JP2018522915A5 - - Google Patents
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- Publication number
- JP2018522915A5 JP2018522915A5 JP2018506862A JP2018506862A JP2018522915A5 JP 2018522915 A5 JP2018522915 A5 JP 2018522915A5 JP 2018506862 A JP2018506862 A JP 2018506862A JP 2018506862 A JP2018506862 A JP 2018506862A JP 2018522915 A5 JP2018522915 A5 JP 2018522915A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- isothiazolo
- thiazin
- fluorophenyl
- tetrahydro
- 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.)
- Granted
Links
- -1 ii) Independently Chemical group 0.000 claims 47
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical group 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 6
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 208000037259 Amyloid Plaque Diseases 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000037765 diseases and disorders Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- BWBHNKMXZHIPGB-UHFFFAOYSA-N 4-cyano-3-methylpyridine-2-carboxamide Chemical compound CC1=C(C#N)C=CN=C1C(N)=O BWBHNKMXZHIPGB-UHFFFAOYSA-N 0.000 claims 1
- HRHNVVBCKXBGOT-UHFFFAOYSA-N 5-methoxypyrazine-2-carboxamide Chemical compound COC1=CN=C(C(N)=O)C=N1 HRHNVVBCKXBGOT-UHFFFAOYSA-N 0.000 claims 1
- 102100021257 Beta-secretase 1 Human genes 0.000 claims 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15180767.4 | 2015-08-12 | ||
| EP15180767 | 2015-08-12 | ||
| PCT/EP2016/068830 WO2017025491A1 (en) | 2015-08-12 | 2016-08-08 | Bace1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018522915A JP2018522915A (ja) | 2018-08-16 |
| JP2018522915A5 true JP2018522915A5 (https=) | 2019-09-12 |
| JP6895424B2 JP6895424B2 (ja) | 2021-06-30 |
Family
ID=53835951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506862A Expired - Fee Related JP6895424B2 (ja) | 2015-08-12 | 2016-08-08 | Ｂａｃｅ１阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10246468B2 (https=) |
| EP (1) | EP3334742B1 (https=) |
| JP (1) | JP6895424B2 (https=) |
| CN (1) | CN107683283B (https=) |
| WO (1) | WO2017025491A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017025491A1 (en) * | 2015-08-12 | 2017-02-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
| KR102567590B1 (ko) | 2018-09-06 | 2023-08-17 | 다이이찌 산쿄 가부시키가이샤 | 신규 고리형 디뉴클레오티드 유도체 및 그 항체 약물 콘쥬게이트 |
| JP7495430B2 (ja) | 2019-04-17 | 2024-06-04 | バード・アクセス・システムズ，インコーポレーテッド | 長尺状医療部材を安定させるための固定装置およびカテーテルアセンブリの固定方法 |
| CN116059192B (zh) | 2019-11-13 | 2024-10-29 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| AU2024222719A1 (en) | 2023-02-16 | 2025-08-21 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2014111055A (ru) * | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| EP2852596B1 (en) * | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| PE20150021A1 (es) * | 2012-05-24 | 2015-01-28 | Hoffmann La Roche | 5-amino[1,4]tiazinas como inhibidores de bace1 |
| CN104968660A (zh) * | 2013-01-22 | 2015-10-07 | 霍夫曼-拉罗奇有限公司 | 作为bace1抑制剂的氟-[1,3]噁嗪类化合物 |
| WO2014150331A1 (en) * | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use |
| CN105683199B (zh) * | 2013-12-20 | 2018-06-26 | 豪夫迈·罗氏有限公司 | 5-芳基-1-亚氨基-1-氧代-[1，2，4]噻二嗪 |
| JP6594403B2 (ja) * | 2014-07-25 | 2019-10-23 | エフ．ホフマン−ラ ロシュ アーゲー | ピリジル−トリアザビシクル |
| JP6568937B2 (ja) * | 2014-10-10 | 2019-08-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂａｃｅ１阻害剤 |
| JP6554547B2 (ja) * | 2014-11-03 | 2019-07-31 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂａｃｅ１阻害剤 |
| WO2017025491A1 (en) * | 2015-08-12 | 2017-02-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
-
2016
- 2016-08-08 WO PCT/EP2016/068830 patent/WO2017025491A1/en not_active Ceased
- 2016-08-08 CN CN201680031828.0A patent/CN107683283B/zh not_active Expired - Fee Related
- 2016-08-08 EP EP16754452.7A patent/EP3334742B1/en not_active Not-in-force
- 2016-08-08 JP JP2018506862A patent/JP6895424B2/ja not_active Expired - Fee Related
- 2016-08-08 US US15/735,890 patent/US10246468B2/en not_active Expired - Fee Related
-
2019
- 2019-02-13 US US16/274,911 patent/US10696691B2/en not_active Expired - Fee Related
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