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 (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112017003658B1 (pt) | 2014-08-28 | 2022-12-06 | Asceneuron Sa | Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica |
| AU2017222964B2 (en) | 2016-02-25 | 2020-01-02 | Asceneuron S. A. | Glycosidase inhibitors |
| US11612599B2 (en) | 2016-02-25 | 2023-03-28 | Asceneuron Sa | Glycosidase inhibitors |
| EP3585783A2 (en) | 2016-02-25 | 2020-01-01 | Asceneuron SA | Sulfoximine glycosidase inhibitors |
| EP3419976B1 (en) | 2016-02-25 | 2021-04-07 | Asceneuron SA | Acid addition salts of piperazine derivatives |
| 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 |
| CN112543648A (zh) * | 2018-07-31 | 2021-03-23 | 伊莱利利公司 | 组合疗法 |
| CN112469476B (zh) * | 2018-07-31 | 2024-07-16 | 伊莱利利公司 | 5-甲基-4-氟-噻唑-2-基化合物 |
| US12016852B2 (en) | 2018-08-22 | 2024-06-25 | Asceneuron Sa | Pyrrolidine glycosidase inhibitors |
| US11731972B2 (en) | 2018-08-22 | 2023-08-22 | Asceneuron Sa | Spiro compounds as glycosidase inhibitors |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| EP3841093B1 (en) | 2018-08-22 | 2023-06-21 | Asceneuron SA | Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors |
| IL315564A (en) * | 2018-09-19 | 2024-11-01 | 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 |
| AR117252A1 (es) | 2018-12-05 | 2021-07-21 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa de morfolinilo, piperazinilo, oxazepanilo y diazepanilo |
| 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 |
| CN114929337A (zh) | 2019-12-18 | 2022-08-19 | 詹森药业有限公司 | Oga抑制剂化合物 |
| JP2023507184A (ja) | 2019-12-18 | 2023-02-21 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｏｇａ阻害剤化合物 |
| 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 |
| BR112023002013A2 (pt) | 2020-08-03 | 2023-05-02 | Biogen Ma Inc | Formas cristalinas de um inibidor de o-glicoproteína-2-acetamido-2-desóxi-3-d-glucopiranosidase |
| CN118139880A (zh) * | 2021-10-22 | 2024-06-04 | 伊莱利利公司 | O-连接的n-乙酰葡糖胺水解酶(oga)抑制剂联合治疗 |
| JP2025506411A (ja) | 2022-02-03 | 2025-03-11 | イーライ リリー アンド カンパニー | アルツハイマー病の診断及び治療のための局所タウイメージング |
| 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 |
| EP1976848A2 (en) * | 2005-12-21 | 2008-10-08 | 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 |
| ES2723883T3 (es) * | 2013-03-14 | 2019-09-03 | Merck Patent Gmbh | Inhibidores de glicosidasa |
| US9732065B2 (en) * | 2013-05-30 | 2017-08-15 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
| BR112017003658B1 (pt) * | 2014-08-28 | 2022-12-06 | Asceneuron Sa | Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica |
| US10913733B2 (en) | 2015-12-18 | 2021-02-09 | Alectos Therapeutics Inc. | Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof |
| CN110300752A (zh) * | 2016-12-16 | 2019-10-01 | 詹森药业有限公司 | 单环oga抑制剂化合物 |
-
2018
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 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 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/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 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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