Method for inhibiting inflammatory disease
First Claim
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1. A method for treating an inflammatory disease, said method comprising administering to an individual having an inflammatory disease a therapeutically effective amount of a compound having the formula:
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or a pharmaceutically acceptable salt thereof;
wherein;
R1 is C1-C6-alkyl;
R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, C1-C5-alkyl, 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-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2 and NH2;
Y is a heteroatom; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy.
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Abstract
The present invention relates to methods for effectively inhibiting inflammatory diseases, such as Crohn'"'"'s disease and ulcerative colitis. In other aspects, this invention relates to methods of reducing or inhibiting granulomas.
45 Citations
20 Claims
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1. A method for treating an inflammatory disease, said method comprising administering to an individual having an inflammatory disease a therapeutically effective amount of a compound having the formula:
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or a pharmaceutically acceptable salt thereof; wherein;
R1 is C1-C6-alkyl;
R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, C1-C5-alkyl, 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-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2 and NH2;
Y is a heteroatom; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, aryl, hydroxyl, C1-C4-alkoxy, halogen, NO2 and NH2;
R6, R7, are each independently selected from the group consisting of hydrogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, aryl, hydroxyl, C1-C4-alkoxy, halogen, NO2 and NH2;
R8 and R9 are iodine; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy.
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3. The method in accordance with claim 1, wherein the compound is methyl-3,5-diiodo-4-(4′
- -methoxyphenoxy)benzoate.
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4. The method in accordance with claim 1, wherein said inflammatory disease is centralized in a tissue or organ.
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5. The method in accordance with claim 1, wherein said compound is formulated in a pharmaceutically acceptable form with an excipient or carrier.
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6. The method in accordance with claim 1, wherein said compound is formulated in a liposome.
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7. The method in accordance with claim 6, wherein said liposome is conjugated to a targeting moiety which is specific for endothelial cells.
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8. The method in accordance with claim 1, wherein said inflammatory disease is an inflammatory bowel disease.
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9. The method in accordance with claim 8, wherein said inflammatory bowel disease is selected from the group consisting of Crohn'"'"'s disease and ulcerative colitis.
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10. The method in accordance with claim 1, wherein said inflammatory disease is selected from the group consisting of psoriasis, sarcoidosis and rheumatoid arthritis.
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11. The method in accordance with claim 1, wherein said inflammatory disease is in a human being.
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12. A method of inhibiting granulomas, said method comprising contacting a tissue or organ having said granulomas with an inhibiting amount of a compound having the formula:
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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 a heteroatom; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy.- View Dependent Claims (13, 14, 15, 16, 17, 18)
R1 is methyl or ethyl; R2, R3, R4 and R5 are each independently selected from group consisting of hydrogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, aryl, hydroxyl, C1-C4-alkoxy, halogen, NO2 and NH2;
R6, R7, are each independently selected from the group consisting of hydrogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, aryl, hydroxyl, C1-C4-alkoxy, halogen, NO2 and NH2;
R8 and R9 are iodine; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy.
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14. The method in accordance with claim 12, wherein the compound is methyl-3,5-diiodo-4-(4′
- -methoxyphenoxy)benzoate.
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15. The method in accordance with claim 12, wherein said granuloma is in a mammalian subject.
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16. The method in accordance with claim 12, wherein said compound is formulated in a pharmaceutically acceptable form with an excipient or carrier.
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17. The method in accordance with claim 12, wherein said compound is formulated in a liposome.
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18. The method in accordance with claim 17, wherein said liposome is conjugated to a targeting moiety which is specific for endothelial cells.
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19. A method for prophylactically treating inflammation, said method comprising administering to an individual who has come in contact with an agent of inflammation a therapeutically effective amount of a compound having the formula:
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or pharmaceutically acceptable salt thereof; wherein;
R1 is C1-C6-alkyl;
R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, C1-C5-alkyl, 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-alkynyl, aryl, hydroxyl, C1-C6-alkoxy, halogen, NO2 and NH2;
Y is a heteroatom; and
X is selected from the group consisting of a bond, oxygen, sulfur, —
CH2— and
carboxy, thereby prophylactically treating inflammation.- View Dependent Claims (20)
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Specification
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Current AssigneeNovici Biotech LLC., SRI International, Inc.
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Original AssigneeLarge Scale Biology Corporation, SRI International, Inc.
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InventorsLaderoute, Keith R., Waleh, Nahid, Tuse, Daniel, Hiebert, Charles
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Primary Examiner(s)KRASS, FREDERICK F
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Application NumberUS09/656,144Time in Patent Office706 DaysField of Search514/532, 514/535, 514/543, 424/450US Class Current514/532CPC Class CodesA61K 31/192 having aromatic groups, e.g...A61K 31/235 having an aromatic ring att...A61K 31/565 not substituted in position...
