Phthalazine derivatives for treating inflammatory diseases

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S248000, C514S252030, C514S279000, C514S300000, C514S303000, C544S236000, C544S237000, C544S238000, C544S268000, C546S113000, C546S268100

Reexamination Certificate

active

06911440

ABSTRACT:
The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I,the substituents being defined in the specification;as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

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Hennequin et al., “Design and Structure-Activity Relationship of a New Class of Potent VEGF Receptor Tyrosine Kinase Inhibitors,” J. Med. Chem., vol. 42, No. 26, pp. 5369-5389 (1999).
Ishihara H. et al., “Pharmacological Characterization of a novel, potent and selective phosphodiesterase 5 inhibitor, E4010,” Jpn. J. Pharmacol., vol. 76, p. 175 (1998).
Watanabe N. et al., “4-benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5,” J. Med. Chem., vol. 41, pp. 3367-3372 (1998).

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