EA201100794A1 - Замещенные пиримидины, предназначенные для лечения заболеваний, таких как рак - Google Patents
Замещенные пиримидины, предназначенные для лечения заболеваний, таких как ракInfo
- Publication number
- EA201100794A1 EA201100794A1 EA201100794A EA201100794A EA201100794A1 EA 201100794 A1 EA201100794 A1 EA 201100794A1 EA 201100794 A EA201100794 A EA 201100794A EA 201100794 A EA201100794 A EA 201100794A EA 201100794 A1 EA201100794 A1 EA 201100794A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- treatment
- diseases
- cancer
- intended
- substituted pyrimidines
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
В заявке описаны соединения общей формулы (1)в которой значения А, В, X, R-Rопределены в п.1 формулы изобретения, которые применимы для лечения заболеваний, характеризующихся чрезмерной или аномальной пролиферацией клеток, и их применение для приготовления лекарственного средства, обладающего указанными выше характеристиками.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08169807 | 2008-11-24 | ||
EP09169654 | 2009-09-07 | ||
PCT/EP2009/065768 WO2010058032A2 (en) | 2008-11-24 | 2009-11-24 | New compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201100794A1 true EA201100794A1 (ru) | 2012-01-30 |
EA021997B1 EA021997B1 (ru) | 2015-10-30 |
Family
ID=42115425
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201100794A EA021997B1 (ru) | 2008-11-24 | 2009-11-24 | Замещенные пиримидины, предназначенные для лечения заболеваний, таких как рак |
Country Status (26)
Country | Link |
---|---|
US (4) | US8846689B2 (ru) |
EP (1) | EP2367800B9 (ru) |
JP (1) | JP5622740B2 (ru) |
KR (1) | KR101710058B1 (ru) |
CN (2) | CN104478865B (ru) |
AP (1) | AP2960A (ru) |
AR (1) | AR074210A1 (ru) |
AU (1) | AU2009317170B2 (ru) |
BR (1) | BRPI0922801B1 (ru) |
CA (1) | CA2744351C (ru) |
CL (1) | CL2011001215A1 (ru) |
CO (1) | CO6511283A2 (ru) |
EA (1) | EA021997B1 (ru) |
EC (1) | ECSP11011079A (ru) |
ES (1) | ES2664499T3 (ru) |
GE (1) | GEP20146072B (ru) |
IL (1) | IL212814B (ru) |
MA (1) | MA32811B1 (ru) |
MX (1) | MX337116B (ru) |
MY (1) | MY176944A (ru) |
NZ (1) | NZ592925A (ru) |
PE (1) | PE20120034A1 (ru) |
TN (1) | TN2011000259A1 (ru) |
TW (1) | TWI491605B (ru) |
UY (1) | UY32259A (ru) |
WO (1) | WO2010058032A2 (ru) |
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TWI491605B (zh) | 2008-11-24 | 2015-07-11 | Boehringer Ingelheim Int | 新穎化合物 |
TW201024281A (en) | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
EP2464633A1 (en) | 2009-08-14 | 2012-06-20 | Boehringer Ingelheim International GmbH | Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives |
US20120244141A1 (en) | 2010-09-28 | 2012-09-27 | Boehringer Ingelheim International Gmbh | Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors |
DK2675794T3 (da) * | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
CA2827171C (en) | 2011-02-17 | 2019-04-09 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
US9187453B2 (en) | 2012-03-28 | 2015-11-17 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
EP3417852B1 (en) * | 2013-09-09 | 2020-02-19 | Peloton Therapeutics, Inc. | Aryl ethers and uses thereof |
US10155726B2 (en) | 2015-03-11 | 2018-12-18 | Peloton Therapeutics, Inc. | Substituted pyridines and uses thereof |
WO2016144825A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Aromatic compounds and uses thereof |
WO2016145045A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Compositions for use in treating glioblastoma |
WO2016145032A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Compositions for use in treating pulmonary arterial hypertension |
US10335388B2 (en) | 2015-04-17 | 2019-07-02 | Peloton Therapeutics, Inc. | Combination therapy of a HIF-2-alpha inhibitor and an immunotherapeutic agent and uses thereof |
US20170066778A1 (en) * | 2015-09-04 | 2017-03-09 | Aunova Medchem LLC | Solubility for target compounds |
KR20220101677A (ko) | 2019-11-18 | 2022-07-19 | 인엑스메드 (난징) 컴퍼니 리미티드 | Nras 돌연변이를 갖는 종양을 치료하기 위한 약물의 제조에서의 fak 억제제의 용도 |
CN114728005A (zh) * | 2019-11-28 | 2022-07-08 | 应世生物科技(南京)有限公司 | Bi853520在癌症治疗中的用途 |
CN117599060A (zh) * | 2020-02-05 | 2024-02-27 | 应世生物科技(南京)有限公司 | Bi853520与化疗药物的联用 |
AU2021323235A1 (en) * | 2020-08-03 | 2023-03-02 | Inxmed (Nanjing) Co., Ltd. | Solid form of compound |
TW202313044A (zh) | 2021-08-16 | 2023-04-01 | 大陸商應世生物科技(南京)有限公司 | In10018與pld的聯用 |
US20250049828A1 (en) | 2021-12-10 | 2025-02-13 | Inxmed (Nanjing) Co., Ltd. | Pharmaceutical composition for treating tumors and use |
WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
AU2022422848A1 (en) * | 2021-12-21 | 2024-06-13 | Wigen Biomedicine Technology (shanghai) Co., Ltd. | Compound as fak inhibitor and use thereof |
CN118574825A (zh) * | 2022-02-28 | 2024-08-30 | 微境生物医药科技(上海)有限公司 | 作为fak抑制剂的化合物及其用途 |
CN119343139A (zh) * | 2022-06-24 | 2025-01-21 | 应世生物科技(南京)有限公司 | 治疗肿瘤的药物组合及用途 |
CN117462553A (zh) * | 2022-07-20 | 2024-01-30 | 益方生物科技(上海)股份有限公司 | 药物组合产品以及组合疗法 |
EP4578449A1 (en) * | 2022-08-24 | 2025-07-02 | Inxmed (Nanjing) Co., Ltd. | Pharmaceutical combination of fak inhibitor and microtubule inhibitor and use thereof |
CN118580221A (zh) * | 2023-03-02 | 2024-09-03 | 应世生物科技(南京)有限公司 | 化合物的固体形式 |
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GB9705361D0 (en) * | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
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GB0004890D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0004886D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
EP2090571B1 (de) | 2001-10-17 | 2012-05-16 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung |
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MY147449A (en) | 2003-08-15 | 2012-12-14 | Novartis Ag | 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders |
EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
US7521457B2 (en) * | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
GB0419160D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
KR20070057798A (ko) | 2004-09-30 | 2007-06-07 | 티보텍 파마슈티칼즈 리미티드 | Hiv를 저해하는 5-탄소환 또는 복소환으로 치환된피리미딘 |
JP2008526997A (ja) | 2005-01-14 | 2008-07-24 | ニューロジェン・コーポレーション | ヘテロアリール置換キノリン−4−イルアミン類縁体 |
US20070032514A1 (en) | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
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2009
- 2009-11-23 TW TW098139766A patent/TWI491605B/zh active
- 2009-11-23 AR ARP090104511A patent/AR074210A1/es not_active Application Discontinuation
- 2009-11-24 AP AP2011005706A patent/AP2960A/xx active
- 2009-11-24 GE GEAP200912270A patent/GEP20146072B/en unknown
- 2009-11-24 UY UY0001032259A patent/UY32259A/es not_active Application Discontinuation
- 2009-11-24 KR KR1020117014264A patent/KR101710058B1/ko active Active
- 2009-11-24 ES ES09756513.9T patent/ES2664499T3/es active Active
- 2009-11-24 MX MX2011005420A patent/MX337116B/es active IP Right Grant
- 2009-11-24 EA EA201100794A patent/EA021997B1/ru not_active IP Right Cessation
- 2009-11-24 WO PCT/EP2009/065768 patent/WO2010058032A2/en active Application Filing
- 2009-11-24 JP JP2011536901A patent/JP5622740B2/ja active Active
- 2009-11-24 CA CA2744351A patent/CA2744351C/en active Active
- 2009-11-24 NZ NZ592925A patent/NZ592925A/xx unknown
- 2009-11-24 CN CN201410635154.8A patent/CN104478865B/zh active Active
- 2009-11-24 BR BRPI0922801-2A patent/BRPI0922801B1/pt active IP Right Grant
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