- Simple preparation method of vatalanib
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The invention provides a simple preparation method of vatalanib. The method comprises the following steps: carrying out a Grignard reaction on 4-halomethylpyridine (III) and metallic magnesium to prepare a corresponding Grignard reagent, carrying out addition on the Grignard reagent and phthalonitrile, condensing the obtained addition product and hydrazine hydrate to prepare 1-amino-4-(pyridin-4-yl)methylpyridazine (IV), and carrying out a substitution reaction on the 1-amino-4-(pyridin-4-yl)methylpyridazine (IV) and 4-halochlorobenzene (V) to obtain the vatalanib (II). The method of the invention has the advantages of small amount of generated wastewater, small toxicity of the raw materials, safety, environmental friendliness, and high safety of the prepared vatalanib; and the finally prepared product has a high purity and a high yield.
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- METHOD FOR TREATING OCULAR NEOVASCULAR DISEASES
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The invention relates to the use of certain phthalazines in the preparation of medicaments for the treatment of ocular neovascularization.
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(2010/11/28)
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- COMPOUNDS FOR IMMUNOPOTENTIATION
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Methods of stimulating an immune response and treating patients responsive thereto with 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-diones, staurosporine analogs, derivatized pyridazines, chromen-4-ones, indolinones, quinazolines, nucleoside analogs, and other small molecules are disclosed.
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Page/Page column 126
(2010/02/15)
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- Method for delivering drugs to the retina
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The invention relates to methods for the delivery of certain phthalazine derivatives to the retina(s) of a subject in need of treatment.
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- Ocular therapy
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A method for treating a subject suffering from epiretinal membrane formation or retinal detachment due to epiretinal membrane formation is disclosed. The method comprises administering a compound of the formula: wherein n is 0 to 2, R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl; and Z is unsubstituted or substituted pyridyl, an N-oxide thereof, wherein 1 or more N atoms carry an oxygen atom, or a salt thereof.
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- Method for treating ocular neovascular diseases
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The invention relates to the use of certain phthalazines in the preparation of medicaments for the treatment of ocular neovascularization.
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- Method for treating ocular neovascular diseases
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The invention relates to the use of certain phthalazines in the preparation of medicaments for the treatment of ocular neovascularization.
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- New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis
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The sprouting of new blood vessels, or angiogenesis, is necessary for any solid tumor to grow large enough to cause life-threatening disease. Vascular endothelial growth factor (VEGF) is one of the key promoters of tumor induced angiogenesis. VEGF receptors, the tyrosine kinases Flt-1 and KDR, are expressed on vascular endothelial cells and initiate angiogenesis upon activation by VEGF. 1-Anilino-(4-pyridylmethyl)-phthalazines, such as CGP 79787D (or PTK787/ZK222584), reversibly inhibit Flt-1 and KDR with IC50 values 50 = 34 nM). Modification of the 1-anilino moiety afforded derivatives with higher selectivity for the VEGF receptor tyrosine kinases Flt-1 and KDR compared to the related receptor tyrosine kinases PDGF-R and c-Kit. Since these 1-anilino-(4-pyridylmethyl)phthalazines are orally well absorbed, these compounds qualify for further profiling and as candidates for clinical evaluation.
- Bold, Guido,Altmann, Karl-Heinz,Frei, J?rg,Lang, Marc,Manley, Paul W.,Traxler, Peter,Wietfeld, Bernhard,Brüggen, Josef,Buchdunger, Elisabeth,Cozens, Robert,Ferrari, Stefano,Furet, Pascal,Hofmann, Francesco,Martiny-Baron, Georg,Mestan, Jürgen,R?sel, Johannes,Sills, Matthew,Stover, David,Acemoglu, Figan,Boss, Eugen,Emmenegger, René,L?sser, Laurent,Masso, Elvira,Roth, Rosemarie,Schlachter, Christian,Vetterli, Werner,Wyss, Dominique,Wood, Jeanette M.
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p. 2310 - 2323
(2007/10/03)
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