Non-sedating barbiturate compounds as neuroprotective agents
AssigneeTaro Pharmaceutical Industries Ltd.
InventorsDaniel A Moros, Barrie Levitt, Avraham Yacobi
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Abstract
Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative side-effects such as anesthesia and death
Claims25
A method for providing neuroprotection in a mammal at risk for cerebral ischemia, comprising administering to the mammal an effective neuroprotective dose of a non-sedating barbiturate.
A method for providing neuroprotection to a mammal in need of neuroprotection, comprising administering to the mammal a non-sedating barbiturate in a dose sufficient to provide a neuroprotective effect, the non-sedating barbiturate having the structure:
- 2
- wherein R1 and R2 may be the same or different and are independently hydrogen;
- lower alkyl, optionally substituted by lower alkoxy;
- CH2OR5, wherein R5 is lower alkyl, alkylaryl or benzyl;
- CO2R6, wherein R6 is lower alkyl or aryl;
- COR7, wherein R7 is hydrogen, lower alkyl or aryl;
- or CH(OR8)2, wherein R8 is a lower alkyl group;
- and
- wherein R3 and R4 may be the same or different and are independently hydrogen;
- aryl optionally containing one or more heteroatoms selected from the group consisting of N, S and O;
- phenyl;
- phenyl substituted with a halogen or lower alkyl group;
- benzyl;
- ring substituted benzyl having one or more halogens, lower alkyl groups or both;
- lower alkyl;
- or lower alkyl substituted with an aromatic moiety;
- provided that at least one of R3 and R4 is an aromatic ring containing moiety;
- and salts thereof.
An article of manufacture comprising a container comprising a pharmaceutical composition and a label with indications for use as a neuroprotectant, the pharmaceutical composition comprising:
- a non-sedating barbiturate pound in an amount effective for neuroprotection upon administration to a subject of neuroprotection;
- and
- a pharmaceutically acceptable carrier or excipient
A method of providing neuroprotection comprising
- (a) identifying a subject in need of cerebral neuroprotection,
- (b) selecting a non-sedative barbiturate compound capable of neuroprotecting said subject, and
- (c) administering to said subject an effective neuroprotective dose of said compound, thereby providing said neuroprotection.
Dependencies are inferred from the claim text.