (en) | 2014-08-08 | 2017-06-14 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| WO2017061534A1 (en) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dihydrothiazine derivatives |
| JP2017071603A (ja) * | 2015-10-09 | 2017-04-13 | 塩野義製薬株式会社 | ジヒドロチアジンまたはジヒドロオキサジン誘導体を含有する医薬組成物 |
| EP3423450B1 (en) * | 2016-03-01 | 2019-11-27 | H. Hoffnabb-La Roche Ag | Bace 1 inhibitors |
| CN112313238B (zh) | 2018-04-27 | 2025-01-17 | 盐野义制药株式会社 | 具有选择性bace1抑制活性的四氢吡喃并噁嗪衍生物 |
| KR102467525B1 (ko) | 2020-11-26 | 2022-11-14 | 이대근 | 작업자 중개 장치 |
| AU2023259936A1 (en) | 2022-04-28 | 2024-11-28 | Daiichi Sankyo Company, Limited | Benzotriazole compound |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI270549B (en) | 2002-12-26 | 2007-01-11 | Taisho Pharmaceutical Co Ltd | Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with cyclic amino group |
| US20110206607A1 (en) | 2007-05-10 | 2011-08-25 | Roger Olsson | Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors |
| JP4520533B2 (ja) | 2008-01-18 | 2010-08-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 縮合アミノジヒドロチアジン誘導体 |
| JP2012051807A (ja) | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | アリールイミダゾール化合物 |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| 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 |
| PH12013501480A1 (en) | 2011-01-13 | 2022-10-26 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| TW201247635A (en) * | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| AU2012266544A1 (en) * | 2011-06-07 | 2013-11-21 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| CN103608344B (zh) * | 2011-06-07 | 2016-11-23 | 霍夫曼-拉罗奇有限公司 | [1,3]噁嗪类 |
| UY34278A (es) * | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| NZ625684A (en) | 2012-01-26 | 2016-02-26 | Hoffmann La Roche | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| 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 |
-
2014
- 2014-04-08 JP JP2016506890A patent/JP6574756B2/ja active Active
- 2014-04-08 CA CA2900433A patent/CA2900433C/en active Active
- 2014-04-08 EP EP14715908.1A patent/EP2984086A1/en not_active Withdrawn
- 2014-04-08 KR KR1020157031878A patent/KR102247765B1/ko not_active Expired - Fee Related
- 2014-04-08 AU AU2014253275A patent/AU2014253275B2/en not_active Ceased
- 2014-04-08 SG SG11201508412XA patent/SG11201508412XA/en unknown
- 2014-04-08 PE PE2015002129A patent/PE20151748A1/es unknown
- 2014-04-08 MY MYPI2015002528A patent/MY174747A/en unknown
- 2014-04-08 MA MA44948A patent/MA44948A1/fr unknown
- 2014-04-08 US US14/783,478 patent/US11447478B2/en active Active
- 2014-04-08 MA MA38556A patent/MA38556A1/fr unknown
- 2014-04-08 BR BR112015019412A patent/BR112015019412A8/pt not_active Application Discontinuation
- 2014-04-08 CN CN201480019357.2A patent/CN105431430B/zh not_active Expired - Fee Related
- 2014-04-08 WO PCT/EP2014/056985 patent/WO2014166906A1/en active Application Filing
- 2014-04-08 MX MX2015014083A patent/MX2015014083A/es unknown
- 2014-04-08 EA EA201591541A patent/EA027860B1/ru not_active IP Right Cessation
- 2014-08-04 UA UAA201510494A patent/UA119141C2/uk unknown
-
2015
- 2015-07-30 IL IL240263A patent/IL240263A0/en active IP Right Grant
- 2015-09-29 CL CL2015002897A patent/CL2015002897A1/es unknown
- 2015-10-12 PH PH12015502365A patent/PH12015502365B1/en unknown
-
2016
- 2016-04-20 HK HK16104540.9A patent/HK1216533A1/zh not_active IP Right Cessation
-
2018
- 2018-10-16 JP JP2018194983A patent/JP6681451B2/ja not_active Expired - Fee Related
-
2019
- 2019-03-20 IL IL265496A patent/IL265496A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US11447478B2 (en) | 2022-09-20 |
| CL2015002897A1 (es) | 2016-06-03 |
| KR20150142001A (ko) | 2015-12-21 |
| HK1216533A1 (zh) | 2016-11-18 |
| US20160052920A1 (en) | 2016-02-25 |
| PH12015502365A1 (en) | 2016-02-22 |
| BR112015019412A8 (pt) | 2019-11-12 |
| JP2016515638A (ja) | 2016-05-30 |
| AU2014253275B2 (en) | 2018-10-18 |
| EA201591541A1 (ru) | 2016-02-29 |
| MA38556A1 (fr) | 2017-09-29 |
| MY174747A (en) | 2020-05-13 |
| SG11201508412XA (en) | 2015-11-27 |
| CA2900433A1 (en) | 2014-10-16 |
| UA119141C2 (uk) | 2019-05-10 |
| EP2984086A1 (en) | 2016-02-17 |
| JP6681451B2 (ja) | 2020-04-15 |
| EA027860B1 (ru) | 2017-09-29 |
| CA2900433C (en) | 2021-06-22 |
| WO2014166906A1 (en) | 2014-10-16 |
| JP6574756B2 (ja) | 2019-09-11 |
| IL265496A (en) | 2019-05-30 |
| BR112015019412A2 (pt) | 2017-07-18 |
| AU2014253275A1 (en) | 2015-07-16 |
| CN105431430B (zh) | 2019-05-28 |
| MX2015014083A (es) | 2016-07-26 |
| MA44948A1 (fr) | 2020-06-30 |
| PH12015502365B1 (en) | 2019-04-12 |
| JP2019031532A (ja) | 2019-02-28 |
| NZ710050A (en) | 2021-03-26 |
| CN105431430A (zh) | 2016-03-23 |
| KR102247765B1 (ko) | 2021-05-06 |
| IL240263A0 (en) | 2015-09-24 |
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