JP6389830B2 - 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 - Google Patents
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 Download PDFInfo
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- 0 CC(C1)(*2cc(NC(c(cc3)ncc3C#N)=O)ccc2F)N=C(N)O[C@@]1C(F)(F)F Chemical compound CC(C1)(*2cc(NC(c(cc3)ncc3C#N)=O)ccc2F)N=C(N)O[C@@]1C(F)(F)F 0.000 description 14
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- BELAMVBTIPPFFA-WFASDCNBSA-N C[C@](C1)(c2cc(Oc3ncccn3)ccc2F)N=C(N)O[C@@H]1C(F)(F)F Chemical compound C[C@](C1)(c2cc(Oc3ncccn3)ccc2F)N=C(N)O[C@@H]1C(F)(F)F BELAMVBTIPPFFA-WFASDCNBSA-N 0.000 description 1
- UMHIFKHNODSZCU-RLFYNMQTSA-N C[C@]([C@H]1F)(c2cc(NC(c(nc3)ccc3C#N)=O)ccc2F)N=C(N)O[C@@H]1C(F)(F)F Chemical compound C[C@]([C@H]1F)(c2cc(NC(c(nc3)ccc3C#N)=O)ccc2F)N=C(N)O[C@@H]1C(F)(F)F UMHIFKHNODSZCU-RLFYNMQTSA-N 0.000 description 1
- VBRNPACCSYLXRZ-MGPUTAFESA-N Cc1c(C(Nc(cc2[C@](CF)(C3)N=C(N)O[C@@H]3C(F)(F)F)ccc2F)=O)nc2[n]1cccc2 Chemical compound Cc1c(C(Nc(cc2[C@](CF)(C3)N=C(N)O[C@@H]3C(F)(F)F)ccc2F)=O)nc2[n]1cccc2 VBRNPACCSYLXRZ-MGPUTAFESA-N 0.000 description 1
- LZWBCAALZFCYGM-HNAYVOBHSA-N Cc1cc(C)c(C(Nc(cc2)cc([C@](CF)(C3)N=C(N)O[C@@H]3C(F)(F)F)c2F)=O)nc1 Chemical compound Cc1cc(C)c(C(Nc(cc2)cc([C@](CF)(C3)N=C(N)O[C@@H]3C(F)(F)F)c2F)=O)nc1 LZWBCAALZFCYGM-HNAYVOBHSA-N 0.000 description 1
- LYSVSZDZWGUCLE-SCLBCKFNSA-N Cc1cc(NC(c(cn2)ncc2OC)=O)cc([C@](CF)(C2)N=C(N)O[C@@H]2C(F)(F)F)c1F Chemical compound Cc1cc(NC(c(cn2)ncc2OC)=O)cc([C@](CF)(C2)N=C(N)O[C@@H]2C(F)(F)F)c1F LYSVSZDZWGUCLE-SCLBCKFNSA-N 0.000 description 1
- NDJNUSRDWZMVAP-HJULIUOESA-N NC(OC(C[C@@H](CF)c1cc(NC(c(cc2)ncc2Br)=O)ccc1F)C(F)(F)F)=N Chemical compound NC(OC(C[C@@H](CF)c1cc(NC(c(cc2)ncc2Br)=O)ccc1F)C(F)(F)F)=N NDJNUSRDWZMVAP-HJULIUOESA-N 0.000 description 1
- WHLWHSRVCYOJLJ-KBPBESRZSA-N NC(O[C@@H](C1)C(F)(F)F)=N[C@@H]1c1cc(NC(c(nc2)ccc2Cl)=O)ccc1F Chemical compound NC(O[C@@H](C1)C(F)(F)F)=N[C@@H]1c1cc(NC(c(nc2)ccc2Cl)=O)ccc1F WHLWHSRVCYOJLJ-KBPBESRZSA-N 0.000 description 1
- BRPDMTKDYSZVAZ-WMLDXEAASA-N NC(O[C@@H](C1)C(F)(F)F)=N[C@]1(CF)c1cc(NC(c(nc2)ccc2Cl)=S)ccc1F Chemical compound NC(O[C@@H](C1)C(F)(F)F)=N[C@]1(CF)c1cc(NC(c(nc2)ccc2Cl)=S)ccc1F BRPDMTKDYSZVAZ-WMLDXEAASA-N 0.000 description 1
- YFNCOFBWQJRCLM-AJPWXKBRSA-N NC(O[C@@H](CC1c2cc(C#Cc3cccc4c3cc[nH]4)ccc2F)C(F)(F)F)=NC1F Chemical compound NC(O[C@@H](CC1c2cc(C#Cc3cccc4c3cc[nH]4)ccc2F)C(F)(F)F)=NC1F YFNCOFBWQJRCLM-AJPWXKBRSA-N 0.000 description 1
- KWIPIEOKQCFDRY-UHFFFAOYSA-N NC(c(nc1)ccc1C#N)=O Chemical compound NC(c(nc1)ccc1C#N)=O KWIPIEOKQCFDRY-UHFFFAOYSA-N 0.000 description 1
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
- C07D413/14—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
- 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
- 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
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
- C07D413/02—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
-
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—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
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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- 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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361771615P | 2013-03-01 | 2013-03-01 | |
| US61/771,615 | 2013-03-01 | ||
| US201361826431P | 2013-05-22 | 2013-05-22 | |
| US61/826,431 | 2013-05-22 | ||
| US201461928898P | 2014-01-17 | 2014-01-17 | |
| US61/928,898 | 2014-01-17 | ||
| PCT/US2014/019100 WO2014134341A1 (en) | 2013-03-01 | 2014-02-27 | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016511258A JP2016511258A (ja) | 2016-04-14 |
| JP2016511258A5 JP2016511258A5 (enExample) | 2017-03-30 |
| JP6389830B2 true JP6389830B2 (ja) | 2018-09-12 |
Family
ID=50349866
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015560325A Active JP6389830B2 (ja) | 2013-03-01 | 2014-02-27 | 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 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9296734B2 (enExample) |
| EP (1) | EP2961749B1 (enExample) |
| JP (1) | JP6389830B2 (enExample) |
| AU (2) | AU2014223334C1 (enExample) |
| CA (1) | CA2902212C (enExample) |
| MX (1) | MX366855B (enExample) |
| TW (1) | TW201446758A (enExample) |
| UY (1) | UY35361A (enExample) |
| WO (1) | WO2014134341A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| RU2012129168A (ru) † | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| EA201591614A1 (ru) | 2013-03-08 | 2015-12-30 | Эмджен Инк. | Соединения 1,3-оксазин-2-амина, конденсированные с перфторированным циклопропилом, в качестве ингибиторов бета-секретазы и способы их применения |
| WO2014166906A1 (en) * | 2013-04-11 | 2014-10-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
| EA031132B1 (ru) | 2014-02-19 | 2018-11-30 | Х. Лундбекк А/С | 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| PE20181015A1 (es) | 2015-08-12 | 2018-06-26 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 |
| TW201726651A (zh) | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
| WO2017061534A1 (en) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dihydrothiazine derivatives |
| CA3009478A1 (en) | 2015-12-25 | 2017-06-29 | Shionogi & Co., Ltd. | Process and intermediates for preparation of thiazine derivatives |
| US20190055231A1 (en) * | 2016-03-01 | 2019-02-21 | Hoffmann-La Roche Inc. | Bace1 inhibitors |
| WO2018112086A1 (en) * | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| CN110546153B (zh) * | 2017-04-27 | 2022-09-06 | 巴斯夫欧洲公司 | 制备旋光2,3-二氢噻唑并[3,2-a]嘧啶-4-鎓化合物的方法 |
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