PE20181492A1 - Compuestos sustituidos de 4-fenilpiridina como agonistas de tgr5 no sistemicos - Google Patents

Compuestos sustituidos de 4-fenilpiridina como agonistas de tgr5 no sistemicos

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Publication number
PE20181492A1
PE20181492A1 PE2018001117A PE2018001117A PE20181492A1 PE 20181492 A1 PE20181492 A1 PE 20181492A1 PE 2018001117 A PE2018001117 A PE 2018001117A PE 2018001117 A PE2018001117 A PE 2018001117A PE 20181492 A1 PE20181492 A1 PE 20181492A1
Authority
PE
Peru
Prior art keywords
alkyl
alkoxy
independently
phenylpyridine
compounds
Prior art date
Application number
PE2018001117A
Other languages
English (en)
Inventor
Jason G Lewis
Michael Robert Leadbetter
Jeremy Caldwell
Dean Dragoli
Noah Bell
Jeffrey W Jacobs
Patricia Finn
Rakesh Jain
Tao Chen
Matthew Siegel
Original Assignee
Ardelyx 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 Ardelyx Inc filed Critical Ardelyx Inc
Publication of PE20181492A1 publication Critical patent/PE20181492A1/es

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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
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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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4425—Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
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Abstract

Referido a un compuesto de formula(I´), en donde Q es C=(O), -CH2-, -NR5- u -O-; X1 es CR6 o N; X2 es CR7 o N; X3 es CR8 o N; X4 es CR9 o N; Y es CRb o N; Ra y Rb son cada uno, independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros, entre otros; R1 es H, alquilo(C1-C6), alcoxi(C1-C6), entre otros; R2 y R2´son cada uno independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros; cada R3 es, de modo independientemente, alquilo(C1-C6), alcoxi(C1-C6), haloalquilo(C1-C6), entre otros; R4 es H, alquilo(C1-C6), alcoxi(C1-C6), entre otros; R5 es H-, -C(O)alquilo(C1-C6) o -C(O)Oalquilo(C1-C6), entre otros; cada R6 y R9 es, de modo independientemente, H, alquilo(C1-C6), alcoxi(C1-C6), entre otros; cada R7 y R8 es, de modo independientemente, H, alquenilo(C1-C8), alquinilo(C1-C6), entre otros; n es 0, 1 o 2. Estos, son compuestos sustituidos de 4-fenilpiridina, agonista de TGR5 no sistemico. Tambien se refiere a metodos para preparar estos compuestos, y su utilidad en el tratamiento de diarrea inducida por quimioterapia, diabetes, entre otras enfermedades y trastornos asociados con TGR5.
PE2018001117A 2015-12-18 2016-12-19 Compuestos sustituidos de 4-fenilpiridina como agonistas de tgr5 no sistemicos PE20181492A1 (es)

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