JP2020503293A5 - - Google Patents
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- Publication number
- JP2020503293A5 JP2020503293A5 JP2019531733A JP2019531733A JP2020503293A5 JP 2020503293 A5 JP2020503293 A5 JP 2020503293A5 JP 2019531733 A JP2019531733 A JP 2019531733A JP 2019531733 A JP2019531733 A JP 2019531733A JP 2020503293 A5 JP2020503293 A5 JP 2020503293A5
- Authority
- JP
- Japan
- Prior art keywords
- tautomer
- compound
- pharmaceutically acceptable
- oxazine
- dihydro
- 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
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- 150000001875 compounds Chemical class 0.000 claims 92
- 150000003839 salts Chemical class 0.000 claims 40
- -1 2-propynyloxy Chemical group 0.000 claims 22
- 206010012289 Dementia Diseases 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 6
- 229920002554 vinyl polymer Polymers 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims 4
- GZPHSAQLYPIAIN-UHFFFAOYSA-N 3-pyridinecarbonitrile Chemical compound N#CC1=CC=CN=C1 GZPHSAQLYPIAIN-UHFFFAOYSA-N 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- NPVLTRVVFXHZFP-SUDDELGHSA-N (1R,5S,6R)-5-[5-[(Z)-2-(5-bromopyridin-2-yl)-2-fluoroethenyl]-2-fluorophenyl]-5-(difluoromethyl)-2-oxa-4-azabicyclo[4.1.0]hept-3-en-3-amine Chemical compound BrC=1C=CC(=NC=1)/C(=C/C=1C=CC(=C(C=1)[C@]1(N=C(O[C@@H]2C[C@H]12)N)C(F)F)F)/F NPVLTRVVFXHZFP-SUDDELGHSA-N 0.000 claims 2
- ZOVHIIZTAZMGBH-MUWWNJSCSA-N (3R,6R)-3-[2-fluoro-5-[(Z)-2-fluoro-2-[5-(2,2,3,3-tetrafluoropropoxy)pyrazin-2-yl]ethenyl]phenyl]-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-5-amine Chemical compound C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)c1cc(\C=C(/F)c2cnc(OCC(F)(F)C(F)F)cn2)ccc1F ZOVHIIZTAZMGBH-MUWWNJSCSA-N 0.000 claims 2
- BBZZNAFTKLSHGA-OTEYBFNZSA-N (4R,5R)-4-[5-[(Z)-2-(5-chloropyrazin-2-yl)-2-fluoroethenyl]-2-fluorophenyl]-4-methyl-5-(2,2,2-trifluoroethoxy)-5,6-dihydro-1,3-oxazin-2-amine Chemical compound C[C@@]1(N=C(N)OC[C@@H]1OCC(F)(F)F)C1=C(F)C=CC(\C=C(/F)C2=CN=C(Cl)C=N2)=C1 BBZZNAFTKLSHGA-OTEYBFNZSA-N 0.000 claims 2
- MRJDCHZAQCMNRN-DRRIMPMXSA-N 5-[(Z)-2-[3-[(3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-3-yl]-4-fluorophenyl]-1-fluoroethenyl]pyrazine-2-carbonitrile Chemical compound C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)C1=C(F)C=CC(\C=C(/F)C2=NC=C(N=C2)C#N)=C1 MRJDCHZAQCMNRN-DRRIMPMXSA-N 0.000 claims 2
- ZIGJKNSPSNZHBM-SCRWAHJHSA-N 6-[(Z)-2-[3-[(1R,5S,6R)-3-amino-5-(difluoromethyl)-2-oxa-4-azabicyclo[4.1.0]hept-3-en-5-yl]-4-fluorophenyl]-1-fluoroethenyl]pyridine-3-carbonitrile Chemical compound NC=1O[C@@H]2C[C@@H]2[C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)\C=C(/F)\C1=NC=C(C#N)C=C1 ZIGJKNSPSNZHBM-SCRWAHJHSA-N 0.000 claims 2
- XROVXQIOOHYIEI-QMBGAUKWSA-N 6-[(Z)-2-[3-[(3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-3-yl]-4-fluorophenyl]-1-fluoroethenyl]pyridine-3-carbonitrile Chemical compound NC1=N[C@](CO[C@]1(C(F)(F)F)C)(C)C=1C=C(C=CC=1F)\C=C(/F)\C1=NC=C(C#N)C=C1 XROVXQIOOHYIEI-QMBGAUKWSA-N 0.000 claims 2
- MYSYGHGDPRBXTH-CFVWZZDWSA-N 6-[(Z)-2-[6-[(3R,6R)-5-amino-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-3-yl]-5-fluoropyridin-2-yl]-1-fluoroethenyl]pyridine-3-carbonitrile Chemical compound C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)C1=C(F)C=CC(\C=C(/F)C2=CC=C(C=N2)C#N)=N1 MYSYGHGDPRBXTH-CFVWZZDWSA-N 0.000 claims 2
- WCRACBGOKSPQOO-YBSJANCESA-N 6-[(Z)-2-[6-[(4R)-2-amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-1-fluoroethenyl]pyridine-3-carbonitrile Chemical compound NC=1OCC([C@@](N=1)(C)C1=C(C=CC(=N1)\C=C(/F)\C1=NC=C(C#N)C=C1)F)(F)F WCRACBGOKSPQOO-YBSJANCESA-N 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 2
- 206010002022 amyloidosis Diseases 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 230000002490 cerebral effect Effects 0.000 claims 2
- 210000001175 cerebrospinal fluid Anatomy 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- PMSVVUSIPKHUMT-UHFFFAOYSA-N cyanopyrazine Chemical compound N#CC1=CN=CC=N1 PMSVVUSIPKHUMT-UHFFFAOYSA-N 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 230000007505 plaque formation Effects 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- YFHYGSFFXCLGBK-SUDDELGHSA-N (1R,5S,6R)-5-[5-[(Z)-2-(5-chloropyridin-2-yl)-2-fluoroethenyl]-2-fluorophenyl]-5-(difluoromethyl)-2-oxa-4-azabicyclo[4.1.0]hept-3-en-3-amine Chemical compound NC1=N[C@@](C(F)F)([C@H]2C[C@H]2O1)c1cc(\C=C(/F)c2ccc(Cl)cn2)ccc1F YFHYGSFFXCLGBK-SUDDELGHSA-N 0.000 claims 1
- GNGCALJQBOTLAV-JXSYVVILSA-N (3R,6R)-3-[5-[(Z)-2-(5-chloropyrazin-2-yl)-2-fluoroethenyl]-2-fluorophenyl]-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-5-amine Chemical compound C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)C1=C(F)C=CC(\C=C(/F)C2=CN=C(Cl)C=N2)=C1 GNGCALJQBOTLAV-JXSYVVILSA-N 0.000 claims 1
- NUQAAASQOFLUMN-RNAGXQGASA-N (3R,6R)-3-[5-[(Z)-2-(5-chloropyridin-2-yl)-2-fluoroethenyl]-2-fluorophenyl]-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-oxazin-5-amine Chemical compound C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)C1=C(F)C=CC(\C=C(/F)C2=NC=C(Cl)C=C2)=C1 NUQAAASQOFLUMN-RNAGXQGASA-N 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 206010048327 Supranuclear palsy Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- TURAMGVWNUTQKH-UHFFFAOYSA-N propa-1,2-dien-1-one Chemical group C=C=C=O TURAMGVWNUTQKH-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434711P | 2016-12-15 | 2016-12-15 | |
| US62/434,711 | 2016-12-15 | ||
| US201762570425P | 2017-10-10 | 2017-10-10 | |
| US62/570,425 | 2017-10-10 | ||
| PCT/US2017/066177 WO2018112081A1 (en) | 2016-12-15 | 2017-12-13 | Oxazine derivatives as beta-secretase inhibitors and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020503293A JP2020503293A (ja) | 2020-01-30 |
| JP2020503293A5 true JP2020503293A5 (cg-RX-API-DMAC10.html) | 2021-01-28 |
| JP7177773B2 JP7177773B2 (ja) | 2022-11-24 |
Family
ID=60888744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531733A Active JP7177773B2 (ja) | 2016-12-15 | 2017-12-13 | β－セクレターゼ阻害剤としてのオキサジン誘導体および使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10947223B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP3555080B1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP7177773B2 (cg-RX-API-DMAC10.html) |
| AU (1) | AU2017376441B2 (cg-RX-API-DMAC10.html) |
| CA (1) | CA3047286A1 (cg-RX-API-DMAC10.html) |
| MA (1) | MA52722A (cg-RX-API-DMAC10.html) |
| MX (1) | MX388696B (cg-RX-API-DMAC10.html) |
| WO (1) | WO2018112081A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2012129168A (ru) † | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| WO2018112086A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
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2017
- 2017-12-13 WO PCT/US2017/066177 patent/WO2018112081A1/en not_active Ceased
- 2017-12-13 JP JP2019531733A patent/JP7177773B2/ja active Active
- 2017-12-13 US US16/466,211 patent/US10947223B2/en active Active
- 2017-12-13 CA CA3047286A patent/CA3047286A1/en active Pending
- 2017-12-13 MA MA052722A patent/MA52722A/fr unknown
- 2017-12-13 MX MX2019007101A patent/MX388696B/es unknown
- 2017-12-13 AU AU2017376441A patent/AU2017376441B2/en active Active
- 2017-12-13 EP EP17822984.5A patent/EP3555080B1/en active Active