Kaohsiung Medical University

National Science Council

Chang Gung University

Pharmaceutical Industry Technology and Development Center

Chang Gung University of Science and Technology

National Science Council (taiwan)

Yeh-Long Chen

Cherng-Chyi Tzeng

Chih-Hua Tseng

Mei-Ling Ho

Je-Ken Chang

Tian-Lu Cheng

Yin-Chih Fu

Gwo-Jaw Wang

Jing-Jer Lin

Chih-Ming Lu

Ta-Chun Cheng

Kai-Wen Cheng

Wei-Fen Luo

Pei-Jung Lu

Che-Ming Teng

Feng-Nien Ko

Tsong-Long Hwang

Yu-Wen Chen

Tai-Chi Wang

Bor-Ruey Huang

Kuan-Han Lee

Kai-Wen Chang

The present invention provides novel pyrazolo[4,3-c]quinoline derivatives exhibiting specifically inhibition activity to microbiota &#x3b2;-glucuronidase, whereby providing potent activities to prevent chemotherapy-induced diarrhea (CID) of cancers. Therefore, the compounds of the present invention can be used as (1) chemotherapy-adjuvant to prevent chemotherapy-induced diarrhea (CID) and enhance chemotherapeutic efficiency of cancers; (2) health-food supplement to prevent the carcinogens induced colon carcinoma.

Pyrazolo[4,3-c]quinoline derivatives for inhibition of &#x3b2;-glucuronidase

Pyrazolo[4,3-C] quinoline derivatives for inhibition of &#x3b2;-glucuronidase

Disclosed herein are compounds of formula (I), and pharmaceutical compositions comprising the same. The compounds of formula (I) are neutrophilic inflammation inhibitors, thus, they are useful for treatment and/or prophylaxis of inflammatory diseases and/or disorders associated with abnormal activation of neutrophils, such as ARDS, ALI, COPD, lung fibrosis, chronic bronchitis, pulmonary emphysema, &#x3b1;-1 anti-trypsin deficiency, cystic fibrosis, idiopathic pulmonary fibrosis, liver injury, steatohepatitis, liver fibrosis, damages caused by ischemia and reperfusion, myocardial infarction, shock, stroke, and organ transplantation, ulcerative cholitis, vasculitis, SLE, sepsis, SIRS, arthritis, psoriasis, atopic dermatitis, and inflammatory skin diseases. 

Neutrophil inflammation inhibitor and uses thereof

Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt thereof,wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives and their uses in the manufacture of pharmaceutical compositions and in the treatment of cancers.

4-anilinofuro[2,3-b]quinoline derivatives, their preparation processes, and pharmaceutical compositions comprising the same

Disclosed herein are indolo[3,2-c]quinoline compounds of formula (I):  or a pharmaceutically acceptable salt thereof, wherein R and m are given the definitions as set forth in the Specification and Claims. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.

[object Object]

An isoxazole derivative is provided. The isoxazole derivative has following formula: 

Isoxazole derivatives and pharmaceutical compositions comprising the same

Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I):  Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.

Imino-indeno[1,2-c] quinoline derivatives, their preparation processes, and pharmaceutical compositions comprising the same

Indolo[3,2-c]quinoline compounds of formula (I) shown below. Each variable in this formula is defined herein. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase. 

An isoflavone derivative is provided. The isoxazole derivative has following formula:  wherein Rand R, independently, include C-Calkyl optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy, and Rincludes hydrogen, hydroxy or C-Calkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis including an isoflavone derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Isoflavone derivatives and pharmaceutical compositions comprising the same

4-anilinofuro &lsqb;3,2-c&rsqb; quinoline derivatives, and preparation processes and uses of the same

The present invention discloses a novel 6-fluoro-1,4-dihydro-7-&lsqb;4-(2-hydroxyiminoethyl)-1-piperazinyl&rsqb;-4-oxoquinoline-3-carboxylic acid derivatives (formula I), with a process for their preparation, and with pharmaceutical compositions containing them as the active ingredient for the treatment of bacterial infections and/or renal cancer diseases.

6-fluoro-1,4-dihydro-7-&lsqb;4-(2-hydroxyiminoethyl)-1-piperazinyl&rsqb;-4-oxoquinoline-3-carboxylic acid derivatives, their preparation and pharmaceutical compositions

The present invention provides antineoplastic .alpha.-methylene-.gamma.-butyrolactones represented by the general formula �I! wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro and amino;.sub.2 R represents hydrogen, halide, (C.sub.1 -C.sub.4)alkyl or benzyl; X represents N; or wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro and amino; R.sub.2 represents Cl, F, or benzyl; X represents CH. These .alpha.-methylene-.gamma.-butyrolactones may be administered with an inert diluent or with a pharmaceutically acceptable carrier in controlling the growth of a neoplasm in a patient afflicted with a neoplasm disease. ##STR1##

Antineoplastic .alpha.-methylene-.gamma.-butyrolactones

The present inventors have discovered three classes of novel .alpha.-methylene-.gamma.-butyrolactones with excellent antiplatelet activity. As a result of intensive studies, it has been found that compounds represented by the formula I-III are potent inhibitors of platelet aggregation. ##STR1## For the formula I, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino. For the formula II, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.2 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino; R.sub.3 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino. For the formula III, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.4 represents hydrogen, hydroxy, (C.sub.1 -C.sub.4) alkyl. The present invention also provides a cost-efficient method for the preparation of formula I-III. Formula I-III may be administered orally or parenterly with an inert diluent or with a pharmaceutically acceptable carrier in the treatment or the prevention of cardiovascular disease.

Growing community of inventors

Kaohsiung, Taiwan

Yeh-Long Chen