Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1995-02-09
1998-01-27
Grumbling, Matthew V.
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
514249, 514250, 544353, 544356, C07D24138
Patent
active
057123950
ABSTRACT:
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.
REFERENCES:
patent: 3435064 (1969-03-01), Schipper et al.
patent: 3582315 (1971-06-01), Soper
patent: 3647793 (1972-03-01), Soper
patent: 4001017 (1977-01-01), Baumann et al.
patent: 5480883 (1996-01-01), Spada et al.
Choudhury, J.C.S. Perkins Transactions, 1974 (1), Oct. 1974, 129-132.
Kane et al., Heterocycles, 16(9), 1981, 1449-1452.
Saeed et al., Chem. Abs. 105:108,033, 1986.
Gazit, Aviv et al., "Tyrphostins. 3. Structure-Activity Relationship Studies of .alpha.-Substituted Benzylidenemalononitrile 5-S-Aryltyrphostins", J. Med. Chem., 36:3556-3564 (1993). derivatives and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising such as active ingredient", Chemical Abstracts, vol. 117, abstract No. 212519, (1990).
Merlin, Jean Claude et al., "Resonance Raman study of phenylhydrazonopropanedinitriles", Can. J. Chem., 63:1840-1844 (1985).
Miyoshi, Hideto et al., "Quantitative analyses of the uncoupling activity of substituted phenols with mitochondria from flight muscles of house flies", Biochimica et Biophysica Acta, 935:312-321 (1988).
Ohmichi, Masahide et al., "The Tyrokinase Kinase Inhibitor Tyrphostin Blocks the Cellular Actions of Nerve Growth Factor", Biochemistry, 32:4650-4658 (1993).
Stout, David M. et al., "Synthesis and Antiarrhythmic and Parasympatholytic Properties of Substituted Phenols. 1. Heteroarylamine Derivatives", J. Med. Chem., 26:808-813 (1983).
Vogel, M. et al., "Synthese von-4-substituierten 329, Heft 1:101-107 (1987).
App Harald
Gazit Aviv
Levitzki Alexander
McMahon Gerald M.
Tang Peng Cho
Grumbling Matthew V.
Sugen
Yissum Research Development Corp.
LandOfFree
Compounds for the treatment of disorders related to vasculogenes does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Compounds for the treatment of disorders related to vasculogenes, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Compounds for the treatment of disorders related to vasculogenes will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-343569