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PE20180529A1 - Agonistas de triazol del receptor apj - Google Patents

Agonistas de triazol del receptor apj

Info

Publication number
PE20180529A1
PE20180529A1 PE2017002442A PE2017002442A PE20180529A1 PE 20180529 A1 PE20180529 A1 PE 20180529A1 PE 2017002442 A PE2017002442 A PE 2017002442A PE 2017002442 A PE2017002442 A PE 2017002442A PE 20180529 A1 PE20180529 A1 PE 20180529A1
Authority
PE
Peru
Prior art keywords
apj receptor
triazole
monocyclic
methoxy
formula
Prior art date
Application number
PE2017002442A
Other languages
English (en)
Inventor
Ning Chen
Xiaoqi Chen
Yinhong Chen
Alan C Cheng
Richard V Connors
Jeffrey Deignan
Paul John Dransfield
Xiaohui Du
Zice Fu
Julie Anne Heath
Daniel B Horne
Jonathan Houze
Matthew R Kaller
Aarif Yusuf Khakoo
David John Kopecky
Su-Jen Lai
Zhihua Ma
Lawrence R Mcgee
Julio C Medina
Jeffrey Thomas Mihalic
Nobuko Nishimura
Steven H Olson
Vatee Pattaropong
Gayathri Swaminath
Xiaodong Wang
Kevin Yang
Wen-Chen Yeh
Mikkel V Debenedetto
Robert P Farrell
Simon J Hedley
Ted C Judd
Frank Kayser
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of PE20180529A1 publication Critical patent/PE20180529A1/es

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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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Abstract

Se refiere a un compuesto agonista de triazol del receptor APJ de formula I o II o una sal farmaceuticamente aceptable del mismo, un tautomero del mismo, un estereoisomero donde: R1 es piridilo, piridonilo, entre otros; R2 es -H o alquilo C1-C4 o esta ausente como en la formula II; R3 es un alquilo C1-C10 opcionalmente sustituido en R3a y otros donde R3a es -F, -Cl, -CN, entre otros; R4 es arilo C6-C10 monociclico o biciclico, un grupo heteroarilo monociclico o biciclico, entre otros. Son compuestos preferidos: (1R, 2S)-N-(4-(2,6-dimetoxifenil)-5-(6-metoxi-2-piridinil)-4H-1,2,4-triazol-3-il)-1-metoxi-1-(5-metil-2-pirimidinil)-2-propansulfonamida, entre otros. La presente invencion es util para el tratamiento de afecciones cardiovasculares como lo es la insuficiencia cardiaca cronica entre otras.
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