EA201490493A1 - Пирано[3,2-d][1,3]тиазол в качестве ингибиторов гликозидазы - Google Patents

Пирано[3,2-d][1,3]тиазол в качестве ингибиторов гликозидазы

Info

Publication number
EA201490493A1
EA201490493A1 EA201490493A EA201490493A EA201490493A1 EA 201490493 A1 EA201490493 A1 EA 201490493A1 EA 201490493 A EA201490493 A EA 201490493A EA 201490493 A EA201490493 A EA 201490493A EA 201490493 A1 EA201490493 A1 EA 201490493A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
glyozidase
pirano
tiazole
alzheimer
Prior art date
Application number
EA201490493A
Other languages
English (en)
Other versions
EA022562B1 (ru
Inventor
Мэриэн Доннелли
Хой Цю
Генри Юй
Лесли Лю-Буджалски
Андреас Гоутопоулос
Original Assignee
Мерк Патент Гмбх
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
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

Abstract

Новые соединения формулы (I), где R-Rи X имеют значения, указанные в формуле изобретения, являются ингибиторами гликозидазы и могут применяться, кроме прочего, для лечения болезни Альцгеймера.
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 true EA201490493A1 (ru) 2014-06-30
EA022562B1 EA022562B1 (ru) 2016-01-29

Family

ID=46759099

Family Applications (1)

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

Country Status (21)

Country Link
US (2) US8884023B2 (ru)
EP (1) EP2748171B1 (ru)
JP (1) JP5893738B2 (ru)
KR (1) KR102008032B1 (ru)
CN (1) CN103930428B (ru)
AU (1) AU2012298949B2 (ru)
CA (1) CA2845149C (ru)
DK (1) DK2748171T3 (ru)
EA (1) EA022562B1 (ru)
ES (1) ES2568603T3 (ru)
HK (1) HK1196607A1 (ru)
HR (1) HRP20160334T1 (ru)
HU (1) HUE029390T2 (ru)
IL (1) IL231008A (ru)
MX (1) MX358463B (ru)
PL (1) PL2748171T3 (ru)
RS (1) RS54773B1 (ru)
SG (1) SG2014009617A (ru)
SI (1) SI2748171T1 (ru)
WO (1) WO2013028715A1 (ru)
ZA (1) ZA201400387B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2592285C2 (ru) * 2010-11-08 2016-07-20 Алектос Терапьютикс Инк. Селективные ингибиторы гликозидазы и их применение

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101979036B1 (ko) 2010-12-23 2019-05-15 알렉토스 테라퓨틱스 인크. 선택적인 글리코시다아제 저해제 및 이의 용도
US8927507B2 (en) 2011-03-24 2015-01-06 Ernest J. McEachern Selective glycosidase inhibitors and uses thereof
EP2691407B1 (en) * 2011-03-31 2017-02-22 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2726492B1 (en) 2011-06-27 2017-11-01 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
CA2840013C (en) 2011-06-27 2021-02-09 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
US9199949B2 (en) 2011-06-27 2015-12-01 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
CA2845149C (en) * 2011-08-25 2019-12-31 Merck Patent Gmbh Pyrano[3,2-d] [1,3]thiazole as glycosidase inhibitors
WO2014032188A1 (en) 2012-08-31 2014-03-06 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
EP2890676B1 (en) 2012-08-31 2018-12-05 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
CA2890115A1 (en) 2012-10-31 2014-05-08 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
BR112017003658B1 (pt) 2014-08-28 2022-12-06 Asceneuron Sa Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica
WO2017047439A1 (ja) * 2015-09-18 2017-03-23 東レ株式会社 筐体
JP2019510006A (ja) 2016-02-25 2019-04-11 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
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
CN109071526B (zh) 2016-02-25 2023-02-28 阿森纽荣股份公司 哌嗪衍生物的酸加成盐
EP3419972B1 (en) 2016-02-25 2023-07-26 Asceneuron SA Glycosidase inhibitors
WO2019037860A1 (en) 2017-08-24 2019-02-28 Asceneuron S.A. LINEAR INHIBITORS OF GLYCOSIDASE
WO2020039029A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Spiro compounds as glycosidase inhibitors
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
WO2021086966A1 (en) * 2019-10-29 2021-05-06 Biogen Ma Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2599843C (en) * 2005-03-01 2013-08-27 Simon Fraser University Selective glycosidase inhibitors, methods of making inhibitors, and uses thereof
ATE445624T1 (de) * 2006-01-30 2009-10-15 Irm Llc Verbindungen und zusammensetzungen als ppar- modulatoren
EP2322529B1 (en) * 2006-08-31 2017-12-06 Simon Fraser University Selective glycosidase inhibitors and uses thereof
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
WO2012061927A1 (en) 2010-11-08 2012-05-18 Alectos Therapeutics, Inc. Selective glycosidase inhibitors and uses thereof
WO2012061972A1 (en) 2010-11-08 2012-05-18 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
KR101979036B1 (ko) 2010-12-23 2019-05-15 알렉토스 테라퓨틱스 인크. 선택적인 글리코시다아제 저해제 및 이의 용도
CA2845149C (en) * 2011-08-25 2019-12-31 Merck Patent Gmbh Pyrano[3,2-d] [1,3]thiazole as glycosidase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2592285C2 (ru) * 2010-11-08 2016-07-20 Алектос Терапьютикс Инк. Селективные ингибиторы гликозидазы и их применение

Also Published As

Publication number Publication date
RS54773B1 (sr) 2016-10-31
JP5893738B2 (ja) 2016-03-23
AU2012298949A1 (en) 2014-01-30
US20140243370A1 (en) 2014-08-28
DK2748171T3 (en) 2016-05-09
AU2012298949B2 (en) 2016-09-22
HRP20160334T1 (hr) 2016-05-06
ZA201400387B (en) 2015-05-27
ES2568603T3 (es) 2016-05-03
US20150018318A1 (en) 2015-01-15
CN103930428A (zh) 2014-07-16
CN103930428B (zh) 2016-05-11
IL231008A (en) 2016-04-21
CA2845149C (en) 2019-12-31
HK1196607A1 (zh) 2014-12-19
HUE029390T2 (en) 2017-02-28
MX358463B (es) 2018-08-22
BR112014004219A2 (pt) 2017-03-14
KR20140054007A (ko) 2014-05-08
KR102008032B1 (ko) 2019-08-06
US8884023B2 (en) 2014-11-11
MX2014002031A (es) 2014-03-21
PL2748171T3 (pl) 2016-06-30
IL231008A0 (en) 2014-03-31
SI2748171T1 (sl) 2016-06-30
CA2845149A1 (en) 2013-02-28
EA022562B1 (ru) 2016-01-29
EP2748171B1 (en) 2016-02-03
EP2748171A1 (en) 2014-07-02
US9469657B2 (en) 2016-10-18
WO2013028715A1 (en) 2013-02-28
JP2014527060A (ja) 2014-10-09
SG2014009617A (en) 2014-05-29

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