WO2019196965A3 - Préparation pharmaceutique pour traitement d'un mélanome malin - Google Patents

Préparation pharmaceutique pour traitement d'un mélanome malin Download PDF

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Publication number
WO2019196965A3
WO2019196965A3 PCT/CZ2019/000018 CZ2019000018W WO2019196965A3 WO 2019196965 A3 WO2019196965 A3 WO 2019196965A3 CZ 2019000018 W CZ2019000018 W CZ 2019000018W WO 2019196965 A3 WO2019196965 A3 WO 2019196965A3
Authority
WO
WIPO (PCT)
Prior art keywords
nmol
μmol
malignant melanoma
pharmacy preparation
gant61
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/CZ2019/000018
Other languages
English (en)
Other versions
WO2019196965A2 (fr
Inventor
Jiri VACHTENHEIM
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Matematicko-Fyzikalni Fakulta University Karlovy V Praze
Original Assignee
Matematicko-Fyzikalni Fakulta University Karlovy V Praze
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 Matematicko-Fyzikalni Fakulta University Karlovy V Praze filed Critical Matematicko-Fyzikalni Fakulta University Karlovy V Praze
Publication of WO2019196965A2 publication Critical patent/WO2019196965A2/fr
Publication of WO2019196965A3 publication Critical patent/WO2019196965A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/403—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 carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

L'invention concerne une préparation pharmaceutique destinée au traitement d'un mélanome malin contenant une combinaison de principes actifs, à savoir le GANT61, l'Obatoclax sous la forme avantageuse de son sel mésylate, et un agent choisi dans le groupe constitué par (+)-JQ1, SGI-7079, GSK343, GSK126, HA15, la concentration des principes actifs dans la combinaison triple spécifique nécessaire pour éradiquer les cellules tumorales étant la suivante : a) GANT61 de 10 à 20 µmol/l ; b) Obatoclax de 150 à 300 nmoles/l ; c1) (+)-JQ1 de 125 à 500 nmoles/l ; c2) SGI-7079 de 125 à 500 nmoles/l ; c3) GSK343 de 0,25 à 1,0 µmol/l ; c4) GSK126 de 25 à 100 nmoles/l ; et c5) HA15 de 2,5 à 10 µmol/l. Toutes les combinaisons triples sont hautement efficaces dans les expériences réalisées sur des cultures cellulaires de cellules de mélanome humain, toutes les cellules tumorales ayant été éradiquées au plus tard au 7ème jour après l'application.
PCT/CZ2019/000018 2018-04-11 2019-04-10 Préparation pharmaceutique pour traitement d'un mélanome malin Ceased WO2019196965A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CZ2018-181A CZ308400B6 (cs) 2018-04-11 2018-04-11 Farmaceutický přípravek pro léčení maligního melanomu
CZPV2018-181 2018-04-11

Publications (2)

Publication Number Publication Date
WO2019196965A2 WO2019196965A2 (fr) 2019-10-17
WO2019196965A3 true WO2019196965A3 (fr) 2020-01-16

Family

ID=66349211

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CZ2019/000018 Ceased WO2019196965A2 (fr) 2018-04-11 2019-04-10 Préparation pharmaceutique pour traitement d'un mélanome malin

Country Status (2)

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CZ (1) CZ308400B6 (fr)
WO (1) WO2019196965A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4201928A1 (fr) * 2021-12-21 2023-06-28 Institut National de la Santé et de la Recherche Médicale (INSERM) Composés de benzène sulfonamide thiazole et leur utilisation pour le traitement de cancers

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106963765A (zh) * 2017-03-28 2017-07-21 上海交通大学医学院附属第九人民医院 Ezh2抑制剂化合物在制备治疗眼部黑色素瘤的药物中的应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201041892A (en) * 2009-02-09 2010-12-01 Supergen Inc Pyrrolopyrimidinyl Axl kinase inhibitors
JP5864546B2 (ja) * 2010-05-07 2016-02-17 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インダゾール
WO2014072486A1 (fr) * 2012-11-09 2014-05-15 INSERM (Institut National de la Santé et de la Recherche Médicale) Nouveaux composés de benzènesulfonamide-thiazole
RU2016122654A (ru) * 2013-11-08 2017-12-14 Дана-Фарбер Кэнсер Инститьют, Инк. Комбинированная терапия злокачественной опухоли с использованием ингибиторов бромодоменового и экстратерминального (вет) белка

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106963765A (zh) * 2017-03-28 2017-07-21 上海交通大学医学院附属第九人民医院 Ezh2抑制剂化合物在制备治疗眼部黑色素瘤的药物中的应用

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
AHMAD NAJEM ET AL: "New Drug Combination Strategies in Melanoma: Current Status and Future Directions", ANTICANCER RESEARCH - INTERNATIONAL JOURNAL OF CANCER RESEARCH AND TREATMENT, vol. 37, no. 11, 23 October 2017 (2017-10-23), GR, pages 5941 - 5953, XP055598454, ISSN: 0250-7005, DOI: 10.21873/anticanres.12041 *
CEREZO MICHAËL ET AL: "Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance", CANCER CELL, CELL PRESS, US, vol. 29, no. 6, 26 May 2016 (2016-05-26), pages 805 - 819, XP029601428, ISSN: 1535-6108, DOI: 10.1016/J.CCELL.2016.04.013 *
JESSAMY C. TIFFEN ET AL: "Targeting activating mutations of EZH2 leads to potent cell growth inhibition in human melanoma by derepression of tumor suppressor genes", ONCOTARGET, vol. 6, no. 29, 12 August 2015 (2015-08-12), XP055642576, DOI: 10.18632/oncotarget.4809 *
JUDITH MÜLLER ET AL: "Low MITF/AXL ratio predicts early resistance to multiple targeted drugs in melanoma", NATURE COMMUNICATIONS, vol. 5, no. 1, 15 December 2014 (2014-12-15), XP055642880, DOI: 10.1038/ncomms6712 *
KATERINA VLCKOVÁ ET AL: "GLI inhibitor GANT61 kills melanoma cells and acts in synergy with obatoclax", INTERNATIONAL JOURNAL OF ONCOLOGY, vol. 49, no. 3, September 2016 (2016-09-01), GR, pages 953 - 960, XP055597647, ISSN: 1019-6439, DOI: 10.3892/ijo.2016.3596 *
LUCA PAOLUZZI ET AL: "BET and BRAF inhibitors act synergistically against BRAF- mutant melanoma", CANCER MEDICINE, vol. 5, no. 6, 11 May 2016 (2016-05-11), GB, pages 1183 - 1193, XP055598079, ISSN: 2045-7634, DOI: 10.1002/cam4.667 *
PAUL K PAIK ET AL: "A phase I study of obatoclax mesylate, a Bcl-2 antagonist, plus topotecan in solid tumor malignancies", CANCER CHEMOTHERAPY AND PHARMACOLOGY, SPRINGER, BERLIN, DE, vol. 66, no. 6, 18 February 2010 (2010-02-18), pages 1079 - 1085, XP019843381, ISSN: 1432-0843 *
XIAOLIANG WU ET AL: "AXL kinase as a novel target for cancer therapy", ONCOTARGET, vol. 5, 16 October 2014 (2014-10-16), XP055242570 *

Also Published As

Publication number Publication date
WO2019196965A2 (fr) 2019-10-17
CZ2018181A3 (cs) 2019-10-30
CZ308400B6 (cs) 2020-07-29

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