US2013289000A1PendingUtilityA1
Boron-containing small molecules
Est. expirySep 4, 2028(~2.1 yrs left)· nominal 20-yr term from priority
A61P 7/06A61P 9/00A61P 9/10A61P 9/14A61P 37/08A61P 9/04A61P 43/00A61P 3/10A61P 39/00A61P 31/04A61P 31/18A61P 3/00A61P 25/00A61P 29/00A61P 33/06A61P 27/14A61P 31/08A61P 25/28A61P 27/02A61P 17/06A61P 17/00A61P 1/04A61P 17/02A61P 1/18A61P 11/00A61P 11/06A61P 13/12A61P 19/02A61P 1/16C07F 5/025A61P 1/00A61P 19/08A61P 21/00
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Claims
Abstract
This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound having a structure according to the formula:
wherein
X is selected from the group consisting of CH, C(CN), CR b and N;
Y is selected from the group consisting of CH, C(CN), CR b and N;
a is 0 or 1;
b is 0 or 1;
R d is selected from the group consisting of H, unsubstituted C 1 -C 6 alkyl, COR 10 , and —C(O)OR 10 ,
wherein R 10 is H or unsubstituted C 1 -C 6 alkyl;
with the proviso that when X or Y is C(CN), then a is 0;
with the proviso that when X or Y is CR b , then b is 0;
with the proviso that X and Y cannot both be C(CN);
with the proviso that X and Y cannot both be CR b ;
R b is selected from the group consisting of OR 4 , NR 4 R 5 , SR 4 , —S(O)R 4 , —S(O) 2 R 4 , —S(O) 2 NR 4 R 5 , —C(O)R 4 , —C(O)OR 4 , —C(O)NR 4 R 5 , nitro, cyano, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl,
wherein
R 4 and R 5 are each independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl
with the proviso that that R 4 and R 5 , together with the atoms to which they are attached, are optionally combined to form a 5- to 7-membered substituted or unsubstituted heterocycloalkyl ring
or a salt thereof.
2 . The compound of claim 1 , having a structure which is
3 . The compound of claim 1 , having a structure which is
4 . The compound of claim 1 , having a structure which is
5 . The compound of claim 1 , having a structure which is
6 . The compound of claim 1 , having a structure which is
7 . The compound of claim 1 , having a structure which is
8 . The compound of a preceding claim, wherein R b is OR 4 , and R 4 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl.
9 . The compound of a preceding claim, wherein R b is OR 4 , and R 4 is substituted or unsubstituted alkyl.
10 . The compound of claim 1 , having a structure which is selected from the group consisting of
11 . The compound of any of claims 1 - 8 , wherein R b is OR 4 , and R 4 is cycloalkylsubstituted alkyl.
12 . The compound of claim 1 , having a structure which is selected from the group consisting of
13 . The compound of any of claims 1 - 8 , wherein R b is OR 4 , and R 4 is substituted or unsubstituted heteroalkyl.
14 . The compound of claim 1 , having a structure which is selected from the group consisting of
15 . The compound of any of claims 1 - 8 , wherein R b is NR 4 R 5 , and R 4 and R 5 are each independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl.
16 . The compound of any of claims 1 - 8 , wherein R b is NHR 5 , and R 5 is selected from the group consisting of substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl.
17 . The compound of any of claims 1 - 8 , wherein R b is NHR 5 , and R 5 is substituted or unsubstituted heteroalkyl.
18 . The compound of claim 1 , having a structure which is selected from the group consisting of
19 . A pharmaceutical formulation comprising:
(a) the compound of any preceding claim; (b) a pharmaceutically acceptable excipient.
20 . The formulation of claim 19 , wherein the formulation is in a unit dosage form.
21 . The formulation of claim 19 , wherein the formulation is for oral or topical use.
22 . A method of decreasing the release of a cytokine or a chemokine, the method comprising: contacting a cell with the compound of claim 1 , wherein the release of the cytokine or chemokine by the cell is decreased.
23 . The method according to claim 22 , wherein the cytokine is selected from the group consisting of IL-1α, IL-1β, IL-2, IL-3, IL-6, IL-7, IL-9, IL-12, IL-17, IL-18, IL-23, TNF-α, LT, LIF, Oncostatin, IFNα, IFNβ and IFN-γ.
24 . The method according to claim 22 , wherein the cytokine is selected from the group consisting of IL-1β, IL-2, IL-4, IL-5, IL-6, IL-8, IL-10, IL-12, IL-23, TNF-α and IFN-γ.
25 . The method according to claim 22 , wherein the cytokine is selected from the group consisting of IL-2, IL-5, IL-10, IL-12, IL-23, TNF-α and IFN-γ.
26 . The method according to claim 22 , wherein the chemokine is selected from the group consisting of IL-8, Gro-α, MIP-1, MCP-1, PGE2, ENA-78, and RANTES.
27 . A method of treating a condition, in an animal, the method comprising administering to the animal a therapeutically effective amount of the compound of claim 1 , thereby treating the condition.
28 . The method of claim 27 , wherein the condition is selected from the group consisting of arthritis, rheumatoid arthritis, an inflammatory bowel disease, psoriasis, a pulmonary disease, multiple sclerosis, a neurodegenerative disorder, congestive heart failure, stroke, aortic valve stenosis, kidney failure, lupus, pancreatitis, allergy, fibrosis, anemia, atherosclerosis, a metabolic disease, a bone disease, a cardiovascular disease, a chemotherapy/radiation related complication, diabetes type I, diabetes type II, a liver disease, a gastrointestinal disorder, an ophthamological disease, allergic conjunctivitis, diabetic retinopathy, Sjogren's syndrome, uveitis, a pulmonary disorder, a renal disease, dermatitis, HIV-related cachexia, cerebral malaria, ankylosing spondolytis, leprosy, anemia and fibromyalgia.
29 . The method of claim 27 , wherein the condition is selected from the group consisting of psoriasis, atopic dermatitis, rheumatoid arthritis, an inflammatory bowel disease, asthma and chronic obstructive pulmonary disease.
30 . The method of claim 27 , wherein the condition is psoriasis, said psoriasis is selected from the group consisting of plaque psoriasis, flexural psoriasis, Guttate psoriasis, pustular psoriasis, nail psoriasis and erythrodermic psoriasis.
31 . The method of claim 30 , wherein the psoriasis is selected from the group consisting of plaque psoriasis and nail psoriasis.
32 . A method of inhibiting a phosphodiesterase (PDE), the method comprising: contacting the phosphodiesterase with a compound of claim 1 , thereby inhibiting the phosphodiesterase.
33 . The method of claim 32 , wherein said phosphodiesterase is selected from the group consisting of phosphodiesterase4 (PDE4) and phosphodiesterase7 (PDE7).Join the waitlist — get patent alerts
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