267 results about "Acetylcholinesterase inhibitor" patented technology

The invention provides a method of preventing, delaying, or reversing the progression of Alzheimer's disease by administering an A.beta..sub.42 lowering agent to a mammal under conditions in which levels of A.beta..sub.42 are selectively reduced, levels of A.beta..sub.38 are increased, and levels of A.beta..sub.40 are unchanged. The invention provides methods and materials for developing and identifying A.beta..sub.42 lowering agents. In addition, the invention provides methods for identifying agents that increase the risk of developing, or hasten progression of, Alzheimer's disease. The invention also provides compositions of A.beta..sub.42 lowering agents and antioxidants, A.beta..sub.42 lowering agents and non-selective secretase inhibitors, as well as A.beta..sub.42 lowering agents and acetylcholinesterase inhibitors. The invention also provides kits containing A.beta..sub.42 lowering agents, antioxidants, non-selective secretase inhibitors, and/or acetylcholinesterase inhibitors as well as instructions related to dose regimens for A.beta..sub.42 lowering agents, antioxidants, non-selective secretase inhibitors, and acetylcholinesterase inhibitors.

This invention describes the administration of multiple therapeutic agents with insulin in conjunction with bexarotene, ketamine, monoclonal antibodies Etanercept, IGF-1, and acetylcholine esterase inhibitors physostigmine, for treatment of Alzheimer's disease and other neurodegenerative diseases. Insulin, improves memory; also augments and amplifies the effects of the adjuvant therapeutic agents (paracrine and intracrine effects) and consequently reduces the β amyloid, its soluble precursors, prevents damage to the neuronal skeletal network (taupathy), and blocks glutamate excitotoxicity, reduces brain inflammation, prevents apoptosis, and increases the acetylcholine levels in the neurons and synapses; by using a combination of insulin, bexarotene, ketamine, Etanercept, IGF-1, and physostigmine therapeutic agents. The results are achieved by using the specially designed Iontophoresis incorporated olfactory mucosal delivery (ORE) catheter device located at the olfactory nerves, sphenoid sinus, and adjacent structures described here, to transport the large molecules of therapeutic agents to treat AD delivered to the CNS bypassing BBB from ORE.

Methods and compositions of the invention employ acetylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer's disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.

A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and/or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence. Further, the combination of rivastigmine and glycopyrrolate has been effective in significantly improving cognitive function in patients suffering from acute dementia or cognitive impairment.

The invention provides a method of preventing, delaying, or reversing the progression of Alzheimer's disease by administering an Aβ₄₂ lowering agent to a mammal under conditions in which levels of Aβ₄₂ are selectively reduced, levels of Aβ₃₈ are increased, and levels of Aβ₄₀ are unchanged. The invention provides methods and materials for developing and identifying Aβ₄₂ lowering agents. In addition, the invention provides methods for identifying agents that increase the risk of developing, or hasten progression of, Alzheimer's disease. The invention also provides compositions of Aβ₄₂ lowering agents and antioxidants, Aβ₄₂ lowering agents and non-selective secretase inhibitors, as well as Aβ₄₂ lowering agents and acetylcholinesterase inhibitors. The invention also provides kits containing Aβ₄₂ lowering agents, antioxidants, non-selective secretase inhibitors, and/or acetylcholinesterase inhibitors as well as instructions related to dose regimens for Aβ₄₂ lowering agents, antioxidants, non-selective secretase inhibitors, and acetylcholinesterase inhibitors.

The present invention describes methods of treating dementia comprising administering an effective daily dose of N-(2-(6-fluoro-1H-indol-3-yl)ethyl-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.

The present invention relates to the treatment of behavioral disorders, especially agitation, associated with a central nervous system (CNS) disorder, especially Alzheimer's disease (AD), cerebrovascular disease (VaD), or Down's Syndrome, in a mammal, comprising administering to said mammal an 1-aminocyclohexane, alone or in combination with a acetylcholinesterase inhibitor. In one embodiment, the 1-aminocyclohexane is memantine.

The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof:

In the formula (I), R¹, R², R³ and R⁴ are the same as or different from each other.

The invention provides a method of preventing, delaying, or reversing the progression of Alzheimer's disease by administering an Aβ₄₂ lowering agent to a mammal under conditions in which levels of Aβ₄₂ are selectively reduced, levels of Aβ₃₈ are increased, and levels of Aβ₄₀ are unchanged. The invention provides methods and materials for developing and identifying Aβ₄₂ lowering agents. In addition, the invention provides methods for identifying agents that increase the risk of developing, or hasten progression of, Alzheimer's disease. The invention also provides compositions of Aβ₄₂ lowering agents and antioxidants, Aβ₄₂ lowering agents and non-selective secretase inhibitors, as well as Aβ₄₂ lowering agents and acetylcholinesterase inhibitors. The invention also provides kits containing Aβ₄₂ lowering agents, antioxidants, non-selective secretase inhibitors, and/or acetylcholinesterase inhibitors as well as instructions related to dose regimens for Aβ₄₂ lowering agents, antioxidants, non-selective secretase inhibitors, and acetylcholinesterase inhibitors.

The present invention provides a novel compound useful as a medicament, an acetylcholinesterase inhibitor, and an agent for preventing, treating and improving various kinds of senile dementia, Alzheimer-type senile dementia, cerebrovascular dementia or attention deficit hyperactivity disorder, namely, 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanone)-2-yl]methylpiperidine represented by the following formula:or a pharmaceutically acceptable salt thereof, and a process for producing the same.

The invention belongs to the technical field of medicine, and relates to a thiazolo(3,2-b)-1,2,4-triazine derivative and applications thereof. The thiazolo(3,2-b)-1,2,4-triazine derivative includes stereoisomers and pharmaceutically applicable salts of the compound, and has a general structural formula as shown follow. The thiazolo(3,2-b)-1,2,4-triazine derivative and the salts added by pharmaceutically applicable acids of the compound can be used by combining with the existing medicaments or separately as acetylcholinesterase inhibitors for enhancing the memory of patients suffering from dementia and alzheimer.

The invention relates to methods and compositions for improving cognitive function by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an acetylcholinesterase inhibitor (AChEI) or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In particular, it relates to the use of a combination of an SV2A inhibitor and an AChEI in treating a central nervous system disorder with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, amyotrophic lateral sclerosis (ALS), and cancer-therapy-related cognitive impairment.

The present invention provides methods and compositions for improving cognitive function by administering a GABA_B receptor antagonist and an acetylcholinesterase inhibitor.

There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetylcholinesterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetylcholinesterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetylcholinesterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT₃ receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholinesterase inhibitor are also described.

In accordance with the present invention, it has been unexpectedly found that the administration of an acetylcholinesterase inhibitor in combination with a tricyclic antidepressant having anti-muscarinic properties provides a highly effective and well tolerated treatment for nicotine dependence and dementias, such as Alzheimer's disease (AD). In one aspect, it is effective in the treatment of nicotine dependence, as well as in the treatment and mitigation of nicotine withdrawal symptoms and in the effectuation of smoking cessation. In another aspect, it is effect in the treatment and mitigation of dementias such as Alzheimer's disease.

The present invention relates to an application of acetylcholinesterase inhibitor for curing diabetes. The described inhibitor includes all the compounds which can inhibit acetylcholinesterase activity and have the action for curing diabetes. The invented experimental results show that these inhibitors have the actions of inhibiting beta-cell death and reducing blood sugar concentration of diabetic model mouse, and can effectively cure or improve diabetes symptom.