ES2587745T3 - Derivados de imidazo[2,1]tiazol-3-ona útiles como agentes de diagnóstico para la enfermedad de Alzheimer - Google Patents

Derivados de imidazo[2,1]tiazol-3-ona útiles como agentes de diagnóstico para la enfermedad de Alzheimer Download PDF

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Publication number
ES2587745T3
ES2587745T3 ES13745668.7T ES13745668T ES2587745T3 ES 2587745 T3 ES2587745 T3 ES 2587745T3 ES 13745668 T ES13745668 T ES 13745668T ES 2587745 T3 ES2587745 T3 ES 2587745T3
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Prior art keywords
halogen
substituted
alkyl
hydrogen
7alkyl
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ES13745668.7T
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English (en)
Inventor
Luca Gobbi
Henner Knust
Andreas Koblet
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

Un compuesto de fórmula**Fórmula** en el que Ar es fenilo, piridinilo, 2,3-dihidro-benzo[1,4]dioxinilo, 1,3-dihidro-indol-2-ona, pirazinilo, isoxazol-3-ilo, imidazolilo, tiofenilo o pirimidinilo; R es alquilo-C1-7 o alquilo-C1-7 sustituido por halógeno; R1 es hidrógeno, halógeno, hidroxi, alcoxi-C1-7, alquilo-C1-7 y alcoxi-C1-7 sustituido por halógeno; R2 es hidrógeno, alquilo-C1-7; R3 es hidrógeno, halógeno, alquilo-C1-7, alquilo-C1-7 sustituido por halógeno, alcoxi-C1-7, alcoxi-C1-7 sustituido por halógeno, O(CH2)mO(CH2)mO-alquilo-C1-7 sustituido por halógeno, ciano, alcoxi-C1-7 sustituido por hidroxi, alqueniloxi-C1-7, C(O)OH, heterocicloalquilo seleccionado de morfolinilo, pirrolidinilo o pirrolidin-2-ona, o es heteroarilo seleccionado entre imidazolilo sustituido por alquilo-C1-7, o es NR'R" y R'/R" son independientemente uno del otro hidrógeno o alquilo-C1-7 o-C(O)-alquilo-C1-7; o es-C(O)NR4R5 y R4 es hidrógeno o alquilo-C1-7 y R5 es hidrógeno, alquilo-C1-7, alquenilo-C1-7,-(CH2)mO-alquilo-C1-7 sustituido por halógeno, alquilo-C1-7 sustituido por halógeno,-(CH2)n-fenilo opcionalmente sustituido por halógeno,-(CH2) mNHC(O)-alquilo-C1-7, o-(CH2)mNH2, o R4 y R5 pueden formar junto con el átomo de N al que están unidos, un anillo de piperidina o azetidina, que puede estar sustituido por halógeno; o es-C(O)O-alquilo-C1-7 sustituido por halógeno; n es 1 o 2; m es 1, 2 o 3; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o su correspondiente enantiómero y/o isómeros ópticos de los mismos.
ES13745668.7T 2012-08-14 2013-08-06 Derivados de imidazo[2,1]tiazol-3-ona útiles como agentes de diagnóstico para la enfermedad de Alzheimer Active ES2587745T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12180367 2012-08-14
EP12180367 2012-08-14
PCT/EP2013/066447 WO2014026881A1 (en) 2012-08-14 2013-08-06 Imidazo[2,1]thiazol-3-one derivatives useful as diagnostic agents for alzheimer's disease

Publications (1)

Publication Number Publication Date
ES2587745T3 true ES2587745T3 (es) 2016-10-26

Family

ID=46851292

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13745668.7T Active ES2587745T3 (es) 2012-08-14 2013-08-06 Derivados de imidazo[2,1]tiazol-3-ona útiles como agentes de diagnóstico para la enfermedad de Alzheimer

Country Status (12)

Country Link
US (1) US20150157739A1 (es)
EP (1) EP2885306B1 (es)
JP (1) JP6228980B2 (es)
KR (1) KR20150042787A (es)
CN (1) CN104411709B (es)
BR (1) BR112015000447A2 (es)
CA (1) CA2876459A1 (es)
ES (1) ES2587745T3 (es)
HK (1) HK1206343A1 (es)
MX (1) MX2015001546A (es)
RU (1) RU2015106437A (es)
WO (1) WO2014026881A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105560831A (zh) * 2016-01-08 2016-05-11 肖鉴 一种治疗不孕不育的中药组合物
MY196981A (en) 2016-07-22 2023-05-16 Ac Immune Sa Compounds for imaging tau protein aggregates
US10865207B2 (en) 2016-07-22 2020-12-15 Ac Immune S.A. Compounds for imaging Tau protein aggregates
WO2018189108A1 (en) * 2017-04-12 2018-10-18 Dsm Ip Assets B.V. A process for preparation of an imidazothiazolone compound
US11306089B2 (en) 2018-01-24 2022-04-19 Life Molecular Imaging Limited Gamma-carboline compounds for the detection of Tau aggregates
EP3743426A1 (en) 2018-01-24 2020-12-02 AC Immune SA Azacarboline compounds for the detection of tau aggregates

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008070875A2 (en) * 2006-12-08 2008-06-12 Roskamp Research Llc Polyhydroquinoline compounds and dihydropyridine compounds for inhibiting beta-amyloid production
RU2518892C2 (ru) * 2008-09-23 2014-06-10 Виста Лабораториз Лтд. Лиганды для агрегированных молекул тау-белка
CN103739605B (zh) * 2009-03-23 2016-08-17 伊莱利利公司 用于检测神经障碍的显像剂
WO2012078909A1 (en) * 2010-12-08 2012-06-14 Proteostasis Therapeutics, Inc. Thiazolpyrimidine proteostasis regulators

Also Published As

Publication number Publication date
KR20150042787A (ko) 2015-04-21
CA2876459A1 (en) 2014-02-20
HK1206343A1 (zh) 2016-01-08
EP2885306B1 (en) 2016-06-01
JP6228980B2 (ja) 2017-11-08
JP2015524830A (ja) 2015-08-27
CN104411709B (zh) 2016-08-24
WO2014026881A1 (en) 2014-02-20
CN104411709A (zh) 2015-03-11
BR112015000447A2 (pt) 2017-06-27
MX2015001546A (es) 2015-05-11
EP2885306A1 (en) 2015-06-24
RU2015106437A (ru) 2016-10-10
US20150157739A1 (en) 2015-06-11

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