AR094277A1 - Derivados de fumarato sustituidos con deuterio - Google Patents

Derivados de fumarato sustituidos con deuterio

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Publication number
AR094277A1
AR094277A1 ARP130105025A ARP130105025A AR094277A1 AR 094277 A1 AR094277 A1 AR 094277A1 AR P130105025 A ARP130105025 A AR P130105025A AR P130105025 A ARP130105025 A AR P130105025A AR 094277 A1 AR094277 A1 AR 094277A1
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AR
Argentina
Prior art keywords
disease
deuterium
hydrogen
sulfur
nitrogen
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Application number
ARP130105025A
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English (en)
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Biogen Idec Inc
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Publication of AR094277A1 publication Critical patent/AR094277A1/es

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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/593Dicarboxylic acid esters having only one carbon-to-carbon double bond
    • C07C69/60Maleic acid esters; Fumaric acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/225Polycarboxylic acids
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    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
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    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • C07C229/34Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings

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Abstract

Se proporciona un método para tratar, profilaxis, o mejorar una enfermedad que comprende administrar a un sujeto que necesita tratamiento para la enfermedad una cantidad eficaz de un compuesto de fórmula (1) descrito en el presente. En una realización, el método es una enfermedad neurodegenerativa, por ejemplo esclerosis múltiple, esclerosis lateral amiotrófica, enfermedad de Parkinson, enfermedad de Huntington o mal de Alzheimer. Reivindicación 1: Un compuesto caracterizado porque tiene la de fórmula (1) o una sal farmacéuticamente aceptable de este, en donde cada uno de R¹ y R², independientemente, es hidrógeno, deuterio, metilo deuterado, etilo deuterado, alifático C₁₋₆, fenilo, anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 7 miembros, anillo heterocíclico monocíclico saturado o parcialmente insaturado de 3 - 7 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, y azufre, o un anillo heteroarilo de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, y azufre, y cada uno de R³ y R⁴, independientemente, es hidrógeno o deuterio, en donde uno de R³ y R⁴ es deuterio y con la condición de que R¹ y R² no sean hidrógeno al mismo tiempo.
ARP130105025A 2012-12-21 2013-12-20 Derivados de fumarato sustituidos con deuterio AR094277A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261745115P 2012-12-21 2012-12-21

Publications (1)

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AR094277A1 true AR094277A1 (es) 2015-07-22

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ARP130105025A AR094277A1 (es) 2012-12-21 2013-12-20 Derivados de fumarato sustituidos con deuterio

Country Status (8)

Country Link
US (2) US20140179779A1 (es)
EP (2) EP2934503B1 (es)
JP (2) JP6506174B2 (es)
CN (1) CN105142628A (es)
AR (1) AR094277A1 (es)
ES (1) ES2733961T3 (es)
TW (1) TW201436790A (es)
WO (1) WO2014100728A1 (es)

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CN106946701B (zh) * 2017-03-28 2020-05-15 重庆纽源生物科技有限公司 一种水杨酸基富马酸盐衍生物及在治疗帕金森症和其他神经退行性疾病应用
WO2020094767A1 (en) 2018-11-08 2020-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of nrf2 activators for the treatment of staphylococcus aureus infections
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JP7406566B2 (ja) * 2019-04-17 2023-12-27 イクシェル ファーマ エルエルシー フマル酸モノメチルのプロドラッグ
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JP2016510317A (ja) 2016-04-07

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