Synergistic nutritional compositions for treating seizures and chronic inflammatory diseases

Inventors

SAMANT, Rajaram • Tongra, Rajendra Prasad

Assignees

Celagenex Research India Pvt Ltd

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Publication Number

US-11229626-B2

Patent

Publication Date

2022-01-25

Expiration Date


Abstract

The invention disclosed herein relates to novel synergistic nutritional compositions for treating seizures and chronic inflammatory diseases. Particularly, the invention relates to potent and stable synergistic nutritional composition comprising combination of therapeutically active non-competitive amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPAR) antagonists and nuclear factor erythroid 2-related factor 2 (NRF2) activators, present in weight ratio of 1:0.001 to 1:0.5, along with pharmaceutically acceptable excipients. Further, the present synergistic nutritional composition is useful for treating conditions associated with seizure, fibrosis and diabetes.

Core Innovation

The invention relates to a stable, synergistic nutritional composition that includes a therapeutic exogenous combination of tridecanoin and white crystalline L-ergothioneine. The composition includes the actives in a defined weight ratio and is described as novel and stable.

The disclosed concept positions tridecanoin as a non-competitive AMPAR antagonist and as an AMPAR antagonist decanoic acid precursor. In combination with L-ergothioneine, the invention describes modulation of cellular signaling related to oxidative stress and antioxidant defense through NRF2 activation and the KEAP1/ARE pathway, together with AMPAR channel inhibition and modulation of mitochondrial function and related bioenergetic parameters.

The invention additionally describes an orally active anti-seizure nutritional composition formed with pharmaceutically acceptable excipients. It specifies a synergistic combination of tridecanoin and L-ergothioneine with an alternate weight-ratio range and frames the resulting composition as useful for treating neurological seizure disorders and related chronic conditions.

Claims Coverage

The independent claims define two composition variants. Both center on a synergistic, stable nutritional formulation using tridecanoin and white crystalline L-ergothioneine with defined weight-ratio ranges and pharmaceutically acceptable excipients, with one claim further specifying oral activity and anti-seizure use.

Therapeutic exogenous tridecanoin and L-ergothioneine nutritional composition

A novel, stable, synergistic nutritional composition comprising a therapeutic exogenous combination of an effective amount of tridecanoin and white crystalline L-ergothioneine, present in a weight ratio of 1:0.001 to 1:0.5 along with pharmaceutically acceptable excipients.

Orally active anti-seizure nutritional composition of tridecanoin and L-ergothioneine

A stable, orally active anti-seizure nutritional composition comprising a synergistic combination of a therapeutically effective amount of tridecanoin and L-ergothioneine, wherein the tridecanoin and the L-ergothioneine are present in a weight ratio of 1:0.002 to 1:0.2 along with pharmaceutically acceptable excipients.

Overall, the claim coverage protects two composition variants that both require tridecanoin and white crystalline L-ergothioneine in defined weight-ratio ranges plus pharmaceutically acceptable excipients, with one independent claim also specifying oral activity and anti-seizure use.

Stated Advantages

Stable synergistic nutritional composition.

Orally active anti-seizure nutritional composition.

Useful for treating a broad range of neurological seizure disorders and related conditions, including multiple additional diseases.

Documented Applications

Treatment of neurological seizure disorders, including epilepsy and seizure types such as reflex epilepsy, epileptic seizures, nonepileptic seizures, provoked seizures, idiopathic generalized epilepsy, convulsion, absence seizures, atonic seizures, tonic seizures, clonic seizures, myoclonic seizures, febrile seizure, generalized seizures, focal seizures, temporal lobe seizures, neocortical epilepsy, and infantile spasms.

Treatment of additional diseases described in the document, including fibrotic disorder, kidney diseases associated with nephrectomy, renal fibrosis, glomerular sclerosis, end stage renal disease, diabetic nephropathy, renal failure progression associated with hypertension, infarct, tumor, diabetes mellitus, autoimmunity, and alcoholic fatty liver disease (ALFD) with insulin regulation.

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