AR109560A1 - Compuestos moduladores de receptores tipo toll - Google Patents

Compuestos moduladores de receptores tipo toll

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Publication number
AR109560A1
AR109560A1 ARP170102436A ARP170102436A AR109560A1 AR 109560 A1 AR109560 A1 AR 109560A1 AR P170102436 A ARP170102436 A AR P170102436A AR P170102436 A ARP170102436 A AR P170102436A AR 109560 A1 AR109560 A1 AR 109560A1
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AR
Argentina
Prior art keywords
optionally substituted
alkyl
nitrogen
oxygen
heteroatoms selected
Prior art date
Application number
ARP170102436A
Other languages
English (en)
Inventor
Jeff Zablocki
Michael R Mish
Richard L Mackman
Gregory Chin
Original Assignee
Gilead Sciences Inc
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Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR109560A1 publication Critical patent/AR109560A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/04—Ortho-condensed 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
    • C07D487/04—Ortho-condensed 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
    • C07D495/04—Ortho-condensed systems

Abstract

Esta solicitud se refiere en general a compuestos moduladores de receptores de tipo toll y composiciones farmacéuticas que, entre otras cosas, modulan receptores de tipo toll (por ejemplo TLR8), y métodos para fabricarlos y usarlos. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: R¹ es -H, alquilo C₁₋₄, o haloalquilo C₁₋₄; R² es alquilo C₁₋₆ o haloalquilo C₁₋₆; R³ es alcóxido C₁₋₄ opcionalmente sustituido con 1 RX; cada RX es independientemente -ORY, heterociclilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre opcionalmente sustituido con 1 a 3 RZ; fenilo opcionalmente sustituido con 1 a 3 RZ; o heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre opcionalmente sustituido con 1 a 3 RZ; RY es alquilo C₁₋₄, haloalquilo C₁₋₄, o heteroarilo de 5 a 10 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno, y azufre opcionalmente sustituido con 1 a 3 RZ; Q es N, CH, o CR⁴; o R³ y R⁴ se toman juntos para formar cicloalquilo C₅₋₆; heterociclilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre; fenilo; o heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre, en donde: cicloalquilo C₅₋₆, y fenilo están cada uno opcionalmente independientemente sustituido con 1 a 3 R⁵; cada R⁵ es independientemente halógeno, -OH, -NH₂, -CN, alquilo C₁₋₄ opcionalmente sustituido con 1 a 3 RZ, haloalquilo C₁₋₄, alcóxido C₁₋₄, -C(O)OH, -C(O)alquilo C₁₋₄, -C(O)O-alquilo C₁₋₄, -C(O)NH₂, -C(O)NH(alquilo C₁₋₄), -C(O)N(alquilo C₁₋₄)₂, -N(H)C(O)alquilo C₁₋₄, -S(O)₂alquilo C₁₋₄, o heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno, y azufre opcionalmente sustituido con 1 a 3 RZ; heteroarilo de 5 a 6 miembros está opcionalmente sustituido con 1 a 3 R⁶; cada R⁶ es independientemente halógeno, -OH, -NH₂, -CN, alquilo C₁₋₄ opcionalmente sustituido con 1 fenilo opcionalmente sustituido con 1 a 3 RZ; haloalquilo C₁₋₄, alcóxido C₁₋₄, -S(O)₂alquilo C₁₋₄; heterociclilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionado de oxígeno, nitrógeno, y azufre opcionalmente sustituido con 1 a 3 RZ; fenilo opcionalmente sustituido con 1 a 3 RZ; o heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionado de oxígeno, nitrógeno, y azufre opcionalmente sustituido con 1 a 3 RZ; heterociclilo de 5 a 6 miembros está opcionalmente sustituido con 1 a 3 R⁷; R⁷ es halógeno, -OH, alquilo C₁₋₄, alcóxido C₁₋₄, o -C(O)R⁸; cada R⁸ es independientemente alquilo C₁₋₄ opcionalmente sustituido con -CN o -NH₂; haloalquilo C₁₋₄; cicloalquilo C₅₋₆, heterociclilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre opcionalmente sustituido con 1 a 3 RZ; o heteroarilo de 5 a 10 miembros que tiene de 1 a 3 heteroátomos seleccionados de oxígeno, nitrógeno y azufre opcionalmente sustituido con 1 a 3 RZ; y cada RZ es independientemente -NH₂, alquilo C₁₋₄, halógeno, -CN, -O-alquilo C₁₋₄, haloalquilo C₁₋₄, o -C(O)NH₂; con la condición de que la fórmula (1) no sea, un compuesto de la fórmula (2).
ARP170102436A 2016-09-02 2017-09-01 Compuestos moduladores de receptores tipo toll AR109560A1 (es)

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US201662383162P 2016-09-02 2016-09-02

Publications (1)

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AR109560A1 true AR109560A1 (es) 2018-12-26

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US (3) US10370342B2 (es)
EP (1) EP3507276B1 (es)
JP (1) JP6746776B2 (es)
KR (1) KR102268448B1 (es)
CN (1) CN109923106B (es)
AR (1) AR109560A1 (es)
AU (1) AU2017318601B2 (es)
CA (1) CA3035346A1 (es)
ES (1) ES2906581T3 (es)
MA (1) MA46093A (es)
PL (1) PL3507276T3 (es)
PT (1) PT3507276T (es)
SI (1) SI3507276T1 (es)
TW (2) TWI660948B (es)
WO (1) WO2018045144A1 (es)

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