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US 11,530,181 B2Granted
IL-6 inhibitors and methods of treatment
AssigneeUniversity of Florida Research Foundation, Inc.
InventorsChenglong Li, Liguang Mao
Life of this patent
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Abstract
The instant invention describes compounds having IL-6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.
Claims20
A compound of Formula (XV), or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is selected from the group consisting of pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, oxatriazolyl, pyrazinyl, pyridyl, pyridazinyl, pyrimidinyl, azetidinonyl, azetidinethionyl, pyrrolidinonyl, pyrrolidinethionyl, piperidinonyl, piperidinethionyl, tetrahydropyrimidinonyl, tetrahydropyrimidinethionyl, imidazolidinonyl, imidazolidinethionyl, 1,3-diazetidinonyl, 1,3-diazetidinethionyl, 1,2-oxazetidinyle, 1,2-thiazetidinyl, isoxazolidinyl, isothiazolidinyl, 1,2-oxazinanyl, 1,2-thiazinanyl, pyrimidinedionyl, 5-methylpyrimidine-2,4(1H,3H)-dionyl, isoxazol-5(2H)-onyl, 1,7-dihydro-2H-pyrrolo[2,3-d]pyrimidine-2,4(3H)-dionyl, 1,4,5,6-tetrahydro-7H-indol-7-onyl, 1H-pyrrolo[2,3-b]pyridyl, quinazoline-2,4(1H,3H)-dionyl, furo[2,3-d]pyrimidine-2,4(1H,3H)-dionyl, 1,3-dihydro-2H-benzo[d]imidazol-2-onyl, 1H-indole-4,7-dionyl, 5,6-dimethyl-1H-indole-4,7-dionyl, 5,6-dihydro-1H-indole-4,7-dionyl, 4,5-dihydropyrano[3,4-b]pyrrol-7(1H)-onyl, 1,4,5,6-tetrahydro-7H-pyrrolo[2,3-c]pyridin-7-onyl, 1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-onyl, pyrano[3,4-b]pyrrol-7(1H)-onyl, 1,3-dihydro-2H-imidazol-2-onyl, 4-fluoro-1H-pyrazolyl, 3,4-difluoro-1H-pyrazolyl, 3-fluoro-1H-pyrazolyl, 4-chloro-1H-pyrazolyl, 3,4-dichloro-1H-pyrazolyl, 3-chloro-1H-pyrazolyl, 3-methoxy-1H-pyrazolyl, 1H-pyrazol-3-yl acetate, 4-methoxy-1H-pyrazolyl, 1H-pyrazol-4-yl acetate, N-(1H-pyrazol-4-yl)acetamidyl, N,N-dimethyl-1H-pyrazol-4-amino, N,N-dimethyl-1H-pyrazol-3-amino, 4-(trifluoromethyl)-1H-pyrazolyl, 3-(trifluoromethyl)-1H-pyrazolyl, N-(1H-pyrazol-3-yl)acetamide, and 1H-pyrazol-3-amino;
- each R2 is independently halo, cyano, —OR5, NO2, alkyl, or —NR6R7;
- each R4 is independently halo, cyano, —OR5, NO2, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, or —NR6R7;
- each R5 is independently hydrogen or alkyl;
- each R6 is independently hydrogen or alkyl;
- each R7 is independently hydrogen or alkyl;
- D is —O—;
- Y is a bond, —O—N(R6)—;
- n is 0, 1, or 2;
- o is 0;
- and
- p is 2, 3, or 4.
10 more elements
A compound of formula:
- N-(3-(1H-pyrazol-5-yl)phenyl)-3-(piperidin-1-yl)benzamide (LLM437);
- or
- N-(3-(1H-pyrazol-5-yl)phenyl)-3-(piperidin-1-ylmethyl)benzamide (LLM438);
- or pharmaceutically acceptable salt thereof.
1 more element
Dependencies are inferred from the claim text.