CN110198940B - 作为oga抑制剂的n-[4-氟-5-[[(2s,4s)-2-甲基-4-[(5-甲基-1,2,4-噁二唑-3-基)甲氧基]-1-哌啶基]甲基]噻唑-2-基]乙酰胺 - Google Patents
作为oga抑制剂的n-[4-氟-5-[[(2s,4s)-2-甲基-4-[(5-甲基-1,2,4-噁二唑-3-基)甲氧基]-1-哌啶基]甲基]噻唑-2-基]乙酰胺 Download PDFInfo
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- CN110198940B CN110198940B CN201880008537.9A CN201880008537A CN110198940B CN 110198940 B CN110198940 B CN 110198940B CN 201880008537 A CN201880008537 A CN 201880008537A CN 110198940 B CN110198940 B CN 110198940B
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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
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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
-
- 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
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- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762451137P | 2017-01-27 | 2017-01-27 | |
| US62/451137 | 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 |
|---|---|
| CN110198940A CN110198940A (zh) | 2019-09-03 |
| CN110198940B true CN110198940B (zh) | 2022-09-23 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880008537.9A Active CN110198940B (zh) | 2017-01-27 | 2018-01-19 | 作为oga抑制剂的n-[4-氟-5-[[(2s,4s)-2-甲基-4-[(5-甲基-1,2,4-噁二唑-3-基)甲氧基]-1-哌啶基]甲基]噻唑-2-基]乙酰胺 |
Country Status (36)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102043337B1 (ko) | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| JP2019510006A (ja) | 2016-02-25 | 2019-04-11 | 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 |
| ES2879351T3 (es) | 2016-02-25 | 2021-11-22 | Asceneuron Sa | Sales de derivados de piperazina obtenidas por adición de ácidos |
| MA43680A (fr) | 2016-02-25 | 2018-11-28 | Asceneuron Sa | Inhibiteurs de glycosidases |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine 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 |
| CA3108158C (en) * | 2018-07-31 | 2023-05-16 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| JP2021530552A (ja) * | 2018-07-31 | 2021-11-11 | イーライ リリー アンド カンパニー | 併用療法 |
| US11731972B2 (en) | 2018-08-22 | 2023-08-22 | Asceneuron Sa | Spiro compounds as glycosidase inhibitors |
| WO2020039027A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Pyrrolidine glycosidase inhibitors |
| EA202190275A1 (ru) | 2018-08-22 | 2021-08-02 | Асенейрон С. А. | Сукцинатные и фумаратные кислотно-аддитивные соли производных пиперазина, пригодные в качестве ингибиторов гликозидазы |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| AU2019344922B2 (en) * | 2018-09-19 | 2025-02-06 | 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 |
| WO2021123294A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| WO2021123297A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | 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 |
| UY39366A (es) | 2020-08-03 | 2022-02-25 | Biogen Ma Inc | Formas cristalinas de un inhibidor de la o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| WO2023070064A1 (en) | 2021-10-22 | 2023-04-27 | Eli Lilly And Company | O-glcnacase (oga) inhibitor combination therapy |
| KR20240145486A (ko) | 2022-02-03 | 2024-10-07 | 일라이 릴리 앤드 캄파니 | 알츠하이머병을 진단 및 치료하기 위한 국소 타우 영상화 |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102015667A (zh) * | 2008-05-02 | 2011-04-13 | 伊莱利利公司 | 作为用于治疗阿尔茨海默氏病的bace抑制剂的氨基二氢噻嗪衍生物 |
| WO2014159234A1 (en) * | 2013-03-14 | 2014-10-02 | Merck Patent Gmbh | Glycosidase inhibitors |
Family Cites Families (10)
| 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 |
| 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 |
| WO2011140640A1 (en) | 2010-05-11 | 2011-11-17 | Simon Fraser University | Selective glycosidase inhibitors and uses thereof |
| 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 |
| US10913733B2 (en) | 2015-12-18 | 2021-02-09 | Alectos Therapeutics Inc. | Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof |
| JP2020503298A (ja) * | 2016-12-16 | 2020-01-30 | ヤンセン ファーマシューティカ エヌ．ベー． | 単環式ｏｇａ阻害剤化合物 |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102015667A (zh) * | 2008-05-02 | 2011-04-13 | 伊莱利利公司 | 作为用于治疗阿尔茨海默氏病的bace抑制剂的氨基二氢噻嗪衍生物 |
| WO2014159234A1 (en) * | 2013-03-14 | 2014-10-02 | Merck Patent Gmbh | Glycosidase inhibitors |
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