Compounds advantageous in the treatment of central nervous system diseases and disorders
Inventors
Pesyan, Amir • Balandrin, Manuel M.
Assignees
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Publication Number
US-9206143-B2
Publication Date
2015-12-08
Expiration Date
Abstract
A series of novel compounds showing anticonvulsant activity is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
Core Innovation
The invention is directed to compounds represented by Formula I, wherein X, Y, and Z define a set of substituted compounds within Formula I. The compounds are central nervous system focused novel amide compounds and are claimed as anticonvulsant agents.
The invention is focused on compounds of Formula I that can be used for treating and/or preventing epilepsy-related conditions through administration to a subject. The background problem being addressed is related to epilepsy and epilepsy-related conditions, including convulsions, spasticity, restlessness syndromes, movement disorders, and status epilepticus.
The disclosure addresses the need for anticonvulsant activity and CNS modulation for CNS diseases, and the compounds are framed as agents that modulate CNS inhibitory/excitatory neurotransmission rather than full suppression, with the aim of avoiding overt sedation and/or paralysis. The compounds are associated with anticonvulsant activity and described as pharmaceutical composition candidates using pharmaceutically acceptable carriers and excipients with a therapeutically effective amount.
Claims Coverage
The independent claim coverage provided includes one independent compound claim (Formula I) with dependent coverage for pharmaceutical compositions and a method of treating and/or preventing epilepsy-related conditions. The inventive features are centered on the Formula I substituent pattern, pharmaceutical compositions containing pharmaceutically acceptable excipients, and treating or preventing epilepsy-related conditions.
Formula I compound substituent definition
A compound represented by Formula I wherein X is one of a Cl atom in the para position, a F atom in the para or meta position, a CF3 group in the para or meta position, a OCF3 group in the para or meta position, or a Cl atom in the meta position and a OCH3 group in the para position; Y is one of a CH3 or H; and Z is one of a CH3 or H.
Pharmaceutical composition with pharmaceutically acceptable excipient and therapeutically effective amount
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of the compound of Formula I.
Carrier-containing pharmaceutical composition
The pharmaceutical composition in which the excipient includes a carrier.
Treating and/or preventing epilepsy-related conditions by administration
A method for treating and/or preventing epilepsy-related conditions by administering to a subject a therapeutically effective amount of the compound of Formula I.
Coverage is anchored on a Formula I substituent framework and extends to pharmaceutical compositions containing pharmaceutically acceptable excipients, including carriers, and to methods of treating and/or preventing epilepsy-related conditions by administration to a subject.
Stated Advantages
Modulates CNS inhibitory/excitatory neurotransmission without full suppression.
Aims to avoid overt sedation and/or paralysis.
Provides anticonvulsant activity for epilepsy and related neurological conditions.
Documented Applications
Treating and/or preventing epilepsy-related conditions by administering the Formula I compound to a subject.
Use as anticonvulsant agents with therapeutic scope including epilepsy/convulsions and status epilepticus.
Stated CNS disease applications include spasticity, anxiety, depression, insomnia, migraine, schizophrenia, Parkinson’s disease, Alzheimer’s disease, and bipolar disorder.
Stated additional applications include chronic/neuropathic pain as an analgesic, neuroprotective agents for stroke/stroke injury, Huntington’s disease, and traumatic brain and/or spinal cord injuries.
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