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US 12,595,243 B2Granted
Modulators of extracellular signal-regulated kinase
AssigneeGen1E Lifesciences Inc.
InventorsAdam Galan, Ritu Lal, Chakk Ramesha
Life of this patent
Estimating the term…
Abstract
Modulators of extracellular signal-regulated kinase, pharmaceutical compositions thereof, and uses of the compound and pharmaceutical compositions thereof for treating cancer and pulmonary diseases are disclosed.
Claims17
A compound having the structure of Formula (2):
- or a pharmaceutically acceptable salt thereof, wherein,
- R2 is selected from —O—, —NH—, and —N(—CH3)—;
- R3 is selected from C1-3 alkane-diyl and C1-3 heteroalkane-diyl;
- R4 is absent or is selected from C1-2 alkane-diyl, C1-2 heteroalkane-diyl, substituted C1-2 alkane-diyl, and substituted C1-2 heteroalkane-diyl;
- R5 is selected from C5-10 cycloalkyl, C5-20 aryl, C5-10 heterocycloalkyl, C5-20 heteroaryl, substituted C5-10 cycloalkyl, substituted C5-20 aryl, substituted C5-10 heterocycloalkyl, and substituted C5-20 heteroaryl;
- and
- R6 is absent or is selected from C1-3 alkyl and C1-3 alkoxy,
- wherein the compound is not selected from:
- 1,1-dioxido-2,3-dihydrothiophen-3-yl naphthalene-2-sulfonate (1);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl [1,1′-biphenyl]-4-sulfonate (17);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-phenoxybenzenesulfonate (18);
- (S)-1,1-dioxido-2,3-dihydrothiophen-3-yl 4-phenoxybenzenesulfonate (21);
- and
- (R)-1,1-dioxido-2,3-dihydrothiophen-3-yl 4-phenoxybenzenesulfonate (22).
11 more elements
A compound selected from:
- 3-([1,1′-biphenyl]-4-ylmethoxy)-2,3-dihydrothiophene 1,1-dioxide (5);
- 3-((4-phenoxybenzyl)oxy)-2,3-dihydrothiophene 1,1-dioxide (6);
- 1-([1,1′-biphenyl]-4-yl)-2-((1,1-dioxido-2,3-dihydrothiophen-3-yl)oxy) ethan-1-one (9);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl [1,1′-biphenyl]-4-ylcarbamate (11);
- 1-([1,1′-biphenyl]-4-yl)-3-(1,1-dioxido-2,3-dihydrothiophen-3-yl) urea (13);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-phenoxybenzoate (23);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl [1,1′-biphenyl]-4-carboxylate (24);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(benzyloxy)benzenesulfonate (27);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-benzylbenzenesulfonate (28);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(phenoxymethyl)benzenesulfonate (29);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-cyclohexylbenzenesulfonate (34);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(cyclohexyloxy)benzenesulfonate (36);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-benzoylbenzenesulfonate (38);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(hydroxy (phenyl)methyl)benzenesulfonate (39);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 2-methyl-4-phenoxybenzenesulfonate (40);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 2-methoxy-4-phenoxybenzenesulfonate (41);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-benzyl-3-methylbenzenesulfonate (42);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 3-methoxy-4-phenoxybenzenesulfonate (43);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(phenylthio)benzenesulfonate (44);
- 1,1-dioxido-2,3-dihydrothiophen-3-yl 4-(phenylsulfonyl)benzenesulfonate (45);
- and
- a pharmaceutically acceptable salt of any of the foregoing.
19 more elements
The compound 1,1-dioxido-2,3-dihydrothiophen-3-yl 2-methyl-4-phenoxybenzenesulfonate (40) or a pharmaceutically acceptable salt thereof:
Dependencies are inferred from the claim text.