AR120167A1 - Agonistas de gpr119 - Google Patents

Agonistas de gpr119

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Publication number
AR120167A1
AR120167A1 ARP200102771A ARP200102771A AR120167A1 AR 120167 A1 AR120167 A1 AR 120167A1 AR P200102771 A ARP200102771 A AR P200102771A AR P200102771 A ARP200102771 A AR P200102771A AR 120167 A1 AR120167 A1 AR 120167A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
nhc
fluoroalkyl
substituted
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ARP200102771A
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English (en)
Inventor
Iyassu Sebhat
Shuwen He
Christopher Moyes
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Kallyope Inc
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Publication of AR120167A1 publication Critical patent/AR120167A1/es

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    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D401/04—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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Esta solicitud está dirigida, al menos en parte, a agonistas de GPR119 útiles para el tratamiento de afecciones o trastornos que involucran el eje intestino-cerebro. En algunas formas de realización, los agonistas de GPR119 son compuestos restringidos al intestino. En algunas formas de realización, la afección o trastorno es un trastorno metabólico, tal como diabetes, obesidad, esteatohepatitis no alcohólica (NASH) o un trastorno nutricional tal como el síndrome del intestino corto. Reivindicación 1: Un compuesto de la fórmula (1) o una sal, solvato, estereoisómero o profármaco apto para uso farmacéutico del mismo, siendo que: K es un resto de fórmula (2) ó (3); R¹ es hidrógeno, -OH, C₁₋₈ alquilo, C₃₋₈ cicloalquilo, o heterocicloalquilo de 3 a 8 miembros, siendo que el alquilo, cicloalquilo, y heterocicloalquilo no están sustituidos o están sustituidos con 1 - 3 sustituyentes a seleccionar considerando cada uno en forma independiente a partir de halógeno, -OH, y -O(C₁₋₆ alquilo); cada R² y R³ considerado en forma independiente es hidrógeno, C₁₋₆ alquilo, o C₁₋₆ fluoroalquilo; o R² y R³ en el mismo átomo de carbono considerados conjuntamente forman =O; R⁴ es hidrógeno, C₁₋₈ alquilo, C₁₋₈ fluoroalquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₈ cicloalquilo, C₅₋₈ cicloalquenilo, heterocicloalquilo de 4 a 8 miembros, -[(CH₂)ʳ-Z]ₜ-R⁶, -[(CHRᵈ)ʳ-Z]ₜ-R⁶, o -[(C(Rᵈ)₂)ʳ-Z]ₜ-R⁶; siendo que cada alquilo, fluoroalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, y heterocicloalquilo de 4 a 8 miembros no está sustituido o está sustituido con 1 - 6 grupos Rᶜ; R⁵ es C₁₋₈ alquilo, C₁₋₈ fluoroalquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₈ cicloalquilo, C₅₋₈ cicloalquenilo, heterocicloalquilo de 4 a 8 miembros, -[(CH₂)ʳ-Z]ₜ-R⁶, -[(CHRᵈ)ʳ-Z]ₜ-R⁶, o -[(C(Rᵈ)₂)ʳ-Z]ₜ-R⁶; siendo que cada alquilo, fluoroalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, y heterocicloalquilo de 4 a 8 miembros está sustituido con 1 - 6 grupos Rᶜ; cada Z considerado en forma independiente es -CH₂O-, -CH₂NRᵈ-, -CH₂N⁺(Rᵈ)₂-, -NH-C(=O)-NH-, -C(=O)NH-, -CH₂S(=O)₂-, o -CH₂S(=O)-; cada r considerado en forma independiente es 1 - 6; cada t considerado en forma independiente es 1 - 6; R⁶ es hidrógeno, C₁₋₈ alquilo, C₁₋₈ fluoroalquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₈ cicloalquilo, C₅₋₈ cicloalquenilo, o heterocicloalquilo de 4 a 8 miembros, siendo que el alquilo, fluoroalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, o heterocicloalquilo de 4 a 8 miembros no está sustituido o está sustituido con 1 - 6 grupos Rᶜ; o R⁴ y R⁵ considerados conjuntamente con el nitrógeno al cual están unidos forman un heterocicloalquilo de 4 a 8 miembros, el cual no está sustituido o está sustituido con 1 - 6 grupos Rᶜ; R⁷ es hidrógeno, C₁₋₄ alquilo, o C₁₋₄ fluoroalquilo; R⁸ es C₁₋₈ alquilo, C₁₋₈ fluoroalquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₈ cicloalquilo, C₅₋₈ cicloalquenilo, heterocicloalquilo de 4 a 8 miembros, -[(CH₂)ʳ-Z]ₜ-R⁶, -[(CHRᵈ)ʳ-Z]ₜ-R⁶, o -[(CRᵈ₂)ʳ-Z]ₜ-R⁶; siendo que cada alquilo, fluoroalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, y heterocicloalquilo de 4 a 8 miembros está sustituido con 1 - 6 grupos Rᵉ; o R⁸ es -(C₁₋₈ alquil)-NH-R⁹, -(C₁₋₈ alquil)-C(=O)NH-R⁹, -(C₁₋₈ alquil)-C(=O)-N(R⁹)₂, o -(C₁₋₈ alquil)-NHC(=O)NH-R⁹; siendo que el alquilo no está sustituido o está sustituido con 1 - 6 grupos Rᶜ; cada R⁹ considerado en forma independiente es C₁₋₈ alquilo, o C₁₋₈ fluoroalquilo que está sustituido con 1 - 6 grupos Rᶜ; o dos R⁹ considerados conjuntamente con el nitrógeno al cual están unidos forman un heterocicloalquilo de 4 a 6 miembros, el cual está sustituido con 1 - 6 grupos Rᶜ; cada Rᶜ considerado en forma independiente es -OH, -CH₂OH, -CH₂CH₂OH, -NH₂, -CH₂NH₂, -NH(Rᵈ), -CH₂NH(Rᵈ), -N(Rᵈ)₂, -CH₂N(Rᵈ)₂, -N(Rᵈ)₃⁺, -C(=O)OH, -CH₂C(=O)OH, -CH₂CH₂C(=O)OH, -S(=O)₂OH, -S(=O)OH, -S(=O)₂NH₂, -P(=O)(OH)₂, -P(=O)(OH)(Rᵈ), -P(=O)(OH)(H), P(=O)(OH)(ORᵈ), -B(OH)₂, -B(ORᵈ)(OH), -NHCONHS(=O)₂(Rᵈ), -N(Rᵈ)CONHS(=O)₂(Rᵈ), -NHCON(Rᵈ)S(=O)₂(Rᵈ), -C(=O)NHS(=O)₂(Rᵈ), -S(=O)₂NHC(=O)Rᵈ, -NHC(=NH)NH₂, -NHC(=NH)NHRᵈ, -NHC(=NH)N(Rᵈ)₂, -N(Rᵈ)C(=NH)NH₂, -N(Rᵈ)C(=NH)NH(Rᵈ), -N(Rᵈ)C(=NH)N(Rᵈ)₂, -NHC(=N(Rᵈ))NH₂, -NHC(=N(Rᵈ))NHRᵈ, -NHC(=N(Rᵈ))N(Rᵈ)₂, -N(Rᵈ)C(=N(Rᵈ))NH₂, -N(Rᵈ)C(=N(Rᵈ))NHRᵈ, -N(Rᵈ)C(=N(Rᵈ))N(Rᵈ)₂, -NHC(=NH)NHC(=NH)NH₂, -N(Rᵈ)C(=NH)NHC(=NH)NH₂, un resto seleccionado del grupo de fórmulas (4), o un heterociclo de 4 a 6 miembros, el cual no está sustituido o está sustituido con 1, 2, 3 ó 4 sustituyentes a seleccionar a partir de C₁₋₆ alquilo, -O-(C₁₋₆ alquil), -OH, =O y =S; cada Rᵈ considerado en forma independiente es C₁₋₆ alquilo, C₁₋₆ fluoroalquilo, o C₃₋₆ cicloalquilo; cada Rᵉ considerado en forma independiente es -OH, -CH₂OH, -CH₂CH₂OH, -N(Rᵈ)₃⁺, -C(=O)OH, -CH₂C(=O)OH, -CH₂CH₂C(=O)OH, -S(=O)₂OH, -S(=O)OH, -S(=O)₂NH₂, -P(=O)(OH)₂, -P(=O)(OH)(Rᵈ), -P(=O)(OH)(H), -P(=O)(OH)(ORᵈ), -B(OH)₂, -B(ORᵈ)(OH), -NHCONHS(=O)₂(Rᵈ), -N(Rᵈ)CONHS(=O)₂(Rᵈ), -NHCON(Rᵈ)S(=O)₂(Rᵈ), -C(=O)NHS(=O)₂(Rᵈ), -S(O)₂NHC(O)Rᵈ, -NHC(=NH)NH₂, -NHC(=NH)NHRᵈ, -NHC(=NH)N(Rᵈ)₂, -N(Rᵈ)C(=NH)NH₂, -N(Rᵈ)C(=NH)NH(Rᵈ), -N(Rᵈ)C(=NH)N(Rᵈ)₂, -NHC(=N(Rᵈ))NH₂, -NHC(=N(Rᵈ))NHRᵈ, -NHC(=N(Rᵈ))N(Rᵈ)₂, -N(Rᵈ)C(=N(Rᵈ))NH₂, -N(Rᵈ)C(=N(Rᵈ))NHRᵈ, -N(Rᵈ)C(=N(Rᵈ))N(Rᵈ)₂, -NHC(=NH)NHC(=NH)NH₂, N(Rᵈ)C(=NH)NHC(=NH)NH₂, un resto seleccionado del grupo de fórmulas (4), un heterociclo de 4 a 6 miembros, el cual no está sustituido o está sustituido con 1, 2, 3 ó 4 sustituyentes a seleccionar a partir de C₁₋₆ alquilo, -O-(C₁₋₆ alquil), -OH, =O y =S; el anillo A es fenilo o heteroarilo monocíclico de 5 - 6 miembros; cada Rᵃ considerado en forma independiente es halógeno, -CN, C₁₋₆ alquilo, C₁₋₆ fluoroalquilo, o C₃₋₆ cicloalquilo; X, cuando K es fórmula (2), es -O-, -NRN-, *-CH₂O-, *-CH₂NRN-, *-C(=O)O-, *-C(=O)NRN-, *-CH₂C(=O)O-, *-CH₂C(=O)NRN-, *-OC(=O)-, *-NRNC(=O)-, *-CH₂OC(=O)-, o *-CH₂NRNC(=O)-, donde * representa el punto de unión al Anillo A; RN es hidrógeno o C₁₋₄ alquilo; o X, cuando K es fórmula (3) es -O-, -NRN-, *-CH₂O-, *-CH₂NRN-, *-C(=O)O-, *-C(=O)NRN-, *-CH₂C(=O)O-, *-CH₂C(=O)NRN-, *-OC(=O)-, *-CH₂OC(=O)-, o *-CH₂NRNC(=O)-, donde * representa el punto de unión al Anillo A; RN es hidrógeno o C₁₋₄ alquilo; cada R¹¹ considerado en forma independiente es hidrógeno, flúor, -OH, C₁₋₆ alquilo, o C₁₋₆ alcoxi; cada R¹² considerado en forma independiente es hidrógeno, flúor, o C₁₋₆ alquilo; o, cuando K es fórmula (2) dos R¹¹ considerados conjuntamente con los átomos intervinientes a los cuales están unidos forman un C₃₋₆ cicloalquilo; o, cuando K es fórmula (3) dos R¹¹ considerados conjuntamente con los átomos intervinientes a los cuales están unidos forman un C₄₋₆ cicloalquilo; R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, y R²⁰ son, considerando cada uno en forma independiente, hidrógeno, C₁₋₆ alquilo, C₁₋₆ alcoxi, o C₁₋₆ fluoroalquilo; o R¹³ y R¹⁷ o R¹³ y R¹⁹ o R¹⁵ y R¹⁹ considerados conjuntamente con los átomos intervinientes a los cuales están unidos forman un anillo; R²¹ es hidrógeno, C₁₋₆ alquilo, o C₁₋₆ fluoroalquilo; o R²¹ y un R¹¹ considerados conjuntamente con los átomos intervinientes a los cuales están unidos forman un C₃₋₆ cicloalquilo; W es fenilo o heteroarilo monocíclico de 5 - 6 miembros, siendo que el fenilo o heteroarilo no está sustituido o está sustituido con 1, 2, ó 3 sustituyentes a seleccionar a partir de Rᵇ; cada Rᵇ considerado en forma independiente es halógeno, -OH, -CN, -C(O)OH, -C(O)O(C₁₋₆ alquil), C₁₋₆ alquilo, C₁₋₆ alcoxi, C₃₋₆ cicloalquilo, fenilo, o heteroarilo de 5 a 6 miembros; siendo que cada alquilo, alcoxi, y cicloalquilo no está sustituido o está sustituido con 1, 2, ó 3 sustituyentes a seleccionar a partir de halógeno, -OH, C₁₋₆ alquilo, y C₁₋₆ alcoxi; o W es -C(=O)O-R²²; R²² es C₁₋₆ alquilo, C₃₋₆ cicloalquilo, o heterocicloalquilo de 3 a 6 miembros, siendo que el alquilo, cicloalquilo, y heterocicloalquilo están sustituidos o no están sustituidos con 1 - 3 sustituyentes a seleccionar, considerando cada uno en forma independiente, a partir de flúor, -OH, C₁₋₆ alquilo, C₁₋₆ haloalquilo o C₃₋₆ cicloalquilo; m es 1 - 4; n es 0 - 4; p es 1 ó 2; q es 1 ó 2; y s es 1 ó 2.
ARP200102771A 2019-10-07 2020-10-07 Agonistas de gpr119 AR120167A1 (es)

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US (2) US11512065B2 (es)
EP (1) EP4041722A4 (es)
JP (1) JP2022552655A (es)
KR (1) KR20220150270A (es)
CN (1) CN114945560A (es)
AR (1) AR120167A1 (es)
AU (1) AU2020363377A1 (es)
BR (1) BR112022006546A2 (es)
CA (1) CA3156985A1 (es)
CL (1) CL2022000856A1 (es)
IL (1) IL291985A (es)
MX (1) MX2022004142A (es)
TW (1) TW202128640A (es)
UY (1) UY38908A (es)
WO (1) WO2021071837A1 (es)

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BR112022006546A2 (pt) 2019-10-07 2022-08-30 Kallyope Inc Agonistas de gpr119
WO2023250323A1 (en) * 2022-06-24 2023-12-28 Kallyope, Inc. Gpr119 and gpr40 agonist combination therapies for gut-brain axis disorders

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