- NERAMEXANE SALTS
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This invention relates to novel salts of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane).
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Paragraph 0091-0094
(2015/01/06)
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- METHOD OF PREPARING NERAMEXANE
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Method of producing a salt of 1-amino-1,3,3,5,5-pentamethylcyclohexane comprising steps (i) to (v): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone; (ii) converting 3,3,5,5-tetramethylcyclohexanone obtained in step (i) to 1- hydroxy-1,3,3,5,5-pentamethylcyclohexane; (iii) converting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane obtained in step (ii) to 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane; (iv) converting 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane obtained in step (iii) to 1-amino-1,3,3,5,5-pentamethylcyclohexane; wherein at least one of 3,3,5,5-tetramethylcyclohexanone, 1-hydroxy-1,3,3,5,5- pentamethylcyclohexane, 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, is not subjected to a purification step.
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Page/Page column 39
(2011/02/24)
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- METHOD OF PREPARING NERAMEXANE
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Method of preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane or a pharmaceutically acceptable salt thereof, comprising at least two steps selected from the following steps (i) to (iv): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone in the presence of methylmagnesium chloride; (N) converting 3,3,5,5-tetramethylcyclohexanone to 1-hydroxy-1,3,3,5,5- pentamethylcyclohexane in the presence of methylmagnesium chloride; (iii) converting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane to 1-chloroacetamido- 1,3,3,5,5-pentamethylcyclohexane in the presence of chloroacetonitrile in acidic solution; (iv) converting 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane to 1-amino- 1,3,3,5,5-pentamethylcyclohexane in the presence of thiourea in water.
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Page/Page column 41
(2011/02/24)
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- METHOD OF PREPARING 1-AMINO-1,3,3,5,5-PENTAMETHYLCYCLOHEXANE
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The invention relates to a method of producing 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof comprising the step of heating a mixture comprising 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, thiourea and water.
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Page/Page column 13
(2011/02/24)
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- Novel treatment for alzheimer's disease
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The present invention concerns a new pharmaceutical composition comprising an antagonist and a co-agonist of the N-methyl-D-aspartate-type glutamate receptor (NMDAR). The inventors found that the co-administration of these two compounds effectively inhibits production of amyloide-β peptide. In patient's suffering from Alzheimer's disease, these peptides are deposited in the extracellular matrix forming neuritic "plaques". Therefore, the present inventors identified a new possibility for prophylaxis and/or treatment of Alzheimer's disease by stopping the continued formation of neuropathological extracellular deposits.
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- METHODS OF TREATING CNS DISORDERS
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The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.
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- Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
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The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
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- NMDA receptor antagonists and their use in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau
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Aminocyclohexane and aminoalkylcyclohexane compounds, which are systemic-ally-active as NMDA receptor antagonists, are effective in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau, method of treating disorders resulting from or associated with abnormal hyperphosphorylation of microtubule associated protein tau, and pharmaceutical compositions comprising the same.
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- A practical synthesis of tert-alkylamines via the ritter reaction with chloroacetonitrile
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Ritter reaction of tertiary alcohols with chloroacetonitrile and subsequent cleavage of chloroacetyl group in the resulting chloroacetamide with thiourea is an efficient procedure for synthesis of tert-alkylamines.
- Jirgensons,Kauss,Kalvinsh,Gold
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p. 1709 - 1712
(2007/10/03)
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- Synthesis and structure-affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site
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A series of 1,3,5-alkylsubstituted cyclohexylamines 2 were synthesized as ligands for the N-methyl-D-aspartate (NMDA) receptor phencyclidine (PCP) binding site. Pure diastereomers with defined configuration of amino group 2- ax and 2-eq were obtained. The optimal size of 1,3,5-substituents was determined for cyclohexylamines 2 with an equatorial amino group in the lowest energy conformation using Hansch analysis. According to the data, the lipophilic part of cyclohexylamines 2 does not discriminate between hydrophobic regions of the PCP binding site but rather recognizes this site as a whole lipophilic pocket. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
- Jirgensons, Aigars,Kauss, Valerjans,Kalvinsh, Ivars,Gold, Markus R.,Danysz, Wojciech,Parsons, Chris G.,Quack, Gunter
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p. 555 - 565
(2007/10/03)
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- 1-AMINO-ALKYLCYCLOHEXANE NMDA RECEPTOR ANTAGONISTS
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Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.
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- 1-amino-alkylcyclohexane NMDA receptor antagonists
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Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.
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