EA200300265A1 - Производные хиназолина в качестве ингибиторов киназы - Google Patents
Производные хиназолина в качестве ингибиторов киназыInfo
- Publication number
- EA200300265A1 EA200300265A1 EA200300265A EA200300265A EA200300265A1 EA 200300265 A1 EA200300265 A1 EA 200300265A1 EA 200300265 A EA200300265 A EA 200300265A EA 200300265 A EA200300265 A EA 200300265A EA 200300265 A1 EA200300265 A1 EA 200300265A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- phosphorylation
- kinases
- inhibit
- nitrogen
- pharmaceutically acceptable
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 3
- 230000026731 phosphorylation Effects 0.000 abstract 3
- 238000006366 phosphorylation reaction Methods 0.000 abstract 3
- 102000020233 phosphotransferase Human genes 0.000 abstract 3
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- -1 nitrogen-containing heterocyclic compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 230000002792 vascular Effects 0.000 abstract 2
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 102000009465 Growth Factor Receptors Human genes 0.000 abstract 1
- 108010009202 Growth Factor Receptors Proteins 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 206010061989 glomerulosclerosis Diseases 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
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- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- 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
Abstract
Настоящее изобретение относится к азотсодержащим гетероциклическим соединениям и их фармацевтически приемлемым солям, которые обладают ингибирующей активностью в отношении фосфорилирования киназ, ингибирующего активность последних. Изобретение относится также к способу ингибирования киназ и лечению болезненных состояний у млекопитающих путем ингибирования фосфорилирования киназ. Особым аспектом настоящего изобретения является обеспечение азотсодержащих гетероциклических соединений и их фармацевтически приемлемых солей, которые ингибируют фосфорилирование рецептора фактора роста из тромбоцитов, для торможения аномального клеточного роста и клеточного блуждания и способ предотвращения или лечения клеточно-пролиферативных заболеваний, таких как артериосклероз, васкулярная реобструкция, рак и гломерулосклероз.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22612200P | 2000-08-18 | 2000-08-18 | |
PCT/US2001/041752 WO2002016351A1 (en) | 2000-08-18 | 2001-08-17 | Quinazoline derivatives as kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200300265A1 true EA200300265A1 (ru) | 2003-12-25 |
EA005809B1 EA005809B1 (ru) | 2005-06-30 |
Family
ID=22847639
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200300265A EA005809B1 (ru) | 2000-08-18 | 2001-08-17 | Производные хиназолина в качестве ингибиторов киназы |
Country Status (25)
Country | Link |
---|---|
US (5) | US6982266B2 (ru) |
EP (3) | EP2277877A1 (ru) |
JP (1) | JP5073147B2 (ru) |
KR (1) | KR100831116B1 (ru) |
CN (1) | CN100358890C (ru) |
AT (1) | ATE402169T1 (ru) |
AU (1) | AU8544901A (ru) |
BR (1) | BR0113356A (ru) |
CA (1) | CA2426440C (ru) |
CY (1) | CY1110460T1 (ru) |
CZ (1) | CZ304061B6 (ru) |
DE (1) | DE60134990D1 (ru) |
DK (1) | DK1315715T3 (ru) |
EA (1) | EA005809B1 (ru) |
ES (1) | ES2311023T3 (ru) |
HK (1) | HK1057206A1 (ru) |
HU (1) | HU228668B1 (ru) |
IL (2) | IL154514A0 (ru) |
MX (1) | MXPA03001359A (ru) |
NO (1) | NO323782B1 (ru) |
NZ (1) | NZ524461A (ru) |
PT (1) | PT1315715E (ru) |
SI (1) | SI1315715T1 (ru) |
WO (1) | WO2002016351A1 (ru) |
ZA (1) | ZA200301510B (ru) |
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BR0113356A (pt) * | 2000-08-18 | 2004-04-20 | Millennium Pharm Inc | Derivados de quinazolina como inibidores de quinase |
DE60143204D1 (de) | 2000-08-18 | 2010-11-18 | Kyowa Hakko Kirin Co Ltd | N-aryl-ä4-Ä7-(alkoxy)Chinazolin-4-ylÜPiperazinylüCarboxamid-Verbindungen als PDGF-Rezeptoren Hemmer |
AU2001293208A1 (en) | 2000-08-18 | 2002-03-04 | Cor Therapeutics, Inc. | Nitrogenous heterocyclic compounds |
JP4564713B2 (ja) * | 2000-11-01 | 2010-10-20 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 窒素性複素環式化合物、ならびに窒素性複素環式化合物およびその中間体を作製するための方法 |
EP1490362A2 (en) | 2001-03-08 | 2004-12-29 | Millennium Pharmaceuticals, Inc. | (homo)piperazine substituted quinolines for inhibiting the phosphorylation of kinases |
CA2470480C (en) | 2001-12-27 | 2010-12-14 | Theravance, Inc. | Indolinone derivatives useful as protein kinase inhibitors |
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WO2007012042A1 (en) * | 2005-07-20 | 2007-01-25 | Millennium Pharmaceuticals, Inc. | New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide |
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UA95641C2 (en) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
WO2008053270A2 (en) * | 2006-10-31 | 2008-05-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of an egfr antagonist for the treatment of glomerolonephritis |
JP5250901B2 (ja) * | 2007-02-23 | 2013-07-31 | 学校法人慶應義塾 | アニリノキナゾリン系化合物及びその用途 |
US7998966B2 (en) | 2007-04-13 | 2011-08-16 | Supergen, Inc. | Axl kinase inhibitors |
WO2010059239A2 (en) | 2008-11-21 | 2010-05-27 | Millennium Pharmaceuticals, Inc | Lactate salt of 4-(6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders |
US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
CN102942529B (zh) * | 2012-11-09 | 2015-06-24 | 贵州大学 | 4-(4-取代哌嗪)-5,6,7-三烷氧基喹唑啉类化合物及其制备方法和应用 |
US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
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WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
CN106083715A (zh) * | 2016-06-01 | 2016-11-09 | 谢阳 | 一种喹啉、喹唑啉类化合物及其药物组合物和应用 |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
JP2019534260A (ja) | 2016-10-07 | 2019-11-28 | アラクセス ファーマ エルエルシー | Rasの阻害剤としての複素環式化合物およびその使用方法 |
WO2018140514A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
BR112019024674A2 (pt) | 2017-05-25 | 2020-06-16 | Araxes Pharma Llc | Inibidores covalentes da kras |
TW201906832A (zh) | 2017-05-25 | 2019-02-16 | 美商亞瑞克西斯製藥公司 | 用於癌症治療之化合物及其使用方法 |
US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
SG11202009443RA (en) | 2018-04-05 | 2020-10-29 | Sumitomo Dainippon Pharma Oncology Inc | Axl kinase inhibitors and use of the same |
CN108570039B (zh) * | 2018-04-25 | 2022-09-23 | 上海美迪西生物医药股份有限公司 | 一类具有抑制抗凋亡蛋白活性的化合物及其制备和应用 |
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CN115108999B (zh) * | 2019-07-26 | 2023-11-03 | 暨南大学 | 一种苯基哌嗪喹唑啉类化合物或其药学上可接受的盐、制法与用途 |
CN111773440A (zh) * | 2020-05-22 | 2020-10-16 | 南京大学 | 一种基于类酶催化反应的抗凝血材料 |
WO2023081923A1 (en) | 2021-11-08 | 2023-05-11 | Frequency Therapeutics, Inc. | Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof |
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TW225528B (ru) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
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DE60143204D1 (de) | 2000-08-18 | 2010-11-18 | Kyowa Hakko Kirin Co Ltd | N-aryl-ä4-Ä7-(alkoxy)Chinazolin-4-ylÜPiperazinylüCarboxamid-Verbindungen als PDGF-Rezeptoren Hemmer |
BR0113356A (pt) * | 2000-08-18 | 2004-04-20 | Millennium Pharm Inc | Derivados de quinazolina como inibidores de quinase |
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2001
- 2001-08-17 BR BR0113356-0A patent/BR0113356A/pt active Search and Examination
- 2001-08-17 US US10/344,736 patent/US6982266B2/en not_active Expired - Fee Related
- 2001-08-17 NZ NZ52446101A patent/NZ524461A/xx not_active IP Right Cessation
- 2001-08-17 CZ CZ20030765A patent/CZ304061B6/cs not_active IP Right Cessation
- 2001-08-17 AT AT01964612T patent/ATE402169T1/de active
- 2001-08-17 HU HU0302615A patent/HU228668B1/hu not_active IP Right Cessation
- 2001-08-17 EP EP10182322A patent/EP2277877A1/en not_active Withdrawn
- 2001-08-17 IL IL15451401A patent/IL154514A0/xx active IP Right Grant
- 2001-08-17 EP EP08075237A patent/EP1964839A3/en not_active Ceased
- 2001-08-17 CN CNB018173527A patent/CN100358890C/zh not_active Expired - Fee Related
- 2001-08-17 DE DE60134990T patent/DE60134990D1/de not_active Expired - Lifetime
- 2001-08-17 JP JP2002521452A patent/JP5073147B2/ja not_active Expired - Fee Related
- 2001-08-17 KR KR1020037002381A patent/KR100831116B1/ko not_active IP Right Cessation
- 2001-08-17 DK DK01964612T patent/DK1315715T3/da active
- 2001-08-17 CA CA2426440A patent/CA2426440C/en not_active Expired - Fee Related
- 2001-08-17 AU AU8544901A patent/AU8544901A/xx active Pending
- 2001-08-17 EP EP01964612A patent/EP1315715B1/en not_active Expired - Lifetime
- 2001-08-17 EA EA200300265A patent/EA005809B1/ru not_active IP Right Cessation
- 2001-08-17 ES ES01964612T patent/ES2311023T3/es not_active Expired - Lifetime
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2003
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- 2003-02-18 IL IL154514A patent/IL154514A/en not_active IP Right Cessation
- 2003-02-26 ZA ZA200301510A patent/ZA200301510B/en unknown
- 2003-11-28 HK HK03108720A patent/HK1057206A1/xx not_active IP Right Cessation
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2005
- 2005-08-22 US US11/210,028 patent/US7560461B2/en not_active Expired - Fee Related
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2008
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2009
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2012
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2014
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