AR083798A1 - Inhibidores selectivos de glucosidasas y sus usos - Google Patents

Inhibidores selectivos de glucosidasas y sus usos

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Publication number
AR083798A1
AR083798A1 ARP110104166A ARP110104166A AR083798A1 AR 083798 A1 AR083798 A1 AR 083798A1 AR P110104166 A ARP110104166 A AR P110104166A AR P110104166 A ARP110104166 A AR P110104166A AR 083798 A1 AR083798 A1 AR 083798A1
Authority
AR
Argentina
Prior art keywords
alkenyl
alkyl
maximum number
compounds
fluorine
Prior art date
Application number
ARP110104166A
Other languages
English (en)
Original Assignee
Merck Sharp & Dohme
Alectos Therapeutics Inc
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
Priority claimed from PCT/CN2010/078528 external-priority patent/WO2012061972A1/en
Application filed by Merck Sharp & Dohme, Alectos Therapeutics Inc filed Critical Merck Sharp & Dohme
Publication of AR083798A1 publication Critical patent/AR083798A1/es

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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Anesthesiology (AREA)
  • Diabetes (AREA)

Abstract

Se refiere a compuestos que inhiben selectivamente glucosidasas, a usos de los compuestos y a composiciones farmacéuticas que incluyen los compuestos, y a métodos para tratar enfermedades y trastornos relacionados con el déficit o la sobreexpresión de O-GlcNAcasa, y/o la acumulación o el déficit de O-GlcNAc.Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de dicho compuesto, en la que: cada R es independientemente H o C(O)CH3; R1 y R2 se seleccionan independientemente entre el grupo que consiste en: H, alquilo C1-6, alquenilo C2-6, alcoxi C1-6, -(CH2)n-ciclopropilo y -(CH2)n-ciclobutilo, en el que n es 0, 1, 2, 3 ó 4; o R1 y R2 pueden estar unidos junto con el átomo de nitrógeno al que están unidos para formar azetidina, pirrolidina, piperidina, o isoxazolidina, estando dichos alquilo C1-6, alquenilo C2-6, alcoxi C1-6, -(CH2)n-ciclopropilo, -(CH2)n-ciclobutilo, azetidina, pirrolidina, piperidina o isoxazolidina opcionalmente sustituidos uno hasta el número máximo de sustituyentes con flúor, hidroxi y metilo; R3 se selecciona entre el grupo que consiste en: alquilo C1-8, alquenilo C2-8, alquenilo C2-8, cicloalquilo C3-6, arilo y heteroarilo, cada uno opcionalmente sustituido de uno hasta el número máximo de sustituyentes por flúor y OH; R4 se selecciona entre el grupo que consiste en: H, F, alquilo C1-8, alquenilo C2-8 y alquinilo C2-8, excluyendo cada uno, hidrógeno opcionalmente sustituido de uno hasta el número máximo de sustituyentes por flúor y OH; o R3 y R4 y el átomo de carbono al que están unidos pueden unirse entre sí para formar vinilo o un anillo carbocíclico o heterocíclico de 3 a 7 miembros, conteniendo opcionalmente dicho anillo carbocíclico o heterocíclico de 3 a 7 miembros un doble enlace y estando opcionalmente sustituido de uno hasta el número máximo de sustituyentes por flúor y OH; y R5 se selecciona entre H, F, OH y OC(O)CH3; con la condición de que cuando R4 es F, entonces R5 es distinto de OH y OC(O)CH3.
ARP110104166A 2010-11-08 2011-11-08 Inhibidores selectivos de glucosidasas y sus usos AR083798A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2010/078528 WO2012061972A1 (en) 2010-11-08 2010-11-08 Selective glycosidase inhibitors and uses thereof
US41859610P 2010-12-01 2010-12-01
PCT/CN2011/080691 WO2012062157A1 (en) 2010-11-08 2011-10-12 Pyrano[3,2-d]thiazol derivatives and uses thereof as selective glycosidase inhibitors

Publications (1)

Publication Number Publication Date
AR083798A1 true AR083798A1 (es) 2013-03-20

Family

ID=46051261

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104166A AR083798A1 (es) 2010-11-08 2011-11-08 Inhibidores selectivos de glucosidasas y sus usos

Country Status (12)

Country Link
EP (1) EP2637503B1 (es)
JP (1) JP5965407B2 (es)
KR (1) KR101922266B1 (es)
AR (1) AR083798A1 (es)
AU (2) AU2011326186A1 (es)
BR (1) BR112013011441B8 (es)
CA (1) CA2816798C (es)
ES (1) ES2600028T3 (es)
MX (1) MX336611B (es)
RU (1) RU2592285C2 (es)
TW (1) TW201249848A (es)
WO (1) WO2012064680A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009276223B2 (en) 2008-08-01 2015-04-02 Simon Fraser University Selective glycosidase inhibitors and uses thereof
EP2569291B1 (en) 2010-05-11 2016-04-06 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
WO2012083435A1 (en) * 2010-12-23 2012-06-28 Alectos Therapeutics, Inc. Selective glycosidase inhibitors and uses thereof
EP2688899B1 (en) 2011-03-24 2017-02-22 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
WO2013000086A1 (en) 2011-06-27 2013-01-03 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
KR102054744B1 (ko) 2011-06-27 2019-12-11 알렉토스 테라퓨틱스 인크. 선택적인 글리코시다아제 저해제 및 이의 용도
JP6178843B2 (ja) * 2012-05-08 2017-08-09 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 透過性グリコシダーゼインヒビターおよびその用途
WO2014032185A1 (en) 2012-08-31 2014-03-06 Alectos Therapeutics Inc. Glycosidase inhibitors and uses thereof
EP2890675A4 (en) 2012-08-31 2016-01-13 Alectos Therapeutics Inc GLYCOSIDASE INHIBITORS AND USES THEREOF
WO2014067003A1 (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
JP6994819B2 (ja) 2016-07-26 2022-02-04 三菱電機株式会社 照明具および照明装置
RU2748383C1 (ru) * 2020-10-21 2021-05-25 федеральное государственное автономное образовательное учреждение высшего образования "Казанский (Приволжский) федеральный университет" (ФГАОУ ВО КФУ) Способ терапии болезни Тея-Сакса и болезни Сандхоффа с помощью генетически модифицированных мезенхимных стволовых клеток человека со сверхэкспрессией β-гексозаминидазы A
WO2024083820A1 (en) 2022-10-18 2024-04-25 Institut National de la Santé et de la Recherche Médicale Method and composition for determining the level of o-glcnacylation in horses

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1441749A1 (ru) * 1987-03-16 1996-01-10 Институт Тонкой Органической Химии Им.А.Л.Мнджояна 2-АМИНО-5,5-ДИМЕТИЛ-4,5-ДИГИДРО-7Н-ПИРАНО [4,3-d] ТИАЗОЛ, ОБЛАДАЮЩИЙ ТРАНКВИЛИЗИРУЮЩЕЙ АКТИВНОСТЬЮ
JP5154954B2 (ja) 2005-03-01 2013-02-27 サイモン フレイザー ユニバーシティ 選択的なグリコシダーゼインヒビター、インヒビターを作製する方法、およびインヒビターの使用
JP5380293B2 (ja) * 2006-08-31 2014-01-08 サイモン・フレーザー・ユニバーシティ 選択的グリコシダーゼ阻害剤およびその使用
CA2732335A1 (en) 2008-08-01 2010-02-04 Simon Fraser University Selective glycosidase inhibitors and uses thereof
AU2009276223B2 (en) 2008-08-01 2015-04-02 Simon Fraser University Selective glycosidase inhibitors and uses thereof
US20110301217A1 (en) 2008-09-16 2011-12-08 David Jaro Vocadlo Selective Glycosidase Inhibitors and Uses Thereof
CN103930428B (zh) 2011-08-25 2016-05-11 默克专利有限公司 用作糖苷酶抑制剂的吡喃并[3,2-d][1,3]噻唑

Also Published As

Publication number Publication date
AU2011326186A8 (en) 2013-08-01
EP2637503B1 (en) 2016-09-14
TW201249848A (en) 2012-12-16
KR20130129974A (ko) 2013-11-29
ES2600028T3 (es) 2017-02-06
JP2013541596A (ja) 2013-11-14
KR101922266B1 (ko) 2018-11-26
CA2816798C (en) 2019-02-26
JP5965407B2 (ja) 2016-08-03
BR112013011441B1 (pt) 2021-11-09
AU2016202186B2 (en) 2017-10-12
RU2013126531A (ru) 2014-12-20
BR112013011441A2 (pt) 2016-07-19
AU2011326186A1 (en) 2013-05-23
EP2637503A4 (en) 2014-04-09
AU2016202186A1 (en) 2016-04-28
MX336611B (es) 2016-01-22
MX2013005118A (es) 2013-07-29
BR112013011441B8 (pt) 2023-04-18
CA2816798A1 (en) 2012-05-18
WO2012064680A1 (en) 2012-05-18
EP2637503A1 (en) 2013-09-18
RU2592285C2 (ru) 2016-07-20

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