Patent classifications
A61P25/10
T type calcium channel inhibitors
The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R.sub.1 is C.sub.1-C.sub.4 alkyl, hydroxy, or C.sub.1-C.sub.4 alkoxy; Z is NH, NCH.sub.3, O, S, or CH.sub.2; Y is NH, O, or CH.sub.2 with the proviso that Y and Z are not the same; R.sub.2 is H, halo, NH.sub.2, C.sub.1-C.sub.4 alkyl, hydroxy, or C.sub.1-C.sub.4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R.sub.3 is H, halo, NH.sub.2, C.sub.1-C.sub.4 alkyl, hydroxy, or C.sub.1-C.sub.4 alkoxy. ##STR00001##
METHODS OF TREATING AND PREVENTING/REDUCING THE LIKELIHOOD OF MESIAL TEMPORAL LOBE EPILEPSY (TLE)
The invention provides methods of treatment that prevent the onset of Mesial temporal lobe epilepsy (TLE) in a subject, or which reduce the severity of TLE in a subject, by administering a NKCC1 inhibitor to the subject after the subject has suffered from an insult known to precipitate TLE.
Conjugate comprising an active MMP-9-binding peptide
The present invention provides a novel peptide that has an amino acid sequence represented by SEQ ID NO: 18, and binds to an active protease but does not bind to a pro-protease.
1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
The present invention relates to novel 1,2,4-triazolo[4,3-a]pyridine compounds as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor subtype 2 (mGluR2). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which mGluR2 subtype of metabotropic receptors is involved.
Dihydroxy aromatic heterocyclic compound
Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
METHODS OF TREATING EPILEPSY OR STATUS EPILEPTICUS
Described herein are methods of treating epilepsy or status epilepticus, e.g., convulsive status epilepticus, e.g., early status epilepticus, established status epilepticus, refractory status epilepticus, super-refractory status epilepticus, e.g., super-refractory generalized status epilepticus; non-convulsive status epilepticus, e.g., generalized status epilepticus, complex partial status epilepticus; generalized periodic epileptiform discharges; periodic lateralized epileptiform discharges; a seizure, e.g., acute repetitive seizures, cluster seizures, the method comprising administering to the subject a neuroactive steroid.
NOVEL PYRIMIDINYL-DIAZOSPIRO COMPOUNDS
The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
Use of cannabinoids in the treatment of epilepsy
The present invention relates to the use of cannabidiol (CBD) in the treatment of focal seizures. In one embodiment the patients suffering from focal seizures are children and young adults. CBD appears particularly effective in reducing focal seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; CDKL5; Neuronal ceroid lipofuscinoses (NCL); febrile infection related epilepsy syndrome (FIRES); Aicardi syndrome and brain abnormalities in comparison to other seizure types. Significantly CBD additionally is very effective in the reduction of a sub-type of focal seizures, focal seizures with impairment.
Use of Cannabinoids in the Treatment of Epilepsy
The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of treatment-resistant epilepsy (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
1,2,4-triazolo[4,3-a]pyridine compounds and their use as positive allosteric modulators of mGluR2 receptors
The present invention relates to novel 1,2,4-triazolo[4,3-a]pyridine compounds as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor subtype 2 (mGluR2). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which mGluR2 subtype of metabotropic receptors is involved.