National Taiwan University

National Yang Ming Chiao Tung University

Other

National Health Research Institutes

China Medical University

National Applied Research Laboratories

Tseng, Yufeng Jane

Chung-Ming Sun

Yufeng Jane Tseng

Chih-Min Liu

Yu-Li Liu

Hai-Gwo Hwu

Wen-Sung Lai

Kuo-Hsiung Lee

Sheng-Chu Kuo

Che-Ming Teng

Shiow-Lin Pan

Tian-Shung Wu

Li-Jiau Huang

Jai-Sing Yang

Li-Chen Chou

Chih-Shiang Chang

Tzong-Der Way

Jing-Gung Chung

Jang-Chang Lee

Chien-Ting Chen

Ching-Che Huang

Shih-Ming Huang

Min-Liang Kuo

Hueih-Min Chen

Chih-Yu Huang

The present invention provides novel substituted benzimidazole derivatives used as DAAO inhibitors and for treatment and/or prevention of neurological disorders.

Substituted benzimidazole derivatives as D-amino acid oxidase (DAAO) inhibitors

The invention utilizes virtual screening strategy to seek for current market drugs as anti-schizophrenia therapy drug repurposing. Drug repurposing strategy finds new uses other than the original medical indications of existing drugs. Finding new indications for such drugs will benefit patients who are in needs for a potential new therapy sooner since known drugs are usually with acceptable safety and pharmacokinetic profiles. In this study, repurposing marketed drugs for DAAO inhibitor as new schizophrenia therapy was performed with virtual screening on marketed drugs and its metabolites. The identified and available drugs and compounds were further confirmed with in vitro DAAO enzymatic inhibitory assay.

Use of known compounds as D-amino acid oxidase inhibitors

The present invention provides novel substituted benzimidazole derivatives of formula (I) used as DAAO inhibitors and for treatment and/or prevention of neurological disorders. 

The present invention relates to a quinic acid derivative, preparation process of the same and pharmaceutical uses thereof. The quinic acid derivative has a quinic acid-like structure which binds to CD28, blocks T-cell signal 2 pathway via CD28, and suppresses T-cell activation. The C-1 carboxyl group, the C-3 hydroxyl group and the C-4 hydroxyl group of quinic acid are modified to attenuate the cytotoxicity of the quinic acid derivative. The preparation process of the quinic acid derivative comprises 2 steps of: treating quinic acid with the first reagent in the presence of the acid catalyst to form an immediate; and treating the immediate with the second reagent to from the quinic acid derivative. With the ability to suppress T-cell activation, the quinic acid derivative is used to treats an autoimmune disease, an allergy, transplant rejection or other related immune disorder.

Quinic acid derivative, process for preparation and uses thereof

2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Naform) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

2-phenyl-4-quinolones as anticancer agents

2-selenophene-4-quinolones as anticancer agents

2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Naform) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

Hydrophilic derivatives of 2-selenophene-4-quinolones as anticancer agents

2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and &#x39b;/, &#x39b;/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

Hydrophilic derivatives of 2-aryl-4-quinolones as anticancer agents

Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds. 

Bicyclic heteroaryl compounds

This invention relates to indazole compounds of formula (I) or (II) shown below. Each variable in formula (I) or (II) is defined in the specification. These compounds can be used to treat cancer. 

Indazole compounds

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Hsinchu, Taiwan

Chung-Ming Sun