EA200701233A1 - Производные хиназолина в качестве mtki - Google Patents
Производные хиназолина в качестве mtkiInfo
- Publication number
- EA200701233A1 EA200701233A1 EA200701233A EA200701233A EA200701233A1 EA 200701233 A1 EA200701233 A1 EA 200701233A1 EA 200701233 A EA200701233 A EA 200701233A EA 200701233 A EA200701233 A EA 200701233A EA 200701233 A1 EA200701233 A1 EA 200701233A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- hydrogen
- het
- optionally substituted
- alkyloxy group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- 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
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы (I), их N-оксидным формам, фармацевтически приемлемым аддитивным солям и стереохимически изомерным формам, где Z означает NH; Y означает -С-алкил-, -С-алкил-NR-С-алкил-, -C-алкил-NR-CO-C-алкил-, -С-алкил-NR-Н-СО-NH-С-алкил- или -C-алкил-NR-CO-CRR-NH-; Xозначает О или -О-С-алкил-; Xозначает прямую связь, C-алкил, -CO-C-алкил- или NR-C-алкил; Rозначает водород или галоген; Rозначает галоген, ацетилен или Het; Rозначает водород или цианогруппу; Rозначает Ar-С-алкилоксигруппу, C-алкилоксигруппу или C-алкилоксигруппу, замещенную одним или, в тех случаях, когда это возможно, двумя или более заместителями, выбранными из Het, NRR, гидроксигруппы и С-алкилокси-С-алкилоксигруппы; Rозначает водород или C-алкил; Rозначает C-алкил, замещенный NRRили C-алкилсульфонилом; Rозначает водород или C-алкил-; Rозначает Ar-сульфонил или C-алкилоксикарбонил, необязательно замещенный фенилом; Rи Rозначают водород, C-алкил или Rи R, вместе взятые с атомом углерода, с котором они связаны, образуют С-циклоалкил; Rозначает C-алкил и Rозначает водород в том случае, когда Rи R, вместе взятые с атомом углерода, с котором они связаны, образуют С-циклоалкил; R, R, Rи R, каждый независимо, означают водород или C-алкилкарбонил; Hetозначает 2-бора-1,3-диоксоланил; Hetозначает пиперидинил, пиперазинил, морфолинил, тиоморфолинил или 1,1-диоксотиоморфолинил, при этом указанный Hetнеобязательно замещен C-алкилоксикарбонилом или NRR-С-алкилом; Arи Arозначают фенил; Arозначает фенил, необязательно замещенный нитрогруппой.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US63422804P | 2004-12-08 | 2004-12-08 | |
EP04106383 | 2004-12-08 | ||
PCT/EP2005/056609 WO2006061417A2 (en) | 2004-12-08 | 2005-12-08 | Macrocyclic quinazole derivatives and their use as mtki |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200701233A1 true EA200701233A1 (ru) | 2007-10-26 |
EA013995B1 EA013995B1 (ru) | 2010-08-30 |
Family
ID=34930015
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200701233A EA013995B1 (ru) | 2004-12-08 | 2005-12-08 | Производные хиназолина в качестве mtki |
Country Status (22)
Country | Link |
---|---|
US (1) | US20100152174A1 (ru) |
EP (1) | EP1828201B1 (ru) |
JP (1) | JP5140431B2 (ru) |
KR (1) | KR101320431B1 (ru) |
CN (2) | CN101072781B (ru) |
AR (1) | AR051985A1 (ru) |
AU (1) | AU2005313350B2 (ru) |
BR (1) | BRPI0518394B8 (ru) |
CA (1) | CA2588764C (ru) |
DK (1) | DK1828201T3 (ru) |
EA (1) | EA013995B1 (ru) |
ES (1) | ES2559305T3 (ru) |
HU (1) | HUE027253T2 (ru) |
JO (1) | JO3088B1 (ru) |
MX (1) | MX2007006820A (ru) |
MY (1) | MY148503A (ru) |
NZ (1) | NZ555496A (ru) |
PA (1) | PA8654501A1 (ru) |
SI (1) | SI1828201T1 (ru) |
TW (2) | TWI511970B (ru) |
UA (1) | UA91522C2 (ru) |
WO (1) | WO2006061417A2 (ru) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
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PA8603801A1 (es) * | 2003-05-27 | 2004-12-16 | Janssen Pharmaceutica Nv | Derivados de la quinazolina |
ES2305887T3 (es) | 2003-12-18 | 2008-11-01 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidinas como agentes antiproliferativos. |
NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
US8492377B2 (en) * | 2006-07-13 | 2013-07-23 | Janssen Pharmaceutica Nv | MTKI quinazoline derivatives |
AU2007310843A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Macrocyclic quinazoline derivatives as VEGFR3 inhibitors |
AU2007310845A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of MTKI 1 for treating or preventing bone cancer |
DK2170827T3 (da) * | 2007-06-21 | 2013-11-18 | Janssen Pharmaceutica Nv | Indolin-2-oner og aza-indolin-2-oner |
WO2009016132A1 (en) * | 2007-07-27 | 2009-02-05 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
EP2350075B1 (en) | 2008-09-22 | 2014-03-05 | Array Biopharma, Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
ES2669581T7 (es) | 2008-10-22 | 2020-07-29 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirimidina como inhibidores de TRK quinasa |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
ES2628418T3 (es) | 2010-05-20 | 2017-08-02 | Array Biopharma, Inc. | Compuestos macrocíclicos como inhibidores de la TRK cinasa |
JP6382997B2 (ja) * | 2014-02-07 | 2018-08-29 | エクセセーラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物および組成物 |
MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
MA39822A (fr) | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
TWI746426B (zh) | 2014-11-16 | 2021-11-21 | 美商亞雷生物製藥股份有限公司 | (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型 |
KR20180102544A (ko) | 2015-10-26 | 2018-09-17 | 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 | Trk 억제제-내성 암에서의 점 돌연변이 및 이의 관련 방법 |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
PE20181888A1 (es) | 2016-04-04 | 2018-12-11 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
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-
2005
- 2005-11-28 JO JOP/2005/0188A patent/JO3088B1/ar active
- 2005-12-05 PA PA20058654501A patent/PA8654501A1/es unknown
- 2005-12-06 MY MYPI20055704A patent/MY148503A/en unknown
- 2005-12-07 TW TW102141302A patent/TWI511970B/zh active
- 2005-12-07 TW TW094143060A patent/TWI432440B/zh active
- 2005-12-07 AR ARP050105124A patent/AR051985A1/es not_active Application Discontinuation
- 2005-12-08 BR BRPI0518394A patent/BRPI0518394B8/pt active IP Right Grant
- 2005-12-08 JP JP2007544918A patent/JP5140431B2/ja active Active
- 2005-12-08 EP EP05826362.5A patent/EP1828201B1/en active Active
- 2005-12-08 WO PCT/EP2005/056609 patent/WO2006061417A2/en active Application Filing
- 2005-12-08 CA CA2588764A patent/CA2588764C/en active Active
- 2005-12-08 MX MX2007006820A patent/MX2007006820A/es active IP Right Grant
- 2005-12-08 CN CN2005800420435A patent/CN101072781B/zh active Active
- 2005-12-08 DK DK05826362.5T patent/DK1828201T3/en active
- 2005-12-08 CN CN201110392750.4A patent/CN102532163B/zh active Active
- 2005-12-08 US US11/720,693 patent/US20100152174A1/en not_active Abandoned
- 2005-12-08 HU HUE05826362A patent/HUE027253T2/en unknown
- 2005-12-08 AU AU2005313350A patent/AU2005313350B2/en active Active
- 2005-12-08 UA UAA200705396A patent/UA91522C2/ru unknown
- 2005-12-08 KR KR1020077013133A patent/KR101320431B1/ko active IP Right Grant
- 2005-12-08 ES ES05826362.5T patent/ES2559305T3/es active Active
- 2005-12-08 EA EA200701233A patent/EA013995B1/ru not_active IP Right Cessation
- 2005-12-08 SI SI200532035T patent/SI1828201T1/sl unknown
- 2005-12-08 NZ NZ555496A patent/NZ555496A/en unknown
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