US2012258936A1PendingUtilityA1
Inositol hexakisphosphate analogs and uses thereof
Est. expiryApr 6, 2031(~4.7 yrs left)· nominal 20-yr term from priority
C07F 9/117C07F 9/06A61P 31/04C07F 9/177C07F 9/70
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Claims
Abstract
Provided herein are analog and derivative compounds of inositol hexakisphosphate effective to treat a Clostridium difficile infection and to neutralize the bacterial toxins produced by the same. In addition, methods of treating the C. difficile infection and for neutralizing its toxins with the compounds are provided.
Claims
exact text as granted — not AI-modified1 . An inositol hexakisphosphate analog having a chemical structure of Formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 independently are —PO(OH) 2 , —PS(OH) 2 , —PSe(OH) 2 , or —AsO 3 ; at least one of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 is —PS(OH) 2 , —PSe(OH) 2 , or —AsO 3 ; and R 1 and R 3 are not both —PS(OH) 2 or —PSe(OH) 2 when R 2 , R 4 , R 5 , and R 6 are —PO(OH) 2 .
2 . The analog of claim 1 , wherein R 1 and one of R 2 , R 4 , R 5 , or R 6 are —PS(OH) 2 .
3 . The analog of claim 1 , wherein R 1 , R 2 , and one of R 3 , R 4 , R 5 , or R 6 are —PS(OH) 2 .
4 . The analog of claim 1 , wherein R 1 , R 4 , and one of R 2 , R 3 , R 5 , or R 6 are —PS(OH) 2 .
5 . The analog of claim 1 , wherein R 1 , R 5 , and one of R 2 , R 3 , R 4 , or R 6 is —PS(OH) 2 .
6 . The analog of claim 1 , wherein R 1 , R 6 and one of R 2 , R 3 , R 4 , or R 5 are —PS(OH) 2 .
7 . The analog of claim 1 , wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are —PS(OH) 2 .
8 . The analog of claim 7 , wherein the inositol analog is a myo-inositol analog.
9 . The analog of claim 1 , wherein R 1 and one of R 2 , R 4 , R 5 , or R 6 are —PSe(OH) 2 .
10 . The analog of claim 1 , wherein R 1 , R 2 , and one of R 3 , R 4 , R 5 , or R 6 are —PSe(OH) 2 .
11 . The analog of claim 1 , wherein R 1 , R 4 , and one of R 2 , R 3 , R 5 , or R 6 are —PSe(OH) 2 .
12 . The analog of claim 1 , wherein R 1 , R 5 , and one of R 2 , R 3 , R 4 , or R 6 is —PSe(OH) 2 .
13 . The analog of claim 1 , wherein R 1 , R 6 and one of R 2 , R 3 , R 4 , or R 5 are —PSe(OH) 2 .
14 . The analog of claim 1 , wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are —PSe(OH) 2 .
15 . The analog of claim 14 , wherein the inositol analog is a myo-inositol analog.
16 . The analog of claim 1 , wherein nitric oxide (NO) is bound to at least one of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 .
17 . The analog of claim 16 , wherein NO is bound to —PS(OH) 2 , or —PSe(OH) 2 .
18 . The analog of claim 16 , wherein NO is covalently bound.
19 . The analog of claim 16 , wherein NO is ionically bound.
20 . A pharmaceutical composition comprising the analog of claim 1 and a pharmaceutically acceptable carrier.
21 . A method for neutralizing a Clostridium difficile bacterial toxin, comprising contacting the C. difficile bacterial toxin with the analog of claim 1 .
22 . The method of claim 21 , wherein the Clostridium difficile bacterial toxin is TcdA, TcdB, or TcdA and TcdB.
23 . A method for treating a subject having a Clostridium difficile infection, comprising: administering to the subject an effective dose of the analog of claim 1 .
24 . The method of claim 23 , wherein the analog is administered orally.
25 . An inositol hexakisphosphate analog having a chemical structure of Formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 independently are —PO(OH) 2 , or —PO(OH) 2 NO, and at least one of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 is —PO(OH) 2 NO.Cited by (0)
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