JP2018140987A5 - - Google Patents
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- Publication number
- JP2018140987A5 JP2018140987A5 JP2018045585A JP2018045585A JP2018140987A5 JP 2018140987 A5 JP2018140987 A5 JP 2018140987A5 JP 2018045585 A JP2018045585 A JP 2018045585A JP 2018045585 A JP2018045585 A JP 2018045585A JP 2018140987 A5 JP2018140987 A5 JP 2018140987A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- compound
- pharmaceutically acceptable
- tetrahydrofuro
- thiazin
- 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
- 150000003839 salts Chemical class 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 27
- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims description 9
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims description 4
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 238000002441 X-ray diffraction Methods 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 238000001228 spectrum Methods 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 3
- 102100021257 Beta-secretase 1 Human genes 0.000 description 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 description 1
- JJADJMODPHLYCB-DAESXHAQSA-N N-[3-[(4aS,5S,7aS)-2-amino-5-(1,1-difluoroethyl)-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide Chemical compound NC=1SC[C@H]2[C@@](N=1)(CO[C@@H]2C(C)(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(C=C1)C#N JJADJMODPHLYCB-DAESXHAQSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562154242P | 2015-04-29 | 2015-04-29 | |
| US62/154,242 | 2015-04-29 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567244A Division JP2017515831A (ja) | 2015-04-29 | 2016-04-22 | 選択的ｂａｃｅ１阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018140987A JP2018140987A (ja) | 2018-09-13 |
| JP2018140987A5 true JP2018140987A5 (https=) | 2019-05-30 |
| JP6777668B2 JP6777668B2 (ja) | 2020-10-28 |
Family
ID=55861291
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567244A Withdrawn JP2017515831A (ja) | 2015-04-29 | 2016-04-22 | 選択的ｂａｃｅ１阻害剤 |
| JP2018045585A Active JP6777668B2 (ja) | 2015-04-29 | 2018-03-13 | 選択的ｂａｃｅ１阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567244A Withdrawn JP2017515831A (ja) | 2015-04-29 | 2016-04-22 | 選択的ｂａｃｅ１阻害剤 |
Country Status (40)
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR103680A1 (es) * | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| AR110470A1 (es) * | 2016-10-21 | 2019-04-03 | Lilly Co Eli | Terapia de combinación para tratar la enfermedad de alzheimer |
| US11559528B2 (en) * | 2019-09-05 | 2023-01-24 | The Cleveland Clinic Foundation | BACE1 inhibition for the treatment of cancer |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20070135A1 (es) | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| PL2233474T3 (pl) | 2008-01-18 | 2015-12-31 | Eisai R&D Man Co Ltd | Skondensowana pochodna aminodihydrotiazyny |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| JP5666304B2 (ja) | 2008-09-30 | 2015-02-12 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| WO2011071057A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US20140235626A1 (en) * | 2011-04-26 | 2014-08-21 | Shionogi & Co., Ltd. | Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them |
| AR086539A1 (es) | 2011-05-24 | 2014-01-08 | Bristol Myers Squibb Co | COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE |
| WO2014015125A1 (en) | 2012-07-19 | 2014-01-23 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative salts and uses thereof |
| JP2014101354A (ja) | 2012-10-24 | 2014-06-05 | Shionogi & Co Ltd | Ｂａｃｅ１阻害作用を有するオキサジン誘導体 |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| JOP20170106A1 (ar) | 2016-05-20 | 2017-11-20 | Lilly Co Eli | مركبات تترا هيدرو فوروكسازين واستخداماتها كمثبطات bace1 انتقائية |
| US20210355138A1 (en) | 2016-08-11 | 2021-11-18 | Eli Lilly And Company | Aminothiazinies and their use as bace1 inhibitors |
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2016
- 2016-04-13 AR ARP160100992A patent/AR104241A1/es unknown
- 2016-04-15 TW TW105111913A patent/TWI619719B/zh not_active IP Right Cessation
- 2016-04-22 US US15/135,580 patent/US10011610B2/en active Active
- 2016-04-22 AU AU2016254980A patent/AU2016254980B2/en not_active Ceased
- 2016-04-22 PL PL16719728T patent/PL3288949T3/pl unknown
- 2016-04-22 PT PT167197284T patent/PT3288949T/pt unknown
- 2016-04-22 JP JP2016567244A patent/JP2017515831A/ja not_active Withdrawn
- 2016-04-22 DK DK16719728.4T patent/DK3288949T3/da active
- 2016-04-22 KR KR1020177030721A patent/KR101979534B1/ko not_active Expired - Fee Related
- 2016-04-22 CN CN201680024772.6A patent/CN107531728B/zh active Active
- 2016-04-22 CR CR20170433A patent/CR20170433A/es unknown
- 2016-04-22 HK HK18103304.5A patent/HK1243709A1/zh unknown
- 2016-04-22 MY MYPI2017704013A patent/MY180727A/en unknown
- 2016-04-22 PE PE2017001998A patent/PE20180048A1/es unknown
- 2016-04-22 BR BR112017020180-1A patent/BR112017020180A2/pt not_active Application Discontinuation
- 2016-04-22 EP EP16719728.4A patent/EP3288949B1/en active Active
- 2016-04-22 ME MEP-2019-353A patent/ME03660B/me unknown
- 2016-04-22 SI SI201630511T patent/SI3288949T1/sl unknown
- 2016-04-22 MX MX2017013694A patent/MX2017013694A/es unknown
- 2016-04-22 HU HUE16719728A patent/HUE047160T2/hu unknown
- 2016-04-22 HR HRP20192237TT patent/HRP20192237T1/hr unknown
- 2016-04-22 MA MA41975A patent/MA41975B1/fr unknown
- 2016-04-22 SG SG11201708003WA patent/SG11201708003WA/en unknown
- 2016-04-22 WO PCT/US2016/028896 patent/WO2016176118A1/en not_active Ceased
- 2016-04-22 RS RS20191653A patent/RS59729B1/sr unknown
- 2016-04-22 MD MDE20180225T patent/MD3288949T2/ro unknown
- 2016-04-22 NZ NZ735249A patent/NZ735249A/en not_active IP Right Cessation
- 2016-04-22 TN TNP/2017/000448A patent/TN2017000448A1/en unknown
- 2016-04-22 ES ES16719728T patent/ES2765646T3/es active Active
- 2016-04-22 EA EA201792109A patent/EA032293B1/ru not_active IP Right Cessation
- 2016-04-22 CA CA2981091A patent/CA2981091A1/en active Pending
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2017
- 2017-08-31 IL IL254252A patent/IL254252A0/en unknown
- 2017-10-17 DO DO2017000240A patent/DOP2017000240A/es unknown
- 2017-10-17 SV SV2017005547A patent/SV2017005547A/es unknown
- 2017-10-18 CL CL2017002651A patent/CL2017002651A1/es unknown
- 2017-10-20 CO CONC2017/0010725A patent/CO2017010725A2/es unknown
- 2017-10-26 PH PH12017501955A patent/PH12017501955A1/en unknown
- 2017-10-27 EC ECIEPI201771769A patent/ECSP17071769A/es unknown
- 2017-10-27 GT GT201700227A patent/GT201700227A/es unknown
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2018
- 2018-03-13 JP JP2018045585A patent/JP6777668B2/ja active Active
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2019
- 2019-12-04 CY CY20191101285T patent/CY1122375T1/el unknown