Methods for inhibiting angiogenesis
First Claim
Patent Images
1. A method of inhibiting angiogenesis in a tissue or organ in which same is intended, said method comprising contacting said tissue or organ with an anti-angiogenic amount of a compound having the formula:
- ##STR9## or a pharmaceutically acceptable salt thereof;
wherein;
R1 is C1 -C6 -alkyl;
R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ;
R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ;
Y is O or S; and
X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil.
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Accused Products
Abstract
The present invention relates to methods for effectively inhibiting unwanted angiogenesis. More particularly, this invention relates to methods of treating diseases that show unwanted angiogenesis and to delivering anti-angiogenic activity to a mammal. In other aspects this invention relates to methods of reducing the level of tumor necrosis factor α.
21 Citations
24 Claims
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1. A method of inhibiting angiogenesis in a tissue or organ in which same is intended, said method comprising contacting said tissue or organ with an anti-angiogenic amount of a compound having the formula:
- ##STR9## or a pharmaceutically acceptable salt thereof;
wherein;R1 is C1 -C6 -alkyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; Y is O or S; and X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- ##STR9## or a pharmaceutically acceptable salt thereof;
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8. A method of treating a mammalian disease associated with undesired and uncontrolled angiogenesis and treatable by inhibiting same, said method comprising administering to a mammal in need thereof an anti-angiogenic amount of a compound having the formula ##STR10## or a pharmaceutically acceptable salt thereof;
- wherein;
R1 is C1 -C6 -alkyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; Y is O or S; and X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil. - View Dependent Claims (9, 10, 11, 12, 14)
- wherein;
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13. A method of inhibiting the vascularization of endothelial cells, said method comprising contacting a tissue or organ comprising said endothelial cells in which same is intended with an anti-angiogenic amount of a compound having the formula ##STR11## or a pharmaceutically acceptable salt thereof;
- wherein;
R1 is C1 -C6 -alkyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; Y is O or S; and X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil. - View Dependent Claims (15, 16, 17)
- wherein;
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18. A method of inhibiting the growth of a tumor in a mammal in need thereof, said method comprising:
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(a) administering to said mammal an anti-angiogenic amount of a compound having the formula;
##STR12## or a pharmaceutically acceptable salt thereof;
wherein;R1 is C1 -C6 -alkyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; Y is O or S; and X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil; and (b) histologically examining the vascularization of said tumor, thereby determining the inhibition of tumor growth. - View Dependent Claims (19, 20)
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21. A method for reducing the level of tumor necrosis factor α
- (TNF-α
) produced by a cell in which same is intended, said method comprising contacting said cell with a compound having the formula;
##STR13## or a pharmaceutically acceptable salt thereof;
wherein;R1 is C1 -C6 -alkyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; R6, R7, R8 and R9 are each independently selected from the group consisting of hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C6 -alkynyl, aryl, hydroxyl, C1 -C6 -alkoxy, halogen, NO2 and NH2 ; Y is O or S; and X is selected from the group consisting of oxygen, sulfur, --CH2 -- and carboxy or is nil. - View Dependent Claims (22, 23, 24)
- (TNF-α
Specification
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- Resources
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Current AssigneeLarge Scale Biology Corporation, SRI International, Inc.
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Original AssigneeLarge Scale Biology Corporation, SRI International, Inc.
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InventorsHiebert, Charles, Laderoute, Keith R., Waleh, Nahid, Tuse, Daniel
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Primary Examiner(s)KRASS, FREDERICK F
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Application NumberUS09/274,813Time in Patent Office610 DaysField of Search424/450, 514/532, 514/535, 514/543, 600/562US Class Current514/532CPC Class CodesA61K 31/192 having aromatic groups, e.g...A61K 31/235 having an aromatic ring att...A61P 17/06 AntipsoriaticsA61P 19/02 for joint disorders, e.g. a...A61P 27/02 Ophthalmic agentsA61P 29/00 Non-central analgesic, anti...A61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...A61P 9/10 for treating ischaemic or a...
