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PE20171335A1 - Inhibidores de gingipaina de lisina - Google Patents

Inhibidores de gingipaina de lisina

Info

Publication number
PE20171335A1
PE20171335A1 PE2017000557A PE2017000557A PE20171335A1 PE 20171335 A1 PE20171335 A1 PE 20171335A1 PE 2017000557 A PE2017000557 A PE 2017000557A PE 2017000557 A PE2017000557 A PE 2017000557A PE 20171335 A1 PE20171335 A1 PE 20171335A1
Authority
PE
Peru
Prior art keywords
lysine
gingipaine
inhibitors
compounds
halogen
Prior art date
Application number
PE2017000557A
Other languages
English (en)
Inventor
Andrei Konradi
Stephen S Dominy
Lynch Casey Crawford
Craig Coburn
Joseph VACCA
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 PE20171335A1 publication Critical patent/PE20171335A1/es

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    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • A—HUMAN NECESSITIES
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    • 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
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Abstract

Se refiere a un compuesto de formula I, donde: Z es un grupo tiol reactivo o un grupo tiol reactivo enmascarado; A es -CH2- u -O-; B y D son independientemente H, halogeno, haloalquilo C1-C4 y haloalcoxi C1-C4; R1 es H o un grupo protector amina; R2 es H; R3 es arilo C6-C10, heteroarilo de 5 a 12 miembros, entre otros; L es -O-, alquileno C1-C4, entre otros; R4 es H, halogeno, alquilo C1-C4, entre otros. Son compuestos preferidos los compuestos de formula i), ii), entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tratamiento. Dichos compuestos inhiben la proteasa gingipaina de lisina (Kgp) de la bacteria Porphyromonas gingivalis, siendo utiles en el tratamiento de Alzheimer, cancer, entre otros
PE2017000557A 2014-10-06 2015-10-05 Inhibidores de gingipaina de lisina PE20171335A1 (es)

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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
PL3204352T3 (pl) 2014-10-06 2020-12-14 Cortexyme, Inc. Inhibitory gingipainy lizynowej
EP3374352A4 (en) 2015-11-09 2019-10-02 Cortexyme, Inc. GINGIPAINE ARGININE INHIBITORS
WO2017201322A1 (en) * 2016-05-19 2017-11-23 Cortexyme, Inc. Treatment of osteoarthritis with gingipain blocking agents
RU2019111188A (ru) 2016-09-16 2020-10-20 Кортексим, Инк. Кетоновые ингибиторы лизин-специфичного гингипаина
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