CN104837835A - Vegfr3抑制剂 - Google Patents

Vegfr3抑制剂 Download PDF

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Publication number
CN104837835A
CN104837835A CN201380052157.2A CN201380052157A CN104837835A CN 104837835 A CN104837835 A CN 104837835A CN 201380052157 A CN201380052157 A CN 201380052157A CN 104837835 A CN104837835 A CN 104837835A
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CN
China
Prior art keywords
alkyl
compound
group
methyl
mmol
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
Application number
CN201380052157.2A
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English (en)
Chinese (zh)
Inventor
理查德·查尔斯·福伊齐克
内尔·崔
本杰明·约瑟夫·莫罗
凯瑟琳·法埃·赫姆利
吉琳·伊利莎白·伦尼斯
米歇尔·昂·卡梅里诺
丹尼·加纳梅
保罗·安托尼·斯图普尔
罗米纳·勒塞纳
威廉默斯·约翰尼斯·安东尼厄斯·克斯滕
安德鲁·约翰·哈维
伊恩·彼得·霍姆斯
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Cancer Therapeutics CRC Pty Ltd
Original Assignee
Cancer Therapeutics CRC Pty Ltd
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Filing date
Publication date
Application filed by Cancer Therapeutics CRC Pty Ltd filed Critical Cancer Therapeutics CRC Pty Ltd
Priority to CN201710144110.9A priority Critical patent/CN106986832A/zh
Publication of CN104837835A publication Critical patent/CN104837835A/zh
Pending legal-status Critical Current

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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
    • C07D401/02—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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380052157.2A 2012-08-17 2013-08-16 Vegfr3抑制剂 Pending CN104837835A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710144110.9A CN106986832A (zh) 2012-08-17 2013-08-16 Vegfr3抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261684254P 2012-08-17 2012-08-17
US61/684,254 2012-08-17
PCT/AU2013/000912 WO2014026242A1 (en) 2012-08-17 2013-08-16 Vegfr3 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201710144110.9A Division CN106986832A (zh) 2012-08-17 2013-08-16 Vegfr3抑制剂

Publications (1)

Publication Number Publication Date
CN104837835A true CN104837835A (zh) 2015-08-12

Family

ID=50101125

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201380052157.2A Pending CN104837835A (zh) 2012-08-17 2013-08-16 Vegfr3抑制剂
CN201710144110.9A Pending CN106986832A (zh) 2012-08-17 2013-08-16 Vegfr3抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201710144110.9A Pending CN106986832A (zh) 2012-08-17 2013-08-16 Vegfr3抑制剂

Country Status (8)

Country Link
US (2) US9266864B2 (enExample)
EP (1) EP2885292A4 (enExample)
JP (1) JP2015524825A (enExample)
CN (2) CN104837835A (enExample)
AU (1) AU2013302319A1 (enExample)
CA (1) CA2882270A1 (enExample)
HK (1) HK1209104A1 (enExample)
WO (1) WO2014026242A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN109982658A (zh) * 2016-10-27 2019-07-05 加利福尼亚大学董事会 整合素α9的阻断抑制淋巴管瓣形成并促进移植物存活

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015123722A1 (en) * 2014-02-19 2015-08-27 Bionomics Limited Inhibitors
CN112972492B (zh) 2015-12-16 2024-11-08 沃尔特及伊莱萨霍尔医学研究院 Nk细胞中对细胞因子诱导的sh2蛋白的抑制
EP4026849A1 (en) * 2016-09-26 2022-07-13 Ensemble Group Holdings Methods of assessing and treating cancer in subjects having dysregulated lymphatic systems using a combination of vegfr-3 and pd-1 or pd-l1 inhibitors
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
CN114853740B (zh) * 2021-02-03 2023-08-01 药雅科技(上海)有限公司 炔类嘧啶化合物作为fgfr抑制剂的制备方法和用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2463989A1 (en) * 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pyrimidine derivatives, pharmaceutical compositions containing these compounds, the use thereof and process for the preparation thereof
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 (12)

* Cited by examiner, † Cited by third party
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TW200922590A (en) * 2007-09-10 2009-06-01 Curis Inc VEGFR inhibitors containing a zinc binding moiety
EP2367826A4 (en) 2008-11-06 2012-07-04 Astrazeneca Ab MODULATORS OF THE PROTEIN -AMYLOID
UA103351C2 (uk) * 2008-12-05 2013-10-10 Ебботт Леборетріз ПОХІДНІ ТІЄНО[3,2-c]ПІРИДИНУ ЯК ІНГІБІТОРИ КІНАЗ ДЛЯ ЗАСТОСУВАННЯ В ЛІКУВАННІ РАКУ
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
WO2010130757A1 (en) * 2009-05-14 2010-11-18 Boehringer Ingelheim International Gmbh New combination therapy in treatment of oncological and fibrotic diseases
JP6185839B2 (ja) * 2010-09-14 2017-08-23 ノバルティス アーゲー Ｂｒａｆ阻害薬とｖｅｇｆ阻害薬との組み合わせ
WO2012110774A1 (en) 2011-02-17 2012-08-23 Cancer Therapeutics Crc Pty Limited Selective fak inhibitors
KR101682417B1 (ko) 2011-02-25 2016-12-06 주식회사유한양행 다이아미노피리미딘 유도체 및 그의 제조방법
EA027982B1 (ru) 2012-07-17 2017-09-29 Санофи Применение ингибиторов vegfr-3 для лечения гепатоклеточной карциномы
WO2014027199A1 (en) * 2012-08-14 2014-02-20 Cancer Therapeutics Crc Pty Ltd Fak and flt3 inhibitors
US9238644B2 (en) * 2012-08-17 2016-01-19 Cancer Therapeutics Crc Pty Limited VEGFR3 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2463989A1 (en) * 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pyrimidine derivatives, pharmaceutical compositions containing these compounds, the use thereof and process for the preparation thereof
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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109982658A (zh) * 2016-10-27 2019-07-05 加利福尼亚大学董事会 整合素α9的阻断抑制淋巴管瓣形成并促进移植物存活
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

Also Published As

Publication number Publication date
CA2882270A1 (en) 2014-02-20
JP2015524825A (ja) 2015-08-27
EP2885292A4 (en) 2015-07-01
US9266864B2 (en) 2016-02-23
CN106986832A (zh) 2017-07-28
US20150225377A1 (en) 2015-08-13
US20140080798A1 (en) 2014-03-20
WO2014026242A1 (en) 2014-02-20
HK1209104A1 (en) 2016-03-24
AU2013302319A1 (en) 2015-02-26
EP2885292A1 (en) 2015-06-24

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