JP2018527387A5 - - Google Patents
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- Publication number
- JP2018527387A5 JP2018527387A5 JP2018514794A JP2018514794A JP2018527387A5 JP 2018527387 A5 JP2018527387 A5 JP 2018527387A5 JP 2018514794 A JP2018514794 A JP 2018514794A JP 2018514794 A JP2018514794 A JP 2018514794A JP 2018527387 A5 JP2018527387 A5 JP 2018527387A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyloxy
- cyclopropyl
- alkyl
- monohalo
- cyclopropyloxy
- 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
- 125000003545 alkoxy group Chemical group 0.000 claims description 56
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 25
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 22
- 206010012289 Dementia Diseases 0.000 claims description 18
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 claims description 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000001153 fluoro group Chemical group F* 0.000 claims description 10
- 208000024827 Alzheimer disease Diseases 0.000 claims description 9
- 125000005843 halogen group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims description 5
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims description 5
- 201000010374 Down Syndrome Diseases 0.000 claims description 5
- 201000002832 Lewy body dementia Diseases 0.000 claims description 5
- 208000018737 Parkinson disease Diseases 0.000 claims description 5
- 206010039966 Senile dementia Diseases 0.000 claims description 5
- 208000010877 cognitive disease Diseases 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000001425 triazolyl group Chemical group 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000009829 Lewy Body Disease Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 206010044688 Trisomy 21 Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15186394 | 2015-09-23 | ||
| EP15186394.1 | 2015-09-23 | ||
| EP16172005 | 2016-05-30 | ||
| EP16172005.7 | 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 JP2018527387A (ja) | 2018-09-20 |
| JP2018527387A5 true JP2018527387A5 (https=) | 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 (https=) |
| EP (1) | EP3353163B1 (https=) |
| JP (1) | JP2018527387A (https=) |
| KR (1) | KR20180053357A (https=) |
| CN (1) | CN108026069A (https=) |
| AU (1) | AU2016328589A1 (https=) |
| BR (1) | BR112018005591A2 (https=) |
| CA (1) | CA2995161A1 (https=) |
| EA (1) | EA035026B1 (https=) |
| HK (1) | HK1254800A1 (https=) |
| IL (1) | IL258217A (https=) |
| MX (1) | MX2018003565A (https=) |
| TW (1) | TW201726651A (https=) |
| WO (1) | WO2017050978A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20210261561A1 (en) * | 2018-04-23 | 2021-08-26 | Shionogi & Co., Ltd. | Bicyclic heterocycle derivatives having selective bace1 inhibitory activity |
| AU2019258575A1 (en) | 2018-04-27 | 2020-10-29 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
| 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 |
| 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 |
| 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 |
| MX339640B (es) * | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED 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 |
| 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 |
| 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 |
| KR20160115936A (ko) * | 2014-02-19 | 2016-10-06 | 하. 룬드벡 아크티에셀스카브 | 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘 |
-
2016
- 2016-09-21 TW TW105130403A patent/TW201726651A/zh unknown
- 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 CN CN201680055231.XA patent/CN108026069A/zh active Pending
- 2016-09-23 AU AU2016328589A patent/AU2016328589A1/en not_active Abandoned
- 2016-09-23 BR BR112018005591A patent/BR112018005591A2/pt not_active Application Discontinuation
- 2016-09-23 JP JP2018514794A patent/JP2018527387A/ja active Pending
- 2016-09-23 HK HK18113885.1A patent/HK1254800A1/zh unknown
- 2016-09-23 MX MX2018003565A patent/MX2018003565A/es unknown
- 2016-09-23 WO PCT/EP2016/072710 patent/WO2017050978A1/en not_active Ceased
- 2016-09-23 CA CA2995161A patent/CA2995161A1/en not_active Abandoned
- 2016-09-23 EA EA201890769A patent/EA035026B1/ru not_active IP Right Cessation
- 2016-09-23 US US15/761,304 patent/US20180334447A1/en not_active Abandoned
-
2018
- 2018-03-19 IL IL258217A patent/IL258217A/en unknown