AR111284A1 - Agonistas del receptor farnesoide x y usos de los mismos - Google Patents

Agonistas del receptor farnesoide x y usos de los mismos

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Publication number
AR111284A1
AR111284A1 ARP180100608A ARP180100608A AR111284A1 AR 111284 A1 AR111284 A1 AR 111284A1 AR P180100608 A ARP180100608 A AR P180100608A AR P180100608 A ARP180100608 A AR P180100608A AR 111284 A1 AR111284 A1 AR 111284A1
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Argentina
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alkyl
substituted
unsubstituted
nr15c
fluoroalkyl
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ARP180100608A
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English (en)
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Johnny Y Nagasawa
Nicholas D Smith
Steven P Govek
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Metacrine Inc
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Publication of AR111284A1 publication Critical patent/AR111284A1/es

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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K9/0029—Parenteral nutrition; Parenteral nutrition compositions as drug carriers
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    • A—HUMAN NECESSITIES
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61K9/4841—Filling excipients; Inactive ingredients
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuestos que son antagonistas del receptor farnesoide X, métodos para hacer dichos compuestos, composiciones farmacéuticas y medicamentos que comprenden dichos compuestos y métodos para utilizar dichos compuestos en el tratamiento de afecciones, enfermedades o trastornos asociados con la actividad del receptor X farnesoide. Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1), o una sal o solvato farmacéuticamente aceptable del mismo, en la que, X¹ es CH o N; R¹ es H, D, halógeno, -CN, -OH, -SH, -N(R¹⁵)₂, -NR¹⁵S(=O)₂(alquilo C₁₋₄), -S(alquilo C₁₋₄), -S(=O)(alquilo C₁₋₄), -S(=O)₂(alquilo C₁₋₄), -S(=O)₂N(R¹⁵)₂, -OC(=O)(alquilo C₁₋₄), -CO₂H, -CO₂(alquilo C₁₋₄), -C(=O)N(R¹⁵)₂, -NR¹⁵C(=O)(alquilo C₁₋₄), -NR¹⁵C(=O)O(alquilo C₁₋₄), -OC(=O)N(R¹⁵)₂, -NR¹⁵C(=O)N(R¹⁵)₂, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, deuteroalquilo C₁₋₄, deuteroalcoxi C₁₋₄, fluoroalquilo C₁₋₄,fluoroalcoxi C₁₋₄, heteroalquilo C₁₋₄, o heterocicloalquilo C₂₋₅ monocíclico sustituido o no sustituido; X² es CR² o N; R² es H, D, halógeno, -CN, -OH, -SH, -N(R¹⁵)₂, NR¹⁵S(=O)₂(alquilo C₁₋₄), -S(alquilo C₁₋₄), -S(=O)(alquilo C₁₋₄), -S(=O)₂(alquilo C₁₋₄), -S(=O)₂N(R¹⁵)₂, -OC(=O)(alquilo C₁₋₄), -CO₂H, -CO₂(alquilo C₁₋₄), -C(=O)N(R¹⁵)₂, -NR¹⁵C(=O)(alquilo C₁₋₄), -NR¹⁵C(=O)O(alquilo C₁₋₄), -OC(=O)N(R¹⁵)₂, -NR¹⁵C(=O)N(R¹⁵)₂, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, deuteroalquilo C₁₋₄, deuteroalcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, o heteroalquilo C₁₋₄, o heterocicloalquilo C₂₋₅ monocíclico sustituido o no sustituido; o R¹ y R² se toman juntos con los átomos de intervención para formar un anillo de 5 miembros fusionado sustituido o no sustituido o anillo de 6 miembros fusionado sustituido o no sustituido con 0 - 3 átomos de N y 0 - 2 átomos de O ó S en el anillo; X³ es CR³ o N; R³ es H, D, halógeno, -CN, -OH, -SH, -N(R¹⁵)₂, -NR¹⁵S(=O)₂(alquilo C₁₋₄), -S(alquilo C₁₋₄), -S(=O)(alquilo C₁₋₄), -S(=O)₂(alquilo C₁₋₄), -S(=O)₂ N(R¹⁵)₂, -OC(=O)(alquilo C₁₋₄), -CO₂H, -CO₂(alquilo C₁₋₄), -C(=O)N(R¹⁵)₂, -NR¹⁵C(=O)(alquilo C₁₋₄), alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, deuteroalquilo C₁₋₄, deuteroalcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, heteroalquilo C₁₋₄, o heterocicloalquilo C₂₋₅ monocíclico sustituido o no sustituido; cada X⁴ es independientemente CH o N; R⁴ es H, D, F, o -CH₃; R⁵ es H, D, F, o -CH₃; o R⁴ y R⁵ se toman juntos para formar un puente que es -CH₂- o -CH₂CH₂-; cada R⁶ es independientemente H, D, F, -OH, o -CH₃; m es 0, 1, ó 2; R⁷ es H, D, halógeno, -CN, -OH, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, deuteroalquilo C₁₋₄, deuteroalcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, o heteroalquilo C₁₋₄; L está ausente, es -Y²-L¹-, -L¹-Y²-, ciclopropileno, ciclobutileno o biciclo[1.1.1]pentileno; Y² está ausente, es -O-, -S-, -S(=O)-, -S(=O)₂-, -S(=O)₂NR¹⁵-, -CH₂-, -CH=CH-, -CºC-, -C(=O)-, -C(=O)O-, -OC(=O)-, -OC(=O)O-, -C(=O)NR¹⁵-, -NR¹⁵C(=O)-, -OC(=O)NR¹⁵-, -NR¹⁵C(=O)O-, -NR¹⁵C(=O)NR¹⁵-, -NR¹⁵S(=O)₂-, o -NR¹⁵-; L¹ está ausente o es alquileno C₁₋₄ sustituido o no sustituido; X⁵ es NR⁸ o N; R⁸ es H, D, alquilo C₁₋₆, deuteroalquilo C₁₋₆, fluoroalquilo C₁₋₆, heteroalquilo C₁₋₆, -C(=O)(alquilo C₁₋₄), -CO₂(alquilo C₁₋₄), -C(=O)N(R¹⁵)₂, -S(=O)₂(alquilo C₁₋₄), -S(=O)₂N(R¹⁵)₂, cicloalquilo C₃₋₆ sustituido o no sustituido, o heterocicloalquilo C₂₋₆ monocíclico sustituido o no sustituido, fenilo sustituido o no sustituido, o heteroarilo monocíclico sustituido o no sustituido; R⁹ es H, D, F o -CH₃; Y es -CR¹⁰R¹¹-, -O-, -S-, -S(=O)-, -S(=O)₂-, o -NR¹⁷-; R¹⁰ es H, D, halógeno, -CN, -OH, alquilo C₁₋₆, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₆, fluoroalquilo C₁₋₆, -SR¹², -S(=O)R¹⁴, -S(=O)₂R¹⁴, o -N(R¹²)₂; R¹¹ es H, D, F o -CH₃; o R⁹ y R¹¹ se toman juntos para formar un puente que es -CH₂- o -CH₂CH₂-; cada R¹² es independientemente H, alquilo C₁₋₄, deuteroalquilo C₁₋₄, fluoroalquilo C₁₋₄, heteroalquilo C₁₋₄, cicloalquilo C₃₋₆ sustituido o no sustituido, heterocicloalquilo C₂₋₆ sustituido o no sustituido, fenilo sustituido o no sustituido, bencilo sustituido o no sustituido, heteroarilo monocíclico sustituido o no sustituido; R¹⁴ es alquilo C₁₋₄, deuteroalquilo C₁₋₄, fluoroalquilo C₁₋₄, heteroalquilo C₁₋₄, cicloalquilo C₃₋₆ sustituido o no sustituido, heterocicloalquilo C₂₋₆ sustituido o no sustituido, fenilo sustituido o no sustituido, bencilo sustituido o no sustituido, o heteroarilo monocíclico sustituido o no sustituido; R¹⁵ es H o alquilo C₁₋₆ sustituido o no sustituido; cada R¹⁶ es independientemente H, D, halógeno, -CN, -OH, -N(R¹⁵)₂, -NR¹⁵S(=O)₂(alquilo C₁₋₄), -S(alquilo C₁₋₄), -S(=O)(alquilo C₁₋₄), -S(=O)₂(alquilo C₁₋₄), -C(=O)(alquilo C₁₋₄), OC(=O)(alquilo C₁₋₄), -CO₂H, -CO₂(alquilo C₁₋₄), -NR¹⁵C(=O)(alquilo C₁₋₄), -C(=O)N(R¹⁵)₂, -NR¹⁵C(=O)O(alquilo C₁₋₄), -OC(=O)N(R¹⁵)₂, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, deuteroalquilo C₁₋₄, deuteroalcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, heteroalquilo C₁₋₄, cicloalquilo C₃₋₆ sustituido o no sustituido, heterocicloalquilo C₂₋₆ monocíclico sustituido o no sustituido, fenilo sustituido o no sustituido, o heteroarilo monocíclico sustituido o no sustituido; n es 0, 1, ó 2; R¹⁷ es L⁵-R¹⁴; y L⁵ está ausente, es -S(=O)₂-, -C(=O)-, -CO₂-, o -C(=O)N(R¹⁵).
ARP180100608A 2017-03-15 2018-03-15 Agonistas del receptor farnesoide x y usos de los mismos AR111284A1 (es)

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