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US 8,716,310 B2Granted
Dual mechanism inhibitors for the treatment of disease
AssigneeAerie Pharmaceuticals, Inc.
InventorsMitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Abstract
Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Claims12
A compound according to Formula II:
- and salts thereof,
- wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, aryl, C1-C4 alkyl aryl, C1-C4 alkyl heteroaryl, C1-C4 alkyl heterocyclyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 carbonyl, C1-C4 carbonylamino, C1-C4 alkoxy, C1-C4 sulfonyl, C1-C4 sulfonylamino, C1-C4 thioalkyl, C1-C4 carboxyl, or form a ring with each other or with A;
- wherein R3 is hydrogen;
- wherein A is C1-C4 alkyl;
- wherein B is hydrogen, an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, C1-C22 alkyl, C1-C22 alkyl aryl, C1-C22 alkyl heteroaryl, C2-C22 alkenyl, C2-C22 alkynyl, C1-C22 carbonyl, C1-C22 carbonylamino, C1-C22 alkoxy, C1-C22 sulfonyl, C1-C22 sulfonylamino, C1-C22 thioalkyl, or C1-C22 carboxyl;
- wherein X1, X2, and X3 are, independently, hydrogen, halogen, or C1-C4 alkyl;
- wherein the double circle indicates a phenyl ring;
- and
- wherein each Z is independently a bond or C1-C4 alkyl.
6 more elements
Dependencies are inferred from the claim text.