National Science Council

Taipei Medical University

China Medical University

Yung Shin Pharmaceutical Ind. Co., Ltd.

National Taiwan University

Yung Shin Pharm. Ind. Co., Ltd.

University of North Carolina at Chapel Hill

The Ohio State University

Carlsbad Technology, Inc.

Other

Industrial Technology Research Institute

National Science Council of Republic of China

China Medical University Hospital

Medical and Pharmaceutical Industry Technology and Development Center

National Science Council of Taiwan

Che-Ming Teng

Sheng-Chu Kuo

Shiow-Lin Pan

Tian-Shung Wu

Fang-Yu Lee

Li-Jiau Huang

Jih-Hwa Guh

Kuo-Hsiung Lee

Jing-Ping Liou

Li-Chen Chou

Chih-Shiang Chang

Feng-Nien Ko

Chung-Ming Sun

Jai-Sing Yang

Fang Yu Lee

Tzong-Der Way

Jing-Gung Chung

Sheu-Meei Yu

Jang-Chang Lee

Chien-Ting Chen

Ching-Che Huang

Shih-Ming Huang

On Lee

Chien-Chih Chen

Ching-Shih Chen

Wen-Ta Chiu

Hui-po Wang

Ming-Jai Su

Wen-Mei Fu

Kuo-Sheng Hung

Pei-Wen Shan

Huei-Ting Chen

Eric I C Li

Ya-Bing Fan

Ya-Lan Chen

Hsing-Jin Liu

Xiaoming Yang

Shwu-Jen Wu

Pan-Chyr Yang

Yang-Chang Wu

Cherng-Chyi Tzeng

Woei-Cherng Shyu

Ing-Jun Chen

Kenneth F Bastow

Qian Shi

Yeh-Long Chen

Chun-Nan Lin

Chen-Huan Lin

Chun-Jen Chen

Jin-Bin Wu

Chrong-Shiong Hwang

Tur-Fu Huang

Tse-Ming Hong

Tsang-Miao Huang

Shoei-Sheng Lee

Kai-Wei Chang

Min-Tsang Hsieh

Ling-Chu Chang

Chien Huang Lin

Hsin-Yi Hung

Shorong-Shii Liou

Shuenn-Chen Yang

Rong-Sen Yang

Mei-Hua Hsu

Chih-Hsin Tang

Chi-Ying Hung

Jih-Pyang Wang

Sheng-Chih Chen

Chun-Li Wang

Wei-Ling Chang

Masuo Goto

Ying-Qian Liu

Yong-Long Zhao

Mei-Ling Shih

Liu Yang

Hua-Sin Chen

Mei-Juan Wang

Zhi-Jun Zhang

Chin-Yi Wu

Keng-Chen Liang

Wei-Lin Chien

Chih-Ya Wang

Fang-Yuan Lee

Ya-Yun Lai

Chung Y Hsu

Ya-Ling Fang

Chia-Ron Yang

Hui-Po Wang

Ih-Sheng Chen

Shwu-Jen Liou

Tai-Chi Wang

Yuan-Yi Wang

Keduo Qian

Jang-Feng Lian

Ju-Fang Liu

Jing Ping Liou

This disclosure is related to aromatic compounds of formula (I), and methods of their use in treating medical conditions associated with Heat Shock Protein-90 (HSP90), e.g., cancer. Compounds of formula (I) have the following structure: Also disclosed are pharmaceutical compositions comprising compounds of formula (I).

Heat shock protein 90 inhibitors

Disclosed is hydroxamic acid compounds of Formula (I) set forth herein. Also disclosed are a pharmaceutical composition containing such a compound and a method of using the compound for treating a condition associated with histone deacetylase 6.

Histone deacetylase 6 inhibitors and use thereof

The invention relates to the use of Indoline derivatives, and their effective dose in the prevention and/or treatment of fibrosis diseases. The compound can effectively prevent and/or treat a fibrosis disease without cytotoxicity or genotoxicity.

Indoline derivatives for treatment and/or prevention of fibrosis diseases

The present invention is related to novel 20-sulfonylamidine derivatives of camptothecin (1), method of synthesizing the same, and use thereof as an antitumor agent, for examples an antitumor agent for treating nasopharyngeal, lung, breast or prostate cancer.

[object Object]

Indolyl or indolinyl compounds of formula (I): whereinbond, n, R, R, R, R, R, and R, are defined herein. Also disclosed is a method for treating cancer with these compounds.

Indolyl or indolinyl hydroxamate compounds

The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer. 

Antofine and cryptopleurine derivatives 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.

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

This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.

Piperazinedione compounds

Benzimidazole compounds of formula (I): wherein R, R, R, R, R, X, Y, Z, and Zare defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.

Benzimidazole compounds and their use 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

A fused pyrazolyl compound having an anti-tumor potency of the following formula is synthesized: wherein A is in which n is 0, 1, 2, or 3; Aris benzene, thiophene or furan; Aris furyl; and Aris phenyl; Rand Rindependently are hydrogen, halogen or &#x2014;(CH)OR; Ris hydrogen or alkyl; Ris &#x2014;(CH)-A, wherein r is an integer of 1-5, and Ahas a formula of &#x2014;O&#x2014;C(O)&#x2014;(CRH)&#x2014;NRR; Rand Rindependently are hydrogen, halogen, or alkyl, or Rand Rtogether are &#x2014;O(CH)O&#x2014;; Ris H, halogen, nitro, cyano, alkyl, or aryl; Ris H, alkyl, or aryl; Rand Rindependently are H, alkyl, or aryl; m is 0, 1, 2, 3, 4, 5, or 6; and q is 1, 2, 3, 4, 5, or 6; or a salt thereof.

Fused pyrazolyl compounds having an aminoalkylcarbonyl group

A method for preferentially inhibiting release of pro-inflammatory cytokines over release of anti-inflammatory cytokines using a fused pyrazolyl compound of formula (I): A is R or in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar, Ar, and Ar, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R, R, R, R, R, and R, independently, is R', nitro, halogen, &#x2014;C(O)&#x2014;OR&#x2032;, &#x2014;C(O)&#x2014;SR&#x2032;, &#x2014;C(O)&#x2014;NR&#x2032;R&#x2033;, &#x2014;(CH)OR&#x2032;, &#x2014;(CH)SR&#x2032;, &#x2014;(CH)NR&#x2032;R&#x2033;, &#x2014;(CH)CN, &#x2014;(CH)C(O)&#x2014;OR&#x2032;, &#x2014;(CH)C(O)H, or Rand Rtogether, Rand Rtogether, or Rand Rtogether are &#x2014;O(CH2)O&#x2014;, in which each of R&#x2032; and R&#x2033;, independently, is H, alkyl, cyclyl, aryl, heteroaryl, heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6; and n is 1, 2, or 3. This invention also covers a method of inhibiting activity of NF-&#x3ba;B with such a compound.

Preferential inhibition of release of pro-inflammatory cytokines

Growing community of inventors

Taipei, Taiwan

Che-Ming Teng