WO1997034920B1 - Dosages pour inhibiteurs du recepteur tyrosine kinase kdr/flk-1 - Google Patents
Dosages pour inhibiteurs du recepteur tyrosine kinase kdr/flk-1Info
- Publication number
- WO1997034920B1 WO1997034920B1 PCT/US1997/003378 US9703378W WO9734920B1 WO 1997034920 B1 WO1997034920 B1 WO 1997034920B1 US 9703378 W US9703378 W US 9703378W WO 9734920 B1 WO9734920 B1 WO 9734920B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- vegf
- subset
- receptor
- candidate compounds
- inhibiting
- Prior art date
Links
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 title claims abstract 6
- 238000003556 assay Methods 0.000 title claims 6
- 102000016549 Vascular Endothelial Growth Factor Receptor-2 Human genes 0.000 title 2
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 34
- 238000000034 method Methods 0.000 claims abstract 19
- 230000002401 inhibitory effect Effects 0.000 claims abstract 17
- 230000033115 angiogenesis Effects 0.000 claims abstract 5
- 230000004862 vasculogenesis Effects 0.000 claims abstract 5
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims abstract 3
- 201000010099 disease Diseases 0.000 claims abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 108091008605 VEGF receptors Proteins 0.000 claims 25
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 25
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 14
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 14
- 210000004027 cell Anatomy 0.000 claims 12
- 230000005764 inhibitory process Effects 0.000 claims 8
- 102000005962 receptors Human genes 0.000 claims 8
- 108020003175 receptors Proteins 0.000 claims 8
- 239000003446 ligand Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 4
- 230000026731 phosphorylation Effects 0.000 claims 4
- 238000006366 phosphorylation reaction Methods 0.000 claims 4
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 4
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 4
- 238000007920 subcutaneous administration Methods 0.000 claims 4
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 3
- 238000000423 cell based assay Methods 0.000 claims 3
- 210000002889 endothelial cell Anatomy 0.000 claims 3
- 230000001747 exhibiting effect Effects 0.000 claims 3
- 238000001727 in vivo Methods 0.000 claims 3
- 230000008685 targeting Effects 0.000 claims 3
- IQFYYKKMVGJFEH-XLPZGREQSA-N Thymidine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 IQFYYKKMVGJFEH-XLPZGREQSA-N 0.000 claims 2
- 238000002474 experimental method Methods 0.000 claims 2
- 238000012360 testing method Methods 0.000 claims 2
- DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 claims 1
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 238000012286 ELISA Assay Methods 0.000 claims 1
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- IQFYYKKMVGJFEH-UHFFFAOYSA-N beta-L-thymidine Natural products O=C1NC(=O)C(C)=CN1C1OC(CO)C(O)C1 IQFYYKKMVGJFEH-UHFFFAOYSA-N 0.000 claims 1
- 238000010256 biochemical assay Methods 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000010348 incorporation Methods 0.000 claims 1
- 230000002934 lysing effect Effects 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 229940104230 thymidine Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract 1
Abstract
La présente invention concerne des procédés d'identification de composés et des compositions pharmaceutiques capables d'inhiber sélectivement et potentiellement la transduction du signal de tyrosine kinase KDR/FLK-1 afin d'inhiber la vasculogénèse et/ou l'angiogénèse. La présente invention concerne également des composés et des compositions identifiés à l'aide des procédés de l'invention ainsi que leur utilisation dans le traitement de maladies relatives à une vasculogénèse et/ou une angiogénèse inappropriées.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU20667/97A AU2066797A (en) | 1996-03-21 | 1997-03-04 | Assays for kdr/flk-1 receptor tyrosine kinase inhibitors |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62173496A | 1996-03-21 | 1996-03-21 | |
| US08/621,734 | 1996-03-21 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO1997034920A1 WO1997034920A1 (fr) | 1997-09-25 |
| WO1997034920B1 true WO1997034920B1 (fr) | 1997-10-30 |
Family
ID=24491410
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1997/003378 WO1997034920A1 (fr) | 1996-03-21 | 1997-03-04 | Dosages pour inhibiteurs du recepteur tyrosine kinase kdr/flk-1 |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU2066797A (fr) |
| WO (1) | WO1997034920A1 (fr) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5880141A (en) * | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| WO1998024432A2 (fr) * | 1996-12-05 | 1998-06-11 | Sugen, Inc. | Utilisation de composes a base d'indolinone en tant que modulateurs de proteine kinases |
| AU3850299A (en) * | 1998-05-20 | 1999-12-06 | Kyowa Hakko Kogyo Co. Ltd. | Vegf activity inhibitors |
| EP1084245B1 (fr) | 1998-06-11 | 2006-03-29 | AstraZeneca AB | Recepteur humain tyrosine kinase |
| AU5733099A (en) * | 1998-08-13 | 2000-03-06 | Novartis Ag | Method for treating ocular neovascular diseases |
| CN1172673C (zh) * | 1998-11-23 | 2004-10-27 | 诺瓦提斯公司 | 星形孢菌素衍生物在制备治疗眼睛新血管生成性疾病的药物中的应用 |
| US6214819B1 (en) | 1998-11-23 | 2001-04-10 | Novartis Ag | Method for treating ocular neovascular diseases |
| GB9918057D0 (en) * | 1999-07-30 | 1999-10-06 | Univ Bristol | Therapeutic agents |
| US6271233B1 (en) | 1999-08-10 | 2001-08-07 | Ciba Vision Corporation | Method for treating ocular neovascular diseases |
| CA2381699A1 (fr) * | 1999-08-11 | 2001-02-15 | Eos Biotechnology, Inc. | Nouvelles techniques de diagnostic de l'angiogenese, compositions et techniques de criblage pour modulateurs d'angiogenese |
| AU1347301A (en) * | 1999-10-28 | 2001-05-08 | Procter & Gamble Company, The | The use of a complex of vegfr-2 and neuropilin-1 for identification of novel pro- and anti-angiogenic actives |
| ES2290117T3 (es) | 2000-02-15 | 2008-02-16 | Sugen, Inc. | Inhibidores de proteina quinasa 2-indolina sustituida con pirrol. |
| US7070938B2 (en) * | 2000-06-07 | 2006-07-04 | Ortho-Mcneil Pharmaceutical, Inc. | Method to detect modulators of VEGF kinase domain |
| AU2001276934A1 (en) * | 2000-07-18 | 2002-02-05 | Joslin Diabetes Center Inc. | Methods of modulating fibrosis |
| AR042586A1 (es) | 2001-02-15 | 2005-06-29 | Sugen Inc | 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa |
| US6649367B2 (en) * | 2001-03-22 | 2003-11-18 | Eisai Co., Ltd | Human cancer cell line malignantly altered by expression of angiogenic factor |
| US7268137B2 (en) * | 2002-11-07 | 2007-09-11 | Campochiaro Peter A | Ocular therapy |
| US7771742B2 (en) | 2004-04-30 | 2010-08-10 | Allergan, Inc. | Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods |
| AU2011211380B9 (en) * | 2004-04-30 | 2014-05-08 | Allergan, Inc. | Biodegradable intravitreal tyrosine kinase inhibitor implants |
| WO2005107708A1 (fr) * | 2004-04-30 | 2005-11-17 | Allergan, Inc. | Implants d'inhibiteurs de tyrosine kinase intravitreens, biodegradables |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6177401B1 (en) * | 1992-11-13 | 2001-01-23 | Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften | Use of organic compounds for the inhibition of Flk-1 mediated vasculogenesis and angiogenesis |
| US5700823A (en) * | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| US5840301A (en) * | 1994-02-10 | 1998-11-24 | Imclone Systems Incorporated | Methods of use of chimerized, humanized, and single chain antibodies specific to VEGF receptors |
-
1997
- 1997-03-04 AU AU20667/97A patent/AU2066797A/en not_active Abandoned
- 1997-03-04 WO PCT/US1997/003378 patent/WO1997034920A1/fr active Application Filing
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