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AR118050A1 - Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x - Google Patents

Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x

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AR118050A1
AR118050A1 ARP200100360A ARP200100360A AR118050A1 AR 118050 A1 AR118050 A1 AR 118050A1 AR P200100360 A ARP200100360 A AR P200100360A AR P200100360 A ARP200100360 A AR P200100360A AR 118050 A1 AR118050 A1 AR 118050A1
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alkoxy
substituted
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Pavan Kalyan Kathi
Srinivas Jogi
Subba Reddy Bandreddy
Rishikesh Narayan
Soodamani Thangavel
Firoz Ali Jaipur
Kandhasamy Sarkunan
Srinivas Cheruku
Susheel Jethanand Nara
Dean A Wacker
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Bristol Myers Squibb Co
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/4245—Oxadiazoles
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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
    • A61K31/4439—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/435—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
    • A61K31/444—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)

Abstract

Compuestos heterocíclicos, en particular derivados de 1,2,4-oxadiazol como moduladores del receptor Farnesoide X (FXR), composiciones farmacéuticas que los comprenden y su uso para el tratamiento de diversas enfermedades tales como cáncer, enfermedades inflamatorias, cirrosis biliar primaria (PBC), enfermedad renal crónica y fibrosis pulmonar idiopática (FPI). Reivindicación 1: Un compuesto de la fórmula (1) o un estereoisómero, un tautómero o una sal o solvato del mismo, en el que: X¹ es CR⁵ᵃ o N; X² es CR⁵ᵇ o N; X³ es CR⁵ᶜ o N; X⁴ es CR⁵ᵈ o N; siempre que cero, 1, o 2 de X¹, X², X³, y X⁴ son N; Z¹ y Z² son independientemente CH₂ u O; siempre que al menos uno de Z¹ y Z² es CH₂; a es cero o 1; b es cero, 1, o 2; d es cero, 1, o 2; siempre que Z¹ y Z² son cada uno CH₂ cuando a, b, y d son cada uno cero; Q es un grupo cíclico seleccionado de carbociclilo de 3- a 8-miembros, arilo de 6- a 10-miembros, heterociclilo de 4- a 10-miembros, y heteroarilo de 5- a 10-miembros, en donde dicho grupo cíclico se sustituye por cero a 4 R¹; cada R¹ es independientemente hidrógeno, halo, ciano, hidroxilo, oxo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆ -NH₂, -NH(alquilo C₁₋₆), -N(alquilo C₁₋₆)₂, -C(O)(alquilo C₁₋₆), -C(O)(cicloalquilo C₃₋₆), -NRˣC(O)Rʸ, -C(O)ORˣ, -C(O)NRʷRʷ, -S(O)₂(alquilo C₁₋₆), -S(O)₂(cicloalquilo C₃₋₆), -NRˣS(O)₂(alquilo C₁₋₆), -NRˣS(O)₂(cicloalquilo C₃₋₆), -S(O)₂NRᶻRᶻ, -P(O)RʸRʸ, -(CH₂)₀₋₃(carbociclilo₂)₀₋₃(carbociclilo C₃₋₆), -O(cicloalquilo C₃₋₆), -O(heterociclilo de 4- a 6-miembros), -(CH₂)₀₋₃(heterociclilo₂)₀₋₃(heterociclilo de 4- a 6-miembros), o -(CH₂)₀₋₃(heteroarilo₂)₀₋₃(heteroarilo de 5- ó 6-miembros), en donde cada uno de dicho alquilo, alcoxi, alquenilo, y alquinilo se sustituye por cero a 4 R¹ᵃ y cada uno de dicho cicloalquilo, heterociclilo, y heteroarilo se sustituye por cero a 4 R¹ᵇ; cada R¹ᵃ es independientemente halo, hidroxilo, -NRʷRʷ, oxo, ciano, alcoxi C₁₋₃, haloalcoxi C₁₋₃, -C(O)ORˣ, -C(O)NRʷRʷ, o -NRˣC(O)Rʸ; cada R¹ᵇ es independientemente halo, oxo, ciano, hidroxilo, -NH₂, alquilo C₁₋₆, alcoxi C₁₋₆, -NH(alquilo C₁₋₆), -N(alquilo C₁₋₆)₂, o -NRˣC(O)(alquilo C₁₋₆), en donde cada de dicho alquilo y alcoxi se sustituye por cero a 6 R¹ᵃ; R² es: (i) alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆ o -NRᵛRᵛ, en donde cada uno de dicho alquilo, alquenilo, alquinilo, y alcoxi se sustituye por cero a 6 R²ᵃ; (ii) carbociclilo C₃₋₆, espirobiciclilo C₆₋₈, o heterociclilo de 4- a 6-miembros, en donde cada uno de dicho carbociclilo, espirobiciclilo, y heterociclilo se sustituye por cero a 3 R²ᵇ; o (iii) -CH₂(cicloalquilo C₃₋₆), -CH₂(heterociclilo de 4- a 6-miembros),-NRˣ(CH₂)₀₋₂(cicloalquilo C₃₋₆), -NRˣ(CH₂)₀₋₂(bicicloalquilo C₅₋₈), -NRˣ(CH₂)₀₋₂(espirobiciclilo C₅₋₈), -NRˣ(CH₂)₀₋₂(heterociclilo de 4- a 6-miembros), -NRˣ(CH₂)₀₋₂(heteroarilo de 5- a 6-miembros), -NRˣ(CH₂)₀₋₂(fenilo), -O(CH₂)₀₋₂(cicloalquilo C₃₋₆), -O(CH₂)₀₋₂(bicicloalquilo C₅₋₈), -O(CH₂)₀₋₂(espirobiciclilo C₅₋₈), -O(CH₂)₀₋₂(heterociclilo de 4- a 6-miembros), -O(CH₂)₀₋₂(heteroarilo de 5- a 6-miembros), o -O(CH₂)₀₋₂(fenilo), en donde cada uno de dicho cicloalquilo, heterociclilo, bicicloalquilo, espirobiciclilo, arilo, y heteroarilo se sustituye por cero a 3 R²ᵇ; cada R²ᵃ es independientemente halo, ciano, hidroxilo, oxo, haloalquilo C₁₋₃, alcoxi C₁₋₃, haloalcoxi C₁₋₃, -NRˣRˣ, -C(O)(alquilo C₁₋₆), -C(O)(cicloalquilo C₃₋₆), -NRˣC(O)Rʸ, -C(O)(alquilo C₁₋₆), -C(O)ORˣ, -C(O)NRʷRʷ, -S(O)₂Rʸ, -S(O)₂(fluoroalquilo C₁₋₃), -NRˣS(O)₂(alquilo C₁₋₃), -NRˣS(O)₂(cicloalquilo C₃₋₆), -S(O)₂NRᶻRᶻ, o -P(O)RʸRʸ; cada R²ᵇ es independientemente halo, ciano, hidroxilo, oxo, alquilo C₁₋₆, alcoxi C₁₋₆, -NRˣRˣ, -NRˣC(O)O(alquilo C₁₋₄), -C(O)(alquilo C₁₋₃), o -S(O)₂(alquilo C₁₋₃), en donde cada uno de dicho alquilo y alcoxi se sustituye por cero a 6 R²ᵃ; R³ᵃ y R³ᵇ son independientemente hidrógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, o cicloalquilo C₃₋₆, o R³ᵃ y R³ᵇ, tomados junto con el átomo de carbono al que se unieron, forman un cicloalquilo C₃₋₆; A es: (i) ciano; (ii) fenilo o un heteroarilo de 5- ó 10-miembros que contiene 1 a 4 heteroátomos independientemente seleccionado de N, O, y S, en donde cada de dicho fenilo y heteroarilo se sustituye por cero a 3 R⁴ᵃ; o (iii) un compuesto del grupo de fórmulas (2); cada R⁴ᵃ es independientemente halo, ciano, hidroxilo, -NH₂, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxilo C₁₋₆, -(CH₂)₀₋₃NH(alquilo C₁₋₆), -(CH₂)₀₋₂N(alquilo C₁₋₆)₂, -(CH₂)₀₋₃(cicloalquilo C₃₋₆), o -(CH₂)₀₋₃(heterociclilo de 4 a 6 miembros), en donde cada uno de dicho alquilo, alcoxilo, alquenilo, y alquinilo se sustituye por cero a 6 R⁴ᵈ y cada uno de dicho cicloalquilo y heterociclilo se sustituye por cero a 3 R⁴ᵉ; R⁴ᵇ es alquilo C₁₋₆, -(CH₂)₀₋₃(cicloalquilo₂)₀₋₃(cicloalquilo C₃₋₆), -(CH₂)₀₋₃(heterociclilo₂)₀₋₃(heterociclilo de 4- a 6-miembros), o -(CH₂)₀₋₃(fenilo), en donde cada uno de dicho alquilo se sustituye por cero a 6 R⁴ᵈ y cada uno de dicho cicloalquilo, heterociclilo, y fenilo se sustituye por cero a 3 R⁴ᵉ; cada R⁴ᶜ es independientemente hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, heterociclilo de 4- a 6-miembros, fenilo, o heteroarilo de 5- a 6-miembros; cada R⁴ᵈ es independientemente halo, hidroxilo, -NRˣRˣ, oxo, ciano, alcoxi C₁₋₃, o haloalcoxi C₁₋₃; cada R⁴ᵉ es independientemente halo, oxo, ciano, hidroxilo, -NH₂, alquilo C₁₋₆, alcoxilo C₁₋₆, -NH(alquilo C₁₋₆), o -N(alquilo C₁₋₆)₂, en donde cada uno de dichos alquilo y alcoxilo está sustituido por cero a 6 R⁴ᵈ; cada uno de R⁵ᵃ, R⁵ᵇ, R⁵ᶜ, y R⁵ᵈ es independientemente hidrógeno, halo, hidroxi, ciano, alquilo C₁₋₆ se sustituye por cero a 6 R⁵ᵉ, alcoxi C₁₋₆, se sustituye por cero a 6 R⁵ᵉ, -C(O)ORˣ, -C(O)NRʷRʷ, -S(O)₂Rʸ, -S(O)₂NRᶻRᶻ, o fenilo se sustituye por cero a 3 R⁵ᶠ; cada uno de R⁵ᵉ es independientemente halo, hidroxilo, -NRˣRˣ, oxo, ciano, alcoxilo C₁₋₃, o haloalcoxilo C₁₋₃; cada R⁵ᶠ es independientemente halo, oxo, ciano, hidroxilo, -NH₂, alquilo C₁₋₆, alcoxi C₁₋₆, -NH(alquilo C₁₋₆), o -N(alquilo C₁₋₆)₂, en donde cada uno de dicho alquilo y alcoxi se sustituye por cero a 6 R⁵ᵉ; cada Rᵛ es independientemente hidrógeno, alquilo C₁₋₆, o alternativamente, dos Rᵛ, tomados junto con el átomo de nitrógeno al cual se unen, forman una fracción de anillo bicíclico o espirocíclico de 4- a 7-miembros que contiene cero a 2 heteroátomos adicionales independientemente seleccionados de N, O, y S, en donde cada anillo puede sustituirse por cero a 6 R²ᵃ; cada Rʷ es independientemente hidrógeno, alquilo C₁₋₆, o cicloalquilo C₃₋₆; o alternativamente, dos Rʷ, tomados junto con el átomo de nitrógeno al cual se unen, 4- a 7-miembros que contiene cero a 2 heteroátomos adicionales independientemente seleccionados de N, O, y S; cada Rˣ es independientemente hidrógeno, alquilo C₁₋₆, o cicloalquilo C₃₋₆; cada Rʸ es independientemente alquilo C₁₋₆ o cicloalquilo C₃₋₆; y cada Rᶻ es independientemente hidrógeno, alquilo C₁₋₆, o cicloalquilo C₃₋₆ o alternativamente, dos Rᶻ, tomados junto con el átomo de nitrógeno al cual se unen, forman una fracción de anillo 4- a 7-miembros que contiene cero a 2 heteroátomos adicionales independientemente seleccionados de N, O, y S.
ARP200100360A 2019-02-15 2020-02-11 Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x AR118050A1 (es)

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CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
US20230165853A1 (en) 2021-01-14 2023-06-01 Enyo Pharma Method for treating chronic kidney diseases
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
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