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

Info

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
Authority
EA
Eurasian Patent Office
Prior art keywords
chiral
compound
atoms
compounds
mmol
Prior art date
Application number
EA201490493A
Other languages
English (en)
Russian (ru)
Other versions
EA201490493A1 (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

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/056Triazole or tetrazole radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H9/00Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical
    • C07H9/06Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms

Landscapes

  • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (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

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 (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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201249848A (en) * 2010-11-08 2012-12-16 Merck Sharp & Dohme Selective glycosidase inhibitors and uses thereof
LT2655388T (lt) 2010-12-23 2016-11-10 Alectos Therapeutics Inc. Selektyvieji glikozidazės inhibitoriai ir jų panaudojimas
WO2012126091A1 (en) 2011-03-24 2012-09-27 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2691407B1 (en) * 2011-03-31 2017-02-22 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
WO2013000084A1 (en) 2011-06-27 2013-01-03 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
WO2013000086A1 (en) 2011-06-27 2013-01-03 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
EP2726468B1 (en) 2011-06-27 2017-04-12 Alectos Therapeutics Inc. Selective glycosidase inhibitors and uses thereof
SG2014009617A (en) * 2011-08-25 2014-05-29 Merck Patent Gmbh Pyrano [3, 2 - d] [1, 3] thiazole as glycosidase inhibitors
US9809537B2 (en) 2012-08-31 2017-11-07 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
US9670195B2 (en) 2012-08-31 2017-06-06 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
US9695197B2 (en) 2012-10-31 2017-07-04 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
KR102043337B1 (ko) 2014-08-28 2019-11-11 아셰뉴론 에스아 글리코시다제 저해제
EP3352540B1 (en) * 2015-09-18 2021-03-17 Toray Industries, Inc. Housing
ES2879351T3 (es) 2016-02-25 2021-11-22 Asceneuron Sa Sales de derivados de piperazina obtenidas por adición de ácidos
MA43680A (fr) 2016-02-25 2018-11-28 Asceneuron Sa Inhibiteurs de glycosidases
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
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
US11213525B2 (en) 2017-08-24 2022-01-04 Asceneuron Sa Linear glycosidase inhibitors
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
WO2020039027A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Pyrrolidine glycosidase inhibitors
EA202190275A1 (ru) 2018-08-22 2021-08-02 Асенейрон С. А. Сукцинатные и фумаратные кислотно-аддитивные соли производных пиперазина, пригодные в качестве ингибиторов гликозидазы
US11731972B2 (en) 2018-08-22 2023-08-22 Asceneuron Sa Spiro compounds as glycosidase inhibitors
WO2021086966A1 (en) * 2019-10-29 2021-05-06 Biogen Ma Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2436687A1 (en) * 2005-03-01 2012-04-04 Simon Fraser University Selective glycosidase inhibitors, methods of making inhibitors, and uses thereof
WO2007089667A1 (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
WO2011140640A1 (en) 2010-05-11 2011-11-17 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
LT2655388T (lt) 2010-12-23 2016-11-10 Alectos Therapeutics Inc. Selektyvieji glikozidazės inhibitoriai ir jų panaudojimas
SG2014009617A (en) * 2011-08-25 2014-05-29 Merck Patent Gmbh Pyrano [3, 2 - d] [1, 3] thiazole as glycosidase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

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

Similar Documents

Publication Publication Date Title
EA022562B1 (ru) ПИРАНО[3,2-d][1,3]ТИАЗОЛ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОЗИДАЗЫ
JP7082446B2 (ja) スルホキシイミングリコシダーゼ阻害剤
CA2899088C (en) Thiazole and oxazole compounds as glycosidase inhibitors
CA3053200C (en) Sulfoximine glycosidase inhibitors
US12016852B2 (en) Pyrrolidine glycosidase inhibitors
AU2019200339A1 (en) Glycosidase inhibitors
TWI691486B (zh) 環狀胺衍生物及其醫藥用途
WO2020039028A1 (en) Tetrahydro-benzoazepine glycosidase inhibitors
AU2017400271A1 (en) Sulfoximine glycosidase inhibitors
EP3672959A1 (en) Linear glycosidase inhibitors
HK1196607B (en) Pyrano [3, 2 - d] [1, 3] thiazole as glycosidase inhibitors
CN113735825A (zh) 1,2,3,6-四氢吡啶类化合物及其制备方法和用途
EA037845B1 (ru) Производные 4-гидрокси-2-фенил-1,3-тиазол-5-ил метанона как антагонисты trpm8

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM