Methods, compositions, and formulations for preventing or reducing adverse effects in a patient
OwnerRichard R. Stoverinventor
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Abstract
The present invention provides transdermal administration of AICA riboside, or a prodrugs, analogs, or salts thereof, and/or a blood clotting inhibitor for preventing or reducing adverse side effects in a patient. The type of patient that may benefit includes a patient with decreased left ventricular function, a patient with a prior myocardial infarction, a patient undergoing non-vascular surgery, or a fetus during labor and delivery.
Claims45
A transdermal drug delivery system that substantially maintains contact with a mucous or dermal layer, wherein said system comprises a drug dosing form comprising an AICA riboside compound or analogs thereof, wherein said compound comprises a general formula:
- wherein R1 is a phosphate group, CH2, CO, CH2NH, —NHCH2, —CH2NHCH2, CH2NHCH2R4, —CH2—N(R5)CH2—, —CO—CO—, CH2(R5)N—, CH(R5), S, CH2(CO), N(R5) wherein R5 is hydrogen, optionally substituted C1-12 alkyl, C3-12 cycloalkyl, C1-6 alkoxy, C1-6 alkyl, aryl or heteroaryl, where R1 is not a hydroxyl group;
- R4 is a monocyclic ring comprising 5-7 atoms;
- R3 is NH2;
- R2 is CONH2, CONHCH2R6;
- wherein R6 is a monocyclic ring comprising 5-7 atoms.
A transdermal drug delivery system that substantially maintains contact with a mucous or dermal layer, wherein said system comprises comprising a drug dosing form comprising an AICA riboside compound or analogs thereof, wherein said compound has a general formula:
- or a pharmaceutically acceptable salt thereof wherein X is —O— or —CH2—;
- R1 is hydrogen, amino, hydrocarbylamino, acylamino, or dihydrocarbylaminoalkyleneimino;
- R2 is hydrogen, cyano, hydrocarbylimidate, carboxamideoxime, hydrocarbyloxyamidine, carboxamide, or carboxylic acid or an amide, ester, thioester or salt thereof;
- R3 is hydrogen, hydrocarbyl, amino, hydrocarbylamino, halogen, hydroxy (including tautomeric 2-imidazolone), hydrocarbyloxy, sulfhydryl (including tautomeric 2-imidazolthione), or hydrocarbylthio;
- R4 and R5 are independently hydrogen, alkyl, acyl or hydrocarbyloxycarbonyl;
- R6 is hydrogen, hydrocarbyl, halogen, hydroxy, hydrocarbyloxy, sulfhydryl, hydrocarbylthio, sulfamyloxy, amino, hydrocarbylamino, azido, acyloxy or hydrocarbyloxycarboxy or phosphate ester group or salts thereof;
- provided that when R1 is amino, R2 is unsubstituted carboxamide, R3 is hydrogen;
- R4 and R5 are hydrogen, acyl or hydrocarboxycarbonyl;
- then R6 is not hydroxy, acyloxy or hydrocarbyloxycarboxy.
A method of treating a subject comprising administering transdermally to said subject an AICA riboside compound or analogs thereof to said subject to reduce ischemiarelated disorders, wherein said compound comprises:
- or a combination thereof.
A drug delivery patch that substantially maintains contact with a mucous or dermal layer, wherein said patch comprises a drug dosing form of acadesine.
Dependencies are inferred from the claim text.