AU2013302319A1 - VEGFR3 inhibitors - Google Patents
VEGFR3 inhibitors Download PDFInfo
- Publication number
- AU2013302319A1 AU2013302319A1 AU2013302319A AU2013302319A AU2013302319A1 AU 2013302319 A1 AU2013302319 A1 AU 2013302319A1 AU 2013302319 A AU2013302319 A AU 2013302319A AU 2013302319 A AU2013302319 A AU 2013302319A AU 2013302319 A1 AU2013302319 A1 AU 2013302319A1
- Authority
- AU
- Australia
- Prior art keywords
- compound
- phenyl
- group
- alkyl
- pct
- 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.)
- Abandoned
Links
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- 201000011510 cancer Diseases 0.000 claims abstract description 30
- 238000000034 method Methods 0.000 claims abstract description 26
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 11
- 238000011282 treatment Methods 0.000 claims abstract description 11
- 238000002360 preparation method Methods 0.000 claims abstract description 9
- 230000005764 inhibitory process Effects 0.000 claims abstract description 7
- 230000008569 process Effects 0.000 claims abstract description 5
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- 239000008177 pharmaceutical agent Substances 0.000 claims abstract description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 84
- 239000000203 mixture Substances 0.000 claims description 63
- 125000000217 alkyl group Chemical group 0.000 claims description 62
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 57
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- 229940002612 prodrug Drugs 0.000 claims description 47
- 239000000651 prodrug Substances 0.000 claims description 47
- 229910052757 nitrogen Inorganic materials 0.000 claims description 39
- 239000003795 chemical substances by application Substances 0.000 claims description 38
- 125000001424 substituent group Chemical group 0.000 claims description 38
- 239000012453 solvate Substances 0.000 claims description 35
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 33
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- 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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- 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
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
- C07D401/02—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
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| 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 |
Publications (1)
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| AU2013302319A1 true AU2013302319A1 (en) | 2015-02-26 |
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| JP (1) | JP2015524825A (enExample) |
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| CA (1) | CA2882270A1 (enExample) |
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| WO2015123722A1 (en) * | 2014-02-19 | 2015-08-27 | Bionomics Limited | Inhibitors |
| JP2019505498A (ja) | 2015-12-16 | 2019-02-28 | ザ・ウォルター・アンド・エリザ・ホール・インスティテュート・オブ・メディカル・リサーチ | Nk細胞におけるサイトカイン誘導性sh2タンパク質の阻害 |
| WO2018058125A1 (en) | 2016-09-26 | 2018-03-29 | Ensemble Group Holdings | Methods of assessing and treating cancer in subjects having dysregulated lymphatic systems |
| 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 |
| EP3564232B1 (en) | 2016-12-27 | 2022-01-26 | Riken | Bmp-signal-inhibiting compound |
| 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 |
| 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 |
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| PT1438053E (pt) * | 2001-10-17 | 2008-09-25 | Boehringer Ingelheim Int | Derivados de pirimidina, medicamento contendo estes compostos, sua utilização e processo para a sua preparação |
| TW200922590A (en) * | 2007-09-10 | 2009-06-01 | Curis Inc | VEGFR inhibitors containing a zinc binding moiety |
| MX2011004680A (es) | 2008-11-06 | 2011-05-25 | Astrazeneca Ab | Moduladores de beta amiloide. |
| JP5588458B2 (ja) * | 2008-12-05 | 2014-09-10 | アッヴィ・バハマズ・リミテッド | 癌の治療に使用するためのキナーゼ阻害剤としてのチエノ[3,2−c]ピリジン誘導体 |
| WO2010111406A2 (en) | 2009-03-24 | 2010-09-30 | Myriad Pharmaceuticals, Inc. | Compounds and therapeutic uses thereof |
| EP2647375A1 (en) * | 2009-05-14 | 2013-10-09 | Boehringer Ingelheim International Gmbh | Combination of vargatef and dabigatran for the treatment of oncological and fibrotic diseases |
| DE102010034699A1 (de) | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidinderivate |
| EP2616057A4 (en) * | 2010-09-14 | 2014-03-12 | Glaxosmithkline Ip No 2 Ltd | COMBINATION OF B-RAF AND VEGFR INHIBITORS |
| ES2691673T3 (es) * | 2011-02-17 | 2018-11-28 | Cancer Therapeutics Crc Pty Limited | Inhibidores de Fak |
| DK2675794T3 (da) | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
| KR101682417B1 (ko) | 2011-02-25 | 2016-12-06 | 주식회사유한양행 | 다이아미노피리미딘 유도체 및 그의 제조방법 |
| LT2874625T (lt) | 2012-07-17 | 2017-08-25 | Sanofi | Vegfr-3 slopiklių panaudojimas hepatoceliulinės karcinomos gydymui |
| 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 |
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2013
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- 2013-08-16 HK HK15109686.3A patent/HK1209104A1/xx unknown
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- 2013-08-16 CN CN201710144110.9A patent/CN106986832A/zh active Pending
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Also Published As
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| CN106986832A (zh) | 2017-07-28 |
| WO2014026242A1 (en) | 2014-02-20 |
| HK1209104A1 (en) | 2016-03-24 |
| CA2882270A1 (en) | 2014-02-20 |
| JP2015524825A (ja) | 2015-08-27 |
| CN104837835A (zh) | 2015-08-12 |
| US20150225377A1 (en) | 2015-08-13 |
| US9266864B2 (en) | 2016-02-23 |
| EP2885292A1 (en) | 2015-06-24 |
| EP2885292A4 (en) | 2015-07-01 |
| US20140080798A1 (en) | 2014-03-20 |
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