JP2015520140A5 - - Google Patents
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- Publication number
- JP2015520140A5 JP2015520140A5 JP2015509531A JP2015509531A JP2015520140A5 JP 2015520140 A5 JP2015520140 A5 JP 2015520140A5 JP 2015509531 A JP2015509531 A JP 2015509531A JP 2015509531 A JP2015509531 A JP 2015509531A JP 2015520140 A5 JP2015520140 A5 JP 2015520140A5
- Authority
- JP
- Japan
- Prior art keywords
- tautomer
- compound
- alkyl
- pharmaceutically acceptable
- cycloalkyl
- 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 35
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000001153 fluoro group Chemical group F* 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 *C([C@@]1(C[C@](*)OC2)I)NC(*)=*[C@]12c(ccc(N)c1)c1N Chemical compound *C([C@@]1(C[C@](*)OC2)I)NC(*)=*[C@]12c(ccc(N)c1)c1N 0.000 description 1
- KCRIWCAXODSLRH-FGDXXIHYSA-N C[n]1nc([C@@H]2OC[C@]3(c(c(F)c4)ccc4F)N=C(N)SC[C@@H]3C2)cc1 Chemical compound C[n]1nc([C@@H]2OC[C@]3(c(c(F)c4)ccc4F)N=C(N)SC[C@@H]3C2)cc1 KCRIWCAXODSLRH-FGDXXIHYSA-N 0.000 description 1
- JYDYMWJEZLKIBS-CXMBCZLWSA-N C[n]1ncc([C@@H]2OC[C@]3(c(ccc(F)c4)c4F)N=C(N)SC[C@@H]3C2)c1 Chemical compound C[n]1ncc([C@@H]2OC[C@]3(c(ccc(F)c4)c4F)N=C(N)SC[C@@H]3C2)c1 JYDYMWJEZLKIBS-CXMBCZLWSA-N 0.000 description 1
- FEUAZHJMDOKMNX-FGDXXIHYSA-N C[n]1nccc1[C@@H]1OC[C@]2(c(c(F)c3)ccc3F)N=C(N)SC[C@@H]2C1 Chemical compound C[n]1nccc1[C@@H]1OC[C@]2(c(c(F)c3)ccc3F)N=C(N)SC[C@@H]2C1 FEUAZHJMDOKMNX-FGDXXIHYSA-N 0.000 description 1
- CTLGKGNBFWVQKZ-IXBGWNDUSA-N Cc1c[s]c([C@@H]2OC[C@]3(c(c(F)c4)ccc4F)N=C(N)SC[C@@H]3C2)n1 Chemical compound Cc1c[s]c([C@@H]2OC[C@]3(c(c(F)c4)ccc4F)N=C(N)SC[C@@H]3C2)n1 CTLGKGNBFWVQKZ-IXBGWNDUSA-N 0.000 description 1
- MWNPEMNPLJPNHT-JVMOKEISSA-N NC(SC[C@@H]1C[C@H](c2n[n](C3CC3)cc2)OC2)=N[C@]12c(c(F)c1)ccc1F Chemical compound NC(SC[C@@H]1C[C@H](c2n[n](C3CC3)cc2)OC2)=N[C@]12c(c(F)c1)ccc1F MWNPEMNPLJPNHT-JVMOKEISSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261642480P | 2012-05-04 | 2012-05-04 | |
| US61/642,480 | 2012-05-04 | ||
| PCT/IB2013/053178 WO2013164730A1 (en) | 2012-05-04 | 2013-04-22 | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015520140A JP2015520140A (ja) | 2015-07-16 |
| JP2015520140A5 true JP2015520140A5 (cg-RX-API-DMAC7.html) | 2016-06-16 |
| JP6110937B2 JP6110937B2 (ja) | 2017-04-05 |
Family
ID=48536971
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015509531A Expired - Fee Related JP6110937B2 (ja) | 2012-05-04 | 2013-04-22 | ＡＰＰ、ＢＡＣＥ１、およびＢＡＣＥ２の阻害剤としての複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8962616B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2852597B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6110937B2 (cg-RX-API-DMAC7.html) |
| AR (1) | AR090928A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2872154C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2585262T3 (cg-RX-API-DMAC7.html) |
| TW (1) | TW201406765A (cg-RX-API-DMAC7.html) |
| UY (1) | UY34778A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2013164730A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2751116B1 (en) | 2011-08-31 | 2016-10-12 | Pfizer Inc | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| WO2013164730A1 (en) | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| CA2882389A1 (en) | 2012-09-20 | 2014-03-27 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| WO2014091352A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| EP2935282A1 (en) * | 2012-12-19 | 2015-10-28 | Pfizer Inc. | CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS |
| WO2014120658A1 (en) | 2013-01-29 | 2014-08-07 | Amgen Inc. | Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors |
| JP2016507551A (ja) | 2013-02-13 | 2016-03-10 | ファイザー・インク | ヘテロアリール置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| 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 |
| HK1217486A1 (zh) | 2013-03-08 | 2017-01-13 | Amgen Inc. | 作爲β-分泌酶抑制剂的全氟化环丙基稠合的1，3-恶嗪-2-胺化合物以及其使用方法 |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Ｂａｃｅ抑制劑 |
| US9096615B2 (en) | 2013-07-30 | 2015-08-04 | Amgen Inc. | Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof |
| PE20170327A1 (es) | 2014-04-10 | 2017-04-21 | Pfizer | 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| MA41101A (fr) * | 2014-12-03 | 2017-10-10 | Lilly Co Eli | Dispositif d'injection de médicament automatique comportant une indication audible de progression d'injection |
| US10246429B2 (en) | 2015-08-06 | 2019-04-02 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| EP3353182A1 (en) * | 2015-09-24 | 2018-08-01 | Pfizer Inc | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| EP3353174A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl]amides useful as bace inhibitors |
| EP3353183A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides |
| AU2017376446B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| MA52722A (fr) | 2016-12-15 | 2021-04-14 | Amgen Inc | Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CN107892697B (zh) | 2016-12-26 | 2020-11-03 | 郑州泰基鸿诺医药股份有限公司 | 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物 |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| WO2024079733A1 (en) * | 2022-10-12 | 2024-04-18 | Adama Makhteshim Ltd. | Process for the preparation of aminopyridazine derivatives |
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| WO2013164730A1 (en) | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
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-
2013
- 2013-04-22 WO PCT/IB2013/053178 patent/WO2013164730A1/en not_active Ceased
- 2013-04-22 EP EP13725822.4A patent/EP2852597B1/en not_active Not-in-force
- 2013-04-22 CA CA2872154A patent/CA2872154C/en not_active Expired - Fee Related
- 2013-04-22 ES ES13725822.4T patent/ES2585262T3/es active Active
- 2013-04-22 JP JP2015509531A patent/JP6110937B2/ja not_active Expired - Fee Related
- 2013-05-02 TW TW102115730A patent/TW201406765A/zh unknown
- 2013-05-03 AR ARP130101513A patent/AR090928A1/es unknown
- 2013-05-03 US US13/886,405 patent/US8962616B2/en not_active Expired - Fee Related
- 2013-05-03 UY UY0001034778A patent/UY34778A/es unknown
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2015
- 2015-01-09 US US14/593,587 patent/US20150133438A1/en not_active Abandoned