CN104736533B - Vegfr3抑制剂 - Google Patents
Vegfr3抑制剂 Download PDFInfo
- Publication number
- CN104736533B CN104736533B CN201380052158.7A CN201380052158A CN104736533B CN 104736533 B CN104736533 B CN 104736533B CN 201380052158 A CN201380052158 A CN 201380052158A CN 104736533 B CN104736533 B CN 104736533B
- Authority
- CN
- China
- Prior art keywords
- phenyl
- ethyl
- compound
- pyrimidin
- amino
- 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.)
- Expired - Fee Related
Links
- 0 *C(CC1)CCN1N Chemical compound *C(CC1)CCN1N 0.000 description 19
- XPDIKRMPZNLBAC-UHFFFAOYSA-N CC(C)(C)OC(N(C1)CC1I)=O Chemical compound CC(C)(C)OC(N(C1)CC1I)=O XPDIKRMPZNLBAC-UHFFFAOYSA-N 0.000 description 1
- YCAFGVYPCOAQQZ-UHFFFAOYSA-N CC(C)(C)OC(N(C1)CC1c(cc1)ccc1[N+]([O-])=O)=O Chemical compound CC(C)(C)OC(N(C1)CC1c(cc1)ccc1[N+]([O-])=O)=O YCAFGVYPCOAQQZ-UHFFFAOYSA-N 0.000 description 1
- YRLQFRXDWBFGMK-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1c(cc1)ccc1N)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1c(cc1)ccc1N)=O YRLQFRXDWBFGMK-UHFFFAOYSA-N 0.000 description 1
- KICAATGZGSORBZ-UHFFFAOYSA-N CC(C1C(CCCc(nc(nc2)SC)c2Cl)=CCC=CC=C1)C(N)=O Chemical compound CC(C1C(CCCc(nc(nc2)SC)c2Cl)=CCC=CC=C1)C(N)=O KICAATGZGSORBZ-UHFFFAOYSA-N 0.000 description 1
- YUSDJXUPLQYFJW-UHFFFAOYSA-N CC(c(nc1)ccc1N)=O Chemical compound CC(c(nc1)ccc1N)=O YUSDJXUPLQYFJW-UHFFFAOYSA-N 0.000 description 1
- OQTNJLQWOVTCPV-UHFFFAOYSA-N CCc(cc1)cnc1N Chemical compound CCc(cc1)cnc1N OQTNJLQWOVTCPV-UHFFFAOYSA-N 0.000 description 1
- KDTBEIPBHBHNOY-UHFFFAOYSA-N NC(C1(CC1)c1c(CCc(nc(nc2)Cl)c2Cl)cccc1)=O Chemical compound NC(C1(CC1)c1c(CCc(nc(nc2)Cl)c2Cl)cccc1)=O KDTBEIPBHBHNOY-UHFFFAOYSA-N 0.000 description 1
- MZYDUEWRHJEHIO-UHFFFAOYSA-N NC(C1(CC1)c1ccccc1CCc1nc(Nc2cnc(C(F)(F)F)cc2)ncc1Cl)=O Chemical compound NC(C1(CC1)c1ccccc1CCc1nc(Nc2cnc(C(F)(F)F)cc2)ncc1Cl)=O MZYDUEWRHJEHIO-UHFFFAOYSA-N 0.000 description 1
- WQYSQTBNUZIFNI-UHFFFAOYSA-N Nc1ccc(C2CNC2)cc1 Chemical compound Nc1ccc(C2CNC2)cc1 WQYSQTBNUZIFNI-UHFFFAOYSA-N 0.000 description 1
- IBOZOWZSXZNIHI-UHFFFAOYSA-N Nc1cnc(C(F)(F)F)cc1 Chemical compound Nc1cnc(C(F)(F)F)cc1 IBOZOWZSXZNIHI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- 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
- C07D403/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261684202P | 2012-08-17 | 2012-08-17 | |
| US61/684,202 | 2012-08-17 | ||
| PCT/AU2013/000913 WO2014026243A1 (en) | 2012-08-17 | 2013-08-16 | Vegfr3 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104736533A CN104736533A (zh) | 2015-06-24 |
| CN104736533B true CN104736533B (zh) | 2016-12-07 |
Family
ID=50101126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380052158.7A Expired - Fee Related CN104736533B (zh) | 2012-08-17 | 2013-08-16 | Vegfr3抑制剂 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20160009686A1 (https=) |
| EP (1) | EP2885291A4 (https=) |
| JP (1) | JP2015524826A (https=) |
| CN (1) | CN104736533B (https=) |
| AU (1) | AU2013302320A1 (https=) |
| CA (1) | CA2882158A1 (https=) |
| HK (1) | HK1209105A1 (https=) |
| WO (1) | WO2014026243A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014026242A1 (en) | 2012-08-17 | 2014-02-20 | Cancer Therapeutics Crc Pty Limited | Vegfr3 inhibitors |
| WO2015123722A1 (en) * | 2014-02-19 | 2015-08-27 | Bionomics Limited | Inhibitors |
| CN106588885B (zh) * | 2016-11-10 | 2019-03-19 | 浙江大学 | 2-取代芳环-嘧啶类衍生物及制备和应用 |
| MX2020006641A (es) * | 2017-12-20 | 2021-01-08 | Denali Therapeutics Inc | Proceso para la preparacion de compuestos de pirimidinil-4-aminopi razol. |
| CN111566117A (zh) | 2017-12-29 | 2020-08-21 | 糖模拟物有限公司 | E-选择蛋白和半乳凝素-3的异双功能抑制剂 |
| US11845771B2 (en) | 2018-12-27 | 2023-12-19 | Glycomimetics, Inc. | Heterobifunctional inhibitors of E-selectin and galectin-3 |
| CN109942616A (zh) * | 2019-04-18 | 2019-06-28 | 广东工业大学 | 一种含炔基的芳基酰胺类衍生物及其制备方法和应用 |
| WO2023073148A1 (en) * | 2021-10-29 | 2023-05-04 | Janssen Pharmaceutica Nv | Vascular endothelial growth factor receptor 3 as biomarker for bace2 activity |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008008234A1 (en) * | 2006-07-07 | 2008-01-17 | Targegen, Inc. | 2-amino-5-substituted pyrimidine inhibitors |
| CN101605540A (zh) * | 2006-12-14 | 2009-12-16 | 埃克塞利希斯股份有限公司 | 使用mek抑制剂的方法 |
| CA2808540A1 (en) * | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidine derivatives as fak inhibitors |
| CN103534241A (zh) * | 2011-02-17 | 2014-01-22 | 癌症疗法Crc私人有限公司 | Fak抑制剂 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| BR9707495A (pt) | 1996-02-13 | 1999-07-27 | Zeneca Ltd | Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente |
| US6291455B1 (en) | 1996-03-05 | 2001-09-18 | Zeneca Limited | 4-anilinoquinazoline derivatives |
| GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| DE69837529T2 (de) | 1997-02-12 | 2007-07-26 | Electrophoretics Ltd., Cobham | Proteinmarker für lungenkrebs und deren verwendung |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
| GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
| GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
| SK288365B6 (sk) | 1999-02-10 | 2016-07-01 | Astrazeneca Ab | Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy |
| CZ301689B6 (cs) | 1999-11-05 | 2010-05-26 | Astrazeneca Ab | Derivát chinazolinu a farmaceutický prostredek, který ho obsahuje |
| SI1255752T1 (sl) | 2000-02-15 | 2007-12-31 | Pharmacia & Upjohn Co Llc | S pirolom substituirani zaviralci 2-indolinon protein kinaza |
| NZ522074A (en) | 2000-05-31 | 2004-06-25 | Astrazeneca Ab | Indole derivatives with vascular damaging activity |
| UA73993C2 (uk) | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| IL153484A0 (en) | 2000-07-07 | 2003-07-06 | Angiogene Pharm Ltd | Colchinol derivatives as angiogenesis inhibitors |
| CN1255392C (zh) | 2000-07-07 | 2006-05-10 | 安吉奥金尼药品有限公司 | 作为血管生成抑制剂的秋水仙醇衍生物 |
| ATE407678T1 (de) | 2001-10-17 | 2008-09-15 | Boehringer Ingelheim Pharma | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
| TW200922590A (en) * | 2007-09-10 | 2009-06-01 | Curis Inc | VEGFR inhibitors containing a zinc binding moiety |
| CA2742897A1 (en) | 2008-11-06 | 2010-05-14 | Astrazeneca Ab | Modulators of amyloid beta. |
| AR074481A1 (es) * | 2008-12-05 | 2011-01-19 | Abbott Lab | Derivados de tienopiridina como inhibidores de quinasa |
| WO2010111406A2 (en) | 2009-03-24 | 2010-09-30 | Myriad Pharmaceuticals, Inc. | Compounds and therapeutic uses thereof |
| US20120142703A1 (en) * | 2009-05-14 | 2012-06-07 | Boehringer Ingelheim International Gmbh | New combination therapy in treatment of oncological and fibrotic diseases |
| US20130172378A1 (en) * | 2010-09-14 | 2013-07-04 | Glaxosmithkline Llc | Combination of BRAF and VEGF Inhibitors |
| JP5937112B2 (ja) * | 2011-02-17 | 2016-06-22 | カンサー・セラピューティクス・シーアールシー・プロプライエタリー・リミテッドＣａｎｃｅｒ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｃｒｃ Ｐｔｙ Ｌｉｍｉｔｅｄ | 選択的ｆａｋ阻害剤 |
| KR101682417B1 (ko) | 2011-02-25 | 2016-12-06 | 주식회사유한양행 | 다이아미노피리미딘 유도체 및 그의 제조방법 |
| JP6226981B2 (ja) | 2012-07-17 | 2017-11-08 | サノフイ | 肝細胞癌を処置するためのｖｅｇｆｒ−３阻害剤の使用 |
| WO2014027199A1 (en) * | 2012-08-14 | 2014-02-20 | Cancer Therapeutics Crc Pty Ltd | Fak and flt3 inhibitors |
| CN103113355B (zh) | 2013-02-27 | 2014-08-13 | 无锡爱内特生物科技有限公司 | 一种Bcr/Abl酪氨酸激酶抑制剂及其制备方法和在治疗慢性粒细胞白血病中的应用 |
-
2013
- 2013-08-16 CA CA2882158A patent/CA2882158A1/en not_active Abandoned
- 2013-08-16 US US14/422,093 patent/US20160009686A1/en not_active Abandoned
- 2013-08-16 WO PCT/AU2013/000913 patent/WO2014026243A1/en not_active Ceased
- 2013-08-16 EP EP13829265.1A patent/EP2885291A4/en not_active Withdrawn
- 2013-08-16 US US13/969,037 patent/US9238644B2/en not_active Expired - Fee Related
- 2013-08-16 CN CN201380052158.7A patent/CN104736533B/zh not_active Expired - Fee Related
- 2013-08-16 HK HK15109687.2A patent/HK1209105A1/xx unknown
- 2013-08-16 JP JP2015526836A patent/JP2015524826A/ja active Pending
- 2013-08-16 AU AU2013302320A patent/AU2013302320A1/en not_active Abandoned
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008008234A1 (en) * | 2006-07-07 | 2008-01-17 | Targegen, Inc. | 2-amino-5-substituted pyrimidine inhibitors |
| CN101605540A (zh) * | 2006-12-14 | 2009-12-16 | 埃克塞利希斯股份有限公司 | 使用mek抑制剂的方法 |
| CA2808540A1 (en) * | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidine derivatives as fak inhibitors |
| CN103534241A (zh) * | 2011-02-17 | 2014-01-22 | 癌症疗法Crc私人有限公司 | Fak抑制剂 |
Also Published As
| Publication number | Publication date |
|---|---|
| HK1209105A1 (en) | 2016-03-24 |
| US20140073620A1 (en) | 2014-03-13 |
| EP2885291A1 (en) | 2015-06-24 |
| WO2014026243A1 (en) | 2014-02-20 |
| AU2013302320A1 (en) | 2015-02-26 |
| EP2885291A4 (en) | 2015-11-04 |
| CA2882158A1 (en) | 2014-02-20 |
| US20160009686A1 (en) | 2016-01-14 |
| CN104736533A (zh) | 2015-06-24 |
| JP2015524826A (ja) | 2015-08-27 |
| US9238644B2 (en) | 2016-01-19 |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| EXSB | Decision made by sipo to initiate substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20161207 Termination date: 20170816 |