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 (enExample) | 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 (enExample) |
| EP (1) | EP2852597B1 (enExample) |
| JP (1) | JP6110937B2 (enExample) |
| AR (1) | AR090928A1 (enExample) |
| CA (1) | CA2872154C (enExample) |
| ES (1) | ES2585262T3 (enExample) |
| TW (1) | TW201406765A (enExample) |
| UY (1) | UY34778A (enExample) |
| WO (1) | WO2013164730A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | 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. |
| JP2015529239A (ja) | 2012-09-20 | 2015-10-05 | ファイザー・インク | アルキ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 |
| WO2014091352A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| CA2893333C (en) * | 2012-12-19 | 2017-10-24 | 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 |
| EP2956458B1 (en) | 2013-02-13 | 2017-08-09 | Pfizer Inc | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9233981B1 (en) * | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | アムジエン・インコーポレーテツド | β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法 |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| 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 |
| CA2944971C (en) | 2014-04-10 | 2019-05-07 | Pfizer Inc. | 2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8h)-yl-1,3-thiazol-4-yl amides |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | 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 |
| WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| WO2017051294A1 (en) | 2015-09-24 | 2017-03-30 | 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 |
| EP3353182A1 (en) * | 2015-09-24 | 2018-08-01 | Pfizer Inc | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| CA3047286A1 (en) | 2016-12-15 | 2018-06-21 | 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 |
| EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine 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 |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| WO2024079733A1 (en) * | 2022-10-12 | 2024-04-18 | Adama Makhteshim Ltd. | Process for the preparation of aminopyridazine derivatives |
Family Cites Families (71)
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| ATE239797T1 (de) | 1993-01-25 | 2003-05-15 | Takeda Chemical Industries Ltd | Antikörper gegen beta-amyloid oder derivative davon und seine verwendung |
| US8173127B2 (en) | 1997-04-09 | 2012-05-08 | Intellect Neurosciences, Inc. | Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof |
| DE69839808D1 (de) | 1997-04-09 | 2008-09-11 | Intellect Neurosciences Inc | Für die termini des beta-amyloids spezifische, rekombinante antikörper, dafür kodierende dna und verfahren zu ihrer verwendung |
| US6905686B1 (en) | 1997-12-02 | 2005-06-14 | Neuralab Limited | Active immunization for treatment of alzheimer's disease |
| TWI239847B (en) | 1997-12-02 | 2005-09-21 | Elan Pharm Inc | N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease |
| CZ304211B6 (cs) | 2000-02-24 | 2014-01-08 | Washington University | Humanizovaná protilátka, její fragment a jejich použití, polynukleová kyselina, expresní vektor, buňka a farmaceutický prostředek |
| DE10045112A1 (de) | 2000-09-11 | 2002-03-21 | Merck Patent Gmbh | Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems |
| EP1335738A4 (en) | 2000-11-03 | 2004-09-08 | Proteotech Inc | METHOD FOR ISOLATING AMYLOID-INHIBITING COMPOUNDS AND USE OF COMPOUNDS ISOLATED FROM UNCARIA TOMENTOSA AND RELATED PLANTS |
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| US20040146512A1 (en) | 2002-10-09 | 2004-07-29 | Arnon Rosenthal | Methods of treating Alzheimer's disease using antibodies directed against amyloid beta peptide and compositions thereof |
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| JP4227660B2 (ja) | 2004-05-12 | 2009-02-18 | ファイザー・プロダクツ・インク | ジペプチジルペプチダーゼｉｖインヒビターとしてのプロリン誘導体およびそれらの使用 |
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| US20050267009A1 (en) | 2004-05-28 | 2005-12-01 | Deagle William R | Method of Treatment of Acute and Persistent Pain |
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| EP2511269A4 (en) | 2009-12-11 | 2013-04-24 | Shionogi & Co | FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| WO2013030713A1 (en) * | 2011-08-31 | 2013-03-07 | 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. |
| EP2956458B1 (en) * | 2013-02-13 | 2017-08-09 | Pfizer Inc | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US11497586B2 (en) | 2014-03-21 | 2022-11-15 | Align Technology, Inc. | Segmented orthodontic appliance with elastics |
-
2013
- 2013-04-22 WO PCT/IB2013/053178 patent/WO2013164730A1/en not_active Ceased
- 2013-04-22 JP JP2015509531A patent/JP6110937B2/ja not_active Expired - Fee Related
- 2013-04-22 ES ES13725822.4T patent/ES2585262T3/es active Active
- 2013-04-22 CA CA2872154A patent/CA2872154C/en not_active Expired - Fee Related
- 2013-04-22 EP EP13725822.4A patent/EP2852597B1/en not_active Not-in-force
- 2013-05-02 TW TW102115730A patent/TW201406765A/zh 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
- 2013-05-03 AR ARP130101513A patent/AR090928A1/es unknown
-
2015
- 2015-01-09 US US14/593,587 patent/US20150133438A1/en not_active Abandoned
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