EA022562B1 - ПИРАНО[3,2-d][1,3]ТИАЗОЛ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОЗИДАЗЫ - Google Patents

ПИРАНО[3,2-d][1,3]ТИАЗОЛ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОЗИДАЗЫ Download PDF

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Publication number
EA022562B1
EA022562B1 EA201490493A EA201490493A EA022562B1 EA 022562 B1 EA022562 B1 EA 022562B1 EA 201490493 A EA201490493 A EA 201490493A EA 201490493 A EA201490493 A EA 201490493A EA 022562 B1 EA022562 B1 EA 022562B1
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EA
Eurasian Patent Office
Prior art keywords
chiral
compound
atoms
compounds
mmol
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EA201490493A
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English (en)
Russian (ru)
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EA201490493A1 (ru
Inventor
Мэриэн Доннелли
Хой Цю
Генри Юй
Лесли Лю-Буджалски
Андреас Гоутопоулос
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Мерк Патент Гмбх
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Publication of EA201490493A1 publication Critical patent/EA201490493A1/ru
Publication of EA022562B1 publication Critical patent/EA022562B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/056—Triazole or tetrazole radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H9/00—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical
    • C07H9/06—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201490493A 2011-08-25 2012-08-22 ПИРАНО[3,2-d][1,3]ТИАЗОЛ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОЗИДАЗЫ EA022562B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161527323P 2011-08-25 2011-08-25
PCT/US2012/051785 WO2013028715A1 (en) 2011-08-25 2012-08-22 Pyrano [3, 2 - d] [1, 3] thiazole as glycosidase inhibitors

Publications (2)

Publication Number Publication Date
EA201490493A1 EA201490493A1 (ru) 2014-06-30
EA022562B1 true EA022562B1 (ru) 2016-01-29

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EA201490493A EA022562B1 (ru) 2011-08-25 2012-08-22 ПИРАНО[3,2-d][1,3]ТИАЗОЛ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОЗИДАЗЫ

Country Status (21)

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US (2) US8884023B2 (enExample)
EP (1) EP2748171B1 (enExample)
JP (1) JP5893738B2 (enExample)
KR (1) KR102008032B1 (enExample)
CN (1) CN103930428B (enExample)
AU (1) AU2012298949B2 (enExample)
BR (1) BR112014004219B1 (enExample)
CA (1) CA2845149C (enExample)
DK (1) DK2748171T3 (enExample)
EA (1) EA022562B1 (enExample)
ES (1) ES2568603T3 (enExample)
HR (1) HRP20160334T1 (enExample)
HU (1) HUE029390T2 (enExample)
IL (1) IL231008A (enExample)
MX (1) MX358463B (enExample)
PL (1) PL2748171T3 (enExample)
RS (1) RS54773B1 (enExample)
SG (1) SG2014009617A (enExample)
SI (1) SI2748171T1 (enExample)
WO (1) WO2013028715A1 (enExample)
ZA (1) ZA201400387B (enExample)

Families Citing this family (24)

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TW201249848A (en) 2010-11-08 2012-12-16 Merck Sharp & Dohme Selective glycosidase inhibitors and uses thereof
BR112013016179A2 (pt) 2010-12-23 2018-07-10 Alectos Therapeutics Inc inibidores seletivos da glicosidase e usos dos mesmos.
WO2012126091A1 (en) 2011-03-24 2012-09-27 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US9718854B2 (en) * 2011-03-31 2017-08-01 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
WO2013000085A1 (en) 2011-06-27 2013-01-03 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
MX364602B (es) 2011-06-27 2019-05-02 Alectos Therapeutics Inc Inhibidores selectivos de glicosidasa y usos de los mismos.
WO2013000086A1 (en) 2011-06-27 2013-01-03 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US8884023B2 (en) * 2011-08-25 2014-11-11 Merck Patent Gmbh Pyrano [3,2-D][1,3]thiazole as glycosidase inhibitors
EP2890675A4 (en) 2012-08-31 2016-01-13 Alectos Therapeutics Inc GLYCOSIDASE INHIBITORS AND USES THEREOF
EP2890676B1 (en) 2012-08-31 2018-12-05 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
EP2914604A4 (en) 2012-10-31 2016-07-20 Alectos Therapeutics Inc GLYCOSIDASE INHIBITORS AND USES THEREOF
WO2014100934A1 (en) * 2012-12-24 2014-07-03 Merck Sharp & Dohme Corp. Glycosidase inhibitors and uses thereof
MX381417B (es) 2014-08-28 2025-03-12 Asceneuron Sa Inhibidores de glucosidasa.
US10571963B2 (en) * 2015-09-18 2020-02-25 Toray Industries, Inc. Housing
JP6971999B2 (ja) 2016-02-25 2021-11-24 エースニューロン・ソシエテ・アノニム ピペラジン誘導体の酸付加塩
CN108884077A (zh) 2016-02-25 2018-11-23 阿森纽荣股份公司 糖苷酶抑制剂
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
JP2019506430A (ja) 2016-02-25 2019-03-07 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
US11213525B2 (en) 2017-08-24 2022-01-04 Asceneuron Sa Linear glycosidase inhibitors
WO2020039029A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Spiro compounds as glycosidase inhibitors
US11795165B2 (en) 2018-08-22 2023-10-24 Asceneuron Sa Tetrahydro-benzoazepine glycosidase inhibitors
US12016852B2 (en) 2018-08-22 2024-06-25 Asceneuron Sa Pyrrolidine glycosidase inhibitors
CA3110032A1 (en) 2018-08-22 2020-02-27 Asceneuron S.A. Succinate and fumarate acid addition salts of piperazine derivatives
TW202130643A (zh) * 2019-10-29 2021-08-16 美商百健Ma公司 螺環o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃糖苷酶抑制劑

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WO2008025170A1 (en) * 2006-08-31 2008-03-06 Simon Fraser University Selective glycosidase inhibitors and uses thereof

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AU2007210002A1 (en) * 2006-01-30 2007-08-09 Irm Llc Compounds and compositions as PPAR modulators
CN101595111A (zh) * 2006-08-31 2009-12-02 西蒙·弗雷瑟大学 选择性糖苷酶抑制剂及其用途
US9120781B2 (en) 2010-05-11 2015-09-01 Simon Fraser University Selective glycosidase inhibitors and uses thereof
WO2012061972A1 (en) 2010-11-08 2012-05-18 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
WO2012061927A1 (en) 2010-11-08 2012-05-18 Alectos Therapeutics, Inc. Selective glycosidase inhibitors and uses thereof
BR112013016179A2 (pt) 2010-12-23 2018-07-10 Alectos Therapeutics Inc inibidores seletivos da glicosidase e usos dos mesmos.
US8884023B2 (en) * 2011-08-25 2014-11-11 Merck Patent Gmbh Pyrano [3,2-D][1,3]thiazole as glycosidase inhibitors

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2008025170A1 (en) * 2006-08-31 2008-03-06 Simon Fraser University Selective glycosidase inhibitors and uses thereof

Non-Patent Citations (1)

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KANPP ET AL.: "An allosamizoline/Glucosamine Hybrid NAGase inhibitor", SYNLETT, no. 5 Suppl. 1, 1 May 1997 (1997-05-01), pages 435-436, XP008104081, GEORG THIEME VERLAG, DE, ISSN: 0936-5214, compounds 7, 11 *

Also Published As

Publication number Publication date
SG2014009617A (en) 2014-05-29
CN103930428A (zh) 2014-07-16
US20150018318A1 (en) 2015-01-15
KR102008032B1 (ko) 2019-08-06
HK1196607A1 (zh) 2014-12-19
US20140243370A1 (en) 2014-08-28
IL231008A (en) 2016-04-21
BR112014004219B1 (pt) 2021-11-30
RS54773B1 (sr) 2016-10-31
ES2568603T3 (es) 2016-05-03
BR112014004219A2 (pt) 2017-03-14
EP2748171B1 (en) 2016-02-03
CA2845149A1 (en) 2013-02-28
DK2748171T3 (en) 2016-05-09
ZA201400387B (en) 2015-05-27
MX2014002031A (es) 2014-03-21
EA201490493A1 (ru) 2014-06-30
IL231008A0 (en) 2014-03-31
CN103930428B (zh) 2016-05-11
EP2748171A1 (en) 2014-07-02
HUE029390T2 (en) 2017-02-28
AU2012298949B2 (en) 2016-09-22
WO2013028715A1 (en) 2013-02-28
JP5893738B2 (ja) 2016-03-23
AU2012298949A1 (en) 2014-01-30
SI2748171T1 (sl) 2016-06-30
US8884023B2 (en) 2014-11-11
KR20140054007A (ko) 2014-05-08
HRP20160334T1 (hr) 2016-05-06
CA2845149C (en) 2019-12-31
MX358463B (es) 2018-08-22
US9469657B2 (en) 2016-10-18
JP2014527060A (ja) 2014-10-09
PL2748171T3 (pl) 2016-06-30

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