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
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- 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
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- amino
- methyl
- azabicyclo
- thia
- hept
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- 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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (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 |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| WO2018112086A1 (en) * | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine 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 |
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| 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 |
| CN1502692A (zh) | 1998-09-24 | 2004-06-09 | �������Ŷ���Լ��������˾ | 阿尔茨海默氏疾病分泌酶 |
| 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 |
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| EA201000113A1 (ru) | 2007-08-01 | 2010-08-30 | Пфайзер Инк. | Пиразольные соединения |
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| PE20140623A1 (es) | 2011-06-07 | 2014-05-30 | Hoffmann La Roche | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2 |
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- 2015-08-05 MX MX2017001794A patent/MX381482B/es unknown
- 2015-08-05 CN CN201580054674.2A patent/CN106795147B/zh active Active
- 2015-08-05 JP JP2017506879A patent/JP6576433B2/ja active Active
- 2015-08-05 AU AU2015301028A patent/AU2015301028B2/en active Active
- 2015-08-05 EP EP15766951.6A patent/EP3177618A1/en not_active Withdrawn
- 2015-08-05 CA CA2957544A patent/CA2957544C/en active Active
- 2015-08-05 WO PCT/US2015/043868 patent/WO2016022724A1/en not_active Ceased
- 2015-08-07 UY UY0001036263A patent/UY36263A/es not_active Application Discontinuation
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| CN106795147A (zh) | 2017-05-31 |
| CN106795147B (zh) | 2020-09-22 |
| JP2017523223A (ja) | 2017-08-17 |
| AU2015301028A1 (en) | 2017-03-09 |
| JO3569B1 (ar) | 2020-07-05 |
| CA2957544A1 (en) | 2016-02-11 |
| AR101483A1 (es) | 2016-12-21 |
| UY36263A (es) | 2016-02-29 |
| WO2016022724A1 (en) | 2016-02-11 |
| US20160046618A1 (en) | 2016-02-18 |
| EP3177618A1 (en) | 2017-06-14 |
| US20170267673A1 (en) | 2017-09-21 |
| US9550762B2 (en) | 2017-01-24 |
| CA2957544C (en) | 2023-01-24 |
| MX2017001794A (es) | 2017-06-29 |
| MX381482B (es) | 2025-03-12 |
| AU2015301028B2 (en) | 2019-09-26 |
| TWI614250B (zh) | 2018-02-11 |
| TW201619154A (zh) | 2016-06-01 |
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