Claims for Patent: 9,763,953

Summary for Patent: 9,763,953

Title:	Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
Abstract:	The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.
Inventor(s):	Maelicke Alfred
Assignee:	NEURODYN LIFE SCIENCES INC.
Application Number:	US13861134
Patent Claims:	2. The method of claim 1 , wherein as a result of endogenous enzymatic activity the pro-drug compound GLN-1062 is cleaved after administration to produce the effective agent galantamine.3. The method of claim 2 , wherein cleavage of the pro-drug compound GLN-1062 to produce the effective agent galantamine occurs in the brain of a treated patient.4. The method of claim 1 , wherein the disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , other types of dementia claim 1 , schizophrenia claim 1 , epilepsy claim 1 , stroke claim 1 , poliomyelitis claim 1 , neuritis claim 1 , oxygen and nutrient deficiencies in the brain after hypoxia claim 1 , anoxia claim 1 , asphyxia claim 1 , cardiac arrest claim 1 , chronic fatigue syndrome claim 1 , subsequences of various types of poisoning claim 1 , subsequences of anesthesia claim 1 , spinal cord disorders claim 1 , central nervous system inflammation claim 1 , postoperative delirium and/or subsyndronal postoperative delirium claim 1 , neuropathic pain claim 1 , subsequences of the abuse of alcohol and drugs claim 1 , addictive alcohol and nicotine craving claim 1 , and subsequences of radiotherapy.5. The method of claim 2 , wherein the disease is selected from the group consisting of Alzheimer's disease claim 2 , Parkinson's disease claim 2 , other types of dementia claim 2 , schizophrenia claim 2 , epilepsy claim 2 , stroke claim 2 , poliomyelitis claim 2 , neuritis claim 2 , oxygen and nutrient deficiencies in the brain after hypoxia claim 2 , anoxia claim 2 , asphyxia claim 2 , cardiac arrest claim 2 , chronic fatigue syndrome claim 2 , subsequences of various types of poisoning claim 2 , subsequences of anesthesia claim 2 , spinal cord disorders claim 2 , central nervous system inflammation claim 2 , postoperative delirium and/or subsyndronal postoperative delirium claim 2 , neuropathic pain claim 2 , subsequences of the abuse of alcohol and drugs claim 2 , addictive alcohol and nicotine craving claim 2 , and subsequences of radiotherapy.6. The method of claim 3 , wherein the disease is selected from the group consisting of Alzheimer's disease claim 3 , Parkinson's disease claim 3 , other types of dementia claim 3 , schizophrenia claim 3 , epilepsy claim 3 , stroke claim 3 , poliomyelitis claim 3 , neuritis claim 3 , oxygen and nutrient deficiencies in the brain after hypoxia claim 3 , anoxia claim 3 , asphyxia claim 3 , cardiac arrest claim 3 , chronic fatigue syndrome claim 3 , subsequences of various types of poisoning claim 3 , subsequences of anesthesia claim 3 , spinal cord disorders claim 3 , central nervous system inflammation claim 3 , postoperative delirium and/or subsyndronal postoperative delirium claim 3 , neuropathic pain claim 3 , subsequences of the abuse of alcohol and drugs claim 3 , addictive alcohol and nicotine craving claim 3 , and subsequences of radiotherapy.7. The method of claim 1 , wherein said neurodegenerative claim 1 , psychiatric or neurological disease associated with a cholinergic deficit is Alzheimer's disease.8. The method of claim 4 , wherein said anesthesia is neuroleptic anesthesia.9. The method of claim 5 , wherein said anesthesia is neuroleptic anesthesia.10. The method of claim 6 , wherein said anesthesia is neuroleptic anesthesia.11. The method of claim 1 , wherein the neurodegenerative claim 1 , psychiatric or neurological disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , dementia claim 1 , schizophrenia claim 1 , stroke claim 1 , central nervous system inflammation claim 1 , and epilepsy.12. The method of claim 2 , wherein the neurodegenerative claim 2 , psychiatric or neurological disease is selected from the group consisting of Alzheimer's disease claim 2 , Parkinson's disease claim 2 , dementia claim 2 , schizophrenia claim 2 , stroke claim 2 , central nervous system inflammation claim 2 , and epilepsy.