36 results about "COMT inhibitor" patented technology

The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and / or a COMT inhibitor and / or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A2A receptor antagonist singly or together with a dopamine agonist, and / or a COMT inhibitor, and / or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.

The present invention relates to an association between specific polymorphisms of the COMT polypeptide and the development, or risk of developing, preterm labor and uterine diseases and conditions. Disclosed are therapeutic, preventative and diagnostic methods and compositions relating to pre-term labor, uterine diseases and conditions, and ovarian conditions and diseases. In certain embodiments, such methods and compositions involve a COMT inhibitor.

The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and / or a COMT inhibitor and / or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A2A receptor antagonist singly or together with a dopamine agonist, and / or a COMT inhibitor, and / or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.

Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

The present invention relates to an association between specific polymorphisms of the COMT polypeptide and the development, or risk of developing, preterm labor and uterine diseases and conditions. Disclosed are therapeutic, preventative and diagnostic methods and compositions relating to pre-term labor, uterine diseases and conditions, and ovarian conditions and diseases. In certain embodiments, such methods and compositions involve a COMT inhibitor.

New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

A method for quantitatively measuring catechol-O-methyltransferase activity and application thereof belong to the technical field of biomedicine. The method uses 4-acetic acid-7,8-dihydroxycoumarin as the specific probe substrate of COMT enzyme, which can be specifically catalyzed by COMT enzyme to generate 8-methoxy product and display at 520nm Fluorescence signal, the activity of COMT can be quantitatively determined by detecting the change of fluorescence intensity. The invention can not only be used for quantitative evaluation of COMT enzyme activity in biological samples from different sources, but also can be used for rapid screening of COMT inhibitors in vitro and evaluation of their inhibitory ability. The method can be used to quantitatively evaluate the real activity of COMT enzymes in various in vitro biological samples, realize rapid screening of inhibitors and quantitative evaluation of inhibitory ability; it can be used to evaluate the catalytic activity of different species of COMT and COMT mutants with different amino acid sequences , and then evaluate its ability to metabolize catechols. The method of the invention has the advantages of (1) high selectivity, (2) cheap and easy to obtain; (3) high sensitivity and the like.

A specific fluorescent probe for catechol-O-methyltransferase and its application. The specific probe substrate is 3‑benzothiazole‑7,8‑dihydroxycoumarin (3‑BTD), which can be specifically catalyzed by COMT enzymes to generate 8‑methoxyl products and detect at 520nm A fluorescent signal is displayed at , and the activity of COMT can be quantitatively determined by detecting the change of fluorescence intensity. The probe can not only be used for quantitative evaluation of COMT enzyme activity in biological samples from different sources, but also can be used for rapid screening of COMT inhibitors in vitro and evaluation of their inhibitory ability. This method can be used to quantitatively evaluate the real activity of COMT enzyme in various in vitro biological samples, realize rapid screening of inhibitors and quantitative evaluation of inhibitory ability; it can be used to evaluate the catalytic activity of different species of COMT and COMT mutants with different amino acid sequences , and then evaluate its ability to metabolize catechols. It has the advantages of high sensitivity, high accuracy, strong anti-environmental interference ability, easy high-throughput detection and inhibitor screening.

Novel compounds of general formula I are described which have potentially valuable pharmaceutical properties in the treatment of several central and peripheral nervous system dysfunctions.

The present disclosure relates to a more effective therapeutic agent capable of improving and treating the axial symptoms (particularly freezing of gait symptom) of patients with Parkinson's disease. Such symptoms in patients with Parkinson's disease can be improved and treated by using L-threo-3,4-dihydroxy-phenylserine (DOPS) and a COMT inhibitor in combination together, optionally with an L-DOPA preparation as well. As a result, the axial symptoms difficult to improve with conventional L-DOPA preparations can be treated, and a therapeutic agent and a treatment method are provided for the axial symptoms of patients with Parkinson's disease, particularly those suffering from the disease at a moderate level or higher.