35 results about "COMT inhibitor" patented technology

The invention relates to a preparation method for COMT inhibitor 5, 6, 7, 3', 4'-pentamethoxyl isoflavone, comprising the following steps: mixing 3, 4-dimethoxyphenylacetic acid and oxalyl chloride indichloromethane solution to carry out reflux reaction for 2 to 3 h, and cooling to room temperature; adding 3, 4, 5-trimethoxy sodium phenolate to carry out esterification reaction to carry out Friesrearrangement reaction under the catalysis of Lewis acid boron trifluoride ether; and finally carrying out reaction with DMF with the existence of the Lewis acid boron trifluoride ether; and adding methane sulfonyl chloride to promote Vilsmeier-Haack formylation reaction and subsequent cyclization reaction to obtain light yellow crystals 5, 6, 7, 3', 4'-pentamethoxyl isoflavone. The preparation method has simple and easily available raw materials, simple operation, short reaction time, mild reaction condition, environment protection and high yield of 76 %, and is suitable for industrial production.

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.

It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of trans-thyretin-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 is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A_2A 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 A_2A 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 A_2A 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 A_2A 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.

Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

A pharmaceutical gel composition for intra-intestinal administration is provided and comprises (i) a dopamine replacement agents, (ii) a dopamine decarboxylase inhibitor (DDI), and (iii) a COMT inhibitor.

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.

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.

Compounds of formula (I), wherein E, G, T, R_d, R_e, and R_f are as defined in the disclosure, release levodopa and a COMT inhibitor so that they can be used for the treatment of diseases or conditions, wherein levodopa and inhibition of COMT are indicated to be useful.

The invention relates to the field of COMT inhibitors, particularly to a COMT inhibitor containing a hydrazide structure, a preparation method of the COMT inhibitor, and application of the COMT inhibitor to preparing schizophrenia treating drugs and the like. The chemical formula of the COMT inhibitor is shown as below, in which R1 is an alkyl selected from C1-C5, R2 is selected from H, an alkyl of C1-C10 or a naphthene of C3-C10.

The invention belongs to the technical field of COMT inhibitors, and in particular relates to COMT inhibitors with terminal olefinic bond and hydrazide structures as well as a preparation method of the COMT inhibitors and application of the COMT inhibitors to preparation of medicines for treating schizophrenia, and the like. The general formula (I) of the COMT inhibitors is described in the description.

The invention relates to the field of COMT inhibitors, and particularly relates to a COMT inhibitor comprising a terminal olefinic bond and a hydrazide structure, a preparation method of the COMT inhibitor, and application of the COMT inhibitor to preparation of medicines for treating schizophrenia and the like.

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.