RU2011102797A - Противоопухолевые комбинации из 4-анилино-3-цианохинолинов и капецитабина - Google Patents
Противоопухолевые комбинации из 4-анилино-3-цианохинолинов и капецитабина Download PDFInfo
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- RU2011102797A RU2011102797A RU2011102797/15A RU2011102797A RU2011102797A RU 2011102797 A RU2011102797 A RU 2011102797A RU 2011102797/15 A RU2011102797/15 A RU 2011102797/15A RU 2011102797 A RU2011102797 A RU 2011102797A RU 2011102797 A RU2011102797 A RU 2011102797A
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- treatment regimen
- capecitabine
- administered
- hki
- compound
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- 230000000259 anti-tumor effect Effects 0.000 title 1
- 238000011269 treatment regimen Methods 0.000 claims abstract 38
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims abstract 21
- 229960004117 capecitabine Drugs 0.000 claims abstract 21
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims abstract 18
- 229950008835 neratinib Drugs 0.000 claims abstract 17
- -1 4-anilino-3-cyanoquinoline compound Chemical class 0.000 claims abstract 15
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims abstract 11
- 206010028980 Neoplasm Diseases 0.000 claims abstract 10
- 206010006187 Breast cancer Diseases 0.000 claims abstract 7
- 208000035269 cancer or benign tumor Diseases 0.000 claims abstract 6
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract 5
- IYLIRRZCLARWKQ-UHFFFAOYSA-N 4-anilinoquinoline-3-carbonitrile Chemical class N#CC1=CN=C2C=CC=CC2=C1NC1=CC=CC=C1 IYLIRRZCLARWKQ-UHFFFAOYSA-N 0.000 claims abstract 2
- 206010055113 Breast cancer metastatic Diseases 0.000 claims abstract 2
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims abstract 2
- 239000002145 L01XE14 - Bosutinib Substances 0.000 claims abstract 2
- 229960003736 bosutinib Drugs 0.000 claims abstract 2
- UBPYILGKFZZVDX-UHFFFAOYSA-N bosutinib Chemical compound C1=C(Cl)C(OC)=CC(NC=2C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=CC=2C#N)=C1Cl UBPYILGKFZZVDX-UHFFFAOYSA-N 0.000 claims abstract 2
- 229960001433 erlotinib Drugs 0.000 claims abstract 2
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims abstract 2
- 241000124008 Mammalia Species 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000011282 treatment Methods 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- 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
- A61K31/4709—Non-condensed quinolines 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
- A61K31/496—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
1. Применение 4-анилино-3-цианохинолинового соединения, выбранного из нератиниба, босутиниба и эрлотиниба, и капецитабина в комбинированной схеме лечения новообразования. ! 2. Схема лечения по п.1, где новообразование представляет собой рак молочной железы. ! 3. Схема лечения по п.1, где рак молочной железы выбран из Erb-2-положительного метастатического рака молочной железы и местно распространенного рака молочной железы. ! 4. Схема лечения по п.1, где новообразование представляет собой Erb-2-положительную солидную опухоль. ! 5. Схема лечения по п.1, где один или оба активных компонента предложены в субтерапевтически эффективном количестве. ! 6. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение и капецитабин доставляют перорально. ! 7. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение и капецитабин вводят одновременно последовательно, раздельно, в указанном порядке или в соответствии с конкретными временными отношениями. ! 8. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение вводят в однократной дозе. ! 9. Схема лечения по п.1, где указанное соединение капецитабин вводят в однократной дозе. ! 10. Схема лечения по п.1, где капецитабин вводят в количестве от примерно 1250 мг до примерно 3000 мг в сутки. ! 11. Схема лечения по любому из пп.1-10, где капецитабин вводят по меньшей мере один раз в течение 21 суток. ! 12. Схема лечения по п.11, где схема введения капецитабина продолжается от 3 до 6 циклов. ! 13. Схема лечения по п.1, где HKI-272 вводят в количестве по меньшей мере примерно 40 мг. ! 14. Схема лечения по п.13, где HKI-272 вводят в количестве по меньшей мере примерно 120 мг. ! 15. Схема лечения по п.14, где HKI-272 вводят в ко�
Claims (25)
1. Применение 4-анилино-3-цианохинолинового соединения, выбранного из нератиниба, босутиниба и эрлотиниба, и капецитабина в комбинированной схеме лечения новообразования.
2. Схема лечения по п.1, где новообразование представляет собой рак молочной железы.
3. Схема лечения по п.1, где рак молочной железы выбран из Erb-2-положительного метастатического рака молочной железы и местно распространенного рака молочной железы.
4. Схема лечения по п.1, где новообразование представляет собой Erb-2-положительную солидную опухоль.
5. Схема лечения по п.1, где один или оба активных компонента предложены в субтерапевтически эффективном количестве.
6. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение и капецитабин доставляют перорально.
7. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение и капецитабин вводят одновременно последовательно, раздельно, в указанном порядке или в соответствии с конкретными временными отношениями.
8. Схема лечения по п.1, где 4-анилино-3-цианохинолиновое соединение вводят в однократной дозе.
9. Схема лечения по п.1, где указанное соединение капецитабин вводят в однократной дозе.
10. Схема лечения по п.1, где капецитабин вводят в количестве от примерно 1250 мг до примерно 3000 мг в сутки.
11. Схема лечения по любому из пп.1-10, где капецитабин вводят по меньшей мере один раз в течение 21 суток.
12. Схема лечения по п.11, где схема введения капецитабина продолжается от 3 до 6 циклов.
13. Схема лечения по п.1, где HKI-272 вводят в количестве по меньшей мере примерно 40 мг.
14. Схема лечения по п.13, где HKI-272 вводят в количестве по меньшей мере примерно 120 мг.
15. Схема лечения по п.14, где HKI-272 вводят в количестве по меньшей мере примерно 240 мг.
16. Схема лечения по п.1, где указанное соединение HKI-272 вводят ежесуточно.
17. Схема лечения по п.1, где указанное соединение HKI-272 вводят по меньшей мере один раз в сутки.
18. Схема лечения по п.1, где указанное соединение HKI-272 вводят по меньшей мере в течение 2 непрерывных недель.
19. Схема лечения по п.1, где соединение HKI-272 вводят до указанного соединения капецитабина.
20. Схема лечения по п.1, где соединение HKI-272 вводят после капецитабина.
21. Схема лечения по п.1, где соединение HKI-272 и капецитабин вводят одновременно.
22. Схема лечения по п.1, где введение капецитабина прекращают через примерно 24 недели.
23. Схема лечения рака молочной железы, где один цикл указанной схемы введения составляет 21 сутки, и указанная схема включает:
(а) пероральное введение по меньшей мере одной однократной дозы HKI-272 ежесуточно, начиная с первых суток указанного цикла; и
(б) пероральное введение по меньшей мере одной однократной дозы капецитабина на 1-14 сутки указанного цикла.
24. Продукт, содержащий капецитабин, HKI-272 и по меньшей мере один фармацевтически приемлемый носитель, для одновременного, раздельного или последовательного введения в комбинированной схеме введения для лечения новообразования у млекопитающего.
25. Фармацевтический набор для лечения новообразования у одного отдельного млекопитающего, включающий:
(а) по меньшей мере одну однократную дозу капецитабина и
(б) по меньшей мере одну однократную дозу HKI-272.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8591308P | 2008-08-04 | 2008-08-04 | |
US61/085,913 | 2008-08-04 | ||
US17246609P | 2009-04-24 | 2009-04-24 | |
US61/172,466 | 2009-04-24 | ||
PCT/US2009/052644 WO2010017163A1 (en) | 2008-08-04 | 2009-08-04 | Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine |
Publications (2)
Publication Number | Publication Date |
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RU2011102797A true RU2011102797A (ru) | 2012-09-10 |
RU2498804C2 RU2498804C2 (ru) | 2013-11-20 |
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RU2011102797/15A RU2498804C2 (ru) | 2008-08-04 | 2009-08-04 | Противоопухолевые комбинации из 4-анилино-3-цианохинолинов и капецитабина |
Country Status (26)
Country | Link |
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US (2) | US8669273B2 (ru) |
EP (2) | EP3175853B1 (ru) |
JP (1) | JP5681108B2 (ru) |
KR (2) | KR101434009B1 (ru) |
CN (6) | CN102202667A (ru) |
AU (1) | AU2009279771B2 (ru) |
BR (1) | BRPI0916694B1 (ru) |
CA (1) | CA2730715C (ru) |
CY (1) | CY1118602T1 (ru) |
DK (1) | DK2326329T3 (ru) |
ES (2) | ES2614912T3 (ru) |
HK (1) | HK1218262A1 (ru) |
HR (1) | HRP20170074T1 (ru) |
HU (1) | HUE032958T2 (ru) |
IL (1) | IL210616A (ru) |
LT (1) | LT2326329T (ru) |
MX (1) | MX2011001318A (ru) |
NZ (1) | NZ590464A (ru) |
PL (2) | PL3175853T3 (ru) |
PT (1) | PT2326329T (ru) |
RU (1) | RU2498804C2 (ru) |
SG (2) | SG10201702382RA (ru) |
SI (1) | SI2326329T1 (ru) |
SM (1) | SMT201700084B (ru) |
WO (1) | WO2010017163A1 (ru) |
ZA (1) | ZA201101662B (ru) |
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WO2007056118A1 (en) | 2005-11-04 | 2007-05-18 | Wyeth | Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272 |
US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
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