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PE20190473A1 - Inhibidores cetonicos de gingipain de lisina - Google Patents

Inhibidores cetonicos de gingipain de lisina

Info

Publication number
PE20190473A1
PE20190473A1 PE2019000533A PE2019000533A PE20190473A1 PE 20190473 A1 PE20190473 A1 PE 20190473A1 PE 2019000533 A PE2019000533 A PE 2019000533A PE 2019000533 A PE2019000533 A PE 2019000533A PE 20190473 A1 PE20190473 A1 PE 20190473A1
Authority
PE
Peru
Prior art keywords
alkyl
kingon
lisina
ketonic
inhibitors
Prior art date
Application number
PE2019000533A
Other languages
English (en)
Inventor
Andrei W Konradi
Jr Robert A Galemmo
Stephen S Dominy
Casey C Lynch
Leslie J Holsinger
Original Assignee
Cortexyme 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
Application filed by Cortexyme Inc filed Critical Cortexyme Inc
Publication of PE20190473A1 publication Critical patent/PE20190473A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • 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
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    • 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
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    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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Abstract

Se refiere a un compuesto de formula (I), donde A se selecciona del grupo integrado por -CH2- y -O- ; R1a y R1B se seleccionan, cada uno de manera independiente, del grupo integrado por H, alquilo C1-C4 y un grupo protector de aminas; R2a y R2B pueden ser H, halogeno, haloalquilo C1-C4 y haloalcoxi C1-C4; R3 puede ser cicloalquilo C3-C8, alquilo C3-C8, heterociclilo de 3 a 12 miembros, entre otros; R4 puede ser H y alquilo C1-C4; R5 puede ser haloalquilo C1-C6, entre otros. Dicho compuesto presenta una actividad potente para inhibir la gingipaina de lisina (Kgp) de P. gingivalis que presentan selectividad incrementada por Kgp respecto de proteasas endogenas tales como las catepsinas, y es util en el tratamiento de la enfermedad de Alzheimer, asi como procesos patologicos e infecciosos asociados a P. gingivalis.
PE2019000533A 2016-09-16 2017-09-15 Inhibidores cetonicos de gingipain de lisina PE20190473A1 (es)

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