JP6576433B2 - β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−２−アミン化合物及び使用方法 - Google Patents
β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−２−アミン化合物及び使用方法 Download PDFInfo
- Publication number
- JP6576433B2 JP6576433B2 JP2017506879A JP2017506879A JP6576433B2 JP 6576433 B2 JP6576433 B2 JP 6576433B2 JP 2017506879 A JP2017506879 A JP 2017506879A JP 2017506879 A JP2017506879 A JP 2017506879A JP 6576433 B2 JP6576433 B2 JP 6576433B2
- Authority
- JP
- Japan
- Prior art keywords
- amino
- methyl
- azabicyclo
- thia
- hept
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 CCC(*)C(C)C1C2C(C)C(C3)C3C2C1CC Chemical compound CCC(*)C(C)C1C2C(C)C(C3)C3C2C1CC 0.000 description 27
- GQDVWXBQVYAVGO-UHFFFAOYSA-N C=C(CC1C2C1)C2=C Chemical compound C=C(CC1C2C1)C2=C GQDVWXBQVYAVGO-UHFFFAOYSA-N 0.000 description 1
- TYBSRZRTSLQUSR-UHFFFAOYSA-N C=[O]C(c(cc1)ncc1Cl)=O Chemical compound C=[O]C(c(cc1)ncc1Cl)=O TYBSRZRTSLQUSR-UHFFFAOYSA-N 0.000 description 1
- XHYUSWFVTHVMLT-UHFFFAOYSA-N CC(C(C=CC(N)=CC1)C1=C)=O Chemical compound CC(C(C=CC(N)=CC1)C1=C)=O XHYUSWFVTHVMLT-UHFFFAOYSA-N 0.000 description 1
- IQVLAFPTZKIEBB-UHFFFAOYSA-N CC(C)NC(C)CCCCC1CC1 Chemical compound CC(C)NC(C)CCCCC1CC1 IQVLAFPTZKIEBB-UHFFFAOYSA-N 0.000 description 1
- VUEDDINXSVYZMI-VIFPVBQESA-N C[C@@H](C#C)Oc1cc(C)c(C(OC)=O)nc1 Chemical compound C[C@@H](C#C)Oc1cc(C)c(C(OC)=O)nc1 VUEDDINXSVYZMI-VIFPVBQESA-N 0.000 description 1
- GKXHZZXJGKPNNO-QMMMGPOBSA-N C[C@@H](C#C)Oc1cnc(C(O)=O)c(C)c1 Chemical compound C[C@@H](C#C)Oc1cnc(C(O)=O)c(C)c1 GKXHZZXJGKPNNO-QMMMGPOBSA-N 0.000 description 1
- DVRGDIWEPAZFQK-ZETCQYMHSA-N C[C@@H](C#C)Oc1cnc2c(Cl)nccc2n1 Chemical compound C[C@@H](C#C)Oc1cnc2c(Cl)nccc2n1 DVRGDIWEPAZFQK-ZETCQYMHSA-N 0.000 description 1
- RWZBXFGNRLPLGX-PKBZVPESSA-N C[C@@H](C#C)Oc1ncc(C(Nc(cc2[C@@]3(C)N=C(N)S[C@]4(C(F)F)[C@H]3C4)ccc2F)=O)nc1 Chemical compound C[C@@H](C#C)Oc1ncc(C(Nc(cc2[C@@]3(C)N=C(N)S[C@]4(C(F)F)[C@H]3C4)ccc2F)=O)nc1 RWZBXFGNRLPLGX-PKBZVPESSA-N 0.000 description 1
- GDKIDMDARBCFIJ-KHFQTWQWSA-N C[C@H]1[C@@](C)(c(cc(cc2C)NC(c(nc3)cnc3OCc3nc(C)n[o]3)=O)c2F)N=C(N)S[C@]1(C)C(F)F Chemical compound C[C@H]1[C@@](C)(c(cc(cc2C)NC(c(nc3)cnc3OCc3nc(C)n[o]3)=O)c2F)N=C(N)S[C@]1(C)C(F)F GDKIDMDARBCFIJ-KHFQTWQWSA-N 0.000 description 1
- PFOOVQDZSJCVFL-FZZIBODNSA-N C[C@]([C@@H]1C2)(c(cc(cc3F)N)c3F)N=C(N)S[C@]12C(NC)=O Chemical compound C[C@]([C@@H]1C2)(c(cc(cc3F)N)c3F)N=C(N)S[C@]12C(NC)=O PFOOVQDZSJCVFL-FZZIBODNSA-N 0.000 description 1
- KCCYUVIIKCPVDH-UHFFFAOYSA-N Cc1cc(O)cnc1Br Chemical compound Cc1cc(O)cnc1Br KCCYUVIIKCPVDH-UHFFFAOYSA-N 0.000 description 1
- ZGTXLDWNFBIHJH-UHFFFAOYSA-N Cc1cc(O)cnc1C(OC)=O Chemical compound Cc1cc(O)cnc1C(OC)=O ZGTXLDWNFBIHJH-UHFFFAOYSA-N 0.000 description 1
- AJPPFQKPGJRAKE-UHFFFAOYSA-N Clc1nccc2cc(OCc3ncc[s]3)cnc12 Chemical compound Clc1nccc2cc(OCc3ncc[s]3)cnc12 AJPPFQKPGJRAKE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61P25/28—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
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462035269P | 2014-08-08 | 2014-08-08 | |
| US62/035,269 | 2014-08-08 | ||
| PCT/US2015/043868 WO2016022724A1 (en) | 2014-08-08 | 2015-08-05 | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017523223A JP2017523223A (ja) | 2017-08-17 |
| JP2017523223A5 JP2017523223A5 (enExample) | 2018-09-13 |
| JP6576433B2 true JP6576433B2 (ja) | 2019-09-18 |
Family
ID=54150645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017506879A Active JP6576433B2 (ja) | 2014-08-08 | 2015-08-05 | β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−２−アミン化合物及び使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US9550762B2 (enExample) |
| EP (1) | EP3177618A1 (enExample) |
| JP (1) | JP6576433B2 (enExample) |
| CN (1) | CN106795147B (enExample) |
| AR (1) | AR101483A1 (enExample) |
| AU (1) | AU2015301028B2 (enExample) |
| CA (1) | CA2957544C (enExample) |
| JO (1) | JO3569B1 (enExample) |
| MX (1) | MX381482B (enExample) |
| TW (1) | TWI614250B (enExample) |
| UY (1) | UY36263A (enExample) |
| WO (1) | WO2016022724A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JP6576433B2 (ja) | 2014-08-08 | 2019-09-18 | 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シクロプロピル縮合チアジン−２−アミン化合物及び使用方法 |
| WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| CA3047287A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| JP7148518B2 (ja) | 2016-12-15 | 2022-10-05 | 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二環式チアジンおよびオキサジン誘導体ならびに使用方法 |
| 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. |
| WO2018112083A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| 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 |
| CN115684413A (zh) * | 2022-11-01 | 2023-02-03 | 重庆市涪陵食品药品检验所 | 一种硫酸羟氯喹中硫酸二甲酯和硫酸二乙酯的检测方法 |
Family Cites Families (82)
| 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 |
| KR100691601B1 (ko) | 1998-09-24 | 2007-03-09 | 파마시아 앤드 업존 캄파니 엘엘씨 | 알츠하이머병 세크레타제 |
| US20040234976A1 (en) | 1998-09-24 | 2004-11-25 | Gurney Mark E. | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| CA2548388A1 (en) | 2003-12-15 | 2005-06-30 | 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 |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| AU2006307314C1 (en) * | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| 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 |
| EA201000113A1 (ru) | 2007-08-01 | 2010-08-30 | Пфайзер Инк. | Пиразольные соединения |
| 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 |
| AU2009258496B8 (en) * | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| WO2010013794A1 (en) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| 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 | |
| US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
| EP2514747A4 (en) * | 2009-12-09 | 2013-05-08 | Shionogi & Co | SUBSTITUTED AMINOTHIAZINE DERIVATIVE |
| JP5554346B2 (ja) | 2009-12-09 | 2014-07-23 | 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 |
| 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 |
| 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 |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| WO2012039425A1 (ja) | 2010-09-24 | 2012-03-29 | 株式会社クラレ | ペースト及びその塗膜を電解質膜や電極膜とする高分子トランスデューサ |
| MX2013008111A (es) | 2011-01-12 | 2013-10-30 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos. |
| JP2014505689A (ja) | 2011-01-13 | 2014-03-06 | ノバルティス アーゲー | 代謝障害の処置用ｂａｃｅ−２阻害剤 |
| 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 |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | 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 |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| WO2012147762A1 (ja) * | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | ピリジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| EP2517898A1 (de) | 2011-04-29 | 2012-10-31 | Lanxess Deutschland GmbH | Kieselsäurehaltige Kautschukmischungen mit schwefelhaltigen Additiven |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| 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 |
| 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 |
| MX2013014007A (es) | 2011-06-07 | 2014-03-12 | Hoffmann La Roche | [1,3] oxazinas. |
| 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 |
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| US8476264B2 (en) | 2011-09-21 | 2013-07-02 | Hoffmann-La Roche Inc. | N-(3-(2-amino-6,6-difluoro-4,4A,5,6,7,7A-hexahydro-cyclopenta[E][1,3]oxazin-4-yl)-phenylamides as BACE1 inhibitors |
| IN2014DN03206A (enExample) | 2011-10-13 | 2015-05-22 | Novartis Ag | |
| EP2772485A4 (en) | 2011-10-24 | 2015-06-10 | Takeda Pharmaceutical | BICYCLIC CONNECTION |
| KR101669349B1 (ko) | 2012-01-26 | 2016-10-25 | 에프. 호프만-라 로슈 아게 | 플루오로메틸-5,6-다이하이드로-4h-[1,3]옥사진 |
| 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 |
| DE102012005803A1 (de) | 2012-03-21 | 2013-09-26 | Wacker Neuson Produktion GmbH & Co. KG | Bohr-und/oder Schlaghammer mit belastungsabhängiger Anpassung der Schlagzahl |
| CA2872154C (en) | 2012-05-04 | 2016-08-23 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2 |
| WO2013182638A1 (en) | 2012-06-08 | 2013-12-12 | H. Lundbeck A/S | 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease |
| NZ702253A (en) | 2012-06-26 | 2016-06-24 | 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 |
| WO2014045162A1 (en) | 2012-09-20 | 2014-03-27 | Pfizer Inc. | ALKYL-SUBSTITUTED HEXAHYDROPYRANO[3,4-d] [1,3]THIAZIN-2-ANIME 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 |
| US9416129B2 (en) | 2012-10-17 | 2016-08-16 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
| WO2014062549A1 (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 |
| LT2912041T (lt) | 2012-10-26 | 2017-03-10 | Eli Lilly And Company | Tetrahidropiroltiazino dariniai kaip bace slopikliai |
| US9447085B2 (en) | 2012-12-14 | 2016-09-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use |
| 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 |
| JP6162820B2 (ja) | 2012-12-19 | 2017-07-12 | ファイザー・インク | 炭素環式および複素環式置換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 |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| EP2934534B1 (en) | 2012-12-21 | 2017-12-13 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| BR112015016315A2 (pt) | 2013-01-22 | 2017-07-11 | Hoffmann La Roche | fluoro-[1,3]oxazinas como inibidores de bace1 |
| 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 |
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| AU2014253275B2 (en) | 2013-04-11 | 2018-10-18 | F. Hoffmann-La Roche Ag | BACE1 inhibitors |
| SG11201508814SA (en) | 2013-04-26 | 2015-11-27 | Hoffmann La Roche | Synthesis of bace inhibitors |
| 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 |
| JP6576433B2 (ja) | 2014-08-08 | 2019-09-18 | 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シクロプロピル縮合チアジン−２−アミン化合物及び使用方法 |
-
2015
- 2015-08-05 JP JP2017506879A patent/JP6576433B2/ja active Active
- 2015-08-05 CA CA2957544A patent/CA2957544C/en active Active
- 2015-08-05 EP EP15766951.6A patent/EP3177618A1/en not_active Withdrawn
- 2015-08-05 WO PCT/US2015/043868 patent/WO2016022724A1/en not_active Ceased
- 2015-08-05 CN CN201580054674.2A patent/CN106795147B/zh active Active
- 2015-08-05 AU AU2015301028A patent/AU2015301028B2/en active Active
- 2015-08-05 MX MX2017001794A patent/MX381482B/es unknown
- 2015-08-05 US US14/819,256 patent/US9550762B2/en active Active
- 2015-08-07 AR ARP150102557A patent/AR101483A1/es unknown
- 2015-08-07 TW TW104125848A patent/TWI614250B/zh active
- 2015-08-07 UY UY0001036263A patent/UY36263A/es not_active Application Discontinuation
- 2015-08-09 JO JOP/2015/0190A patent/JO3569B1/ar active
-
2016
- 2016-11-17 US US15/354,877 patent/US20170267673A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MX2017001794A (es) | 2017-06-29 |
| CA2957544C (en) | 2023-01-24 |
| TWI614250B (zh) | 2018-02-11 |
| US20160046618A1 (en) | 2016-02-18 |
| CN106795147A (zh) | 2017-05-31 |
| CN106795147B (zh) | 2020-09-22 |
| JP2017523223A (ja) | 2017-08-17 |
| AR101483A1 (es) | 2016-12-21 |
| US9550762B2 (en) | 2017-01-24 |
| AU2015301028B2 (en) | 2019-09-26 |
| CA2957544A1 (en) | 2016-02-11 |
| EP3177618A1 (en) | 2017-06-14 |
| US20170267673A1 (en) | 2017-09-21 |
| TW201619154A (zh) | 2016-06-01 |
| JO3569B1 (ar) | 2020-07-05 |
| AU2015301028A1 (en) | 2017-03-09 |
| UY36263A (es) | 2016-02-29 |
| WO2016022724A1 (en) | 2016-02-11 |
| MX381482B (es) | 2025-03-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6576433B2 (ja) | β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−２−アミン化合物及び使用方法 | |
| US9085576B2 (en) | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use | |
| US10246429B2 (en) | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use | |
| JP6389830B2 (ja) | ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 | |
| TWI781920B (zh) | 化合物、組合物及方法 | |
| AU2018217860B2 (en) | 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer | |
| US9556135B2 (en) | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use | |
| JP7149271B2 (ja) | β－セクレターゼ阻害剤としての１，４－チアジンジオキシドおよび１，２，４－チアジアジンジオキシド誘導体ならびに使用方法 | |
| TW202045498A (zh) | 作為法尼醇x受體調節劑之經取代雙環化合物 | |
| EP3655406A1 (en) | Substituted pyrrolopyridine-derivatives | |
| JP6322275B2 (ja) | ヤヌスキナーゼ阻害剤としてのｎ−（２−シアノヘテロシクリル）ピラゾロピリドン | |
| US20130018064A1 (en) | Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use | |
| US9096615B2 (en) | Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170426 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20180803 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20180803 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20190411 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20190416 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20190710 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190716 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20190730 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20190820 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6576433 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |