Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1999-08-10
2001-08-07
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S912000
Reexamination Certificate
active
06271233
ABSTRACT:
The invention relates to new phthalazine derivatives for the manufacture of a pharmaceutical preparation for the treatment and prevention of ocular neovascular diseases. It further relates to the treatment and prevention of such ocular diseases the phthalazine derivatives.
BACKGROUND OF THE INVENTION
Two processes, the de novo formation of vessels from differentiating endothelial cells or angioblasts in the developing embryo (vasculogenesis) and the growth of new capillary vessels from existing blood vessels (angiogenesis), are involved in the development of the vascular systems of animal organs and tissues.
Recent findings show that at the centre of the network regulating the growth and differentiation of the vascular system and its components, both during embryonic development and normal growth and in a wide number of pathological anomalies and diseases, lies the angiogenic factor known as “Vascular Endothelial Growth Factor” (=VEGF), along with its cellular receptors. (see, Breier, et al.,
Trends in Cell Biology
6: 454-456, 1996).
VEGF receptors are transmembrane receptor tyrosine kinases. They are characterized by an extracellular domain with seven immunoglobulin-like domains and an intracellular tyrosine kinase domain. Various types of VEGF receptor are known, e.g. VEGFR-1, VEGFR-2, and VEGFR-3.
SUMMARY OF THE INVENTION
It has now been found that phthalazine derivatives of formula I, described below, have advantageous pharmacological properties and inhibit ocular neovascularization, including retinal neovascularization and choroidal neovascularization.
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The 23rd German Cancer conference, Berlin 8-12 Jun. 1998, Germany Needs Interdisciplinary Approach to Cancer Research, International Cancer News, Jun. 8, 1998, pp. 1474-1475.
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Brazzell Romulus Kimbro
Campochiaro Peter Anthony
Kane Frances Elizabeth
Wood Jeanette Marjorie
Ciba Vision Corporation
Fay Zohreh
Wildman David E.
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