MX2016014574A - El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. - Google Patents
El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo.Info
- Publication number
- MX2016014574A MX2016014574A MX2016014574A MX2016014574A MX2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A
- Authority
- MX
- Mexico
- Prior art keywords
- carbon number
- alkyl
- halogen atom
- optionally substituted
- integer
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 208000022679 triple-negative breast carcinoma Diseases 0.000 title abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 12
- 229910052799 carbon Inorganic materials 0.000 abstract 12
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004076 pyridyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 229940044683 chemotherapy drug Drugs 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 230000000394 mitotic effect Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 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
- A61K31/55—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
-
- 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
- A61K31/395—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
-
- 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
-
- 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
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/26—Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Un método de tratamiento de cáncer de mama triple negativo en un mamífero que comprende el paso de: administrar a un paciente una cantidad farmacéuticamente aceptable de un compuesto siendo un compuesto de tienotriazolodiazepina de la fórmula (1) (ver Fórmula) en donde R1 es alquilo que tiene un número de carbonos de 1 a 4, R2 es un átomo de hidrógeno; un átomo de halógeno; o alquilo que tiene un número de carbonos de 1 a 4 opcionalmente sustituido por un átomo de halógeno o un grupo hidroxilo, R3 es un átomo de halógeno; fenilo opcionalmente sustituido por un átomo de halógeno, alquilo que tiene un número de carbonos de 1 a 4, alcoxi que tiene un número de carbonos de 1 a 4 o ciano; -NR5- (CH2)m-R6, en donde R5 es un átomo de hidrógeno o alquilo que tiene un número de carbonos de 1 a 4, m es un número entero de 0-4, y R6 es fenilo o piridilo opcionalmente sustituido por un átomo de halógeno; o -NR7-CO- (CH2)n-R8 en donde R7 es un átomo de hidrógeno o alquilo que tiene un número de carbonos de 1 a 4, n es un número entero de 0 a 2, y R8 es fenilo o piridilo opcionalmente sustituido por un átomo de halógeno y R4 es (CH2)a-CO-NH-R9 en donde a es un número entero de 1-4, y R9 es alquilo que tiene un número de carbonos de 1 a 4; hidroxialquilo que tiene un número de carbonos de 1 a 4; alcoxi que tiene un número de carbonos de 1 a 4; o fenilo o piridilo opcionalmente sustituido con alquilo que tiene un número de carbonos de 1 a 4, alcoxi que tiene un número de carbonos de 1 a 4, amino o un grupo hidroxilo o -(CH2)b-COOR10, en donde b es un número entero de 1 a 4, y R10 es alquilo que tiene un número de carbonos de 1 a 4, o una sal farmacéuticamente aceptable del mismo o un hidrato o solvato del mismo, en combinación con uno o más fármacos de quimioterapia seleccionados del grupo que consiste en inhibidores de m-TOR e inhibidores de la mitosis.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461990457P | 2014-05-08 | 2014-05-08 | |
| US201462012048P | 2014-06-13 | 2014-06-13 | |
| US201462080751P | 2014-11-17 | 2014-11-17 | |
| US201462086400P | 2014-12-02 | 2014-12-02 | |
| US201562150044P | 2015-04-20 | 2015-04-20 | |
| PCT/EP2015/060200 WO2015169951A1 (en) | 2014-05-08 | 2015-05-08 | Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2016014574A true MX2016014574A (es) | 2017-02-23 |
Family
ID=53191652
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016014574A MX2016014574A (es) | 2014-05-08 | 2015-05-08 | El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9968619B2 (es) |
| EP (1) | EP3139959A1 (es) |
| JP (1) | JP2017519727A (es) |
| KR (1) | KR20170002610A (es) |
| CN (1) | CN106852120A (es) |
| AU (1) | AU2015257658A1 (es) |
| BR (1) | BR112016026046A8 (es) |
| CA (1) | CA2947970A1 (es) |
| MX (1) | MX2016014574A (es) |
| RU (1) | RU2016147946A (es) |
| WO (1) | WO2015169951A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| EP4118431A1 (de) * | 2020-03-12 | 2023-01-18 | Heinrich-Heine-Universität Düsseldorf | Inhibition von fkbp1a zur therapie des triple-negativen mammakarzinoms |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| BR112023025562A2 (pt) | 2021-06-08 | 2024-02-20 | Poseidon Innovation Llc | Compostos anticâncer |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1027887B1 (en) * | 1999-02-10 | 2008-08-13 | Pfizer Products Inc. | Matrix controlled release device |
| AU2001264303A1 (en) | 2000-06-16 | 2001-12-24 | Mitsubishi Pharma Corporation | Compositions controlling release ph range and/or speed |
| CN101910182B (zh) * | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| JP2014513062A (ja) * | 2011-03-10 | 2014-05-29 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 癌の処置における使用のためのａｔｉｐ３およびその生物学的に活性なフラグメント |
| EP2863923B1 (en) | 2012-06-25 | 2019-05-08 | Oncoethix GmbH | Thienotriazolodiazepine compounds for the treatment of lymphomas |
| EP2866810B9 (en) * | 2012-06-27 | 2019-06-26 | The Curators Of The University Of Missouri | Induction of estrogen receptor beta by cholesterol biosynthesis inhibitors and methods of treatment of cancer |
| MX2015003771A (es) | 2012-09-28 | 2016-03-04 | Oncoethix Gmbh | Formulacion farmaceutica que contiene compuestos de tienotriazolodiazepina. |
| BR112015007144A2 (pt) * | 2012-10-04 | 2017-12-12 | Ab Science | uso de masitinib para o tratamento de câncer em subpopulações de paciente identificadas usando fatores prognosticadores |
| US9492460B2 (en) * | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| WO2015018523A1 (en) * | 2013-08-06 | 2015-02-12 | Oncoethix Sa | A novel bet-brd inhibitor for treatment of solid tumors |
-
2015
- 2015-05-08 BR BR112016026046A patent/BR112016026046A8/pt not_active IP Right Cessation
- 2015-05-08 CA CA2947970A patent/CA2947970A1/en not_active Abandoned
- 2015-05-08 EP EP15723671.2A patent/EP3139959A1/en not_active Withdrawn
- 2015-05-08 US US15/308,525 patent/US9968619B2/en not_active Expired - Fee Related
- 2015-05-08 AU AU2015257658A patent/AU2015257658A1/en not_active Abandoned
- 2015-05-08 RU RU2016147946A patent/RU2016147946A/ru not_active Application Discontinuation
- 2015-05-08 WO PCT/EP2015/060200 patent/WO2015169951A1/en not_active Ceased
- 2015-05-08 KR KR1020167034522A patent/KR20170002610A/ko not_active Withdrawn
- 2015-05-08 MX MX2016014574A patent/MX2016014574A/es unknown
- 2015-05-08 JP JP2016566962A patent/JP2017519727A/ja active Pending
- 2015-05-08 CN CN201580037334.9A patent/CN106852120A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN106852120A (zh) | 2017-06-13 |
| US20170065607A1 (en) | 2017-03-09 |
| US9968619B2 (en) | 2018-05-15 |
| EP3139959A1 (en) | 2017-03-15 |
| RU2016147946A3 (es) | 2018-12-26 |
| BR112016026046A8 (pt) | 2021-07-20 |
| KR20170002610A (ko) | 2017-01-06 |
| RU2016147946A (ru) | 2018-06-08 |
| BR112016026046A2 (pt) | 2017-08-15 |
| AU2015257658A1 (en) | 2016-11-10 |
| WO2015169951A1 (en) | 2015-11-12 |
| JP2017519727A (ja) | 2017-07-20 |
| CA2947970A1 (en) | 2015-11-12 |
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