| Hexa-, hepta-, and octapeptides having antiangiogenic activity -> Monitor Keywords |
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Hexa-, hepta-, and octapeptides 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 ChainHexa-, hepta-, and octapeptides having antiangiogenic activity description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070167376, Hexa-, hepta-, and octapeptides having antiangiogenic activity. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application is a divisional application of U.S. patent application Ser. No. 10/283,553, filed Oct. 30, 2002 which claims priority to U.S. Provisional Patent Application Ser. No. 60/335,035, 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 (I) Xaa.sub.1-Xaa.sub.2-Xaa.sub.3-Xaa.sub.4-Xaa.sub.5-Xaa.sub.6-Xaa.sub.7- (SEQ ID NO:1) Xaa.sub.8-Xaa.sub.9, or a therapeutically acceptable salt thereof, wherein [0007] 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; [0008] Xaa.sub.2 is selected from the group consisting of alanyl, (1R,4S)-1-aminocyclopen-2-ene-4-carbonyl, asparaginyl, D-asparaginyl, t-butylglycyl, citrullyl, cyclohexylglycyl, glutaminyl, D-glutaminyl, glutamyl, glycyl, histidyl, isoleucyl, leucyl, lysyl(N-epsilon-acetyl), methionyl, norvalyl, phenylalanyl, prolyl, homoseryl, seryl, thienylalanyl, threonyl, D-valyl, and valyl; [0009] Xaa.sub.3 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.4 is selected from the group consisting of allothreonyl, aspartyl, glutaminyl, D-glutaminyl, N-methylglutaminyl, glycyl, histidyl, homoseryl, isoleucyl, lysyl(N-epsilon-acetyl), methionyl, D-norvalyl, N-methylnorvalyl, seryl, N-methylseryl, threonyl, D-threonyl, tryptyl, tyrosyl, tyrosyl(O-methyl), and N-methylvalyl; [0011] Xaa.sub.5 is selected from the group consisting of alanyl, N-methylalanyl, allothreonyl, arginyl, 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.6 is selected from the group consisting of alanyl, alloisoleucyl, aspartyl, citrullyl, isoleucyl, D-isoleucyl, N-methylisoleucyl, leucyl, D-leucyl, lysyl(N-epsilon-acetyl), D-lysyl(N-epsilon-acetyl), norvalyl, phenylalanyl, prolyl, and D-prolyl; [0013] Xaa.sub.7 is selected from the group consisting of arginyl, D-arginyl, citrullyl, histidyl, homoarginyl, lysyl, lysyl(N-epsilon-isopropyl), ornithyl, and 3-(3-pyridyl)alanyl; [0014] Xaa.sub.8 is absent or selected from the group consisting of N-methyl-D-alanyl, 2-aminobutyryl, 2-aminoisobutyryl, D-glutaminyl, homoprolyl, hydroxyprolyl, leucyl, phenylalanyl, prolyl, D-prolyl, and D-valyl; and [0015] Xaa.sub.9 is selected from the group consisting of D-alanylamide, azaglycylamide, glycylamide, lysyl(N-epsilon-acetyl)amide, D-lysyl(N-epsilon-acetyl)amide, hydroxyl, --NHCH(CH.sub.3).sub.2, 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 another embodiment, the present invention provides a pharmaceutical composition comprising a compound of formula (I), or a therapeutically acceptable salt thereof, in combination with a therapeutically acceptable carrier. [0017] In another embodiment, the present invention provides a method of inhibiting angiogenesis in a mammal in recognized need of such treatment comprising administering to the mammal a therapeutically acceptable amount of a compound of formula (I), or a therapeutically acceptable salt thereof. [0018] In another embodiment, the present invention provides a method of treating cancer in a mammal in recognized need of such treatment comprising administering to the mammal a therapeutically acceptable amount of a compound of claim 1 or a therapeutically acceptable salt thereof. DETAILED DESCRIPTION OF THE INVENTION Continue reading about Hexa-, hepta-, and octapeptides having antiangiogenic activity... 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