US2012059176A1PendingUtilityA1
Anti-inflammatory modalities
Est. expiryMar 24, 2025(expired)· nominal 20-yr term from priority
A61P 37/06A61P 35/00A61P 43/00A61P 35/02A61P 37/00A61P 3/06A61P 9/12A61P 9/00A61P 5/30A61P 9/10A61P 29/00A61P 11/00A61P 19/08C07D 493/04A61P 1/00A61P 11/06A61P 19/02A61P 1/04
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Claims
Claims
exact text as granted — not AI-modified1 . Use of a compound of formula (I) in the manufacture of a medicament for the treatment of an inflammatory disease, wherein the compound of formula (I) is:
and salts thereof wherein:
R 1 and R 2 are independently hydroxy, alkoxy or acyloxy,
R 3 is hydroxy, alkoxy, alkyl or halo, and
X is either ═O or hydrogen and hydroxy.
2 . Use according to claim 1 , wherein R 1 and R 2 are hydroxy.
3 . Use according to claim 1 or 2 , wherein R 3 is methyl, bromo, chloro or hydroxy.
4 . Use according to any one of claims 1 to 3 , wherein X is ═O and the compounds are isoflavan-4-ones of the formula (Ia):
and wherein
R 3 is 5-alkyl, 6-halo or 8-halo,
5 . Use according to claim 4 , wherein R 3 is 5-methyl, 6-chloro or 8-bromo.
6 . Use according to any one of claims 1 to 3 , wherin X is hydrogen and hydroxy and the compounds are isoflavan-4-ols of the formula (Ib):
and wherein
R3 is 8-alkyl or 8-hydroxy.
7 . Use according to claim 6 , wherein R 3 is 8-methyl or 8-hydroxy.
8 . Use according to claim 1 , wherein the compound is an 8-substituted isoflavonoid compound of the formula (Ic):
and salts thereof wherein
R 1 and R 2 are independently hydroxy, alkoxy or acyloxy,
R 3 is hydroxy, alkyl or halo, and
X is either ═O or hydrogen and hydroxy.
9 . Use according to claim 8 , wherein
R 1 and R 2 are hydroxy, and R 3 is hydroxy, methyl or bromo.
10 . Use according to claim 1 wherein the compound of formula (I) is selected from compounds 1 to 5:
and pharmaceutically acceptable salts thereof
11 . Use according to any one of claims 1 to 10 , wherein the inflammatory disease or disorder is selected from osteoarthritis, inflammatory bowel disease (ulcerative colitis and Crohn's disease), ulcerative proctitis, distal colitis, autoimmune disorders (SLE, rheumatoid arthritis, glomerulonephritis), asthma and diseases involving pulmonary inflammation, cardiovascular disorders including atherosclerosis, hypertension and lipid dyscrasias and disorders associated with estrogen receptor activation.
12 . Use according to claim 11 , wherein the treatment is for pain, oedema and/or erythema associated with inflammation.
13 . Use according to any one of claims 1 to 12 , wherein the treatment of the inflammatory disorder is absent cardiovascular side effects, is cardioprotective and/or is gut protective.
14 . Use of a thromboxane synthase inhibitor for the manufacture of a medicament for the treatment of inflammation, including pain associated with inflammation.
15 . Use according to claim 14 , wherein the treatment is cardioprotective and/or gut protective.
16 . A pharmaceutical agent comprising a compound of formula (I) according to any one of claims 1 to 10 for the treatment of inflammatory diseases and disorders or as a thromboxane synthase inhibitor.Join the waitlist — get patent alerts
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