RU2015132370A - Химические соединения - Google Patents
Химические соединения Download PDFInfo
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- RU2015132370A RU2015132370A RU2015132370A RU2015132370A RU2015132370A RU 2015132370 A RU2015132370 A RU 2015132370A RU 2015132370 A RU2015132370 A RU 2015132370A RU 2015132370 A RU2015132370 A RU 2015132370A RU 2015132370 A RU2015132370 A RU 2015132370A
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- compound
- pharmaceutically acceptable
- acceptable salt
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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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
- 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
- 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
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- 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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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/156—Polymorphic or mutational markers
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Pathology (AREA)
- Analytical Chemistry (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Hospice & Palliative Care (AREA)
- Microbiology (AREA)
- Molecular Biology (AREA)
- General Engineering & Computer Science (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (28)
1. Соединение формулы (I)
где R1 представляет собой метил или этил; и
R2 представляет собой (С2-3)алкил, замещенный группой гидрокси;
или его фармацевтически приемлемая соль.
2. Соединение по п. 1 или его фармацевтически приемлемая соль, где R2 выбран из групп (1)-(11):
3. Соединение по п. 2 или его фармацевтически приемлемая соль, где R2 выбран из групп (1)-(6), как они определены в п. 2.
4. Соединение по п. 3 или его фармацевтически приемлемая соль, где R2 представляет собой группу (1), как она определена в п. 2.
5. Соединение по п. 1 или его фармацевтически приемлемая соль, где R1 представляет собой метил.
6. Соединение по п. 1 или его фармацевтически приемлемая соль, где R1 представляет собой этил.
7. Соединение по п. 1 или его фармацевтически приемлемая соль, где соединение выбрано из:
1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-метил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-пропан-1-она;
1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-этил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-пропан-1-она;
(3R)-1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-метил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-бутан-1-она;
(3S)-1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-метил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-бутан-1-она;
(2R)-1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-метил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-2-метил-пропан-1-она;
1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-метил-1,2,4-триазол-3-ил]-1-пиперидил]-2-гидрокси-2-метил-пропан-1-она.
8. Соединение, представляющее собой 1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-этил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-пропан-1-он, или его фармацевтически приемлемая соль.
9. Соединение по п. 8, представляющее собой 1-[4-[5-[5-амино-6-(5-трет-бутил-1,3,4-оксадиазол-2-ил)пиразин-2-ил]-1-этил-1,2,4-триазол-3-ил]-1-пиперидил]-3-гидрокси-пропан-1-он.
10. Соединение по п. 1 или его фармацевтически приемлемая соль в кристаллической форме.
11. Соединение по п. 1 или его фармацевтически приемлемая соль для применения в качестве лекарственного средства.
12. Соединение по п. 1 или его фармацевтически приемлемая соль для применения в предупреждении или лечении рака у теплокровного животного, такого как человек.
13. Комбинация, подходящая для применения в лечении рака, содержащая соединение формулы (I) по п. 1 или его фармацевтически приемлемую соль и другой противоопухолевый агент.
14. Фармацевтическая композиция, содержащая соединение формулы (I) или его фармацевтически приемлемую соль по п. 1 и фармацевтически приемлемый разбавитель или носитель.
15. Способ отбора пациента для лечения соединением формулы (I), включающий получение от пациента образца, содержащего опухолевую ДНК или опухолевые клетки; определение того, является ли ген PIK3CA в опухолевых клетках пациента или в опухолевой ДНК пациента, геном дикого типа или мутантным геном; и на основании этого отбор пациента для лечения соединением формулы (I).
16. Способ лечения пациента, страдающего раковым заболеванием, включающий: получение содержащего опухолевые клетки образца от пациента; определение того, является ли ген PIK3CA в опухолевых клетках пациента геном дикого типа или мутантным геном; и введение пациенту эффективного количества соединения формулы (I) по п. 1, если опухолевые клетки содержат мутантный ген PIK3CA.
17. Соединение формулы (I) по п. 1 для лечения раковых заболеваний с опухолевыми клетками, идентифицированными как несущие мутантный ген PIK3CA.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13305078 | 2013-01-23 | ||
| EP13305078.1 | 2013-01-23 | ||
| PCT/GB2014/050163 WO2014114928A1 (en) | 2013-01-23 | 2014-01-22 | Chemical compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2015132370A true RU2015132370A (ru) | 2017-03-02 |
| RU2644769C2 RU2644769C2 (ru) | 2018-02-14 |
Family
ID=47623992
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015132370A RU2644769C2 (ru) | 2013-01-23 | 2014-01-22 | Химические соединения |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9156831B2 (ru) |
| EP (1) | EP2948447B1 (ru) |
| JP (1) | JP6307096B2 (ru) |
| KR (1) | KR102202516B1 (ru) |
| CN (1) | CN104936953B (ru) |
| AP (1) | AP2015008604A0 (ru) |
| AR (1) | AR094553A1 (ru) |
| AU (1) | AU2014208964B2 (ru) |
| BR (1) | BR112015017331B1 (ru) |
| CA (1) | CA2897279C (ru) |
| CL (1) | CL2015002027A1 (ru) |
| CR (1) | CR20150367A (ru) |
| DO (1) | DOP2015000170A (ru) |
| ES (1) | ES2608395T3 (ru) |
| HK (1) | HK1214592A1 (ru) |
| IL (1) | IL239890A0 (ru) |
| MA (1) | MA38287B1 (ru) |
| MX (1) | MX361136B (ru) |
| NI (1) | NI201500096A (ru) |
| PE (1) | PE20151979A1 (ru) |
| PH (1) | PH12015501584A1 (ru) |
| RU (1) | RU2644769C2 (ru) |
| SG (1) | SG11201505631PA (ru) |
| TN (1) | TN2015000313A1 (ru) |
| TW (1) | TWI606047B (ru) |
| UY (1) | UY35275A (ru) |
| WO (1) | WO2014114928A1 (ru) |
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| TW201726140A (zh) | 2015-09-17 | 2017-08-01 | 瑞典商阿斯特捷利康公司 | 治療癌症之新型生物標記及方法 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| CN107137405A (zh) * | 2017-04-14 | 2017-09-08 | 黄德莲 | 一种治疗肾炎的药物组合物 |
| CN110317190A (zh) * | 2018-03-28 | 2019-10-11 | 首都医科大学 | 一种***-羧酸酯类衍生物在医药领域的应用 |
| MX2021004775A (es) | 2018-11-05 | 2021-06-08 | Iovance Biotherapeutics Inc | Expansion de linfocitos infiltrantes de tumores (tils) usando inhibidores de la via de proteina cinasa b (akt). |
| WO2020094363A1 (en) | 2018-11-05 | 2020-05-14 | Syngenta Participations Ag | Pesticidally active azole-amide compounds |
| ES2953140T3 (es) | 2019-03-08 | 2023-11-08 | Syngenta Crop Protection Ag | Compuestos de azol-amida activos de manera plaguicida |
| EP3941912B1 (en) | 2019-03-20 | 2023-12-13 | Syngenta Crop Protection AG | Pesticidally active azole amide compounds |
| WO2020193341A1 (en) | 2019-03-22 | 2020-10-01 | Syngenta Crop Protection Ag | N-[1-(5-bromo-2-pyrimidin-2-yl-1,2,4-triazol-3-yl)ethyl]-2-cyclopropyl-6-(trifluoromethyl)pyridine-4-carboxamide derivatives and related compounds as insecticides |
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