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AR101179A1 - Combinaciones anti-pd-l1 para tratar tumores - Google Patents

Combinaciones anti-pd-l1 para tratar tumores

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Publication number
AR101179A1
AR101179A1 ARP150102205A ARP150102205A AR101179A1 AR 101179 A1 AR101179 A1 AR 101179A1 AR P150102205 A ARP150102205 A AR P150102205A AR P150102205 A ARP150102205 A AR P150102205A AR 101179 A1 AR101179 A1 AR 101179A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
alkenyl
aryl
alkoxy
Prior art date
Application number
ARP150102205A
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English (en)
Inventor
Li Lixin
Original Assignee
Shanghai Birdie Biotech 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 Shanghai Birdie Biotech Inc filed Critical Shanghai Birdie Biotech Inc
Publication of AR101179A1 publication Critical patent/AR101179A1/es

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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • 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
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Mycology (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

Reivindicación 1: Una combinación que comprende: (i) una cantidad eficaz de un antagonista de eje PD-L / PD-1; y (ii) una cantidad eficaz de un agente inmunoterapéutico que es capaz de activar una célula dendrítica plasmocitoide humana, célula dendrítica mieloide o célula NK, o una combinación de estas. Reivindicación 9: La combinación de la reivindicación 8, donde el antagonista de unión de PD-1 es MDX-1106, Merck 3745, CT011, AMP-224 o AMP-514. Reivindicación 15: La combinación de la reivindicación 14, donde el antagonista de unión de PD-L1 se selecciona del grupo que consiste en: YW243.55.S70, MPDL3280A, MDX-1105, MEDI-4736, y MSB0010718C. Reivindicación 20: La combinación de cualquiera de las reivindicaciones 1 a 18, donde dicho agente inmunoterapéutico tiene una estructura de fórmula (1), donde la línea punteada representa un enlace o la ausencia de un enlace; X es S o -NR¹; R¹ es -W⁰-W¹-W²-W³-W⁴; W⁰ es un enlace, alquilo, alquenilo, alquinilo, alcoxi o --alquil-S-alquil--; W¹ es un enlace, --O-- o --NR²--, donde R² es hidrógeno, alquilo o alquenilo; W² es un enlace, --O--, --C(O)--, --C(S)-- o -S(O)₂--; W³ es un enlace, --NR³--, donde R³ es hidrógeno, alquilo o alquenilo; W⁴ es hidrógeno, alquilo, alquenilo, alquinilo, alcoxi, cicloalquilo, arilo ariloxi, heteroarilo o heterociclilo, cada uno de los cuales se encuentra opcionalmente sustituido por uno o más sustituyentes seleccionados del grupo que consiste en hidroxilo, alcoxi, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterociclilo, --NH₂, nitro, --alquil-hidroxilo, --alquil-arilo, --alquil-heteroarilo, --alquil-heterociclilo, --O-R⁴, --O-alquil-R⁴, --alquil-O-R⁴, --C(O)-R⁴, --alquil-C(O)R⁴, --alquil-C(O)-O-R⁴, --C(O)-O-R⁴, --S-R⁴, --S(O)₂-R⁴, --NH-S(O)₂-R⁴, --alquil-S-R⁴, --alquil-S(O)₂-R⁴, --NHR⁴, --NR⁴R⁴,--NH-alquil-R⁴, halógeno, --CN, --NO₂ y, -SH, donde R⁴ es independientemente hidrógeno, alquilo, alquenilo, --alquil-hidroxilo, arilo, heteroarilo, heterociclilo o haloalquilo; Z es hidrógeno, alquilo, alquenilo, alquinilo, alcoxi, arilo, haloalquilo, heteroarilo, heterociclilo, cada uno de los cuales puede encontrarse opcionalmente sustituido por uno o más sustituyentes seleccionados del grupo que consiste en hidroxilo, alcoxi, alquilo, alquenilo, alquinilo, arilo, heteroarilo, heterociclilo, halógeno, ciano, nitro, --N(R⁵)₂, --alcoxi-alquilo, --alcoxi-alquenilo, --C(O)-alquilo, --C(O)-O-alquilo, --O-C(O)-alquilo, --C(O)-N(R⁵)₂, arilo, heteroarilo, --CO-arilo y --CO-heteroarilo, donde cada R⁵ es independientemente hidrógeno, alquilo, haloalquilo, --alquil-arilo o --alquil-heteroarilo; R es hidrógeno; alquilo, alcoxi, haloalquilo, halógeno, arilo, heteroarilo, heterociclilo, cada uno de los cuales se encuentra opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en hidroxilo, alcoxi, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterociclilo, --NH₂, nitro, --alquil-hidroxilo, --alquil-arilo, --alquil-heteroarilo, --alquil-heterociclilo, --O-R⁴, --O-alquil-R⁴, --alquil-O-R⁴, --C(O)-R⁴, --C(O)-NH-R⁴, --C(O)-NR⁴R⁴, --alquil-C(O)-R⁴, --alquil-C(O)-O-R⁴, --C(O)-O-R⁴, --O-C(O)-R⁴, --S-R⁴, --C(O)-S-R⁴, --S-C(O)-R⁴, --S(O)₂-R⁴, --NH-S(O)₂-R⁴, --alquil-S-R⁴, --alquil-S(O)₂-R⁴, --NHR⁴, --NR⁴R⁴, --NH-alquil-R⁴, halógeno, --CN y -SH, donde R⁴ es independientemente hidrógeno, alquilo, alquenilo, alcoxi, --alquil-hidroxilo, arilo, heteroarilo, heterociclilo o haloalquilo; n es 0, 1, 2, 3 ó 4; Y es -NR⁶R⁷-, -CR⁶R⁷R⁸ o -alquil-NH₂, cada uno de los cuales puede encontrarse opcionalmente sustituido por uno o más sustituyentes seleccionados del grupo que consiste en hidroxilo, alcoxi, alquilo, alquenilo, alquinilo, --NH₂, halógeno, --N(R⁵)₂, --alcoxi-alquilo, --alcoxi-alquenilo, --C(O)-alquilo, --C(O)-O-alquilo, --C(O)-N(R⁵)₂, arilo, heteroarilo, --CO-arilo y -CO-heteroarilo, donde R⁶, R⁷ y R⁸ son independientemente hidrógeno, alquilo, alquenilo, alcoxi, alquilamino, dialquilamino, alquiltio, ariltio, --alquil-hidroxilo, --alquil-C(O)-O-R⁹, --alquil-C(O)-R⁹ o -alquil-O-C(O)-R⁹, donde cada R⁵ es independientemente hidrógeno, alquilo, haloalquilo, --alquil-arilo o -alquil-heteroarilo, donde R⁹ es hidrógeno, alquilo, alquenilo, halógeno o haloalquilo; X y Z en conjunto opcionalmente pueden formar un anillo de 5 - 9 miembros. Reivindicación 22: La combinación de cualquiera de las reivindicaciones 1 a 18, donde dicho agente inmunoterapéutico tiene una estructura de fórmula (2), donde V es -NR⁶R⁷, donde cada uno de R⁶ y R⁷ es independientemente hidrógeno, alquilo, alquenilo, alcoxi, alquilamino, dialquilamino, alquiltio, ariltio, --alquil-hidroxilo, --alquil-C(O)-O-R⁹, --alquil-C(O)-R⁹, o -alquil-O-C(O)-R⁹, donde R⁹ es hidrógeno, alquilo, alquenilo, halógeno o haloalquilo; R¹⁰ y R¹¹ son independientemente hidrógeno, alquilo, alquenilo, arilo, haloalquilo, heteroarilo, heterociclilo o cicloalquilo, cada uno de los cuales se encuentra opcionalmente sustituido por uno o más sustituyentes seleccionados del grupo que consiste en hidroxilo, alcoxi, alquilo, alquenilo, alquinilo, halógeno, --N(R⁵)₂, --alcoxi-alquilo, --alcoxi-alquenilo, --C(O)-alquilo, --C(O)-O-alquilo, --C(O)-N(R⁵)₂, arilo, heteroarilo, --CO-arilo y -CO-heteroarilo, donde cada R⁵ es independientemente hidrógeno, alquilo, haloalquilo, --alquil-arilo o -alquil-heteroarilo.
ARP150102205A 2014-07-09 2015-07-10 Combinaciones anti-pd-l1 para tratar tumores AR101179A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201410325480.9A CN105233291A (zh) 2014-07-09 2014-07-09 用于治疗癌症的联合治疗组合物和联合治疗方法

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AR101179A1 true AR101179A1 (es) 2016-11-30

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US (2) US20170056391A1 (es)
EP (1) EP3166640B1 (es)
JP (2) JP2017521421A (es)
KR (1) KR20170020537A (es)
CN (5) CN112546231A (es)
AR (2) AR101180A1 (es)
AU (3) AU2015286042B2 (es)
CA (1) CA2954443A1 (es)
SG (1) SG11201700079VA (es)
TW (1) TW201628652A (es)
WO (1) WO2016004875A1 (es)

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