WO2019196965A3 - Préparation pharmaceutique pour traitement d'un mélanome malin - Google Patents
Préparation pharmaceutique pour traitement d'un mélanome malin Download PDFInfo
- 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
Links
- 201000001441 melanoma Diseases 0.000 title abstract 3
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 title abstract 2
- CVCLJVVBHYOXDC-IAZSKANUSA-N (2z)-2-[(5z)-5-[(3,5-dimethyl-1h-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole Chemical compound COC1=C\C(=C/2N=C3C=CC=CC3=C\2)N\C1=C/C=1NC(C)=CC=1C CVCLJVVBHYOXDC-IAZSKANUSA-N 0.000 abstract 2
- FKSFKBQGSFSOSM-QFIPXVFZSA-N 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-[6-(1-piperazinyl)-3-pyridinyl]-4-indolecarboxamide Chemical compound C1=C2N([C@@H](C)CC)C=C(C)C2=C(C(=O)NCC=2C(NC(C)=CC=2C)=O)C=C1C(C=N1)=CC=C1N1CCNCC1 FKSFKBQGSFSOSM-QFIPXVFZSA-N 0.000 abstract 2
- BCFKACXAIBEPKR-UHFFFAOYSA-N 2-[3-[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-5-methyl-7h-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]acetonitrile Chemical compound C1CN(C)CCN1C(C(=C1)F)=CC=C1NC1=NC(C=2C=C(CC#N)C=CC=2)=C(C(C)=CN2)C2=N1 BCFKACXAIBEPKR-UHFFFAOYSA-N 0.000 abstract 2
- KVQOGDQTWWCZFX-UHFFFAOYSA-N 2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline Chemical compound CN(C)C1=CC=CC=C1CN1C(C=2C=CN=CC=2)N(CC=2C(=CC=CC=2)N(C)C)CCC1 KVQOGDQTWWCZFX-UHFFFAOYSA-N 0.000 abstract 2
- ULNXAWLQFZMIHX-UHFFFAOYSA-N GSK343 Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C=3C=NN(C=3C=C(C=2)C=2C=C(N=CC=2)N2CCN(C)CC2)C(C)C)=C1CCC ULNXAWLQFZMIHX-UHFFFAOYSA-N 0.000 abstract 2
- LBSMEKVVMYSTIH-UHFFFAOYSA-N HA15 Chemical compound C1=CC=C2C(N(C)C)=CC=CC2=C1S(=O)(=O)NC(C=1)=CC=CC=1C1=CSC(NC(C)=O)=N1 LBSMEKVVMYSTIH-UHFFFAOYSA-N 0.000 abstract 2
- DNVXATUJJDPFDM-KRWDZBQOSA-N JQ1 Chemical compound N([C@@H](CC(=O)OC(C)(C)C)C1=NN=C(N1C=1SC(C)=C(C)C=11)C)=C1C1=CC=C(Cl)C=C1 DNVXATUJJDPFDM-KRWDZBQOSA-N 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 229950006584 obatoclax Drugs 0.000 abstract 2
- 210000004881 tumor cell Anatomy 0.000 abstract 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 abstract 1
- 238000004113 cell culture Methods 0.000 abstract 1
Classifications
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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
- A61K31/40—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
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- 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.
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 WO2019196965A2 (fr) | 2018-04-11 | 2019-04-10 | Préparation pharmaceutique pour traitement d'un mélanome malin |
Country Status (2)
Country | Link |
---|---|
CZ (1) | CZ308400B6 (fr) |
WO (1) | WO2019196965A2 (fr) |
Families Citing this family (1)
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)
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2012517426A (ja) * | 2009-02-09 | 2012-08-02 | アステックス ファーマシューティカルズ インコーポレイテッド | ピロロピリミジニルaxlキナーゼ阻害剤 |
WO2011140325A1 (fr) * | 2010-05-07 | 2011-11-10 | Glaxosmithkline Llc | Indazoles |
US9567310B2 (en) * | 2012-11-09 | 2017-02-14 | Inserm (Institut National De La Sante Et De La Recharche Medicale) | Benzene sulfonamide thiazole compounds |
CN105849110B (zh) * | 2013-11-08 | 2019-08-02 | 达纳-法伯癌症研究所有限公司 | 使用溴结构域和额外终端(bet)蛋白抑制剂的用于癌症的组合疗法 |
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2018
- 2018-04-11 CZ CZ2018-181A patent/CZ308400B6/cs not_active IP Right Cessation
-
2019
- 2019-04-10 WO PCT/CZ2019/000018 patent/WO2019196965A2/fr active Application Filing
Patent Citations (1)
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)
Title |
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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 |
---|---|
CZ308400B6 (cs) | 2020-07-29 |
WO2019196965A2 (fr) | 2019-10-17 |
CZ2018181A3 (cs) | 2019-10-30 |
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