CN102695700A - 用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 - Google Patents
用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 Download PDFInfo
- Publication number
- CN102695700A CN102695700A CN201080054924XA CN201080054924A CN102695700A CN 102695700 A CN102695700 A CN 102695700A CN 201080054924X A CN201080054924X A CN 201080054924XA CN 201080054924 A CN201080054924 A CN 201080054924A CN 102695700 A CN102695700 A CN 102695700A
- Authority
- CN
- China
- Prior art keywords
- methyl
- group
- methoxy
- benzamide
- ylamino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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Classifications
-
- 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
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09172026.8 | 2009-10-02 | ||
| EP09172026 | 2009-10-02 | ||
| EP10172460 | 2010-08-11 | ||
| EP10172460.7 | 2010-08-11 | ||
| PCT/EP2010/064628 WO2011039344A1 (en) | 2009-10-02 | 2010-10-01 | Pyrimidine derivatives as protein tyrosine kinase 2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102695700A true CN102695700A (zh) | 2012-09-26 |
Family
ID=43048878
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080054924XA Pending CN102695700A (zh) | 2009-10-02 | 2010-10-01 | 用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 |
Country Status (25)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120244141A1 (en) | 2010-09-28 | 2012-09-27 | Boehringer Ingelheim International Gmbh | Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2012110774A1 (en) | 2011-02-17 | 2012-08-23 | Cancer Therapeutics Crc Pty Limited | Selective fak inhibitors |
| US20130324532A1 (en) | 2011-02-17 | 2013-12-05 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
| JP2015502958A (ja) * | 2011-12-09 | 2015-01-29 | オンコメッド ファーマシューティカルズ インコーポレイテッド | がんの処置のための併用療法 |
| WO2013146963A1 (ja) * | 2012-03-28 | 2013-10-03 | 武田薬品工業株式会社 | 複素環化合物 |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| ES2657451T3 (es) | 2013-04-19 | 2018-03-05 | Incyte Holdings Corporation | Heterocíclicos bicíclicos como inhibidores del FGFR |
| CA2949048A1 (en) | 2013-05-22 | 2014-11-27 | The Regents Of The University Of California | Aurora kinase inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| CN107438607B (zh) | 2015-02-20 | 2021-02-05 | 因赛特公司 | 作为fgfr抑制剂的双环杂环 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| JP7568512B2 (ja) | 2018-05-04 | 2024-10-16 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤の塩 |
| FI3788047T3 (fi) | 2018-05-04 | 2024-11-02 | Incyte Corp | Fgft-estäjän kiinteitä muotoja ja menetelmiä niiden valmistamiseksi |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| TW202313611A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1416423A (zh) * | 2000-03-01 | 2003-05-07 | 阿斯特拉曾尼卡有限公司 | 用作抗肿瘤剂的2,4－二(杂－)芳基氨基(－氧基)－5－取代的嘧啶 |
| WO2004058144A2 (en) * | 2002-12-18 | 2004-07-15 | Glaxo Group Limited | Antibacterial agents |
| CN1633419A (zh) * | 2001-05-29 | 2005-06-29 | 舍林股份公司 | Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用 |
| WO2008038011A1 (en) * | 2006-09-30 | 2008-04-03 | Vernalis (R & D) Limited | Pyrimidine derivatives as aurora a and aurora b inhibitors |
| CN101213179A (zh) * | 2005-07-01 | 2008-07-02 | 贝林格尔·英格海姆国际有限公司 | 用作Aurora抑制剂的2,4-二氨基-嘧啶类化合物 |
| WO2008128231A1 (en) * | 2007-04-16 | 2008-10-23 | Hutchison Medipharma Enterprises Limited | Pyrimidine derivatives |
| CN101346380A (zh) * | 2005-12-21 | 2009-01-14 | 辉瑞产品公司 | 用于治疗异常细胞生长的嘧啶衍生物 |
| CN101511836A (zh) * | 2006-07-06 | 2009-08-19 | 阿斯利康(瑞典)有限公司 | 稠合的嘧啶并化合物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1438053B1 (de) | 2001-10-17 | 2008-09-10 | Boehringer Ingelheim Pharma GmbH & Co.KG | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
| EP1483260A1 (de) * | 2002-03-11 | 2004-12-08 | Schering Aktiengesellschaft | Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel |
| JP4812763B2 (ja) * | 2004-05-18 | 2011-11-09 | ライジェル ファーマシューティカルズ， インコーポレイテッド | シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途 |
| EP1794134A1 (de) * | 2004-09-29 | 2007-06-13 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel |
| AR060890A1 (es) | 2006-05-15 | 2008-07-23 | Boehringer Ingelheim Int | Compuestos derivados de pirimidina y composicion farmaceutica en base a ellos |
| JP2010513406A (ja) * | 2006-12-22 | 2010-04-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌治療のための細胞周期キナーゼ阻害剤としての２−［（フェニルアミノ）−ピリミジン−４−イルアミノ］−シクロペンタンカルボキサミド誘導体及び関連化合物 |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AU2009262068C1 (en) * | 2008-06-27 | 2015-07-02 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| TW201024281A (en) | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
| CN102482277B (zh) | 2009-05-05 | 2017-09-19 | 达纳-法伯癌症研究所有限公司 | 表皮生长因子受体抑制剂及治疗障碍的方法 |
-
2010
- 2010-09-29 US US12/893,240 patent/US8466155B2/en active Active
- 2010-09-30 UY UY0001032916A patent/UY32916A/es not_active Application Discontinuation
- 2010-10-01 TW TW099133534A patent/TW201124386A/zh unknown
- 2010-10-01 AP AP2012006166A patent/AP2012006166A0/xx unknown
- 2010-10-01 AR ARP100103594A patent/AR078513A1/es unknown
- 2010-10-01 MX MX2012003101A patent/MX2012003101A/es active IP Right Grant
- 2010-10-01 KR KR1020127011321A patent/KR20120092617A/ko not_active Withdrawn
- 2010-10-01 JP JP2012531442A patent/JP5702390B2/ja active Active
- 2010-10-01 AU AU2010302648A patent/AU2010302648A1/en not_active Abandoned
- 2010-10-01 NZ NZ598614A patent/NZ598614A/xx not_active IP Right Cessation
- 2010-10-01 CN CN201080054924XA patent/CN102695700A/zh active Pending
- 2010-10-01 WO PCT/EP2010/064628 patent/WO2011039344A1/en active Application Filing
- 2010-10-01 IN IN2714DEN2012 patent/IN2012DN02714A/en unknown
- 2010-10-01 EP EP10759924.3A patent/EP2483249B1/en active Active
- 2010-10-01 EA EA201200552A patent/EA201200552A1/ru unknown
- 2010-10-01 PE PE2012000420A patent/PE20121431A1/es not_active Application Discontinuation
- 2010-10-01 BR BR112012007300A patent/BR112012007300A2/pt not_active IP Right Cessation
- 2010-10-01 CA CA2775418A patent/CA2775418A1/en not_active Abandoned
- 2010-10-01 PH PH1/2012/500527A patent/PH12012500527A1/en unknown
-
2012
- 2012-03-08 ZA ZA2012/01703A patent/ZA201201703B/en unknown
- 2012-03-08 IL IL218543A patent/IL218543A0/en unknown
- 2012-03-26 MA MA34719A patent/MA33606B1/fr unknown
- 2012-03-29 TN TNP2012000142A patent/TN2012000142A1/en unknown
- 2012-04-02 CL CL2012000825A patent/CL2012000825A1/es unknown
- 2012-04-26 EC ECSP12011830 patent/ECSP12011830A/es unknown
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1416423A (zh) * | 2000-03-01 | 2003-05-07 | 阿斯特拉曾尼卡有限公司 | 用作抗肿瘤剂的2,4－二(杂－)芳基氨基(－氧基)－5－取代的嘧啶 |
| CN1633419A (zh) * | 2001-05-29 | 2005-06-29 | 舍林股份公司 | Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用 |
| WO2004058144A2 (en) * | 2002-12-18 | 2004-07-15 | Glaxo Group Limited | Antibacterial agents |
| CN101213179A (zh) * | 2005-07-01 | 2008-07-02 | 贝林格尔·英格海姆国际有限公司 | 用作Aurora抑制剂的2,4-二氨基-嘧啶类化合物 |
| CN101346380A (zh) * | 2005-12-21 | 2009-01-14 | 辉瑞产品公司 | 用于治疗异常细胞生长的嘧啶衍生物 |
| CN101511836A (zh) * | 2006-07-06 | 2009-08-19 | 阿斯利康(瑞典)有限公司 | 稠合的嘧啶并化合物 |
| WO2008038011A1 (en) * | 2006-09-30 | 2008-04-03 | Vernalis (R & D) Limited | Pyrimidine derivatives as aurora a and aurora b inhibitors |
| WO2008128231A1 (en) * | 2007-04-16 | 2008-10-23 | Hutchison Medipharma Enterprises Limited | Pyrimidine derivatives |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2483249A1 (en) | 2012-08-08 |
| KR20120092617A (ko) | 2012-08-21 |
| US8466155B2 (en) | 2013-06-18 |
| PH12012500527A1 (en) | 2012-10-22 |
| ECSP12011830A (es) | 2012-06-29 |
| CL2012000825A1 (es) | 2012-08-24 |
| MX2012003101A (es) | 2012-04-11 |
| AU2010302648A1 (en) | 2012-04-05 |
| MA33606B1 (fr) | 2012-09-01 |
| JP2013506636A (ja) | 2013-02-28 |
| TN2012000142A1 (en) | 2013-09-19 |
| CA2775418A1 (en) | 2011-04-07 |
| JP5702390B2 (ja) | 2015-04-15 |
| IN2012DN02714A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2015-09-11 |
| IL218543A0 (en) | 2012-05-31 |
| WO2011039344A1 (en) | 2011-04-07 |
| AP2012006166A0 (en) | 2012-04-30 |
| US20110237598A1 (en) | 2011-09-29 |
| NZ598614A (en) | 2013-08-30 |
| EA201200552A1 (ru) | 2013-03-29 |
| EP2483249B1 (en) | 2015-12-23 |
| BR112012007300A2 (pt) | 2017-11-07 |
| ZA201201703B (en) | 2014-05-28 |
| PE20121431A1 (es) | 2012-11-10 |
| AR078513A1 (es) | 2011-11-16 |
| UY32916A (es) | 2011-04-29 |
| TW201124386A (en) | 2011-07-16 |
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Application publication date: 20120926 |