AR114235A1 - Inhibidores de gcn2 y usos de los mismos - Google Patents

Inhibidores de gcn2 y usos de los mismos

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Publication number
AR114235A1
AR114235A1 ARP190100195A ARP190100195A AR114235A1 AR 114235 A1 AR114235 A1 AR 114235A1 AR P190100195 A ARP190100195 A AR P190100195A AR P190100195 A ARP190100195 A AR P190100195A AR 114235 A1 AR114235 A1 AR 114235A1
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AR
Argentina
Prior art keywords
nitrogen
oxygen
sulfur
membered
independently selected
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Application number
ARP190100195A
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English (en)
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Vertex Pharma
Merck Patent Gmbh
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Application filed by Vertex Pharma, Merck Patent Gmbh filed Critical Vertex Pharma
Publication of AR114235A1 publication Critical patent/AR114235A1/es

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    • 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
    • C07D487/04—Ortho-condensed systems
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
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  • Endocrinology (AREA)
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Abstract

La presente proporciona compuestos, sus composiciones y métodos de uso de ellos. Reivindicación 1: Un compuesto de la fórmula (1), o una de sus sales farmacéuticamente aceptables, en donde: Anillo A se selecciona de un anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros, fenilo, un anillo carbocíclico aromático bicíclico de 8 - 10 miembros, un anillo heterocíclico monocíclico parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre opcionalmente fusionado con un anillo aromático de 5 - 6 miembros que tiene 0 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heterocíclico espirocíclico parcialmente insaturado de 7 - 12 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heterocíclico bicíclico parcialmente insaturado de 7 - 12 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heteroaromático bicíclico parcialmente insaturado de 7 - 12 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heterocíclico bicíclico en puente parcialmente insaturado de 7 - 12 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heteroaromático bicíclico de 8 - 10 miembros que tiene 1 - 5 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre o Het, en donde Het es un anillo heterocíclico monocíclico de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heterocíclico espirocíclico saturado de 7 - 12 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heterocíclico bicíclico saturado de 7 - 12 miembros que tiene 1 - 3 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre o un anillo heterocíclico bicíclico en puente saturado de 7 - 12 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; Anillo B es un compuesto seleccionado del grupo de fórmulas (2); Anillo C es un compuesto seleccionado del grupo de fórmulas (3); cada R es, de modo independiente, hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, un anillo carbocíclico monocíclico saturado o parcialmente insaturado de 3 - 8 miembros, fenilo, un anillo carbocíclico aromático bicíclico de 8 - 10 miembros, un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre o un anillo heteroaromático bicíclico de 8 - 10 miembros que tiene 1 - 5 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; o dos grupos R se toman juntos opcionalmente para formar una cadena de alquileno C₂₋₄ bivalente; dos grupos R se toman opcionalmente junto con sus átomos intervinientes para formar un anillo monocíclico saturado o parcialmente insaturado de 3 - 7 miembros opcionalmente sustituido que tiene 0 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; cada R’ es, de modo independiente, hidrógeno o un grupo alifático C₁₋₃ opcionalmente sustituido con halógeno; cada uno de R¹ es, de modo independiente, hidrógeno, halógeno, -CN, -NO₂, -C(O)R, -C(O)OR, -C(O)N(R)₂, -C(O)N(R)S(O)₂R, -C(O)N=S(O)(R)₂, -N(R)₂, -N(R)C(O)R, -N(R)C(O)N(R)₂, -N(R)C(O)OR, -N(R)S(O)₂R, -N(R)S(O)₂N(R)₂, -OR, -ON(R)SO₂R, -P(O)(R)₂, -SR, -S(O)R, -S(O)₂R, -S(O)(NH)R, -S(O)₂N(R)₂, -S(NH₂)₂(O)OH, -N=S(O)(R)₂, -C(R)₂S(=O)(=NH)R, -C(R)₂NHSO₂CH₃, -CD₃, -CD₂N(R)S(O)₂R o R; o: dos grupos R¹ se toman juntos opcionalmente para formar =O, =NH o =NS(O)₂R; o dos grupos R¹ se toman juntos opcionalmente para formar una cadena de alquileno C₂₋₄ bivalente; cada uno de R² es, de modo independiente, hidrógeno, halógeno, -CN, -C(O)N(R’)₂, -OR’, -N(R’)₂, -S(O)₂R, -S(O)₂N(R)₂, -O-fenilo o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₃, fenilo, un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre, o heterociclo monocíclico saturado de 4 - 8 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; R³ es hidrógeno, halógeno, -CN, -OR’, -N(R’)₂ o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₃, fenilo o un anillo heteroaromático monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; R⁴ es hidrógeno, halógeno, -CN, -OR, -N=S(O)(R)₂, -N(R)₂ o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₃, un anillo heterocíclico monocíclico saturado o parcialmente insaturado de 4 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre o un anillo heterocíclico espirocíclico saturado o parcialmente insaturado de 7 - 12 miembros que tiene 1 - 2 heteroátomos seleccionados, de modo independiente, de nitrógeno, oxígeno o azufre; m es 0, 1, 2, 3, 4 ó 5; n es 0, 1 ó 2; p es 0 ó 1; y q es 0 ó 1.
ARP190100195A 2018-01-29 2019-01-29 Inhibidores de gcn2 y usos de los mismos AR114235A1 (es)

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US (2) US10988477B2 (es)
EP (1) EP3746075A4 (es)
JP (2) JP7229257B2 (es)
KR (1) KR20200116481A (es)
CN (2) CN118005640A (es)
AR (1) AR114235A1 (es)
AU (1) AU2019211485A1 (es)
BR (1) BR112020015328A2 (es)
CA (1) CA3089762A1 (es)
IL (2) IL301089A (es)
MX (1) MX2020007799A (es)
SG (1) SG11202006701TA (es)
TW (1) TWI816742B (es)
WO (1) WO2019148132A1 (es)

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