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 |
| AU7622698A (en) * | 1996-12-05 | 1998-06-29 | Sugen, Inc. | Use of indolinone compounds as modulators of protein kinases |
| AU3850299A (en) * | 1998-05-20 | 1999-12-06 | Kyowa Hakko Kogyo Co. Ltd. | Vegf activity inhibitors |
| DE69930662T2 (de) * | 1998-06-11 | 2006-12-28 | Astrazeneca Ab | Humane rezeptortyrosinkinase |
| PT1105136E (pt) * | 1998-08-13 | 2007-12-03 | Novartis Ag | Método para tratar doenças oculares neovasculares |
| US6214819B1 (en) | 1998-11-23 | 2001-04-10 | Novartis Ag | Method for treating ocular neovascular diseases |
| EP1131073B1 (fr) * | 1998-11-23 | 2003-10-22 | Novartis AG | Utilisation de derives de staurosporine dans le traitement des neoformations de vaisseaux sanguins oculaires |
| 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 |
| MXPA02001439A (es) * | 1999-08-11 | 2002-08-30 | Eos Biotechnology Inc | Nuevos metodos para el diagnostico de angiogenesis, composiciones y metodos de exhibicion de moduladores de la angiogenesis. |
| 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 |
| JP3663382B2 (ja) | 2000-02-15 | 2005-06-22 | スージェン・インコーポレーテッド | ピロール置換２−インドリノン蛋白質キナーゼ阻害剤 |
| MXPA02012224A (es) * | 2000-06-07 | 2004-08-19 | Johnson & Johnson | Metodo para detectar moduladores del dominio cinasa del factor de crecimiento endotelial vascular. |
| WO2002007747A1 (fr) | 2000-07-18 | 2002-01-31 | Joslin Diabetes Center, Inc. | Procede de modulation de fibrose |
| 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 |
| US8512738B2 (en) * | 2004-04-30 | 2013-08-20 | Allergan, Inc. | Biodegradable intravitreal tyrosine kinase implants |
| 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 |
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 WO PCT/US1997/003378 patent/WO1997034920A1/fr active Application Filing
- 1997-03-04 AU AU20667/97A patent/AU2066797A/en not_active Abandoned
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