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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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.
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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