RU2016146102A - Способ лечения резистентной неходжкинской лимфомы, медуллобластомы и/или alk+ немелкоклеточного рака легкого с применением тиенотриазолодиазепиновых соединений - Google Patents
Способ лечения резистентной неходжкинской лимфомы, медуллобластомы и/или alk+ немелкоклеточного рака легкого с применением тиенотриазолодиазепиновых соединений Download PDFInfo
- Publication number
- RU2016146102A RU2016146102A RU2016146102A RU2016146102A RU2016146102A RU 2016146102 A RU2016146102 A RU 2016146102A RU 2016146102 A RU2016146102 A RU 2016146102A RU 2016146102 A RU2016146102 A RU 2016146102A RU 2016146102 A RU2016146102 A RU 2016146102A
- Authority
- RU
- Russia
- Prior art keywords
- medulloblastoma
- lymphoma
- alk
- diazepin
- thieno
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 27
- 208000002154 non-small cell lung carcinoma Diseases 0.000 title claims 10
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 title claims 10
- 150000001875 compounds Chemical class 0.000 title claims 7
- 206010025323 Lymphomas Diseases 0.000 title claims 4
- 208000000172 Medulloblastoma Diseases 0.000 claims 21
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 10
- 239000007962 solid dispersion Substances 0.000 claims 10
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims 9
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 8
- 229920000642 polymer Polymers 0.000 claims 5
- GNMUEVRJHCWKTO-FQEVSTJZSA-N 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- Chemical compound C([C@@H]1N=C(C2=C(N3C(C)=NN=C31)SC(=C2C)C)C=1C=CC(Cl)=CC=1)C(=O)NC1=CC=C(O)C=C1 GNMUEVRJHCWKTO-FQEVSTJZSA-N 0.000 claims 4
- 101150023956 ALK gene Proteins 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 210000004881 tumor cell Anatomy 0.000 claims 4
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000009477 glass transition Effects 0.000 claims 2
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims 2
- 201000003445 large cell neuroendocrine carcinoma Diseases 0.000 claims 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010003908 B-cell small lymphocytic lymphoma Diseases 0.000 claims 1
- 229940124291 BTK inhibitor Drugs 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 229940124292 CD20 monoclonal antibody Drugs 0.000 claims 1
- 229940126190 DNA methyltransferase inhibitor Drugs 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000014579 classic medulloblastoma Diseases 0.000 claims 1
- 208000014501 desmoplastic/nodular medulloblastoma Diseases 0.000 claims 1
- 230000004069 differentiation Effects 0.000 claims 1
- 239000003968 dna methyltransferase inhibitor Substances 0.000 claims 1
- 101150068690 eml4 gene Proteins 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 229940084434 fungoid Drugs 0.000 claims 1
- 230000002518 glial effect Effects 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 201000005833 large cell medulloblastoma Diseases 0.000 claims 1
- 229940124302 mTOR inhibitor Drugs 0.000 claims 1
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 1
- 201000005776 medullomyoblastoma Diseases 0.000 claims 1
- 208000016056 medullomyoblastoma with myogenic differentiation Diseases 0.000 claims 1
- 201000005803 melanotic medulloblastoma Diseases 0.000 claims 1
- 210000003757 neuroblast Anatomy 0.000 claims 1
- 230000004031 neuronal differentiation Effects 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- 201000006845 reticulosarcoma Diseases 0.000 claims 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims 1
- 238000001694 spray drying Methods 0.000 claims 1
- 210000000130 stem cell Anatomy 0.000 claims 1
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
- A61K31/55—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
- 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
-
- 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
- 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
- A61K9/4891—Coated capsules; Multilayered drug free capsule shells
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (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)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Hematology (AREA)
- Oncology (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)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461987813P | 2014-05-02 | 2014-05-02 | |
| US61/987,813 | 2014-05-02 | ||
| US201461990469P | 2014-05-08 | 2014-05-08 | |
| US201461990459P | 2014-05-08 | 2014-05-08 | |
| US61/990,459 | 2014-05-08 | ||
| US61/990,469 | 2014-05-08 | ||
| PCT/US2015/028798 WO2015168555A1 (en) | 2014-05-02 | 2015-05-01 | Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2016146102A true RU2016146102A (ru) | 2018-06-05 |
| RU2016146102A3 RU2016146102A3 (enExample) | 2018-12-17 |
Family
ID=54359380
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016146102A RU2016146102A (ru) | 2014-05-02 | 2015-05-01 | Способ лечения резистентной неходжкинской лимфомы, медуллобластомы и/или alk+ немелкоклеточного рака легкого с применением тиенотриазолодиазепиновых соединений |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20170095484A1 (enExample) |
| EP (1) | EP3137086A4 (enExample) |
| JP (1) | JP2017514907A (enExample) |
| KR (1) | KR20170002550A (enExample) |
| CN (1) | CN106687117A (enExample) |
| AU (1) | AU2015252940A1 (enExample) |
| CA (1) | CA2947593A1 (enExample) |
| MX (1) | MX2016014299A (enExample) |
| RU (1) | RU2016146102A (enExample) |
| WO (1) | WO2015168555A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102216288B1 (ko) | 2013-03-15 | 2021-02-18 | 인사이트 홀딩스 코포레이션 | Bet 단백질 저해제로서의 삼환식 복소환 |
| ES2635560T3 (es) | 2013-07-08 | 2017-10-04 | Incyte Holdings Corporation | Heterociclos tricíclicos como inhibidores de la proteína NET |
| 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 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| PT3134403T (pt) | 2014-04-23 | 2020-05-18 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7(6h)-onas como inibidores das proteínas bet |
| CN107073011A (zh) * | 2014-08-19 | 2017-08-18 | 翁科埃斯克斯有限公司 | 利用噻吩并三唑并二氮杂*化合物治疗淋巴瘤的方法 |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| US10683305B2 (en) | 2015-04-27 | 2020-06-16 | Concert Pharmaceuticals, Inc. | Deuterated OTX-015 |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CN109715625B (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
| BR112019028088A8 (pt) * | 2017-06-30 | 2022-11-08 | Onxeo | Dispersão sólida amorfa de belinostate, processo de preparação da dispersão sólida amorfa de belinostate e composição farmacêutica |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2412776C (en) * | 2000-06-16 | 2011-03-15 | Mitsubishi Pharma Corporation | Compositions controlling release ph range and/or speed |
| JP5478262B2 (ja) * | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| CN104311562B (zh) * | 2010-05-14 | 2017-07-04 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| CA2877434A1 (en) * | 2012-06-25 | 2014-01-03 | Oncoethix Sa | Method of treating lymphoma using thienotriazolodiazepine compounds |
| BR112015006537A2 (pt) * | 2012-09-28 | 2017-07-04 | Oncoethix Sa | dispersão sólida, formulação farmacêutica, cápsula farmacêutica, e, tablete farmacêutico |
| WO2015018522A1 (en) * | 2013-08-06 | 2015-02-12 | Oncoethix Sa | Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl) |
| WO2015018520A1 (en) * | 2013-08-06 | 2015-02-12 | Oncoethix Sa | A bet-brd inhibitor represents a novel agent for alk positive anaplastic large cell lymphoma |
| KR20160079822A (ko) * | 2013-11-27 | 2016-07-06 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 함유하는 제약 제제를 사용하여 비소세포성 폐암을 치료하는 방법 |
| US9757385B2 (en) * | 2013-11-27 | 2017-09-12 | Merck Sharp & Dohme Corp. | Method of treating leukemia using pharmaceutical formulation containing thienotriazolodiazepine compounds |
-
2015
- 2015-05-01 US US15/308,548 patent/US20170095484A1/en not_active Abandoned
- 2015-05-01 JP JP2017510449A patent/JP2017514907A/ja active Pending
- 2015-05-01 RU RU2016146102A patent/RU2016146102A/ru not_active Application Discontinuation
- 2015-05-01 CN CN201580036829.XA patent/CN106687117A/zh active Pending
- 2015-05-01 MX MX2016014299A patent/MX2016014299A/es unknown
- 2015-05-01 EP EP15786309.3A patent/EP3137086A4/en not_active Withdrawn
- 2015-05-01 WO PCT/US2015/028798 patent/WO2015168555A1/en not_active Ceased
- 2015-05-01 CA CA2947593A patent/CA2947593A1/en not_active Abandoned
- 2015-05-01 KR KR1020167033941A patent/KR20170002550A/ko not_active Withdrawn
- 2015-05-01 AU AU2015252940A patent/AU2015252940A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2947593A1 (en) | 2015-11-05 |
| WO2015168555A1 (en) | 2015-11-05 |
| EP3137086A4 (en) | 2017-12-27 |
| CN106687117A (zh) | 2017-05-17 |
| EP3137086A1 (en) | 2017-03-08 |
| MX2016014299A (es) | 2017-01-27 |
| KR20170002550A (ko) | 2017-01-06 |
| AU2015252940A1 (en) | 2016-11-17 |
| RU2016146102A3 (enExample) | 2018-12-17 |
| JP2017514907A (ja) | 2017-06-08 |
| US20170095484A1 (en) | 2017-04-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20190514 |