PE20191406A1 - 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
- PE20191406A1 PE20191406A1 PE2019001459A PE2019001459A PE20191406A1 PE 20191406 A1 PE20191406 A1 PE 20191406A1 PE 2019001459 A PE2019001459 A PE 2019001459A PE 2019001459 A PE2019001459 A PE 2019001459A PE 20191406 A1 PE20191406 A1 PE 20191406A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- oxadiazol
- thiazol
- piperidyl
- acetamide
- Prior art date
Links
Classifications
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- 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
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- 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
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- 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
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- 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
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- 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
Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable del mismo. En donde dicho compuesto es 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. Este compuesto funciona como inhibidor de beta-N-acetilglucosaminidasa (O-GlcNAcasa - OGA). Tambien se refiere a un proceso para preparar una composicion farmaceutica, siendo util para el tratamiento de enfermedades y trastornos neurodegenerativos, tales como la enfermedad de Alzheimer, paralisis supranuclear progresiva (PSP), entre otros.
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 |
|---|---|
| PE20191406A1 true PE20191406A1 (es) | 2019-10-04 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001459A PE20191406A1 (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 |
| WO2017144637A1 (en) | 2016-02-25 | 2017-08-31 | Asceneuron S. A. | Acid addition salts of piperazine derivatives |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2020028115A1 (en) | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| US11795165B2 (en) | 2018-08-22 | 2023-10-24 | Asceneuron Sa | Tetrahydro-benzoazepine glycosidase inhibitors |
| US12195455B2 (en) | 2018-08-22 | 2025-01-14 | Asceneuron Sa | Succinate and fumarate acid addition salts of piperazine derivatives |
| WO2020039027A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Pyrrolidine glycosidase inhibitors |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| PE20211591A1 (es) | 2018-09-19 | 2021-08-18 | Biogen Ma Inc | Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| 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 |
| US12319679B2 (en) | 2018-12-05 | 2025-06-03 | 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 |
| CA3160367A1 (en) | 2019-12-18 | 2021-06-24 | Jose Manuel Bartolome-Nebreda | Oga inhibitor compounds |
| CA3160405A1 (en) | 2019-12-18 | 2021-06-24 | Jose Manuel Bartolome-Nebreda | Oga inhibitor compounds |
| WO2021123291A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| 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 |
| IL300365A (en) | 2020-08-03 | 2023-04-01 | Biogen Ma Inc | Crystal forms of O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitor |
| IL312045A (en) * | 2021-10-22 | 2024-06-01 | Lilly Co Eli | O-glcnacase (oga) inhibitor combination therapy |
| EP4472679A1 (en) | 2022-02-03 | 2024-12-11 | 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 |
| ES2388547T3 (es) | 2003-04-18 | 2012-10-16 | Eli Lilly And Company | Compuestos de (piperidiniloxi)fenilo, (piperidiniloxi)piridinilo, (piperidinilsulfanil)fenilo y (piperidinilsulfanil)piridinilo como agonistas de 5-HT 1F |
| SE0302116D0 (sv) | 2003-07-21 | 2003-07-21 | Astrazeneca Ab | Novel compounds |
| AU2006331882A1 (en) * | 2005-12-21 | 2007-07-05 | Schering Corporation | Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists |
| WO2008121257A1 (en) * | 2007-03-28 | 2008-10-09 | Merck & Co., Inc. | Substituted pyrido[2,3-d]pyrimidine 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 |
| AU2014241065B2 (en) | 2013-03-14 | 2017-08-31 | Merck Patent Gmbh | Glycosidase inhibitors |
| US9732065B2 (en) * | 2013-05-30 | 2017-08-15 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
| SG11201701315VA (en) * | 2014-08-28 | 2017-03-30 | Asceneuron Sa | Glycosidase inhibitors |
| WO2017106254A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Glycosidase inhibitors and uses thereof |
| US20200079766A1 (en) * | 2016-12-16 | 2020-03-12 | Janssen Pharmaceutica Nv | Monocyclic oga inhibitor compounds |
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2018
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko 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 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
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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 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
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2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
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