TWI863926B - O-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 - Google Patents

O-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 Download PDF

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TWI863926B
TWI863926B TW108133538A TW108133538A TWI863926B TW I863926 B TWI863926 B TW I863926B TW 108133538 A TW108133538 A TW 108133538A TW 108133538 A TW108133538 A TW 108133538A TW I863926 B TWI863926 B TW I863926B
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methyl
acetamide
oxy
thiazol
methylpyrrolidin
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TW108133538A
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Chinese (zh)
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TW202031651A (zh
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納森 根南
凱文 M 庫其安
傑佛瑞 凡索斯
磊 張
萊恩 加恩踏西歐
盈翔 林
芷莉 忻
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美商百健Ma公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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)
  • Diabetes (AREA)
  • 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)
TW108133538A 2018-09-19 2019-09-18 O-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 TWI863926B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
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

Publications (2)

Publication Number Publication Date
TW202031651A TW202031651A (zh) 2020-09-01
TWI863926B true TWI863926B (zh) 2024-12-01

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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=)
MX (1) MX2021003232A (https=)
PE (1) PE20211591A1 (https=)
PH (1) PH12021550439A1 (https=)
SG (1) SG11202102379XA (https=)
TW (1) TWI863926B (https=)
UA (1) UA130690C2 (https=)
UY (1) UY38376A (https=)
WO (1) WO2020061150A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12180205B2 (en) * 2018-09-19 2024-12-31 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
EP3643711A1 (en) 2018-10-24 2020-04-29 Bayer Animal Health GmbH New anthelmintic compounds
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
US12612396B1 (en) 2024-11-20 2026-04-28 Dewpoint Therapeutics, Inc. Modulators of beta catenin and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018109202A1 (en) * 2016-12-16 2018-06-21 Janssen Pharmaceutica Nv Monocyclic oga inhibitor compounds

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
JP2004520347A (ja) 2001-01-15 2004-07-08 グラクソ グループ リミテッド Ldl−受容体発現のインデューサーとしてのアリールピペリジンおよびピペラジン誘導体
BRPI0515500A (pt) 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados piridazina para inibição de estearoil-coa-desaturase
SG172352A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
JP2013526546A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Pde10阻害剤としてのヘテロアリ−ルオキシヘテロシクリル化合物
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013078320A1 (en) 2011-11-21 2013-05-30 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
JP5989805B2 (ja) 2012-02-10 2016-09-07 コンステレーション・ファーマシューティカルズ・インコーポレイテッドConstellation Pharmaceuticals,Inc. メチル基変更酵素の調節物質、組成物及びその使用
WO2013170072A2 (en) 2012-05-09 2013-11-14 Neurop, Inc. Compounds for the treatment of neurological disorders
WO2014067003A1 (en) 2012-10-31 2014-05-08 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
MA38341B1 (fr) 2013-02-11 2018-11-30 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
PT2970272T (pt) 2013-03-14 2019-06-05 Merck Patent Gmbh Inibidores de glicosidase
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
KR20160100408A (ko) 2014-01-06 2016-08-23 리젠 파마슈티컬스 소시에떼 아노님 신규한 글루타미나제 저해제
CN105753814A (zh) 2015-01-01 2016-07-13 成都贝斯凯瑞生物科技有限公司 取代氮杂环衍生物及其应用
US20190359609A1 (en) * 2016-12-16 2019-11-28 Janssen Pharmaceutica Nv Bicyclic oga inhibitor compounds
TWI654978B (zh) 2017-01-27 2019-04-01 美商美國禮來大藥廠 5-甲基-1,2,4-二唑-3-基化合物
JP7453916B2 (ja) * 2018-03-14 2024-03-21 バイオジェン・エムエイ・インコーポレイテッド O-糖タンパク質-2-アセトアミド-2-デオキシ-3-d-グリコピラノシダーゼ阻害剤
US11459324B2 (en) 2018-03-14 2022-10-04 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-D-glycopyranosidase inhibitors
CA3102903A1 (en) 2018-06-20 2019-12-26 Janssen Pharmaceutica Nv Oga inhibitor compounds
US12180205B2 (en) 2018-09-19 2024-12-31 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018109202A1 (en) * 2016-12-16 2018-06-21 Janssen Pharmaceutica Nv Monocyclic oga inhibitor compounds

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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
US12275728B2 (en) 2025-04-15
UA130690C2 (uk) 2026-04-22
PH12021550439A1 (en) 2021-11-29
CN113166137B (zh) 2024-08-16
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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