JOP20190182B1 - أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga - Google Patents
أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط ogaInfo
- Publication number
- JOP20190182B1 JOP20190182B1 JOP/2019/0182A JOP20190182A JOP20190182B1 JO P20190182 B1 JOP20190182 B1 JO P20190182B1 JO P20190182 A JOP20190182 A JO P20190182A JO P20190182 B1 JOP20190182 B1 JO P20190182B1
- Authority
- JO
- Jordan
- Prior art keywords
- methyl
- piperdyl
- oxadiazol
- fluor
- thiazole
- Prior art date
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
- 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
- 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)
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 (2)
| Publication Number | Publication Date |
|---|---|
| JOP20190182A1 JOP20190182A1 (ar) | 2019-07-25 |
| JOP20190182B1 true JOP20190182B1 (ar) | 2023-03-28 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2019/0182A JOP20190182B1 (ar) | 2017-01-27 | 2018-01-19 | أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga |
Country Status (36)
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 (en) | 2016-02-25 | 2023-10-03 | Asceneuron S.A. | Acid addition salts of piperazine derivatives |
| 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 (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 |
| CA3108158C (en) * | 2018-07-31 | 2023-05-16 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| WO2020039027A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Pyrrolidine glycosidase inhibitors |
| 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 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine 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 |
| EP3921316A1 (en) | 2019-02-04 | 2021-12-15 | 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 |
| 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 (en) | 2021-10-22 | 2023-04-27 | Kevin BIGLAN | O-glcnacase (oga) inhibitor combination therapy |
| WO2023150483A1 (en) | 2022-02-03 | 2023-08-10 | 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 |
| 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 |
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| 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 (en) | 2010-05-11 | 2011-11-17 | Simon Fraser University | Selective glycosidase inhibitors and uses thereof |
| RS58768B1 (sr) | 2013-03-14 | 2019-06-28 | Merck Patent Gmbh | Inhibitori glikozidaze |
| EP3006438A4 (en) * | 2013-05-30 | 2017-01-18 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
| KR102043337B1 (ko) | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| EP3389658B1 (en) | 2015-12-18 | 2020-11-25 | Merck Sharp & Dohme Corp. | Glycosidase inhibitors and uses thereof |
| CA3045957A1 (en) * | 2016-12-16 | 2018-06-21 | 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 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en 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
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- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
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2021
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