CR20190320A - N-[4-fluoro-5[[(2s, 4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il) metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga - Google Patents
N-[4-fluoro-5[[(2s, 4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il) metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de ogaInfo
- Publication number
- CR20190320A CR20190320A CR20190320A CR20190320A CR20190320A CR 20190320 A CR20190320 A CR 20190320A CR 20190320 A CR20190320 A CR 20190320A CR 20190320 A CR20190320 A CR 20190320A CR 20190320 A CR20190320 A CR 20190320A
- Authority
- CR
- Costa Rica
- Prior art keywords
- methyl
- oxadiazol
- thiazol
- piperidyl
- acetamide
- Prior art date
Links
- FRVXHWNHGWUTQO-CABZTGNLSA-N N-[4-fluoro-5-[[(2S,4S)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide Chemical compound FC=1N=C(SC=1CN1[C@H](C[C@H](CC1)OCC1=NOC(=N1)C)C)NC(C)=O FRVXHWNHGWUTQO-CABZTGNLSA-N 0.000 title 1
- 229940126137 O-GlcNAcase inhibitor Drugs 0.000 title 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 230000004770 neurodegeneration Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
Classifications
-
- 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
- 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
- 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
- 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
-
- 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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención proporciona un compuesto de Fórmula I: o una sal farmacéuticamente aceptable del mismo, y el uso de compuestos de Fórmula I para el tratamiento de enfermedades y trastornos neurodegenerativos, tales como la enfermedad de Alzheimer.The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula (I) for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762451137P | 2017-01-27 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| CR20190320A true CR20190320A (es) | 2019-08-27 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190320A CR20190320A (es) | 2017-01-27 | 2018-01-19 | N-[4-fluoro-5[[(2s, 4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il) metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US10081625B2 (es) |
| EP (1) | EP3573983B1 (es) |
| JP (1) | JP6738970B2 (es) |
| KR (1) | KR102275338B1 (es) |
| CN (1) | CN110198940B (es) |
| AR (1) | AR110747A1 (es) |
| AU (1) | AU2018213029B2 (es) |
| CA (1) | CA3049141C (es) |
| CL (1) | CL2019001978A1 (es) |
| CO (1) | CO2019007711A2 (es) |
| CR (1) | CR20190320A (es) |
| CY (1) | CY1124257T1 (es) |
| DK (1) | DK3573983T3 (es) |
| DO (1) | DOP2019000187A (es) |
| EA (1) | EA038368B1 (es) |
| EC (1) | ECSP19053616A (es) |
| ES (1) | ES2871949T3 (es) |
| HR (1) | HRP20211011T1 (es) |
| HU (1) | HUE054990T2 (es) |
| IL (1) | IL267693B (es) |
| JO (1) | JOP20190182B1 (es) |
| LT (1) | LT3573983T (es) |
| MA (1) | MA47368B1 (es) |
| MD (1) | MD3573983T2 (es) |
| MX (1) | MX387166B (es) |
| MY (1) | MY197494A (es) |
| PE (1) | PE20191406A1 (es) |
| PH (1) | PH12019501707A1 (es) |
| PL (1) | PL3573983T3 (es) |
| PT (1) | PT3573983T (es) |
| RS (1) | RS61979B1 (es) |
| SI (1) | SI3573983T1 (es) |
| TW (1) | TWI654978B (es) |
| UA (1) | UA123472C2 (es) |
| WO (1) | WO2018140299A1 (es) |
| ZA (1) | ZA201904171B (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201701315VA (en) | 2014-08-28 | 2017-03-30 | Asceneuron Sa | Glycosidase inhibitors |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| CN108884078A (zh) | 2016-02-25 | 2018-11-23 | 阿森纽荣股份公司 | 糖苷酶抑制剂 |
| AU2017222958B2 (en) | 2016-02-25 | 2019-07-18 | Asceneuron S. A. | Glycosidase inhibitors |
| MX381953B (es) | 2016-02-25 | 2025-03-13 | Asceneuron S A | Sales de derivados de piperazina obtenidas por adicion de acidos. |
| TWI669302B (zh) | 2017-05-25 | 2019-08-21 | 美商美國禮來大藥廠 | 5-甲基-1,3,4-<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>二唑-2-基化合物 |
| EP3672959A1 (en) | 2017-08-24 | 2020-07-01 | 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 |
| 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 |
| ES2939043T3 (es) * | 2018-07-31 | 2023-04-18 | Lilly Co Eli | Compuestos de 5-metil-4-fluoro-tiazol-2-ilo |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| US11731972B2 (en) | 2018-08-22 | 2023-08-22 | Asceneuron Sa | Spiro compounds as glycosidase inhibitors |
| US12016852B2 (en) | 2018-08-22 | 2024-06-25 | Asceneuron Sa | Pyrrolidine glycosidase inhibitors |
| BR112021003022A2 (pt) | 2018-08-22 | 2021-05-11 | Asceneuron Sa | sais de adição de ácido de ácido succínico ou ácido fumárico, de ácido monossuccínico, de ácido monofumárico e de adição de ácido succínico ou sal de adição de ácido fumárico, métodos para preparar um sal de adição de ácido do ácido succínico ou ácido fumárico, para tratar uma tauopatia e para inibir uma glicosidase, e, forma de dosagem oral sólida |
| WO2020061150A1 (en) * | 2018-09-19 | 2020-03-26 | 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 |
| UY38498A (es) | 2018-12-05 | 2020-07-31 | Biogen Ma Inc | Inhibidores de o-glucoproteina-2- acetamido-2-desoxi-3-d-glucopiranosidasa de morfolinilo , piperazinilo , oxazepanilo y diazepanilo |
| WO2020163193A1 (en) * | 2019-02-04 | 2020-08-13 | Biogen Ma Inc. | Bicyclic ether o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| 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 |
| EP4077323A1 (en) | 2019-12-18 | 2022-10-26 | Janssen Pharmaceutica NV | Oga inhibitor compounds |
| CN114929337A (zh) | 2019-12-18 | 2022-08-19 | 詹森药业有限公司 | Oga抑制剂化合物 |
| AR123031A1 (es) * | 2020-07-23 | 2022-10-26 | Lilly Co Eli | Régimen de dosis baja y formulación de un compuesto 5-metil-1,2,4-oxadiazol-3-ilo |
| CN116917284A (zh) * | 2020-08-03 | 2023-10-20 | 渤健马萨诸塞州股份有限公司 | O-糖蛋白-2-乙酰胺基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂的结晶形式 |
| MX2024004514A (es) * | 2021-10-22 | 2024-05-07 | Lilly Co Eli | Terapia de combinacion con el inhibidor de o-glcnacasa (oga). |
| US20250064417A1 (en) | 2022-02-03 | 2025-02-27 | Eli Lilly And Company | Regional tau imaging for diagnosing and treating 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 |
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 |
| MX2008008337A (es) * | 2005-12-21 | 2008-09-03 | Schering Corp | Fenoxipiperidinas y sus analogos utiles como antagonistas de histamina h3. |
| 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 |
| WO2011140640A1 (en) | 2010-05-11 | 2011-11-17 | Simon Fraser University | Selective glycosidase inhibitors and uses thereof |
| AU2014241065B2 (en) | 2013-03-14 | 2017-08-31 | Merck Patent Gmbh | Glycosidase inhibitors |
| JP6370294B2 (ja) * | 2013-05-30 | 2018-08-08 | 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 |
| SG11201701315VA (en) | 2014-08-28 | 2017-03-30 | Asceneuron Sa | Glycosidase inhibitors |
| US10913733B2 (en) | 2015-12-18 | 2021-02-09 | Alectos Therapeutics Inc. | Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof |
| CA3045957A1 (en) * | 2016-12-16 | 2018-06-21 | Janssen Pharmaceutica Nv | Monocyclic oga inhibitor compounds |
-
2018
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
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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 CO CONC2019/0007711A patent/CO2019007711A2/es unknown
- 2019-07-18 DO DO2019000187A patent/DOP2019000187A/es unknown
- 2019-07-25 PH PH12019501707A patent/PH12019501707A1/en unknown
- 2019-07-26 EC ECSENADI201953616A patent/ECSP19053616A/es unknown
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2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
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