MA47368B1 - N-[4-fluoro-5-[[(2s,4s)-2-méthyl-4-[(5-méthyl-1,2,4-oxadiazol-3-yl)méthoxy]-1-pipéridyl]méthyl]thiazol-2-yl]acétamide utilisés en tant qu'inhibiteur d'oga - Google Patents
N-[4-fluoro-5-[[(2s,4s)-2-méthyl-4-[(5-méthyl-1,2,4-oxadiazol-3-yl)méthoxy]-1-pipéridyl]méthyl]thiazol-2-yl]acétamide utilisés en tant qu'inhibiteur d'ogaInfo
- Publication number
- MA47368B1 MA47368B1 MA47368A MA47368A MA47368B1 MA 47368 B1 MA47368 B1 MA 47368B1 MA 47368 A MA47368 A MA 47368A MA 47368 A MA47368 A MA 47368A MA 47368 B1 MA47368 B1 MA 47368B1
- Authority
- MA
- Morocco
- Prior art keywords
- methyl
- yoga
- oxadiazol
- thiazol
- piperidyl
- 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
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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 présente invention concerne un composé de formule (i) : ou un sel pharmaceutiquement acceptable de celui-ci ainsi que l'utilisation de composés de formule (i) pour le traitement de maladies et de troubles neurodégénératifs, tels que la maladie d'alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762451137P | 2017-01-27 | 2017-01-27 | |
| PCT/US2018/014331 WO2018140299A1 (fr) | 2017-01-27 | 2018-01-19 | N-[4-fluoro-5-[[(2s,4s)-2-méthyl-4-[(5-méthyl-1,2,4-oxadiazol-3-yl)méthoxy]-1-pipéridyl]méthyl]thiazol-2-yl]acétamide utilisés en tant qu'inhibiteur d'oga |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA47368B1 true MA47368B1 (fr) | 2021-07-29 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA47368A MA47368B1 (fr) | 2017-01-27 | 2018-01-19 | N-[4-fluoro-5-[[(2s,4s)-2-méthyl-4-[(5-méthyl-1,2,4-oxadiazol-3-yl)méthoxy]-1-pipéridyl]méthyl]thiazol-2-yl]acétamide utilisés en tant qu'inhibiteur d'oga |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US10081625B2 (fr) |
| EP (1) | EP3573983B1 (fr) |
| JP (1) | JP6738970B2 (fr) |
| KR (1) | KR102275338B1 (fr) |
| CN (1) | CN110198940B (fr) |
| AR (1) | AR110747A1 (fr) |
| AU (1) | AU2018213029B2 (fr) |
| CA (1) | CA3049141C (fr) |
| CL (1) | CL2019001978A1 (fr) |
| CO (1) | CO2019007711A2 (fr) |
| CR (1) | CR20190320A (fr) |
| CY (1) | CY1124257T1 (fr) |
| DK (1) | DK3573983T3 (fr) |
| DO (1) | DOP2019000187A (fr) |
| EA (1) | EA038368B1 (fr) |
| EC (1) | ECSP19053616A (fr) |
| ES (1) | ES2871949T3 (fr) |
| HR (1) | HRP20211011T1 (fr) |
| HU (1) | HUE054990T2 (fr) |
| IL (1) | IL267693B (fr) |
| JO (1) | JOP20190182B1 (fr) |
| LT (1) | LT3573983T (fr) |
| MA (1) | MA47368B1 (fr) |
| MD (1) | MD3573983T2 (fr) |
| MX (1) | MX387166B (fr) |
| MY (1) | MY197494A (fr) |
| PE (1) | PE20191406A1 (fr) |
| PH (1) | PH12019501707A1 (fr) |
| PL (1) | PL3573983T3 (fr) |
| PT (1) | PT3573983T (fr) |
| RS (1) | RS61979B1 (fr) |
| SI (1) | SI3573983T1 (fr) |
| TW (1) | TWI654978B (fr) |
| UA (1) | UA123472C2 (fr) |
| WO (1) | WO2018140299A1 (fr) |
| ZA (1) | ZA201904171B (fr) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102043337B1 (ko) | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| CA3014572C (fr) | 2016-02-25 | 2023-10-03 | Asceneuron S.A. | Sels d'addition d'acide de derives de piperazine |
| KR20180132629A (ko) | 2016-02-25 | 2018-12-12 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| AU2017222964B2 (en) | 2016-02-25 | 2020-01-02 | Asceneuron S. A. | Glycosidase inhibitors |
| 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 (fr) * | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | Combinaison d'anticorps anti-tau et d'inhibiteur d'oga pour le traitement de maladies caracterisees par une agregation aberrante de tau |
| CA3108158C (fr) * | 2018-07-31 | 2023-05-16 | Eli Lilly And Company | Composes 5-methyl-4-fluoro-thiazol-2-yl |
| WO2020039027A1 (fr) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Inhibiteurs de pyrrolidine glycosidase |
| JP7407171B2 (ja) | 2018-08-22 | 2023-12-28 | 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として有用なピペラジン誘導体のコハク酸付加塩及びフマル酸付加塩 |
| WO2020039028A1 (fr) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Inhibiteurs de tétrahydro-benzoazépine glycosidase |
| WO2020039029A1 (fr) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Composés spiro utilisés en tant qu'inhibiteurs de glycosidases |
| 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 |
| EP3921316A1 (fr) | 2019-02-04 | 2021-12-15 | Biogen MA Inc. | Inhibiteurs d'éther o-glycoprotéine-2-acétamido-2-désoxy-3-d-glucopyranosidase bicycliques |
| WO2021094312A1 (fr) | 2019-11-11 | 2021-05-20 | Janssen Pharmaceutica Nv | Composés inhibiteurs d'oga contenant de la pyrrolidine et de la bicyclohétéroaryle |
| WO2021110656A1 (fr) | 2019-12-02 | 2021-06-10 | Janssen Pharmaceutica Nv | Composés inhibiteurs d'oga |
| WO2021123291A1 (fr) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Composés inhibiteurs d'oga |
| AU2020409728A1 (en) | 2019-12-18 | 2022-08-11 | 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 |
| 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 |
| 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 |
| CA3235104A1 (fr) | 2021-10-22 | 2023-04-27 | Kevin BIGLAN | Polytherapie par un inhibiteur d'o-glcnacase (oga) |
| WO2023150483A1 (fr) | 2022-02-03 | 2023-08-10 | Eli Lilly And Company | Imagerie de tau régionale pour le diagnostic et le traitement de la maladie d'alzheimer |
| WO2024083820A1 (fr) | 2022-10-18 | 2024-04-25 | Institut National de la Santé et de la Recherche Médicale | Méthode et composition pour déterminer le niveau de o-glcnacylation chez des chevaux |
| WO2025184490A1 (fr) * | 2024-03-01 | 2025-09-04 | Biogen Ma Inc. | N-[4-fluor-5-[[(2s,4r)-4-[(6-méthoxy-4-pyrimidnyl)oxy]-2-méthyl-1-pyrrolidinyl]méthyl]-2-thiazolyl]acétamide destiné à être utilisé dans le traitement de la maladie d'alzheimer |
| 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 |
| 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 |
| 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 |
| US20100063032A1 (en) * | 2007-03-28 | 2010-03-11 | Debenham John S | 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 |
| WO2011140640A1 (fr) | 2010-05-11 | 2011-11-17 | Simon Fraser University | Inhibiteurs sélectifs des glycosidases et leurs utilisations |
| RS58768B1 (sr) | 2013-03-14 | 2019-06-28 | Merck Patent Gmbh | Inhibitori glikozidaze |
| EP3006438A4 (fr) * | 2013-05-30 | 2017-01-18 | Sumitomo Dainippon Pharma Co., Ltd. | Dérivé cyclique d'aminométhyl pyrimidine |
| KR102043337B1 (ko) | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| EP3389658B1 (fr) | 2015-12-18 | 2020-11-25 | Merck Sharp & Dohme Corp. | Inhibiteurs de glycosidase et leurs utilisations |
| CA3045957A1 (fr) * | 2016-12-16 | 2018-06-21 | Janssen Pharmaceutica Nv | Composes inhibiteurs d'oga monocyclique |
-
2018
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/fr active Active
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 HR HRP20211011TT patent/HRP20211011T1/hr unknown
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 CA CA3049141A patent/CA3049141C/fr active Active
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/fr not_active Ceased
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 MX MX2019008846A patent/MX387166B/es unknown
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
-
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
-
2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
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