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US 10,092,578 B2Granted
Active agents and their oligomers and polymers
AssigneePolymerix, Inc.
InventorsSuseela Kanamathareddy, Karen J. Giroux
Life of this patent
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Abstract
Conjugates comprising at least two active agents linked by a diglycolic acid or polyglycol diacid linker are disclosed. The invention also concerns oligomers and polymers of these conjugates and their use in therapeutic and industrial applications for localized, immediate or fast release delivery of an active agent, such as an anti-microbial, anti-infective, or antiseptic agent.
Claims16
A compound according to formula (I):
- wherein
- each D is the same or different and is a therapeutic agent selected from 4-sulfanilamidosalicylic acid, amoxicillin, apalcillin, apicycline, aspoxicillin, biapenem, cefadroxil, cefamandole, cefatrizine, cefbuperazone, cefdinir, cefonicid, cefoperazone, cefpiramide, cefprozil, flomoxef, imipenem, lucensomycin, lymecycline, meropenem, moxalactam, nadifloxacin, panipenem, ritipenem, salazosulfadimidine, sulfaloxic acid, carzinophillin A, denopterin, mycophenolic acid, streptonigrin, doxorubicin, paclitaxel, gemcitabine, mycophenolic acid, diflunisal, fendosal, gentisic acid, mesalamine, salicylic acid, salsalate, and sulfasalazine,
- R1 is selected from the group consisting of [(CH2)xO]y(CH2)z—, —(CH2)y—, —[CH═CH—O]y(CH2)z—, —[(CH═CH—CH2—O]y(CH2)z—, [CH2—CH═CH—O]y(CH2)z—, —[(CH2)xO]y(CH═CH)—,
- wherein w is 1 or 2,
- x is 2 or 3, and
- y is equal to an integer from 1 to 10, from 1 to 4, or from 1 to 3,
- z is equal to 1 or 2, and
- the carbon atoms of R1 may be optionally substituted with substituents selected from the group consisting of C1 to C12 alkyl, C1 to C12 alkoxy, C3 to C12 cycloalkyl, C3 to C12 cycloalkoxy, C1 to C12 alkanoyl, C1 to C12 alkanoyloxy, C1 to C12 alkoxy carbonyl, C1 to C12 alkylthio, azido, cyano, nitro, fluoro, chloro, bromo, iodo, hydroxy, oxo, carboxy, aryl, aryloxy, heteroaryl, and heteroaryloxy;
- each X is the same or different and is selected from the group consisting of —O—, —NR2—, —S—, —SO—, and —SO2—,
- wherein R2 is an alkyl group of 1 to 12 carbon atoms.
7 more elements
A topical composition comprising the compound:
- and a dermatologically or pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.