JP6738970B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP6738970B2 JP6738970B2 JP2019537118A JP2019537118A JP6738970B2 JP 6738970 B2 JP6738970 B2 JP 6738970B2 JP 2019537118 A JP2019537118 A JP 2019537118A JP 2019537118 A JP2019537118 A JP 2019537118A JP 6738970 B2 JP6738970 B2 JP 6738970B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- pharmaceutically acceptable
- acceptable salt
- compound
- compound according
- 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.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/09—Geometrical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 JP2020504142A5 (enExample) | 2020-03-19 |
| JP6738970B2 true 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 |
|---|---|---|---|---|
| MX381417B (es) | 2014-08-28 | 2025-03-12 | Asceneuron Sa | Inhibidores de glucosidasa. |
| CN108884077A (zh) | 2016-02-25 | 2018-11-23 | 阿森纽荣股份公司 | 糖苷酶抑制剂 |
| JP2019506430A (ja) | 2016-02-25 | 2019-03-07 | エースニューロン・ソシエテ・アノニム | グリコシダーゼ阻害剤 |
| JP6971999B2 (ja) | 2016-02-25 | 2021-11-24 | エースニューロン・ソシエテ・アノニム | ピペラジン誘導体の酸付加塩 |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine 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 |
| US11213525B2 (en) | 2017-08-24 | 2022-01-04 | Asceneuron Sa | Linear glycosidase inhibitors |
| 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 |
| EP3829634A1 (en) * | 2018-07-31 | 2021-06-09 | Eli Lilly and Company | Combination therapy |
| ES2939043T3 (es) * | 2018-07-31 | 2023-04-18 | Lilly Co Eli | Compuestos de 5-metil-4-fluoro-tiazol-2-ilo |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| CA3110032A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S.A. | Succinate and fumarate acid addition salts of piperazine derivatives |
| US11795165B2 (en) | 2018-08-22 | 2023-10-24 | Asceneuron Sa | Tetrahydro-benzoazepine glycosidase inhibitors |
| US12016852B2 (en) | 2018-08-22 | 2024-06-25 | Asceneuron Sa | Pyrrolidine glycosidase inhibitors |
| CN113166137B (zh) | 2018-09-19 | 2024-08-16 | 比奥根Ma公司 | O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂 |
| 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 |
| EP4327814A3 (en) | 2018-12-05 | 2024-04-24 | Biogen MA Inc. | Morpholinyl, piperazinyl, oxazepanyl and diazepanyl o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| AR117989A1 (es) | 2019-02-04 | 2021-09-08 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa de éter bicíclico |
| 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 |
| AU2020409728A1 (en) | 2019-12-18 | 2022-08-11 | Janssen Pharmaceutica Nv | OGA inhibitor compounds |
| KR20220118484A (ko) | 2019-12-18 | 2022-08-25 | 얀센 파마슈티카 엔.브이. | Oga 억제제 화합물 |
| 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 |
| AR123132A1 (es) | 2020-08-03 | 2022-11-02 | Biogen Ma Inc | Formas cristalinas de un inhibidor de la o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| MX2024004514A (es) * | 2021-10-22 | 2024-05-07 | Lilly Co Eli | Terapia de combinacion con el inhibidor de o-glcnacasa (oga). |
| 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 |
| CN121405694A (zh) * | 2024-07-26 | 2026-01-27 | 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 |
| JP2006523692A (ja) | 2003-04-18 | 2006-10-19 | イーライ リリー アンド カンパニー | ５−ｈｔ１ｆ作用薬としての（ピペリジニルオキシ）フェニル、（ピペリジニルオキシ）ピリジニル、（ピペリジニルスルファニル）フェニル、および（ピペリジニルスルファニル）ピリジニル化合物 |
| SE0302116D0 (sv) | 2003-07-21 | 2003-07-21 | Astrazeneca Ab | Novel compounds |
| JP2009521448A (ja) * | 2005-12-21 | 2009-06-04 | シェーリング コーポレイション | ヒスタミンｈ３アンタゴニストとして有用なフェノキシピペリジンおよびそのアナログ |
| 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 |
| WO2014159234A1 (en) | 2013-03-14 | 2014-10-02 | Merck Patent Gmbh | Glycosidase inhibitors |
| US9732065B2 (en) * | 2013-05-30 | 2017-08-15 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
| MX381417B (es) | 2014-08-28 | 2025-03-12 | Asceneuron Sa | Inhibidores de glucosidasa. |
| WO2017106254A1 (en) | 2015-12-18 | 2017-06-22 | 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 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt 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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10081625B2 (en) | 5-methyl-1,2,4-oxadiazol-3-yl compounds | |
| EP3630755B1 (en) | 5-methyl-1,3,4-oxadiazol-2-yl compounds | |
| WO2012037351A1 (en) | Compounds | |
| NZ754849B2 (en) | 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 | |
| HK40009770A (en) | 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 | |
| HK40009770B (en) | 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 | |
| EP3829716B1 (en) | 5-methyl-4-fluoro-thiazol-2-yl compounds | |
| BR112019013535B1 (pt) | N-4-flúor-5-[[(2s,4s)-2-metil-4-[(5-metil1,2,4-oxadiazol-3-il)metóxi]-1-piperidil]metil]tiazol-2- il]acetamida como inibidor da oga, seu uso, composição farmacêutica e processo para preparação da referida composição | |
| JPWO2008007766A1 (ja) | ベンゾオキサジアゾール誘導体の結晶 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190708 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20190708 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20200703 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20200707 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20200720 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6738970 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |