| Hepta-, octa-and nonapeptides having antiangiogenic activity -> Monitor Keywords |
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Hepta-, octa-and nonapeptides having antiangiogenic activityRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 9 To 11 Peptide Repeating Units In Known Peptide ChainHepta-, octa-and nonapeptides having antiangiogenic activity description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060194737, Hepta-, octa-and nonapeptides having antiangiogenic activity. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority to U.S. Provisional Patent Application Ser. No. 60/335,017, filed on Oct. 31, 2001, which is hereby incorporated by reference. TECHNICAL FIELD [0002] The present invention relates to methods of inhibiting angiogenesis, methods of treating cancer, and compounds having activity useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds. BACKGROUND OF THE INVENTION [0003] Angiogenesis is the fundamental process by which new blood vessels are formed and is essential to a variety of normal body activities (such as reproduction, development and wound repair). Although the process is not completely understood, it is believed to involve a complex interplay of molecules which both stimulate and inhibit the growth of endothelial cells, the primary cells of the capillary blood vessels. Under normal conditions these molecules appear to maintain the microvasculature in a quiescent state (i.e., one of no capillary growth) for prolonged periods that may last for weeks, or in some cases, decades. However, when necessary, such as during wound repair, these same cells can undergo rapid proliferation and turnover within as little as five days. [0004] Although angiogenesis is a highly regulated process under normal conditions, many diseases (characterized as "angiogenic diseases") are driven by persistent unregulated angiogenesis. Otherwise stated, unregulated angiogenesis may either cause a particular disease directly or exacerbate an existing pathological condition. For example, the growth and metastasis of solid tumors have been shown to be angiogenesis-dependent. Based on these findings, there is a continuing need for compounds which demonstrate antiangiogenic activity due to their potential use in the treatment of various diseases such as cancer. [0005] Peptides having angiogenesis inhibiting properties have been described in commonly-owned WO01/38397, WO01/38347, WO99/61476, and U.S. patent application Ser. No. 09/915,956. However, it would be desirable to prepare antiangiogenic compounds having improved profiles of activity and smaller size. SUMMARY OF THE INVENTION [0006] In its principle embodiment, the present invention provides a compound of formula (I) TABLE-US-00001 (SEQ ID NO:1) Xaa.sub.1-Xaa.sub.2-Xaa.sub.3-Xaa.sub.4-Xaa.sub.5-Xaa.sub.6-Xaa.sub.7-Xaa- .sub.8-Xaa.sub.9- Xaa10 (I), or a therapeutically acceptable salt thereof, wherein Xaa.sub.1 is selected from the group consisting of hydrogen and R--(CH.sub.2).sub.n--C(O)--, wherein n is an integer from 0 to 8 and R is selected from the group consisting of alkoxy, alkyl, amino, aryl, carboxyl, cycloalkenyl, cycloalkyl, and heterocycle; [0007] Xaa.sub.2 is selected from the group consisting of alanyl, D-alanyl, (1S,3R)-1-aminocyclopentane-3-carbonyl, (1S,4R)-1-aminocyclopent-2-ene-4-carbonyl, (1R,4S)-1-aminocyclopent-2-ene-4-carbonyl, asparaginyl, 3-cyanophenylalanyl, 4-cyanophenylalanyl, 3,4-dimethoxyphenylalanyl, 4-fluorophenylalanyl, 3-(2-furyl)alanyl, glutaminyl, D-glutaminyl, glycyl, lysyl(N-epsilon acetyl), 4-methylphenylalanyl, norvalyl, and sarcosyl; [0008] Xaa.sub.3 is selected from the group consisting of alanyl, (1R,4S)-1-aminocyclopent-2-ene-4-carbonyl, arginyl, asparaginyl, D-asparaginyl, t-butylglycyl, citrullyl, cyclohexylglycyl, glutaminyl, D-glutaminyl, glutamyl, glycyl, histidyl, isoleucyl, leucyl, lysyl(N-epsilon-acetyl), methionyl, norvalyl, phenylalanyl, N-methylphenylalanyl, prolyl, seryl, 3-(2-thienylalanyl), threonyl, valyl, and N-methylvalyl; [0009] Xaa.sub.4 is selected from the group consisting of D-alanyl, D-alloisoleucyl, D-allylglycyl, D-4-chlorophenylalanyl, D-citrullyl, D-3-cyanophenylalanyl, D-homophenylalanyl, D-homoseryl, isoleucyl, D-isoleucyl, D-leucyl, N-methyl-D-leucyl, D-norleucyl, D-norvalyl, D-penicillaminyl, D-phenylalanyl, D-prolyl, D-seryl, D-thienylalanyl, and D-threonyl; [0010] Xaa.sub.5 is selected from the group consisting of allothreonyl, aspartyl, glutaminyl, D-glutaminyl, N-methylglutaminyl, N-methylglutamyl, glycyl, histidyl, homoseryl, isoleucyl, lysyl(N-epsilon-acetyl), methionyl, seryl, N-methylseryl, threonyl, D-threonyl, tryptyl, tyrosyl, and tyrosyl(O-methyl); [0011] Xaa.sub.6 is selected from the group consisting of alanyl, N-methylalanyl, allothreonyl, glutaminyl, glycyl, homoseryl, leucyl, lysyl(N-epsilon-acetyl), norleucyl, norvalyl, D-norvalyl, N-methylnorvalyl, octylglycyl, ornithyl(N-delta-acetyl), 3-(3-pyridyl)alanyl, sarcosyl, seryl, N-methylseryl, threonyl, tryptyl, valyl, and N-methylvalyl; [0012] Xaa.sub.7 is selected from the group consisting of alanyl, alloisoleucyl, aspartyl, citrullyl, isoleucyl, D-isoleucyl, leucyl, D-leucyl, lysyl(N-epsilon-acetyl), D-lysyl(N-epsilon-acetyl), N-methylisoleucyl, norvalyl, phenylalanyl, prolyl, and D-prolyl; [0013] Xaa.sub.8 is selected from the group consisting of arginyl, D-arginyl, citrullyl, glutaminyl, histidyl, homoarginyl, lysyl, lysyl(N-epsilon-isopropyl), omithyl, and 3-(3-pyridyl)alanyl; [0014] Xaa.sub.9 is absent or selected from the group consisting of N-methyl-D-alanyl, 2-aminobutyryl, D-glutaminyl, homoprolyl, hydroxyprolyl, leucyl, prolyl, D-prolyl, and D-valyl; and [0015] Xaa.sub.10 is selected from the group consisting of D-alanylamide, azaglycylamide, glycylamide, D-lysyl(N-epsilon-acetyl)amide, a group represented by the formula --NH--(CH.sub.2).sub.n--CHR.sup.1R.sup.2; and a group represented by the formula --NHR.sup.3, wherein n is an integer from 0 to 8; R.sup.1 is selected from the group consisting of hydrogen, alkyl, cycloalkenyl, and cycloalkyl; R.sup.2 is selected from the group consisting of hydrogen, alkoxy, alkyl, aryl, cycloalkenyl, cycloalkyl, heterocycle, and hydroxyl, with the proviso that when n is 0, R.sup.2 is other than alkoxy or hydroxyl; and R.sup.3 is selected from the group consisting of hydrogen, cycloalkenyl, cycloalkyl, and hydroxyl. [0016] In a preferred embodiment, the present invention provides a compound of formula (I), or a therapeutically acceptable salt thereof, wherein Xaa.sub.2 is selected from the group consisting of alanyl, D-alanyl, asparaginyl, 4-cyanophenylalanyl, 4-methylphenylalanyl, and norvalyl; and Xaa.sub.1, Xaa.sub.3, Xaa.sub.4, Xaa.sub.5, Xaa.sub.6, Xaa.sub.7, Xaa.sub.8, Xaa.sub.9, and Xaa.sub.10 are as described for formula (I). [0017] In another preferred embodiment, the present invention provides compound of formula (I), or a therapeutically acceptable salt thereof, wherein Xaa.sub.2 is selected from the group consisting of glutaminyl and D-glutaminyl, and Xaa.sub.1, Xaa.sub.3, Xaa.sub.4, Xaa.sub.5, Xaa.sub.6, Xaa.sub.7, Xaa.sub.8, Xaa.sub.9, and Xaa.sub.10 are as described for formula (I). [0018] In another preferred embodiment, the present invention provides a compound of formula (I), or a therapeutically acceptable salt thereof, wherein Xaa.sub.2 is glycyl; Xaa.sub.3 is selected from the group consisting of arginyl, asparaginyl, D-asparaginyl, citrullyl, lysyl(N-epsilon-acetyl), and histidyl; and Xaa.sub.1, Xaa.sub.4, Xaa.sub.5, Xaa.sub.6, Xaa.sub.7, Xaa.sub.8, Xaa.sub.9, and Xaa.sub.10 are as described for formula (I). [0019] In another preferred embodiment, the present invention provides a compound of formula (I), or a therapeutically acceptable salt thereof, wherein Xaa.sub.2 is glycyl; Xaa.sub.3 is selected from the group consisting of valyl and N-methylvalyl, Xaa.sub.6 is selected from the group consisting of norvalyl and N-methylnorvalyl; and Xaa.sub.1, Xaa.sub.4, Xaa.sub.5, Xaa.sub.7, Xaa.sub.8, Xaa.sub.9, and Xaa.sub.10 are as described for formula (I). Continue reading about Hepta-, octa-and nonapeptides having antiangiogenic activity... 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