# US 7,745,426 B2 · Compositions and methods for reducing the risk of epileptic occurrence and/or for treatment of seizure disorders > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,745,426 B2 - Document ID: US7745426B2 - Status: Granted - Kind: B2 - Application number: 10/568,152 - Filed: 2004-08-12 - Published: 2006-10-19 - Granted: 2010-06-29 - Earliest claimed: 2003-08-14 - Assignees: D-Pharm Ltd.; Advanced Neuroprotective Systems Ltd. - Inventors: Svetlana Dolina; Vitaly Shteiman; Marina Vinnikova; Israel Shapiro - Web page: https://patentgrep.com/patent/US7745426B2 ## CPC - C07D 213/63: One oxygen atom - A61P 25/08: Antiepileptics; Anticonvulsants - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C07D 401/12: linked by a chain containing hetero atoms as chain links - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs. ## Claims ### Claim 1 A compound of the formula (I): wherein R′ represents an anti-epileptic drug moiety or an anticonvulsive drug moiety; wherein the drug moiety is selected from the group consisting of phenytoin and other hydantoins; phenobarbital and other barbiturates; primidone, carbamazepine and oxacarbamazepine, valproic acid or its derivatives; oxazolidines; benzo-diazepines; felbamate; gabapentin; lamotrigine; vigabatrin and adrenocorticotropic hormone (ACTH); γ-aminobutyric acid and kynurenic acid; and R is selected from the group consisting of —CH2OH, —CHO and —CH2NH2; or pharmaceutically acceptable salts thereof. ### Claim 2 (depends on 1) The compound according to claim 1, wherein said anti-epileptic drug is selected from the group consisting of phenytoin and other hydantoins; phenobarbital and other barbiturates, primidone, carbamazepine and oxacarbamazepine, valproic acid or its derivatives; oxazolidines; benzo-diazepines; felbamate, gabapentin, lamotrigine, vigabatrin and adrenocorticotropic hormone (ACTH). ### Claim 3 (depends on 1) The compound according to claim 1, wherein R′ represents a moiety of γ-aminobutyric acid and kynurenic acid. ### Claim 4 A pharmaceutical composition comprising a therapeutically effective amount of the compound of the formula (I): and a pharmaceutically acceptable carrier or excipient, wherein R′ represents an anti-epileptic drug moiety or an anticonvulsive drug moiety; wherein the drug moiety is selected from the group consisting of phenytoin and other hydantoins; phenobarbital and other barbiturates; primidone, carbamazepine; and oxacarbamazepine, valproic acid or its derivatives; oxazolidines; benzo-diazepines; felbamate; gabapentin; lamotrigine; vigabatrin and adrenocorticotropic hormone (ACTH); γ-aminobutyric acid and kynurenic acid; and R is selected from the group consisting of —CH2OH, —CHO and —CH2NH2; or pharmaceutically acceptable salts thereof. ### Claim 5 (depends on 4) The pharmaceutical composition according to claim 4, wherein the compound of the formula (I) having R′ in an amount which is no greater than the maximal safe amount for a single administration of the attached anti-epileptic drug moiety or anticonvulsive drug moiety. ### Claim 6 A method of treatment of epilepsy comprising administering to an individual in need thereof a therapeutically effective amount of a compound of the formula (I): wherein R′ represents an anti-epileptic drug moiety or an anticonvulsive drug moiety; wherein the drug moiety is selected from the group consisting of phenytoin and other hydantoins; phenobarbital and other barbiturates; primidone, carbamazepine and oxacarbamazepine, valproic acid or its derivatives; oxazolidines; benzo-diazepines; felbamate; gabapentin; lamotrigine; vigabatrin and adrenocorticotropic hormone (ACTH); γ-aminobutyric acid and kynurenic acid; and R is selected from the group consisting of —CH2OH, —CHO and —CH2NH2; or pharmaceutically acceptable salts thereof. ### Claim 7 A method for preventing epileptic episodes, alleviating epileptic episodes and/or reducing side effects of anti-epileptic drugs comprising the step of administering to a subject a therapeutically effective amount of a compound of the formula (I): wherein R′represents an anti-epileptic drug moiety or an anticonvulsive drug moiety; wherein the drug moiety is selected from the group consisting of phenytoin and other hydantoins; phenobarbital and other barbiturates; primidone, carbamazepine and oxacarbamazepine, valproic acid or its derivatives; oxazolidines; benzo-diazepines; felbamate; gabapentin; lamotrigine; vigabatrin and adrenocorticotropic hormone (ACTH); γ-aminobutyric acid and kynurenic acid; and R is selected from the group consisting of —CH2OH, —CHO and —CH2NH2; or pharmaceutically acceptable salts thereof. ### Claim 8 (depends on 6) The method according to claim 6, wherein said compound is orally administered.