JP2018527387A - ２，３，４，５−テトラヒドロピリジン−６−アミン誘導体 - Google Patents
２，３，４，５−テトラヒドロピリジン−６−アミン誘導体 Download PDFInfo
- Publication number
- JP2018527387A JP2018527387A JP2018514794A JP2018514794A JP2018527387A JP 2018527387 A JP2018527387 A JP 2018527387A JP 2018514794 A JP2018514794 A JP 2018514794A JP 2018514794 A JP2018514794 A JP 2018514794A JP 2018527387 A JP2018527387 A JP 2018527387A
- Authority
- JP
- Japan
- Prior art keywords
- alkyloxy
- alkyl
- mmol
- cyclopropyl
- monohalo
- 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.)
- Pending
Links
- 0 CC(*)(CC1(*)*)C(N)=N[C@]1(C(*)*)c1cc([N+]([O-])=O)cc(C)c1F Chemical compound CC(*)(CC1(*)*)C(N)=N[C@]1(C(*)*)c1cc([N+]([O-])=O)cc(C)c1F 0.000 description 14
- BTZVDHBDOQYASD-GFCCVEGCSA-N C=[Br]c(cc1[C@@](CC=O)(CF)NC(C(F)(F)F)=O)ccc1F Chemical compound C=[Br]c(cc1[C@@](CC=O)(CF)NC(C(F)(F)F)=O)ccc1F BTZVDHBDOQYASD-GFCCVEGCSA-N 0.000 description 1
- OAOVEUGPMQFVIV-UWBLVGDVSA-N CC(C)(C)OC(N[C@@](C)(CCC(C#N)S(C)(=O)=O)c1cc(Br)ccc1F)=O Chemical compound CC(C)(C)OC(N[C@@](C)(CCC(C#N)S(C)(=O)=O)c1cc(Br)ccc1F)=O OAOVEUGPMQFVIV-UWBLVGDVSA-N 0.000 description 1
- LNCJPLFJCVYMIJ-WMLDXEAASA-N CC(C)(C)OC(N[C@]1([C@H](CC(C#N)C#N)O)[F]c2c1cccc2)=O Chemical compound CC(C)(C)OC(N[C@]1([C@H](CC(C#N)C#N)O)[F]c2c1cccc2)=O LNCJPLFJCVYMIJ-WMLDXEAASA-N 0.000 description 1
- SXYPRIFQQFHTAG-UHFFFAOYSA-N CC(C1)(C(N)=NC(C)(c(cc(cc2)NC(c(nc3)cnc3OCF)=O)c2F)S1C=[O]C)C#N Chemical compound CC(C1)(C(N)=NC(C)(c(cc(cc2)NC(c(nc3)cnc3OCF)=O)c2F)S1C=[O]C)C#N SXYPRIFQQFHTAG-UHFFFAOYSA-N 0.000 description 1
- ZRBUWAUVWNTJBJ-GICMACPYSA-N CCC(CC1)(C(N)=N[C@]1(CF)c1ccccc1F)S(C)(=O)=O Chemical compound CCC(CC1)(C(N)=N[C@]1(CF)c1ccccc1F)S(C)(=O)=O ZRBUWAUVWNTJBJ-GICMACPYSA-N 0.000 description 1
- ZKABADWMITUHLU-MRXNPFEDSA-N CCOC(C([C@@](C)(c1ccccc1F)NC(OC(C)(C)C)=O)(F)F)=O Chemical compound CCOC(C([C@@](C)(c1ccccc1F)NC(OC(C)(C)C)=O)(F)F)=O ZKABADWMITUHLU-MRXNPFEDSA-N 0.000 description 1
- SVHLBOPEFKZOCS-GOSISDBHSA-N OCC[C@@](CF)(c1cc(Br)ccc1F)NC(OCc1ccccc1)=O Chemical compound OCC[C@@](CF)(c1cc(Br)ccc1F)NC(OCc1ccccc1)=O SVHLBOPEFKZOCS-GOSISDBHSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/84—Nitriles
- C07D213/85—Nitriles in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15186394.1 | 2015-09-23 | ||
| EP15186394 | 2015-09-23 | ||
| EP16172005.7 | 2016-05-30 | ||
| EP16172005 | 2016-05-30 | ||
| PCT/EP2016/072710 WO2017050978A1 (en) | 2015-09-23 | 2016-09-23 | 2,3,4,5-tetrahydropyridin-6-amine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018527387A true JP2018527387A (ja) | 2018-09-20 |
| JP2018527387A5 JP2018527387A5 (enExample) | 2019-11-14 |
Family
ID=56985626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018514794A Pending JP2018527387A (ja) | 2015-09-23 | 2016-09-23 | ２，３，４，５−テトラヒドロピリジン−６−アミン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20180334447A1 (enExample) |
| EP (1) | EP3353163B1 (enExample) |
| JP (1) | JP2018527387A (enExample) |
| KR (1) | KR20180053357A (enExample) |
| CN (1) | CN108026069A (enExample) |
| AU (1) | AU2016328589A1 (enExample) |
| BR (1) | BR112018005591A2 (enExample) |
| CA (1) | CA2995161A1 (enExample) |
| EA (1) | EA035026B1 (enExample) |
| HK (1) | HK1254800A1 (enExample) |
| IL (1) | IL258217A (enExample) |
| MX (1) | MX2018003565A (enExample) |
| TW (1) | TW201726651A (enExample) |
| WO (1) | WO2017050978A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022511167A (ja) * | 2018-04-23 | 2022-01-31 | 塩野義製薬株式会社 | 選択的ｂａｃｅ１阻害活性を有する二環式複素環誘導体 |
| 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 |
| CN114380736B (zh) * | 2020-10-21 | 2023-10-03 | 复旦大学 | 一种2,3,4,5-四氢吡啶类化合物的合成方法 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011077726A1 (ja) * | 2009-12-24 | 2011-06-30 | 塩野義製薬株式会社 | ４－アミノ－１，３－チアジンまたはオキサジン誘導体 |
| JP2013500247A (ja) * | 2009-07-24 | 2013-01-07 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用 |
| JP2013531645A (ja) * | 2010-06-09 | 2013-08-08 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−２Ｈ−［１，４］オキサジン−３−イル−アミン誘導体 |
| WO2014059185A1 (en) * | 2012-10-12 | 2014-04-17 | Amgen Inc. | Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| WO2015124576A1 (en) * | 2014-02-19 | 2015-08-27 | H. Lundbeck A/S | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| US8815841B2 (en) | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| 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 |
-
2016
- 2016-09-21 TW TW105130403A patent/TW201726651A/zh unknown
- 2016-09-23 CN CN201680055231.XA patent/CN108026069A/zh active Pending
- 2016-09-23 US US15/761,304 patent/US20180334447A1/en not_active Abandoned
- 2016-09-23 BR BR112018005591A patent/BR112018005591A2/pt not_active Application Discontinuation
- 2016-09-23 WO PCT/EP2016/072710 patent/WO2017050978A1/en not_active Ceased
- 2016-09-23 MX MX2018003565A patent/MX2018003565A/es unknown
- 2016-09-23 CA CA2995161A patent/CA2995161A1/en not_active Abandoned
- 2016-09-23 AU AU2016328589A patent/AU2016328589A1/en not_active Abandoned
- 2016-09-23 EA EA201890769A patent/EA035026B1/ru not_active IP Right Cessation
- 2016-09-23 EP EP16770283.6A patent/EP3353163B1/en active Active
- 2016-09-23 HK HK18113885.1A patent/HK1254800A1/zh unknown
- 2016-09-23 KR KR1020187010344A patent/KR20180053357A/ko not_active Withdrawn
- 2016-09-23 JP JP2018514794A patent/JP2018527387A/ja active Pending
-
2018
- 2018-03-19 IL IL258217A patent/IL258217A/en unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013500247A (ja) * | 2009-07-24 | 2013-01-07 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用 |
| WO2011077726A1 (ja) * | 2009-12-24 | 2011-06-30 | 塩野義製薬株式会社 | ４－アミノ－１，３－チアジンまたはオキサジン誘導体 |
| JP2013531645A (ja) * | 2010-06-09 | 2013-08-08 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−２Ｈ−［１，４］オキサジン−３−イル−アミン誘導体 |
| WO2014059185A1 (en) * | 2012-10-12 | 2014-04-17 | Amgen Inc. | Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| WO2015124576A1 (en) * | 2014-02-19 | 2015-08-27 | H. Lundbeck A/S | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
Non-Patent Citations (1)
| Title |
|---|
| ＭＯＬＥＣＵＬＡＲ ＮＥＵＲＯＤＥＧＥＮＥＲＡＴＩＯＮ, vol. 10, JPN6020030965, 2015, pages 11 - 1, ISSN: 0004469713 * |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112018005591A2 (pt) | 2018-10-09 |
| IL258217A (en) | 2018-05-31 |
| CA2995161A1 (en) | 2017-03-30 |
| CN108026069A (zh) | 2018-05-11 |
| KR20180053357A (ko) | 2018-05-21 |
| WO2017050978A1 (en) | 2017-03-30 |
| TW201726651A (zh) | 2017-08-01 |
| EA201890769A1 (ru) | 2018-09-28 |
| EP3353163A1 (en) | 2018-08-01 |
| AU2016328589A1 (en) | 2018-03-01 |
| HK1254800A1 (zh) | 2019-07-26 |
| MX2018003565A (es) | 2018-06-18 |
| EA035026B1 (ru) | 2020-04-20 |
| EP3353163B1 (en) | 2020-02-05 |
| US20180334447A1 (en) | 2018-11-22 |
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