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
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3555080B1 (enExample) |
| JP (1) | JP7177773B2 (enExample) |
| AU (1) | AU2017376441B2 (enExample) |
| CA (1) | CA3047286A1 (enExample) |
| MA (1) | MA52722A (enExample) |
| MX (1) | MX388696B (enExample) |
| WO (1) | WO2018112081A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012006491A (es) † | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| MX394391B (es) | 2016-12-15 | 2025-03-24 | Amgen Inc | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. |
| 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 |
| CA3047288A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| AU2019258575A1 (en) | 2018-04-27 | 2020-10-29 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
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| SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
| JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
| PL205294B1 (pl) | 1998-09-24 | 2010-03-31 | Upjohn Co | Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta |
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2017
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- 2017-12-13 MX MX2019007101A patent/MX388696B/es unknown
- 2017-12-13 MA MA052722A patent/MA52722A/fr unknown
- 2017-12-13 JP JP2019531733A patent/JP7177773B2/ja active Active
- 2017-12-13 EP EP17822984.5A patent/EP3555080B1/en active Active
- 2017-12-13 WO PCT/US2017/066177 patent/WO2018112081A1/en not_active Ceased
- 2017-12-13 US US16/466,211 patent/US10947223B2/en active Active
- 2017-12-13 CA CA3047286A patent/CA3047286A1/en active Pending