63 results about "Apomorphine" patented technology

Described is a new class of small molecule inhibitors of amyloid beta protein (Abeta) aggregation, based on apomorphine. These molecules target the nucleation phase of Abeta self-assembly and interfere effectively with aggregation of Abeta 1-40 into amyloid fibrils in vitro as determined by transmission electron microscopy, Thioflavin T (ThT) fluorescence, and velocity sedimentation. Structure-activity studies using apomorphine analogues demonstrate that 10,11-dihydroxy substitutions of the D ring are preferred for the inhibitory effectiveness of these aporphines, and that methylation of these hydroxyl groups reduces their inhibitory potency. The ability of these small molecules to inhibit Abeta amyloid fibril formation appears to be linked to their ability to undergo auto-oxidation in solution, implicating an auto-oxidation product as the active Abeta inhibitor. Sedimentation velocity and electron microscopy studies demonstrate that apomorphine and analogues facilitate oligomerization of Abeta into short nonfibrillar soluble assemblies, but inhibit Abeta fibrillization.

The present invention provides, in one embodiment, a method of normalizing the timing of sexual response in a mammal comprising the administration of an amount of a central nervous system sexual response initiator in an amount sufficient to produce genital vasodilation but less than the amount required to produce effective vasocongestive arousal. The method is applicable not only to adjusting or normalizing the timing of sexual response in humans, but in the breeding of valuable commercial animals such as horses, cattle, sheep, swine and the like and domesticated pets such as dogs and cats. In an alternative embodiment, the present invention provides a method for the prophylactic treatment of long-term tissue degradation in the genital organs comprising the administration to a mammal of a central nervous system sexual response initiator in an amount sufficient to produce genital vasodilation but less than the amount required to produce effective vasocongestive arousal. The preferred central nervous system sexual response initiator is apomorphine or a pharmaceutically acceptable acid addition salt thereof.

The present invention discloses novel pharmaceutically acceptable salts of aporphine compounds and carboxyl-group containing agents. Also, the present invention discloses methods for preparing the pharmaceutically acceptable salts. These pharmaceutically acceptable salts are suitable for use in treating and/or preventing hyperglycemic disease and/or several oxidative stress related diseases.

The present invention relates to inhalable formulations of apomorphine or its pharmaceutically acceptable salts or esters for use in treating sexual dysfunction. The present invention also relates to methods for preparing the apomorphine formulations as well as to methods for treatment of sexual dysfunction using said formulations and inhalers including said formulations. The present invention further relates to the use of apomorphine in the manufacture of a medicament for treating sexual dysfunction.

A liquid aqueous formulation for the intranasal administration of apomorphine includes:

• • (a) at least about 15 mg/ml of apomorphine; and
  • (b) a solubilising agent selected from
    • (i) at least one polyoxyethylene-polyoxypropylene copolymer (poloxamer);
    • (ii) at least one cyclodextrin; and
    • (iii) at least one cyclodextrin together with chitosan.

The formulations of the invention can be used in the treatment or management of Parkinson's disease and erectile dysfunction.

The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.

Methods and pharmaceutical unit dosage forms for treating Parkinson's disease in a subject (e.g., an “off” episode in a subject having Parkinson's disease) are described. The pharmaceutical unit dosage forms are films having a first portion including particles containing an acid addition salt of apomorphine and a second portion containing a pH neutralizing agent. The pharmaceutical unit dosage forms can be flexible and have toughness greater than 100 g×mm. The methods can involve administering to a subject having Parkinson's disease a therapeutic dose sufficient to produce an apomorphine plasma concentrate of at least 2.64 ng/mL within 45 minutes after the administration. The subject may be identified as having low uptake, medium uptake, or high uptake of apomorphine administered via oral mucosa.

An apomorphine preparation compound of nasal cavity feeding used for curing Parkinson syndrom, male erection disturbance and female sexual disturbance can eliminate or decrease the side effects of bad feeling, dizziness, vomiting and abnormal taste sense occured in the treatment of apomarphine through using preparation compound adding with the vomiting stop medicine. The aromatic substance is added in order to let the nasal cavity have feelings of refreshing and comfort after the medicine is fed and the natural or synthetic high polymer compound is added to liquid preparation in order to delay the retaining period of medicine in nasal cavity. The preparation has the advantage of transmitting the medicine towards the brain and furthermore can be used with convenience, safety, effectivenessand good compliance.

Disclosed are glycoside and orthoester glycoside derivatives of apomorphine and analogs thereof to treat conditions and diseasessuch as erectile dysfunction.

Methods and compositions are described for treating impaired neurological function, including altered state of consciousness disorders, in an individual who has sustained a brain injury comprising administering to the individual apomorphine. Methods and compositions are described for treating impaired neurological function, including altered state of consciousness disorders, in an individual who has sustained a brain injury comprising administering to the individual at least 1000 mg or more of L-dopa (levodopa) per day. The use of potent dopaminergic agents to stimulate emergence from an altered consciousness state, such as a coma, is disclosed.

Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.