AU2018213029B2 - 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 - Google Patents

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 Download PDF

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AU2018213029B2
AU2018213029B2 AU2018213029A AU2018213029A AU2018213029B2 AU 2018213029 B2 AU2018213029 B2 AU 2018213029B2 AU 2018213029 A AU2018213029 A AU 2018213029A AU 2018213029 A AU2018213029 A AU 2018213029A AU 2018213029 B2 AU2018213029 B2 AU 2018213029B2
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methyl
pharmaceutically acceptable
acceptable salt
disease
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AU2018213029A1 (en
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Nicolas Jacques Francois Dreyfus
Peter James LINDSAY-SCOTT
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Eli Lilly and Co
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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)
  • 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)
AU2018213029A 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 Active AU2018213029B2 (en)

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

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AU2018213029A1 AU2018213029A1 (en) 2019-07-04
AU2018213029B2 true AU2018213029B2 (en) 2020-11-05

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US (1) US10081625B2 (https=)
EP (1) EP3573983B1 (https=)
JP (1) JP6738970B2 (https=)
KR (1) KR102275338B1 (https=)
CN (1) CN110198940B (https=)
AR (1) AR110747A1 (https=)
AU (1) AU2018213029B2 (https=)
CA (1) CA3049141C (https=)
CL (1) CL2019001978A1 (https=)
CO (1) CO2019007711A2 (https=)
CR (1) CR20190320A (https=)
CY (1) CY1124257T1 (https=)
DK (1) DK3573983T3 (https=)
DO (1) DOP2019000187A (https=)
EA (1) EA038368B1 (https=)
EC (1) ECSP19053616A (https=)
ES (1) ES2871949T3 (https=)
HR (1) HRP20211011T1 (https=)
HU (1) HUE054990T2 (https=)
IL (1) IL267693B (https=)
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PE (1) PE20191406A1 (https=)
PH (1) PH12019501707A1 (https=)
PL (1) PL3573983T3 (https=)
PT (1) PT3573983T (https=)
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UA (1) UA123472C2 (https=)
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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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MA47368B1 (fr) 2021-07-29
CN110198940B (zh) 2022-09-23
CL2019001978A1 (es) 2019-12-13
PE20191406A1 (es) 2019-10-04
MX387166B (es) 2025-03-19
PT3573983T (pt) 2021-06-17
JP2020504142A (ja) 2020-02-06
JOP20190182A1 (ar) 2019-07-25
RS61979B1 (sr) 2021-07-30
IL267693A (en) 2019-08-29
TWI654978B (zh) 2019-04-01
EP3573983B1 (en) 2021-04-21
MD3573983T2 (ro) 2021-10-31
ZA201904171B (en) 2022-01-26
DK3573983T3 (da) 2021-06-28
ES2871949T3 (es) 2021-11-02
JOP20190182B1 (ar) 2023-03-28
US20180215751A1 (en) 2018-08-02
PL3573983T3 (pl) 2021-10-04
ECSP19053616A (es) 2019-08-30
US10081625B2 (en) 2018-09-25
HUE054990T2 (hu) 2021-10-28
CA3049141C (en) 2021-02-16
JP6738970B2 (ja) 2020-08-12
CA3049141A1 (en) 2018-08-02
EA038368B1 (ru) 2021-08-17
AU2018213029A1 (en) 2019-07-04
HRP20211011T1 (hr) 2021-09-17
BR112019013535A2 (pt) 2020-01-07
MY197494A (en) 2023-06-19
DOP2019000187A (es) 2019-08-15
EP3573983A1 (en) 2019-12-04
KR20190096421A (ko) 2019-08-19
EA201991515A1 (ru) 2020-01-16
NZ754849A (en) 2021-10-29
PH12019501707A1 (en) 2020-03-16
CN110198940A (zh) 2019-09-03
KR102275338B1 (ko) 2021-07-12
CR20190320A (es) 2019-08-27
WO2018140299A1 (en) 2018-08-02
IL267693B (en) 2021-08-31
SI3573983T1 (sl) 2021-08-31
MX2019008846A (es) 2019-09-10
CO2019007711A2 (es) 2019-07-31
TW201836607A (zh) 2018-10-16
AR110747A1 (es) 2019-05-02
CY1124257T1 (el) 2022-07-22
LT3573983T (lt) 2021-07-26
UA123472C2 (uk) 2021-04-07

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