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AR092838A1 - COMPUESTOS TIPO PIRROLO-PIRROLIDINONA COMO INHIBIDORES DE LA INTERACCION ENTRE p53 Y MDM2 Y/O MDM4 - Google Patents

COMPUESTOS TIPO PIRROLO-PIRROLIDINONA COMO INHIBIDORES DE LA INTERACCION ENTRE p53 Y MDM2 Y/O MDM4

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Publication number
AR092838A1
AR092838A1 ARP130101812A ARP130101812A AR092838A1 AR 092838 A1 AR092838 A1 AR 092838A1 AR P130101812 A ARP130101812 A AR P130101812A AR P130101812 A ARP130101812 A AR P130101812A AR 092838 A1 AR092838 A1 AR 092838A1
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Argentina
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alkyl
halo
nr9r10
ch2c
independently selected
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ARP130101812A
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English (en)
Inventor
Mah Robert
Stutz Stefan
Furet Pascal
Vaupel Andrea
Guagnano Vito
Cotesta Simona
Holzer Philipp
Kallen Joerg
Masuya Keiichi
Schlapbach Achim
Original Assignee
Novarits Ag
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Publication of AR092838A1 publication Critical patent/AR092838A1/es

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    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Preparaciones farmacéuticas que comprenden dichos compuestos, usos y uso de tales compuestos en el tratamiento de un trastorno o una enfermedad mediada por la actividad de MDM2 y/o MDM4, y combinaciones que comprenden tales compuestos. Reivindicación 1: Un compuesto de la fórmula (1) o una sal del mismo, en donde: A se selecciona a partir del grupo de fórmulas (2); B se selecciona a partir de los compuestos de fórmula (3) ó (4); cada R¹ es independientemente seleccionado a partir de halo y metilo; R¹ᵃ se selecciona a partir de H, halo y alquilo C₁₋₄; R² se selecciona a partir de cloro, flúor, trifluorometilo, metilo y ciano; R³ se selecciona entre etilo, isopropilo, ciclopropilo, isobutilo, ciclobutilo y ciclopentilo, o R³ es un resto de fórmula (5), en donde R²² se selecciona a partir de OH, OCH₃, NH₂, NHMe, NMe₂, NHCOMe y NHCOH; R⁵ se selecciona a partir de: H; alquilo C₁₋₄-, dicho alquilo C₁₋₄- es opcionalmente sustituido por 1 ó 2 sustituyentes independientemente seleccionados a partir de OH y =O; alquilo C₁₋₄-O-C(O)-(CH₂)ₘ; y ciano; R⁶ se selecciona a partir de: H; alquilo C₁₋₄; alcoxilo C₁₋₄; halo; ciano; y R⁹(R¹⁰)N-(CH₂)ₘ-; R⁷ se selecciona a partir de: H, halo y alquilo C₁₋₄; cada R⁸ se selecciona independientemente a partir de H, alquilo C₁₋₄, -CHF₂, hidroxietilo y metoxietilo-; cada R⁹ se selecciona independientemente a partir de H, metilo o etilo; cada R¹⁰ se selecciona independientemente a partir de H, alcoxilo C₁₋₄ y alquilo C₁₋₄ en donde dicho alcoxilo C₁₋₄ y alquilo C₁₋₄ son cada uno independientemente opcionalmente sustituidos por 1 ó 2 sustituyentes independientemente seleccionados a partir de metoxilo, etoxilo, hidroxilo, halo y S(O)ᵛRʸ; o R⁹ y R¹⁰, junto con el átomo N al que están fijados, pueden unirse para formar un anillo heterocíclico saturado de 5 ó 6 miembros que comprende además que comprende además átomos de carbono de anillo y opcionalmente un heteroátomo de anillo independientemente seleccionado a partir de N, O y S; R¹¹ es H, alquilo C₁₋₄, alcoxilo C₁₋₄ o halo; R¹² es H o halo; R¹³ se selecciona a partir de hidroxilo, alcoxilo C₁₋₂, NH₂, -C(O)OH, -NH(C(O)-CH₃) y -C(O)-NH(CH₃); R¹⁴ se selecciona a partir de H, -C(O)-NR⁹(R¹⁰), alquilo C₁₋₄, -C(O)alquilo C₁₋₄, -C(O)O-alquilo C₁₋₄; R²³A se selecciona a partir de H, halo y alquilo C₁₋₄; R²³B se selecciona a partir de H, y alquilo C₁₋₄; R⁴ᵃ se selecciona a partir del grupo de fórmulas (6); R¹⁵ se selecciona independientemente a partir de OCH₃, OCD₃, OH, CH₂CH₃, OCF₃ y H; R¹⁶ se selecciona a partir de H, -C(O)NR⁹R¹⁰, halo, CN, -O-alquilo C₁₋₄, -C(O)morfolinil-4-ilo, tetrazolilo, -C(O)OH, -CH₂C(O)OH, -S(O)ᵛNR⁹R¹⁰, -CH₂C(O)NR⁹R¹⁰, S(O)ᵛRʸ, OCF₃, hidroxi-azetidin-1-il-carbonilo, -CH₂NR⁹R¹⁰, -CH₂NR⁹-C(O)R¹⁰, CH₂CN, metil-imidazolilo-, -CH₂C(O)O-alquilo C₁₋₄, -N(R⁹)-C(O)-alquilo C₁₋₄, -NR⁹R¹⁰ y alquilo C₁₋₄, en donde dicho alquilo C₁₋₄ es opcionalmente sustituido por 1 ó 2 OH; R¹⁷ se selecciona a partir de H, O-alquilo C₁₋₄, -CH₂C(O)O-alquilo C₁₋₄, -CH₂C(O)OH, -CH₂C(O)NR⁹R¹⁰, -CH₂CN, -NR⁹R¹⁰, -C(O)NR⁹R¹⁰, -CH₂NR⁹R¹⁰ y -C(O)O- alquilo C₁₋₄; R¹⁸ se selecciona a partir de O-alquilo C₁₋₄, OCD₃, H, -NR⁹R¹⁰, CH₂NR⁹R¹⁰ y azetidin-1-ilo, dicho azetidin-1-ilo es opcionalmente sustituido por OH o ambos CH₃ y OH; R²⁰ se selecciona a partir de CH₃, H y -CH₂CH₃; R⁴ᵇ se selecciona a partir de H, CN, halo, alquilo C₁₋₄, -C(O)OH, CH₂C(O)OH y -C(O)O-alquilo C₁₋₄; Rʸ se selecciona a partir de H, alquilo C₁₋₄ y NR⁹R¹⁰; m es 0, 1 ó 2; y v es 0, 1, ó 2; y en donde * indica el punto de unión al resto de la molécula.
ARP130101812A 2012-05-24 2013-05-24 COMPUESTOS TIPO PIRROLO-PIRROLIDINONA COMO INHIBIDORES DE LA INTERACCION ENTRE p53 Y MDM2 Y/O MDM4 AR092838A1 (es)

Applications Claiming Priority (2)

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US201261651354P 2012-05-24 2012-05-24
US201361776052P 2013-03-11 2013-03-11

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AR092838A1 true AR092838A1 (es) 2015-05-06

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Country Link
US (1) US9365576B2 (es)
EP (1) EP2855483B1 (es)
JP (1) JP6171003B2 (es)
CN (1) CN104321325B (es)
AR (1) AR092838A1 (es)
TW (1) TW201400485A (es)
UY (1) UY34820A (es)
WO (1) WO2013175417A1 (es)

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