KR102275338B1 - Oga 억제제로서의 n-[4-플루오로-5-[[(2s,4s)-2-메틸-4-[(5-메틸-1,2,4-옥사디아졸-3-일)메톡시]-1-피페리딜]메틸]티아졸-2-일]아세트아미드 - Google Patents
Oga 억제제로서의 n-[4-플루오로-5-[[(2s,4s)-2-메틸-4-[(5-메틸-1,2,4-옥사디아졸-3-일)메톡시]-1-피페리딜]메틸]티아졸-2-일]아세트아미드 Download PDFInfo
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- KR102275338B1 KR102275338B1 KR1020197021750A KR20197021750A KR102275338B1 KR 102275338 B1 KR102275338 B1 KR 102275338B1 KR 1020197021750 A KR1020197021750 A KR 1020197021750A KR 20197021750 A KR20197021750 A KR 20197021750A KR 102275338 B1 KR102275338 B1 KR 102275338B1
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- pharmaceutically acceptable
- mixture
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- FRVXHWNHGWUTQO-CABZTGNLSA-N C[C@@H](C1)N(Cc([s]c(NC(C)=O)n2)c2F)CC[C@@H]1OCc1n[o]c(C)n1 Chemical compound C[C@@H](C1)N(Cc([s]c(NC(C)=O)n2)c2F)CC[C@@H]1OCc1n[o]c(C)n1 FRVXHWNHGWUTQO-CABZTGNLSA-N 0.000 description 1
- VVHYBDXTTJTWRO-JQWIXIFHSA-N C[C@@H](C[C@H](CC1)OCc2n[o]c(C)n2)N1C(OC(C)(C)C)=O Chemical compound C[C@@H](C[C@H](CC1)OCc2n[o]c(C)n2)N1C(OC(C)(C)C)=O VVHYBDXTTJTWRO-JQWIXIFHSA-N 0.000 description 1
Classifications
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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
-
- 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)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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 | |
| US62/451,137 | 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 |
|---|---|
| KR20190096421A KR20190096421A (ko) | 2019-08-19 |
| KR102275338B1 true KR102275338B1 (ko) | 2021-07-12 |
Family
ID=61157343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197021750A Active KR102275338B1 (ko) | 2017-01-27 | 2018-01-19 | Oga 억제제로서의 n-[4-플루오로-5-[[(2s,4s)-2-메틸-4-[(5-메틸-1,2,4-옥사디아졸-3-일)메톡시]-1-피페리딜]메틸]티아졸-2-일]아세트아미드 |
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 |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| MA43680A (fr) | 2016-02-25 | 2018-11-28 | Asceneuron Sa | Inhibiteurs de glycosidases |
| MA43677A (fr) | 2016-02-25 | 2018-11-28 | Asceneuron Sa | Inhibiteurs de glycosidases |
| KR102800480B1 (ko) | 2016-02-25 | 2025-04-25 | 아셰뉴론 에스아 | 피페라진 유도체의 산 부가 염 |
| 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 |
| 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 |
| US11999726B2 (en) | 2018-07-31 | 2024-06-04 | 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 |
| SG11202101651RA (en) | 2018-08-22 | 2021-03-30 | Asceneuron S A | Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors |
| US12016852B2 (en) | 2018-08-22 | 2024-06-25 | Asceneuron Sa | Pyrrolidine glycosidase inhibitors |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| TWI863926B (zh) | 2018-09-19 | 2024-12-01 | 美商百健Ma公司 | O-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 |
| 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 |
| TW202039482A (zh) * | 2018-12-05 | 2020-11-01 | 美商百健Ma公司 | 嗎啉基、哌嗪基、氧氮雜環庚烷基及二氮雜環庚烷基o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 |
| WO2020163193A1 (en) * | 2019-02-04 | 2020-08-13 | 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 |
| IL293929A (en) | 2019-12-18 | 2022-08-01 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| WO2021123291A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| CN114867725A (zh) | 2019-12-18 | 2022-08-05 | 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 |
| WO2023070064A1 (en) | 2021-10-22 | 2023-04-27 | Eli Lilly And Company | O-glcnacase (oga) inhibitor combination therapy |
| US20250064417A1 (en) | 2022-02-03 | 2025-02-27 | 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014159234A1 (en) | 2013-03-14 | 2014-10-02 | Merck Patent Gmbh | Glycosidase inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8726763D0 (en) | 1987-11-16 | 1987-12-23 | Fujisawa Pharmaceutical Co | Thiazole compounds |
| WO2004094380A1 (en) | 2003-04-18 | 2004-11-04 | Eli Lilly And Company | (piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-ht1f agonists |
| 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 |
| 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 |
| JP6370294B2 (ja) * | 2013-05-30 | 2018-08-08 | 大日本住友製薬株式会社 | 環状アミノメチルピリミジン誘導体 |
| KR102043337B1 (ko) * | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| WO2017106254A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | 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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2018
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
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- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active Active
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en not_active Ceased
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
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2019
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- 2019-06-27 IL IL267693A patent/IL267693B/en unknown
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2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014159234A1 (en) | 2013-03-14 | 2014-10-02 | Merck Patent Gmbh | Glycosidase inhibitors |
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