CA2903215C - Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use - Google Patents
Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use Download PDFInfo
- Publication number
- CA2903215C CA2903215C CA2903215A CA2903215A CA2903215C CA 2903215 C CA2903215 C CA 2903215C CA 2903215 A CA2903215 A CA 2903215A CA 2903215 A CA2903215 A CA 2903215A CA 2903215 C CA2903215 C CA 2903215C
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- Prior art keywords
- independently
- oxa
- pharmaceutically acceptable
- acceptable salt
- alkyl
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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
- 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
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
-
- 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
- C07D413/10—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 carbon chain containing aromatic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361775380P | 2013-03-08 | 2013-03-08 | |
| US61/775,380 | 2013-03-08 | ||
| US201461939580P | 2014-02-13 | 2014-02-13 | |
| US61/939,580 | 2014-02-13 | ||
| PCT/US2014/021412 WO2014138484A1 (en) | 2013-03-08 | 2014-03-06 | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2903215A1 CA2903215A1 (en) | 2014-09-12 |
| CA2903215C true CA2903215C (en) | 2021-07-20 |
Family
ID=50478936
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2903215A Active CA2903215C (en) | 2013-03-08 | 2014-03-06 | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US9085576B2 (enExample) |
| EP (1) | EP2964644B1 (enExample) |
| JP (1) | JP6374889B2 (enExample) |
| KR (1) | KR20150124985A (enExample) |
| CN (1) | CN105164121A (enExample) |
| AP (1) | AP2015008716A0 (enExample) |
| AU (1) | AU2014225604B2 (enExample) |
| BR (1) | BR112015021336A2 (enExample) |
| CA (1) | CA2903215C (enExample) |
| CL (1) | CL2015002516A1 (enExample) |
| CR (1) | CR20150519A (enExample) |
| EA (1) | EA201591614A1 (enExample) |
| HK (1) | HK1217486A1 (enExample) |
| IL (1) | IL240829A0 (enExample) |
| MX (1) | MX374512B (enExample) |
| PE (1) | PE20151794A1 (enExample) |
| PH (1) | PH12015502001A1 (enExample) |
| SG (1) | SG11201507196WA (enExample) |
| TN (1) | TN2015000382A1 (enExample) |
| TW (1) | TW201446760A (enExample) |
| UY (1) | UY35377A (enExample) |
| WO (1) | WO2014138484A1 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| UA110467C2 (uk) † | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| WO2014142219A1 (ja) | 2013-03-13 | 2014-09-18 | アステラス製薬株式会社 | グアニジノ安息香酸エステル化合物 |
| US9428470B2 (en) | 2014-02-13 | 2016-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| US9346776B2 (en) | 2014-02-13 | 2016-05-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| AU2015301028B2 (en) * | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| WO2016044120A1 (en) * | 2014-09-19 | 2016-03-24 | Merck Sharp & Dohme Corp. | Diazine-fused amidine compounds as bace inhibitors, compositions, and their use |
| WO2016118404A1 (en) * | 2015-01-20 | 2016-07-28 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use |
| KR102114536B1 (ko) | 2015-05-07 | 2020-05-22 | 브리스톨-마이어스 스큅 컴퍼니 | RORγ 조정제로서의 트리시클릭 술폰 |
| CN108137548A (zh) * | 2015-08-07 | 2018-06-08 | 拜耳作物科学股份公司 | 作为农药的2-(杂)芳基取代的稠合杂环衍生物 |
| ES2928164T3 (es) | 2015-10-19 | 2022-11-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| EP3165093A1 (en) | 2015-11-05 | 2017-05-10 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| MD3377488T2 (ro) | 2015-11-19 | 2023-02-28 | Incyte Corp | Compuși heterociclici ca imunomodulatori |
| MA44075A (fr) | 2015-12-17 | 2021-05-19 | Incyte Corp | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1 |
| MY199705A (en) | 2015-12-22 | 2023-11-20 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| WO2017192961A1 (en) | 2016-05-06 | 2017-11-09 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2017205464A1 (en) | 2016-05-26 | 2017-11-30 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| KR102685249B1 (ko) | 2016-06-20 | 2024-07-17 | 인사이트 코포레이션 | 면역조절제로서의 복소환식 화합물 |
| MA45669A (fr) | 2016-07-14 | 2019-05-22 | Incyte Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| WO2018044783A1 (en) | 2016-08-29 | 2018-03-08 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| CN106432071B (zh) * | 2016-09-05 | 2019-04-02 | 河北正朗制药有限公司 | 5-氰基-4-甲氧基-2-吡啶甲酸的盐酸盐的制备及其应用 |
| KR20190057388A (ko) | 2016-10-10 | 2019-05-28 | 브리스톨-마이어스 스큅 컴퍼니 | Ror 감마 조정제로서의 트리시클릭 술폰 |
| CA3047285A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| MA54100A (fr) | 2016-12-15 | 2021-10-20 | Amgen Inc | Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| CA3047991A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| EP3558973B1 (en) | 2016-12-22 | 2021-09-15 | Incyte Corporation | Pyridine derivatives as immunomodulators |
| PE20191532A1 (es) | 2016-12-22 | 2019-10-23 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores |
| WO2018119224A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers |
| EP3558989B1 (en) | 2016-12-22 | 2021-04-14 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| RS64055B1 (sr) | 2018-03-30 | 2023-04-28 | Incyte Corp | Heterociklična jedinjenja kao imunomodulatori |
| US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
| MD3790877T2 (ro) | 2018-05-11 | 2023-08-31 | Incyte Corp | Derivați de tetrahidro-imidazo[4,5-c]piridină în calitate de imunomodulatori PD-L1 |
| CN110759860B (zh) * | 2018-07-27 | 2022-10-14 | 江苏瑞科医药科技有限公司 | 一种3-甲酸甲酯-4-甲氧基-5-氰基吡啶的制备方法 |
| CN109430267A (zh) * | 2018-10-24 | 2019-03-08 | 南京华安药业有限公司 | 一种肟草酮水悬浮剂 |
| CN110183392B (zh) * | 2019-06-14 | 2023-03-28 | 河北医科大学 | 一种3-取代苯基-4，5-二氢异噁唑衍生物的制备方法及其用途和中间体 |
| JP7665593B2 (ja) | 2019-08-09 | 2025-04-21 | インサイト・コーポレイション | Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩 |
| AR120109A1 (es) | 2019-09-30 | 2022-02-02 | Incyte Corp | Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores |
| PE20230407A1 (es) | 2019-11-11 | 2023-03-07 | Incyte Corp | Sales y formas cristalinas de un inhibidor de pd-1/pd-l1 |
| CN110885329B (zh) | 2019-12-16 | 2020-12-15 | 诚达药业股份有限公司 | 一种1,7-萘啶衍生物的合成方法 |
| CN113087669B (zh) * | 2019-12-23 | 2023-11-17 | 南京药石科技股份有限公司 | 一种4-氰基-5-溴嘧啶的制备方法 |
| US12617803B2 (en) | 2020-05-05 | 2026-05-05 | Basf Se | Condensed isoxazoline derivatives and their use as herbicides |
| TW202233616A (zh) | 2020-11-06 | 2022-09-01 | 美商英塞特公司 | 用於製備ｐｄ－１／ｐｄ－ｌ１抑制劑以及其鹽及結晶形式之方法 |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
| WO2022099075A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Crystalline form of a pd-1/pd-l1 inhibitor |
| TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Ａｌｋ﹘５抑制劑和彼之用途 |
| CN121986099A (zh) | 2023-04-05 | 2026-05-05 | 摩玛治疗公司 | 半饱和二环衍生物和相关用途 |
| CN118852012A (zh) * | 2024-09-26 | 2024-10-29 | 山东国邦药业有限公司 | 一种高收率的二氟吡唑酸的合成方法 |
Family Cites Families (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5441870A (en) | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
| SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
| AU6383396A (en) | 1995-06-07 | 1996-12-30 | Athena Neurosciences, Inc. | Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition |
| US20040234976A1 (en) | 1998-09-24 | 2004-11-25 | Gurney Mark E. | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
| KR20070013361A (ko) | 1998-09-24 | 2007-01-30 | 파마시아 앤드 업존 캄파니 엘엘씨 | 알츠하이머병 세크레타제 |
| EP2335701B1 (en) | 2003-12-15 | 2012-07-11 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2612854B1 (en) | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors |
| WO2008062739A1 (en) | 2006-11-20 | 2008-05-29 | Japan Tobacco Inc. | Pyrazoles and use thereof as drugs |
| TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| KR20100007956A (ko) | 2007-05-03 | 2010-01-22 | 화이자 리미티드 | 나트륨 채널 조절제로서의 2-피리딘 카복스아마이드 유도체 |
| ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| 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 |
| WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011058763A1 (ja) | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
| EP2514747A4 (en) | 2009-12-09 | 2013-05-08 | Shionogi & Co | SUBSTITUTED AMINOTHIAZINE DERIVATIVE |
| WO2011071057A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| JPWO2011071109A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| 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 |
| UA110467C2 (uk) * | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| US8673894B2 (en) * | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| EA201391029A1 (ru) | 2011-01-12 | 2014-01-30 | Новартис Аг | Производные оксазина и их применение при лечении неврологических нарушений |
| EA201391033A1 (ru) | 2011-01-13 | 2014-01-30 | Новартис Аг | Ингибиторы bace-2 для лечения метаболических расстройств |
| US8404680B2 (en) | 2011-02-08 | 2013-03-26 | Hoffmann-La Roche Inc. | N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors |
| 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 |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| MX2013011947A (es) | 2011-04-13 | 2014-01-16 | Merck Sharp & Dohme | Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso. |
| CN103649082A (zh) | 2011-04-26 | 2014-03-19 | 盐野义制药株式会社 | 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂 |
| 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 |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| TW201302763A (zh) | 2011-05-24 | 2013-01-16 | 必治妥美雅史谷比公司 | 用於減少β－類澱粉產生之化合物 |
| US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| AR086653A1 (es) | 2011-06-03 | 2014-01-15 | Bristol Myers Squibb Co | COMPUESTOS PARA LA REDUCCION DE PRODUCCION DE b-AMILOIDE |
| 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 |
| MX2013014007A (es) | 2011-06-07 | 2014-03-12 | Hoffmann La Roche | [1,3] oxazinas. |
| US8987255B2 (en) | 2011-06-07 | 2015-03-24 | Hoffmann-La Roche Inc. | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| 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 |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
| US20130073953A1 (en) | 2011-09-21 | 2013-03-21 | Timothy Onyenobi | News headline screenshot viewing system |
| EA201490774A1 (ru) | 2011-10-13 | 2014-08-29 | Новартис Аг | Новые производные оксазина и их применение при лечении заболевания |
| CA2853221A1 (en) | 2011-10-24 | 2013-05-02 | Tohru Yamashita | Bicyclic compound |
| EP2807155B1 (en) | 2012-01-26 | 2017-04-12 | F. Hoffmann-La Roche AG | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
| HK1206597A1 (en) | 2012-03-20 | 2016-01-15 | 艾朗制药股份有限公司 | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| ES2585262T3 (es) | 2012-05-04 | 2016-10-04 | Pfizer Inc | Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 |
| WO2013182638A1 (en) | 2012-06-08 | 2013-12-12 | H. Lundbeck A/S | 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease |
| SG11201407576YA (en) | 2012-06-26 | 2015-03-30 | Hoffmann La Roche | Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors |
| GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
| CA2882389A1 (en) | 2012-09-20 | 2014-03-27 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9556135B2 (en) | 2012-10-12 | 2017-01-31 | Amgen, Inc. | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2912035A4 (en) * | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| HUE031764T2 (en) | 2012-10-26 | 2017-07-28 | Lilly Co Eli | Tetrahydropyrrolothiazine derivatives as BACE inhibitors |
| EP2931284B1 (en) | 2012-12-14 | 2017-08-23 | Merck Sharp & Dohme Corp. | Bace inhibitors of iminothiadiazine dioxides |
| US9475784B2 (en) | 2012-12-19 | 2016-10-25 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production |
| CA2893333C (en) | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| CA2894919A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5,c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2934534B1 (en) | 2012-12-21 | 2017-12-13 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| HK1210609A1 (en) | 2013-01-22 | 2016-04-29 | 霍夫曼-拉罗奇有限公司 | Fluoro-[1,3]oxazines as bace1 inhibitors |
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| BR112015022879B8 (pt) | 2013-03-15 | 2022-08-30 | Univ Brigham Young | Aparelho compreendendo uma espuma compósita uniforme e método para medir tensão de compressão usando o dito aparelho |
| PE20151748A1 (es) | 2013-04-11 | 2015-12-02 | Hoffmann La Roche | Inhibidores de bace1 |
| MX2015014728A (es) | 2013-04-26 | 2016-03-07 | Hoffmann La Roche | Sintesis de inhibidores de beta secretasa (bace). |
| 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 |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
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| US9085576B2 (en) | 2015-07-21 |
| AP2015008716A0 (en) | 2015-09-30 |
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| TW201446760A (zh) | 2014-12-16 |
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| JP2016510758A (ja) | 2016-04-11 |
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| EP2964644B1 (en) | 2018-12-26 |
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| CL2015002516A1 (es) | 2016-03-28 |
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| US20160280695A1 (en) | 2016-09-29 |
| UY35377A (es) | 2014-09-30 |
| WO2014138484A1 (en) | 2014-09-12 |
| US20140275058A1 (en) | 2014-09-18 |
| BR112015021336A2 (pt) | 2017-07-18 |
| CN105164121A (zh) | 2015-12-16 |
| US9611261B2 (en) | 2017-04-04 |
| HK1217486A1 (zh) | 2017-01-13 |
| SG11201507196WA (en) | 2015-10-29 |
| CA2903215A1 (en) | 2014-09-12 |
| EA201591614A1 (ru) | 2015-12-30 |
| JP6374889B2 (ja) | 2018-08-15 |
| AU2014225604B2 (en) | 2018-05-17 |
| AU2014225604A1 (en) | 2015-09-10 |
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