CN113166137B - O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂 - Google Patents

O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂 Download PDF

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CN113166137B
CN113166137B CN201980060829.1A CN201980060829A CN113166137B CN 113166137 B CN113166137 B CN 113166137B CN 201980060829 A CN201980060829 A CN 201980060829A CN 113166137 B CN113166137 B CN 113166137B
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methyl
acetamide
oxy
thiazol
methylpyrrolidin
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CN113166137A (zh
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N.杰农
K.M.古基安
J.韦塞尔斯
L.张
R.吉亚纳塔西奥
E.Y.S.林
Z.辛
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Biogen MA Inc
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Biogen MA Inc
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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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Saccharide Compounds (AREA)
CN201980060829.1A 2018-09-19 2019-09-18 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂 Active CN113166137B (zh)

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CN202411009108.7A CN119219621A (zh) 2018-09-19 2019-09-18 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂

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US201862733484P 2018-09-19 2018-09-19
US62/733,484 2018-09-19
US201862750000P 2018-10-24 2018-10-24
US62/750,000 2018-10-24
PCT/US2019/051661 WO2020061150A1 (en) 2018-09-19 2019-09-18 O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

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CN202411009108.7A Division CN119219621A (zh) 2018-09-19 2019-09-18 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂

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CN113166137A CN113166137A (zh) 2021-07-23
CN113166137B true CN113166137B (zh) 2024-08-16

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CN202411009108.7A Pending CN119219621A (zh) 2018-09-19 2019-09-18 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂

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US (2) US12180205B2 (https=)
EP (1) EP3853226A1 (https=)
JP (2) JP7606960B2 (https=)
KR (1) KR20210060513A (https=)
CN (2) CN113166137B (https=)
AU (1) AU2019344922B2 (https=)
BR (1) BR112021004739A2 (https=)
CA (1) CA3113009A1 (https=)
CL (1) CL2021000646A1 (https=)
CO (1) CO2021004873A2 (https=)
CR (1) CR20210181A (https=)
IL (2) IL315564A (https=)
JO (1) JOP20210036A1 (https=)
MA (1) MA53648A (https=)
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UA (1) UA130690C2 (https=)
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WO2022031701A1 (en) * 2020-08-03 2022-02-10 Biogen Ma Inc. Crystaline forms of an o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitor
KR102533471B1 (ko) * 2020-11-23 2023-05-19 (주) 메디프론디비티 O-GlcNAcase 저해 활성을 갖는 화합물 및 이의 용도
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
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SG11202102379XA (en) 2021-04-29
US20240308995A1 (en) 2024-09-19
IL281514B2 (en) 2025-02-01
IL281514A (en) 2021-04-29
JP2022500472A (ja) 2022-01-04
UY38376A (es) 2020-04-30
AU2019344922A1 (en) 2021-03-25
CO2021004873A2 (es) 2021-07-30
BR112021004739A2 (pt) 2021-06-01
CN119219621A (zh) 2024-12-31
JP2025011144A (ja) 2025-01-23
TWI863926B (zh) 2024-12-01
US12275728B2 (en) 2025-04-15
UA130690C2 (uk) 2026-04-22
PH12021550439A1 (en) 2021-11-29
CN113166137A (zh) 2021-07-23
WO2020061150A1 (en) 2020-03-26
TW202031651A (zh) 2020-09-01
EP3853226A1 (en) 2021-07-28
JOP20210036A1 (ar) 2021-02-25
CL2021000646A1 (es) 2021-09-03
US20220041586A1 (en) 2022-02-10
IL281514B1 (en) 2024-10-01
AU2019344922B2 (en) 2025-02-06
IL315564A (en) 2024-11-01
CA3113009A1 (en) 2020-03-26
CR20210181A (es) 2021-07-01
US12180205B2 (en) 2024-12-31
JP7606960B2 (ja) 2024-12-26
KR20210060513A (ko) 2021-05-26
PE20211591A1 (es) 2021-08-18
MA53648A (fr) 2021-07-28
MX2021003232A (es) 2021-07-16

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