RU2016141569A - Комбинации - Google Patents
Комбинации Download PDFInfo
- Publication number
- RU2016141569A RU2016141569A RU2016141569A RU2016141569A RU2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A
- Authority
- RU
- Russia
- Prior art keywords
- methyl
- combination according
- pyrazol
- pharmaceutically acceptable
- solvate
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- SMWDFEZZVXVKRB-UHFFFAOYSA-N anhydrous quinoline Natural products N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- OLAHOMJCDNXHFI-UHFFFAOYSA-N n'-(3,5-dimethoxyphenyl)-n'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-n-propan-2-ylethane-1,2-diamine Chemical compound COC1=CC(OC)=CC(N(CCNC(C)C)C=2C=C3N=C(C=NC3=CC=2)C2=CN(C)N=C2)=C1 OLAHOMJCDNXHFI-UHFFFAOYSA-N 0.000 claims 3
- PEVJRHJJWVYDQB-UHFFFAOYSA-N n-(2-fluoro-3,5-dimethoxyphenyl)-n-(1h-imidazol-2-ylmethyl)-3-(1-methylpyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine Chemical compound COC1=CC(OC)=C(F)C(N(CC=2NC=CN=2)C=2N=C3N=C(C=NC3=CC=2)C2=CN(C)N=C2)=C1 PEVJRHJJWVYDQB-UHFFFAOYSA-N 0.000 claims 3
- KOAWAWHSMVKCON-UHFFFAOYSA-N 6-[difluoro-(6-pyridin-4-yl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]quinoline Chemical group C=1C=C2N=CC=CC2=CC=1C(F)(F)C(N1N=2)=NN=C1C=CC=2C1=CC=NC=C1 KOAWAWHSMVKCON-UHFFFAOYSA-N 0.000 claims 2
- JRWCBEOAFGHNNU-UHFFFAOYSA-N 6-[difluoro-[6-(1-methyl-4-pyrazolyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline Chemical group C1=NN(C)C=C1C1=NN2C(C(F)(F)C=3C=C4C=CC=NC4=CC=3)=NN=C2C=C1 JRWCBEOAFGHNNU-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- -1 1-methyl-1H-pyrazol-4-yl Chemical group 0.000 claims 1
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000000498 stomach carcinoma Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Classifications
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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
- A61K9/08—Solutions
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
Claims (16)
1. Комбинация первого соединения, выбранного из N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамина или его фармацевтически приемлемой соли или его сольвата и N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амина или его фармацевтически приемлемой соли или его сольвата; и второго соединения, которое является ингибитором cMet.
2. Комбинация по п.1, где первое соединение является N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамином или его фармацевтически приемлемой солью или его сольватом.
3. Комбинация по п.2, где первое соединение является N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамином в форме основания.
4. Комбинация по п.1, где первое соединение является N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амином или его фармацевтически приемлемой солью или его сольватом.
5. Комбинация по п.4, где первое соединение является N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амином в форме основания.
6. Комбинация по любому из предыдущих пунктов, где ингибитор cMet выбран из 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триа-золо[4,3-b]пиридазин-3-ил]метил}хинолина или его фармацевтически приемлемой соли или его сольвата и 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолина или его фармацевтически приемлемой соли или его сольвата.
7. Комбинация по п.6, где ингибитор cMet является 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триазоло[4,3-b]пиридазин-3-ил]метил}хинолином или его фармацевтически приемлемой солью или его сольватом.
8. Комбинация по п.7, где ингибитор cMet является 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триазоло[4,3-b]пиридазин-3-ил]метил}хинолином в форме основания.
9. Комбинация по п.6, где ингибитор cMet является 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолином или его фармацевтически приемлемой солью или его сольватом.
10. Комбинация по п.9, где ингибитор cMet является 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолином в форме основания.
11. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и комбинацию по любому из предыдущих пунктов.
12. Комбинация по любому из пп.1-10 или фармацевтическая композиция по п.11 для применения в качестве лекарственного средства.
13. Применение комбинации по любому из пп.1-10 или фармацевтической композиции по п.11 для производства лекарственного средства для профилактики или лечения, в частности лечения рака.
14. Способ профилактики или лечения рака, включающий введение субъекту, нуждающемуся в этом, комбинации по любому из пп.1-10 или фармацевтической композиции по п.11.
15. Применение по п.13 или способ по п.14 для лечения рака легкого, мочевого пузыря, молочной железы, желудка или гепатоцеллюлярного рака.
16. Фармацевтический продукт, включающий комбинацию по любому из пп.1-10 в качестве комбинированного препарата для одновременного, раздельного или последовательного применения в лечении рака.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14161835 | 2014-03-26 | ||
| EP14161835.5 | 2014-03-26 | ||
| PCT/EP2015/056512 WO2015144804A1 (en) | 2014-03-26 | 2015-03-26 | Combinations |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016141569A true RU2016141569A (ru) | 2018-04-26 |
| RU2016141569A3 RU2016141569A3 (ru) | 2018-11-02 |
| RU2715236C2 RU2715236C2 (ru) | 2020-02-26 |
Family
ID=50389857
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016141569A RU2715236C2 (ru) | 2014-03-26 | 2015-03-26 | Комбинации |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10085982B2 (ru) |
| EP (2) | EP3122358B1 (ru) |
| JP (2) | JP6752715B2 (ru) |
| KR (1) | KR102479693B1 (ru) |
| CN (1) | CN106458999B (ru) |
| AU (1) | AU2015238301B2 (ru) |
| BR (1) | BR112016022056B1 (ru) |
| CA (1) | CA2943682C (ru) |
| CY (1) | CY1123930T1 (ru) |
| DK (1) | DK3122358T3 (ru) |
| ES (1) | ES2856482T3 (ru) |
| HR (1) | HRP20210338T1 (ru) |
| HU (1) | HUE053654T2 (ru) |
| LT (1) | LT3122358T (ru) |
| MA (2) | MA55696A (ru) |
| MX (1) | MX370099B (ru) |
| PL (1) | PL3122358T3 (ru) |
| PT (1) | PT3122358T (ru) |
| RS (1) | RS61536B1 (ru) |
| RU (1) | RU2715236C2 (ru) |
| SI (1) | SI3122358T1 (ru) |
| WO (1) | WO2015144804A1 (ru) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| RU2715893C2 (ru) | 2014-03-26 | 2020-03-04 | Астекс Терапьютикс Лтд | Комбинации ингибитора fgfr и ингибитора igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| SI3353177T1 (sl) | 2015-09-23 | 2020-08-31 | Janssen Pharmaceutica Nv | Triciklični heterocikli za zdravljenje raka |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| EP3365335B1 (en) | 2015-10-23 | 2024-02-14 | Array Biopharma, Inc. | 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases |
| CN113490666A (zh) | 2018-12-19 | 2021-10-08 | 奥瑞生物药品公司 | 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
| AU2019451652A1 (en) * | 2019-06-17 | 2022-01-27 | Instytut Biologii Doswiadczalnej Im. Marcelego Nenckiego Polska Akademia Nauk | Use of marimastat for preventing and/or treating epileptogenesis |
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| SG11201702381QA (en) | 2014-09-26 | 2017-04-27 | Janssen Pharmaceutica Nv | Use of fgfr mutant gene panels in identifying cancer patients that will be responsive to treatment with an fgfr inhibitor |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| MX2017010595A (es) | 2015-02-19 | 2018-11-12 | Bioclin Therapeutics Inc | Métodos, composiciones, y equipos para tratamiento de cáncer. |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| CN105030777B (zh) | 2015-07-14 | 2017-07-21 | 中国人民解放军第三军医大学第三附属医院 | 增强alk‑tki疗效、延缓其耐药的复合物及其制剂 |
| CN105147687A (zh) | 2015-09-28 | 2015-12-16 | 青岛华之草医药科技有限公司 | 一种治疗白血病的药物达沙替尼组合物胶囊 |
| JOP20190280A1 (ar) | 2017-06-02 | 2019-12-02 | Janssen Pharmaceutica Nv | مثبطات fgfr2 لعلاج سرطان الأوعية الصفراوية |
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