53 results about "Muscarinic acetylcholine receptor" patented technology

The invention belongs to the field of medicine, and relates to D-configuration polypeptide with high stability and capable of realizing mediated targeting of acetylcholine receptor high-expression cells and crossing corresponding barrier membranes and a nano drug delivery system thereof as well as an application in in-vivo and in-vitro brain targeting and in treatment of brain diseases and the like. Test results indicate that DCDX and the acetylcholine receptor are combined with IC50 to obtain 84.5nM which is stable in serum and tolerates hydrolysis of protease; the model drug carried by DCDX is specifically taken in by the positive cells expressing the acetylcholine receptor and has an ability of crossing the barrier formed by the kind of cells; and the nano drug delivery system made of a DCDX-modified polymer carrier material can deliver the entrapped model drug to the target tissue while the drug effect is remarkably improved. The D-configuration polypeptide DCDX provided by the invention can mediate active targeting of the drug or nano drug delivery system and has a good application prospect in the diagnosis and treatment of multiple diseases.

The present invention relates to 1-alkyl-3-aniline-5-aryl-pyrazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).

The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.

The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.

The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.

The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.

The present invention discloses compounds of formula I and pharmaceutically acceptable salts thereof, wherein A ¹ 、A ² , D and E are as described in the specification, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy, especially for the treatment of conditions associated with reduced nicotinic transmission.