JP2020504142A5 - - Google Patents
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- Publication number
- JP2020504142A5 JP2020504142A5 JP2019537118A JP2019537118A JP2020504142A5 JP 2020504142 A5 JP2020504142 A5 JP 2020504142A5 JP 2019537118 A JP2019537118 A JP 2019537118A JP 2019537118 A JP2019537118 A JP 2019537118A JP 2020504142 A5 JP2020504142 A5 JP 2020504142A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- alzheimer
- disease
- 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 19
- 150000003839 salts Chemical class 0.000 claims 15
- 208000024827 Alzheimer disease Diseases 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 3
- -1 5-methyl-1,2,4-oxadiazol-3-yl Chemical group 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- FRVXHWNHGWUTQO-UHFFFAOYSA-N CC(C1)N(Cc([s]c(NC(C)=O)n2)c2F)CCC1OCc1n[o]c(C)n1 Chemical compound CC(C1)N(Cc([s]c(NC(C)=O)n2)c2F)CCC1OCc1n[o]c(C)n1 FRVXHWNHGWUTQO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762451137P | 2017-01-27 | 2017-01-27 | |
| US62/451,137 | 2017-01-27 | ||
| PCT/US2018/014331 WO2018140299A1 (en) | 2017-01-27 | 2018-01-19 | N-[4-fluoro-5-[[(2s,4s)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]-1-piperidyl]methyl]thiazol-2-yl]acetamide as oga inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020504142A JP2020504142A (ja) | 2020-02-06 |
| JP2020504142A5 true JP2020504142A5 (https=) | 2020-03-19 |
| JP6738970B2 JP6738970B2 (ja) | 2020-08-12 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019537118A Active JP6738970B2 (ja) | 2017-01-27 | 2018-01-19 | Ｏｇａ阻害剤としてのｎ−［４−フルオロ−５−［［（２ｓ，４ｓ）−２−メチル−４−［（５−メチル−１，２，４−オキサジアゾール−３−イル）メトキシ］−１−ピペリジル］メチル］チアゾール−２−イル］アセトアミド |
Country Status (36)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3868752A1 (en) | 2014-08-28 | 2021-08-25 | Asceneuron SA | Glycosidase inhibitors |
| CN108884078A (zh) | 2016-02-25 | 2018-11-23 | 阿森纽荣股份公司 | 糖苷酶抑制剂 |
| SG11201807012QA (en) | 2016-02-25 | 2018-09-27 | Asceneuron S A | Acid addition salts of piperazine derivatives |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| AU2017222958B2 (en) | 2016-02-25 | 2019-07-18 | Asceneuron S. A. | Glycosidase inhibitors |
| AR111693A1 (es) | 2017-05-25 | 2019-08-07 | Lilly Co Eli | Compuestos de 5-metil-1,3,4-oxadiazol-2-ilo con actividad inhibitoria de oga |
| WO2019037860A1 (en) | 2017-08-24 | 2019-02-28 | Asceneuron S.A. | LINEAR INHIBITORS OF GLYCOSIDASE |
| TWI726329B (zh) | 2018-06-22 | 2021-05-01 | 美商美國禮來大藥廠 | 2,3-二氫呋喃并[2,3-b]吡啶化合物 |
| US11999726B2 (en) | 2018-07-31 | 2024-06-04 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| CA3107788A1 (en) | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | Combination of anti-tau antibody and oga inhibitor for treatment of diseases characterized by aberrant tau aggregation |
| WO2020039027A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Pyrrolidine glycosidase inhibitors |
| IL280841B2 (en) | 2018-08-22 | 2024-12-01 | Asceneuron S A | Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| US12180205B2 (en) * | 2018-09-19 | 2024-12-31 | Biogen Ma Inc. | O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| TWI716107B (zh) | 2018-09-26 | 2021-01-11 | 美商美國禮來大藥廠 | 6-氟-2-甲基苯并[d]噻唑-5-基化合物 |
| ES2968733T3 (es) | 2018-12-05 | 2024-05-13 | Biogen Ma Inc | Derivados morfolinilo, piperazinilo, oxazepanilo y diazepanilo útiles como inhibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| JP7504898B2 (ja) * | 2019-02-04 | 2024-06-24 | バイオジェン・エムエイ・インコーポレイテッド | 二環式エーテルｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グルコピラノシダーゼ阻害剤 |
| WO2021094312A1 (en) | 2019-11-11 | 2021-05-20 | Janssen Pharmaceutica Nv | Pyrrolidine and bicycloheteroaryl containing oga inhibitor compounds |
| WO2021110656A1 (en) | 2019-12-02 | 2021-06-10 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| WO2021123291A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| CN114867725A (zh) | 2019-12-18 | 2022-08-05 | 詹森药业有限公司 | Oga抑制剂化合物 |
| US20230058733A1 (en) | 2019-12-18 | 2023-02-23 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| TW202220650A (zh) * | 2020-07-23 | 2022-06-01 | 美商美國禮來大藥廠 | 5-甲基-1,2,4-噁二唑-3-基化合物之低劑量療法及調配物 |
| WO2022031701A1 (en) * | 2020-08-03 | 2022-02-10 | Biogen Ma Inc. | Crystaline forms of an o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitor |
| AU2022371475A1 (en) | 2021-10-22 | 2024-05-09 | Eli Lilly And Company | O-glcnacase (oga) inhibitor combination therapy |
| CA3243602A1 (en) | 2022-02-03 | 2023-08-10 | Eli Lilly And Company | Regional Tau Imaging for the Diagnosis and Treatment of Alzheimer's Disease |
| WO2024083820A1 (en) | 2022-10-18 | 2024-04-25 | Institut National de la Santé et de la Recherche Médicale | Method and composition for determining the level of o-glcnacylation in horses |
| WO2025184490A1 (en) * | 2024-03-01 | 2025-09-04 | Biogen Ma Inc. | N-[4-fluor-5-[[(2s, 4 r)-4-[(6-methoxy-4-pyrimidinyl)oxy]- 2-methyl-1-pyrrolidinyl] methyl ]-2-thiazolyl]acetamid for use in the treatment of alzheimer disease |
| WO2026021588A1 (zh) * | 2024-07-26 | 2026-01-29 | 浙江同源康医药股份有限公司 | Oga抑制剂及其应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8726763D0 (en) | 1987-11-16 | 1987-12-23 | Fujisawa Pharmaceutical Co | Thiazole compounds |
| MXPA05011223A (es) | 2003-04-18 | 2006-01-26 | Lilly Co Eli | Compuestos de (piperidiniloxi)fenilo, (piperidiniloxi)piridinilo, (piperidinilsulfanil)fenilo y (piperidinilsulfanil)piridinilo como agonistas 5-htif. |
| SE0302116D0 (sv) | 2003-07-21 | 2003-07-21 | Astrazeneca Ab | Novel compounds |
| US7638531B2 (en) * | 2005-12-21 | 2009-12-29 | Schering Corporation | Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists |
| EP2139332A4 (en) * | 2007-03-28 | 2010-04-21 | Merck Sharp & Dohme | SUBSTITUTED PYRIDO [2,3-D] PYRIMIDIN DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| US9120781B2 (en) | 2010-05-11 | 2015-09-01 | Simon Fraser University | Selective glycosidase inhibitors and uses thereof |
| PT2970272T (pt) | 2013-03-14 | 2019-06-05 | Merck Patent Gmbh | Inibidores de glicosidase |
| WO2014192868A1 (ja) * | 2013-05-30 | 2014-12-04 | 大日本住友製薬株式会社 | 環状アミノメチルピリミジン誘導体 |
| EP3868752A1 (en) * | 2014-08-28 | 2021-08-25 | Asceneuron SA | Glycosidase inhibitors |
| EP3389658B1 (en) | 2015-12-18 | 2020-11-25 | Merck Sharp & Dohme Corp. | Glycosidase inhibitors and uses thereof |
| EP3555087A1 (en) * | 2016-12-16 | 2019-10-23 | Janssen Pharmaceutica NV | Monocyclic oga inhibitor compounds |
-
2018
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
-
2019
- 2019-06-26 ZA ZA2019/04171A patent/ZA201904171B/en unknown
- 2019-06-27 IL IL267693A patent/IL267693B/en unknown
- 2019-07-12 CL CL2019001978A patent/CL2019001978A1/es unknown
- 2019-07-18 DO DO2019000187A patent/DOP2019000187A/es unknown
- 2019-07-18 CO CONC2019/0007711A patent/CO2019007711A2/es unknown
- 2019-07-25 PH PH12019501707A patent/PH12019501707A1/en unknown
- 2019-07-26 EC ECSENADI201953616A patent/ECSP19053616A/es unknown
-
2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
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