[go: up one dir, main page]

AR129846A1 - Agonistas de trpml1 con oxazol y usos de estos - Google Patents

Agonistas de trpml1 con oxazol y usos de estos

Info

Publication number
AR129846A1
AR129846A1 ARP230101762A ARP230101762A AR129846A1 AR 129846 A1 AR129846 A1 AR 129846A1 AR P230101762 A ARP230101762 A AR P230101762A AR P230101762 A ARP230101762 A AR P230101762A AR 129846 A1 AR129846 A1 AR 129846A1
Authority
AR
Argentina
Prior art keywords
alkylene
heterocycloalkyl
cycloalkyl
heteroaryl
aryl
Prior art date
Application number
ARP230101762A
Other languages
English (en)
Inventor
James Guy Breitenbucher
Maria Pia Catalani
Ali Munaim Yousif
Original Assignee
Libra Therapeutics 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 Libra Therapeutics Inc filed Critical Libra Therapeutics Inc
Publication of AR129846A1 publication Critical patent/AR129846A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C07D413/04—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 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/48—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

En el presente documento se describen inhibidores de TRPML1 con oxazol y composiciones farmacéuticas que comprenden dichos inhibidores. Los compuestos y composiciones en cuestión son útiles para el tratamiento de trastornos o enfermedades mediadas por TRPML1. Reivindicación 1: Un compuesto de la fórmula (1), o una sal, solvato o estereoisómero farmacéuticamente aceptable de este, caracterizado porque: R¹ es alquilo C₁-C₆ opcionalmente sustituido con uno o más R; R² es alquilo C₁-C₆ opcionalmente sustituido con uno o más R; o R¹ y R² se toman juntos para formar un heterocicloalquilo o heteroarilo; cada uno opcionalmente sustituido con uno o más R¹ᵃ; cada R¹ᵃ es independientemente deuterio, halógeno, -CN, -NO₂, -OH, -ORᵃ, -OC(=O)Rᵃ, -OC(=O)ORᵇ, -OC(=O)NRᶜRᵈ, -SH, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᶜRᵈ, -NRᶜRᵈ, -NRᵇC(=O)NRᶜRᵈ, -NRᵇC(=O)Rᵃ, -NRᵇC(=O)ORᵇ, -NRᵇS(=O)Rᵃ, -NRᵇS(=O)₂Rᵃ, -C(=O)Rᵃ, -C(=O)ORᵇ, -C(=O)NRᶜRᵈ, alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, alquileno C₁-C₆(cicloalquilo), alquileno C₁-C₆(heterocicloalquilo), alquileno C₁-C₆(arilo) o alquileno C₁-C₆(heteroarilo); donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituye independiente y opcionalmente con uno o más R; o dos R¹ᵃ en el mismo átomo se toman juntos para formar un oxo; R³ es alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, cicloalquilo o heterocicloalquilo, donde cada alquilo, alquenilo, alquinilo, cicloalquilo y heterocicloalquilo se sustituye independiente y opcionalmente con uno o más R; el anillo A es arilo o heteroarilo; cada R⁴ es independientemente deuterio, halógeno, -CN, -NO₂, -OH, -ORᵃ, -OC(=O)Rᵃ, -OC(=O)ORᵇ, -OC(=O)NRᶜRᵈ, -O-cicloalquilo, -O-heterocicloalquilo, -SH, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᶜRᵈ, -NRᶜRᵈ, -NRᵇC(=O)NRᶜRᵈ, -NRᵇC(=O)Rᵃ, -NRᵇC(=O)ORᵇ, -NRᵇS(=O)Rᵃ, -NRᵇS(=O)₂Rᵃ, -NRᵇ-cicloalquilo, -NRᵇ-heterocicloalquilo, -C(=O)Rᵃ, -C(=O)ORᵇ, -C(=O)NRᶜRᵈ, alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, alquileno C₁-C₆(cicloalquilo), alquileno C₁-C₆(heterocicloalquilo), alquileno C₁-C₆(arilo) o alquileno C₁-C₆(heteroarilo); donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituye independiente y opcionalmente con uno o más R; n es 0 - 4; cada Rᵃ es independientemente alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, alquileno C₁-C₆(cicloalquilo), alquileno C₁-C₆(heterocicloalquilo), alquileno C₁-C₆(arilo), o alquileno C₁-C₆(heteroarilo); donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituye independiente y opcionalmente con uno o más R; cada Rᵇ es independientemente hidrógeno, alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, alquileno C₁-C₆(cicloalquilo), alquileno C₁-C₆(heterocicloalquilo), alquileno C₁-C₆(arilo) o alquileno C₁-C₆(heteroarilo); donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituye independiente y opcionalmente con uno o más R; cada Rᶜ y Rᵈ son independientemente hidrógeno, alquilo C₁-C₆, haloalquilo C₁-C₆, deuteroalquilo C₁-C₆, hidroxialquilo C₁-C₆, aminoalquilo C₁-C₆, heteroalquilo C₁-C₆, alquenilo C₂-C₆, alquinilo C₂-C₆, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, alquileno C₁-C₆(cicloalquilo), alquileno C₁-C₆(heterocicloalquilo), alquileno C₁-C₆(arilo) o alquileno C₁-C₆(heteroarilo) donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituye independiente y opcionalmente con uno o más R; o Rᶜ y Rᵈ se toman juntos con el átomo al que están unidos para formar un heterocicloalquilo opcionalmente sustituido con uno o más R; y cada R es independientemente deuterio, halógeno, -CN, -OH, -S(=O)alquilo C₁-C₃, -S(=O)₂alquilo C₁-C₃, -S(=O)₂NH₂, -S(=O)₂NHalquilo C₁-C₃, -S(=O)₂N(alquilo C₁-C₃)₂, -NH₂, -NH-alquilo C₁-C₃, -N(alquilo C₁-C₃)₂, -C(=O)alquilo C₁-C₃, -C(=O)OH, -C(=O)O-alquilo C₁-C₃, -C(=O)NH₂, -C(=O)NH-alquilo C₁-C₃, -C(=O)N(alquilo C₁-C₃)₂, alquilo C₁-C₃, alcoxi C₁-C₃, haloalquilo C₁-C₃, deuteroalquilo C₁-C₃, haloalcoxi C₁-C₃, hidroxialquilo C₁-C₃, aminoalquilo C₁-C₃, heteroalquilo C₁-C₃, cicloalquilo C₃-C₆, o heterocicloalquilo de 3 a 6 miembros; donde cada cicloalquilo y heterocicloalquilo se sustituye independiente y opcionalmente con uno o más halógenos; o dos R en el mismo átomo forman un oxo. Reivindicación 3: El compuesto de la reivindicación 1 o 2, o una sal, solvato o estereoisómero farmacéuticamente aceptable de este, caracterizado porque el anillo A es fenilo. Reivindicación 42: El método de la reivindicación 41, caracterizado porque el trastorno o la enfermedad mediada por TRPML1 es envejecimiento, enfermedades óseas, enfermedades cardiovasculares, trastornos congénitos del desarrollo, trastornos oculares, malignidades hematológicas y sólidas, enfermedades infecciosas, enfermedades inflamatorias, enfermedades del hígado, enfermedades metabólicas, enfermedades neurológicas o neurodegenerativas, pancreatitis, enfermedades renales, trastornos musculoesqueléticos, obesidad, enfermedades de almacenamiento lisosómico, cardiomiopatía hipertrófica, cardiomiopatía dilatada, miositis por cuerpos de inclusión, enfermedad de Paget o enfermedades pulmonares.
ARP230101762A 2022-07-07 2023-07-06 Agonistas de trpml1 con oxazol y usos de estos AR129846A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202263359080P 2022-07-07 2022-07-07

Publications (1)

Publication Number Publication Date
AR129846A1 true AR129846A1 (es) 2024-10-02

Family

ID=89454157

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP230101762A AR129846A1 (es) 2022-07-07 2023-07-06 Agonistas de trpml1 con oxazol y usos de estos

Country Status (12)

Country Link
US (1) US12098145B2 (es)
EP (1) EP4551571A1 (es)
JP (1) JP2025525443A (es)
KR (1) KR20250048243A (es)
CN (1) CN119790050A (es)
AR (1) AR129846A1 (es)
AU (1) AU2023303023A1 (es)
CA (1) CA3260698A1 (es)
IL (1) IL317999A (es)
MX (1) MX2025000151A (es)
TW (1) TW202409019A (es)
WO (1) WO2024011155A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119790050A (zh) 2022-07-07 2025-04-08 利布拉医疗公司 噁唑trpml1激动剂及其用途
TW202535364A (zh) * 2024-01-08 2025-09-16 美商利布拉醫療公司 噻唑trpml1促效劑及其用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101504787B1 (ko) 2007-10-24 2015-03-20 아스테라스 세이야쿠 가부시키가이샤 아졸카복사마이드 화합물 또는 그 염
WO2018005713A1 (en) * 2016-06-29 2018-01-04 Congxin Liang Piperazine derivatives as trpml modulators
EP3821947A1 (en) * 2019-11-13 2021-05-19 Libra Therapeutics, Inc. Heterocyclic trpml1 agonists
WO2021127328A1 (en) * 2019-12-19 2021-06-24 Casma Therapeutics, Inc. Trpml modulators
TW202136219A (zh) * 2019-12-19 2021-10-01 美商卡司馬療法公司 Trpml調節劑
WO2022032073A2 (en) * 2020-08-07 2022-02-10 Casma Therapeutics, Inc. Trpml modulators
WO2022076383A1 (en) * 2020-10-06 2022-04-14 Lysoway Therapeutics, Inc. Sulfonanilide and benzylsulfonyl derivatives, and compositions and methods thereof
CN119790050A (zh) 2022-07-07 2025-04-08 利布拉医疗公司 噁唑trpml1激动剂及其用途

Also Published As

Publication number Publication date
IL317999A (en) 2025-02-01
AU2023303023A1 (en) 2025-01-23
CN119790050A (zh) 2025-04-08
US12098145B2 (en) 2024-09-24
MX2025000151A (es) 2025-05-02
US20240158381A1 (en) 2024-05-16
EP4551571A1 (en) 2025-05-14
JP2025525443A (ja) 2025-08-05
CA3260698A1 (en) 2024-01-11
TW202409019A (zh) 2024-03-01
WO2024011155A1 (en) 2024-01-11
KR20250048243A (ko) 2025-04-08

Similar Documents

Publication Publication Date Title
AR129846A1 (es) Agonistas de trpml1 con oxazol y usos de estos
AR121719A1 (es) Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades
AR119698A2 (es) Compuesto amida n-urea sustituida derivado de aminoácido
AR110139A1 (es) COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV
AR113964A1 (es) Carbamoíl ciclohexil ácidos ligados a n de triazol como antagonistas de lpa
AR127488A1 (es) Inhibidores de la proteína que contiene el dominio de prolil hidroxilasa (phd) y usos de los mismos
AR125425A1 (es) Inhibidores de proteina tirosina fosfatasa y sus metodos de uso
AR074021A1 (es) Compuestos heterociclicos fusionados como moduladores del canal ionico
AR094452A1 (es) COMPUESTOS HETEROCÍCLICOS SUSTITUIDOS CON AMIDA ÚTILES COMO MODULADORES DE LAS RESPUESTAS DE IL-12, IL-23 Y/O INFa
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
UY30603A1 (es) Derivados de 2-aril-6-fenil-imidazo[1, 2-a]piridinas, su preparacion y su aplicacion en terapéutica
AR065499A1 (es) Inhibidores de serino proteasas.composiciones farmaceuticas
CU23706B7 (es) Derivados de 1,2,4,5-tetrahidro-3h-benzazepinas, su procedimiento de preparación y las composiciones farmacéuticas que las contienen
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR117900A1 (es) Pirazolopiridinas y triazolopiridinas como inhibidores de a2a / a2b
AR128418A1 (es) Inhibidores de la proteína tirosina fosfatasa y usos de estos
AR110122A1 (es) Fenoxitriazoles
AR129339A1 (es) Inhibidores de parg
BRPI1016232A2 (pt) Composto de carbinol, medicamento, regulador de lxr, composição farmacêutica, método para prevenir e/ou tratar doenças, e, uso do composto de carbinol
AR101638A1 (es) Combinaciones de inhibidores de la recaptación de serotonina-norepinefrina (irsn) y ligandos del receptores sigma
AR085236A1 (es) Compuestos de benzodioxol-piperazina como moduladores de los receptores 5-hty d
PE20081113A1 (es) Inhibidores virales policiclicos
AR120556A1 (es) Compuestos heterocíclicos como inhibidores de delta-5 desaturasa y métodos de uso
AR082534A1 (es) Compuestos que interactuan con proteina reguladora de glucocinasa para el tratamiento de diabetes