WO2015169953A1 - Méthode de traitement d'un gliome à l'aide de composés thiénotriazolodiazépine - Google Patents
Méthode de traitement d'un gliome à l'aide de composés thiénotriazolodiazépine Download PDFInfo
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- WO2015169953A1 WO2015169953A1 PCT/EP2015/060203 EP2015060203W WO2015169953A1 WO 2015169953 A1 WO2015169953 A1 WO 2015169953A1 EP 2015060203 W EP2015060203 W EP 2015060203W WO 2015169953 A1 WO2015169953 A1 WO 2015169953A1
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- 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
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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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
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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
- A61K31/495—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
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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
- A61K31/55—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Abstract
La présente invention concerne une méthode permettant de traiter un gliome chez un mammifère, qui consiste à administrer une dispersion solide comprenant un composé de thiénotriazolodiazépine amorphe de formule (1), ou un hydrate, un solvate ou un sel pharmaceutiquement acceptable de ce composé. Dans la formule (1), R1 représente un groupe alkyle ayant de 1 à 4 atomes de carbone, R2 représente un atome d'hydrogène, un atome d'halogène ou un groupe alkyle ayant de 1 à 4 atomes de carbone facultativement substitué par un atome d'halogène ou un groupe hydroxyle, R3 représente un atome d'halogène, un groupe phényle facultativement substitué par un atome d'halogène, un groupe alkyle ayant de 1 à 4 atomes de carbone, un groupe alcoxy ayant de 1 à 4 atomes de carbone ou un groupe cyano ;— NR5─(CH2)m─R6 où R5 représente un atome d'hydrogène ou un groupe alkyle ayant de 1 à 4 atomes de carbone, m est un nombre entier compris entre 0 et 4, et R6 représente un groupe phényle ou pyridyle facultativement substitué par un atome d'halogène; ou bien —NR7—CO—(CH2)n—R8 où R7 représente un atome d'hydrogène ou un groupe alkyle comprenant de 1 à 4 atomes de carbone, n est un nombre entier compris entre 0 et 2, et R8 représente un groupe phényle ou pyridyle facultativement substitué par un atome d'halogène, et R4 représente ─(CH2)a─CO─NH—R9 où a représente un nombre entier compris entre 1 et 4, et R9 représente un groupe alkyle ayant de 1 à 4 atomes de carbone; un groupe hydroxyalkyle ayant de 1 à 4 atomes de carbone ; un groupe alcoxy ayant de 1 à 4 atomes de carbone; ou un groupe phényle ou pyridyle facultativement substitué par un groupe alkyle ayant de 1 à 4 atomes de carbone, un groupe alcoxy ayant de 1 à 4 atomes de carbone, un groupe amino ou hydroxyle ou — (CH2)b— COOR10 où b représente un nombre entier compris entre 1 et 4, et R10 représente un groupe alkyle ayant de 1 à 4 atomes de carbone.
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461990462P | 2014-05-08 | 2014-05-08 | |
US61/990,462 | 2014-05-08 | ||
US201462012125P | 2014-06-13 | 2014-06-13 | |
US62/012,125 | 2014-06-13 | ||
US201462080739P | 2014-11-17 | 2014-11-17 | |
US62/080,739 | 2014-11-17 | ||
US201462086449P | 2014-12-02 | 2014-12-02 | |
US62/086,449 | 2014-12-02 |
Publications (1)
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WO2015169953A1 true WO2015169953A1 (fr) | 2015-11-12 |
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PCT/EP2015/060203 WO2015169953A1 (fr) | 2014-05-08 | 2015-05-08 | Méthode de traitement d'un gliome à l'aide de composés thiénotriazolodiazépine |
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WO (1) | WO2015169953A1 (fr) |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9533997B2 (en) | 2013-07-08 | 2017-01-03 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9540368B2 (en) | 2014-04-23 | 2017-01-10 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US9624241B2 (en) | 2013-03-15 | 2017-04-18 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9777003B2 (en) | 2013-12-19 | 2017-10-03 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
US10189832B2 (en) | 2016-06-20 | 2019-01-29 | Incyte Corporation | Crystalline solid forms of a BET inhibitor |
US10329305B2 (en) | 2015-10-29 | 2019-06-25 | Incyte Corporation | Amorphous solid form of a BET protein inhibitor |
US11660280B2 (en) | 2017-09-20 | 2023-05-30 | Oklahoma Medical Research Foundation | Treatment of drug resistant gliomas |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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Cited By (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9624241B2 (en) | 2013-03-15 | 2017-04-18 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US10464947B2 (en) | 2013-03-15 | 2019-11-05 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
US11498926B2 (en) | 2013-03-15 | 2022-11-15 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US10919912B2 (en) | 2013-03-15 | 2021-02-16 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9938294B2 (en) | 2013-03-15 | 2018-04-10 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9850257B2 (en) | 2013-07-08 | 2017-12-26 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9533997B2 (en) | 2013-07-08 | 2017-01-03 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9737516B2 (en) | 2013-11-26 | 2017-08-22 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
US9918990B2 (en) | 2013-11-26 | 2018-03-20 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
US9777003B2 (en) | 2013-12-19 | 2017-10-03 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
US10442803B2 (en) | 2013-12-19 | 2019-10-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
US11091484B2 (en) | 2013-12-19 | 2021-08-17 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US11059821B2 (en) | 2014-04-23 | 2021-07-13 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US10781209B2 (en) | 2014-04-23 | 2020-09-22 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US11702416B2 (en) | 2014-04-23 | 2023-07-18 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US9540368B2 (en) | 2014-04-23 | 2017-01-10 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US10472358B2 (en) | 2014-04-23 | 2019-11-12 | Incyte Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US9957268B2 (en) | 2014-04-23 | 2018-05-01 | Incyte Corporation | 1H-pyrrolo[2,3,c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
US10618910B2 (en) | 2014-09-15 | 2020-04-14 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US9834565B2 (en) | 2014-09-15 | 2017-12-05 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US10227359B2 (en) | 2014-09-15 | 2019-03-12 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
US10858372B2 (en) | 2015-10-29 | 2020-12-08 | Incyte Corporation | Amorphous solid form of a BET protein inhibitor |
US10329305B2 (en) | 2015-10-29 | 2019-06-25 | Incyte Corporation | Amorphous solid form of a BET protein inhibitor |
US10626114B2 (en) | 2016-06-20 | 2020-04-21 | Incyte Corporation | Crystalline solid forms of a BET inhibitor |
US10189832B2 (en) | 2016-06-20 | 2019-01-29 | Incyte Corporation | Crystalline solid forms of a BET inhibitor |
US11091480B2 (en) | 2016-06-20 | 2021-08-17 | Incyte Corporation | Crystalline solid forms of a BET inhibitor |
US11377446B2 (en) | 2016-06-20 | 2022-07-05 | Incyte Corporation | Crystalline solid forms of a BET inhibitor |
US11660280B2 (en) | 2017-09-20 | 2023-05-30 | Oklahoma Medical Research Foundation | Treatment of drug resistant gliomas |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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