TW201726651A - 2,3,4,5-四氫吡啶-6-胺衍生物 - Google Patents
2,3,4,5-四氫吡啶-6-胺衍生物 Download PDFInfo
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- TW201726651A TW201726651A TW105130403A TW105130403A TW201726651A TW 201726651 A TW201726651 A TW 201726651A TW 105130403 A TW105130403 A TW 105130403A TW 105130403 A TW105130403 A TW 105130403A TW 201726651 A TW201726651 A TW 201726651A
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- Prior art keywords
- alkyloxy
- alkyl
- compound
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- cyclopropyl
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- VJMRARQYHSPMKG-HNNXBMFYSA-N tert-butyl n-[(2s)-2-(5-bromo-2-fluorophenyl)-4-oxobutan-2-yl]carbamate Chemical compound CC(C)(C)OC(=O)N[C@@](C)(CC=O)C1=CC(Br)=CC=C1F VJMRARQYHSPMKG-HNNXBMFYSA-N 0.000 description 1
- OSBSFAARYOCBHB-UHFFFAOYSA-N tetrapropylammonium Chemical compound CCC[N+](CCC)(CCC)CCC OSBSFAARYOCBHB-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- GZNAASVAJNXPPW-UHFFFAOYSA-M tin(4+) chloride dihydrate Chemical compound O.O.[Cl-].[Sn+4] GZNAASVAJNXPPW-UHFFFAOYSA-M 0.000 description 1
- FWPIDFUJEMBDLS-UHFFFAOYSA-L tin(II) chloride dihydrate Substances O.O.Cl[Sn]Cl FWPIDFUJEMBDLS-UHFFFAOYSA-L 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- PQDJYEQOELDLCP-UHFFFAOYSA-N trimethylsilane Chemical compound C[SiH](C)C PQDJYEQOELDLCP-UHFFFAOYSA-N 0.000 description 1
- 229940094989 trimethylsilane Drugs 0.000 description 1
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960004418 trolamine Drugs 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 238000001195 ultra high performance liquid chromatography Methods 0.000 description 1
- 238000004704 ultra performance liquid chromatography Methods 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
- 229940007718 zinc hydroxide Drugs 0.000 description 1
- 229910021511 zinc hydroxide Inorganic materials 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)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15186394 | 2015-09-23 | ||
| EP16172005 | 2016-05-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201726651A true TW201726651A (zh) | 2017-08-01 |
Family
ID=56985626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105130403A TW201726651A (zh) | 2015-09-23 | 2016-09-21 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
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 |
| KR20210003872A (ko) | 2018-04-27 | 2021-01-12 | 시오노기 앤드 컴파니, 리미티드 | 선택적 bace1 억제 활성을 갖는 테트라하이드로피라노옥사진 유도체 |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| US20120258961A1 (en) * | 2009-12-24 | 2012-10-11 | Shionogi & Co., Ltd. | 4-amino-1,3-thiazine or oxazine derivative |
| 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 |
| EP2580200B1 (en) * | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| 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 |
| 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 |
| TW201446758A (zh) | 2013-03-01 | 2014-12-16 | Amgen Inc | 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途 |
| PE20161225A1 (es) | 2014-02-19 | 2016-12-04 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
-
2016
- 2016-09-21 TW TW105130403A patent/TW201726651A/zh unknown
- 2016-09-23 WO PCT/EP2016/072710 patent/WO2017050978A1/en not_active Ceased
- 2016-09-23 US US15/761,304 patent/US20180334447A1/en not_active Abandoned
- 2016-09-23 EA EA201890769A patent/EA035026B1/ru not_active IP Right Cessation
- 2016-09-23 JP JP2018514794A patent/JP2018527387A/ja active Pending
- 2016-09-23 BR BR112018005591A patent/BR112018005591A2/pt not_active Application Discontinuation
- 2016-09-23 HK HK18113885.1A patent/HK1254800A1/zh unknown
- 2016-09-23 CN CN201680055231.XA patent/CN108026069A/zh active Pending
- 2016-09-23 CA CA2995161A patent/CA2995161A1/en not_active Abandoned
- 2016-09-23 KR KR1020187010344A patent/KR20180053357A/ko not_active Withdrawn
- 2016-09-23 EP EP16770283.6A patent/EP3353163B1/en active Active
- 2016-09-23 MX MX2018003565A patent/MX2018003565A/es unknown
- 2016-09-23 AU AU2016328589A patent/AU2016328589A1/en not_active Abandoned
-
2018
- 2018-03-19 IL IL258217A patent/IL258217A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018527387A (ja) | 2018-09-20 |
| KR20180053357A (ko) | 2018-05-21 |
| EA201890769A1 (ru) | 2018-09-28 |
| EA035026B1 (ru) | 2020-04-20 |
| HK1254800A1 (zh) | 2019-07-26 |
| US20180334447A1 (en) | 2018-11-22 |
| CN108026069A (zh) | 2018-05-11 |
| EP3353163B1 (en) | 2020-02-05 |
| AU2016328589A1 (en) | 2018-03-01 |
| WO2017050978A1 (en) | 2017-03-30 |
| CA2995161A1 (en) | 2017-03-30 |
| EP3353163A1 (en) | 2018-08-01 |
| IL258217A (en) | 2018-05-31 |
| MX2018003565A (es) | 2018-06-18 |
| BR112018005591A2 (pt) | 2018-10-09 |
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