National Science Council

Annji Pharmaceutical Co., Ltd.

Other

Development Center for Biotechnology

Medical and Pharmaceutical Industry Technology and Development Center

Purzer Pharmaceutical Co., Ltd.

Ji-Wang Chern

Pei-Teh Chang

Mao-Hsiung Yen

Chao-Wu Yu

Guan-Yu Lu

Grace Shiahuy Chen

Yue-Jun Lai

Pao-Luh Tao

Feng-Nien Ko

Shih-Chung Hsu

Shan-Shue Wang

Chen-Wei Huang

Chin-Fen Lee

Chun-Tang Chiou

Kuang-Chao Wang

Alexander Gutcait

Hsiu-Wen Liu

Yu-Ling Leu

Chia-Yu Wu

Chia-Yang Shiau

Chia-Yin Chen

Kang-Chien Liu

Ye-Lin Leu

Steve Roffler

Chiung Hua Huang

Pei-Yun Hung

Chan-Hui Huang

Yi-Hsun Ho

Jia-Rong Liu

Hsueh-Yun Lee

Meng-Ling Chen

Kuan-Yu Chen

Hsiao-Chun Wang

Ajit Dhananjay Jagtap

Shin-Yu Lai

Rahul Subhash Talekar

Chun-tang Chiou

Histone deacetylases (HDACs) inhibitors are disclosed according to the following structural formula. The moiety A is a benzene ring, optionally substituted. The moiety B is a benzene ring attached at the 1,4 or 1,3 position, or a cyclohexane ring attached at the 1,4 position, optionally substituted. R and Z are further substituents. The HDACs inhibitors possess cytotoxicities to various cancer cell lines. They are useful for treating a tumor associated with deregulation of the activity of histone deacetylases in a subject in need thereof, in one embodiment, the HDACs inhibitors of the invention are useful for treating glioma, breast cancer, colon cancer, target cell lung cancer, adenocarcinoma of the lung, small cell lung cancer, stomach cancer, liver cancer, ovary adenocarcinoma, pancreas carcinoma, prostate carcinoma, promyiocytic leukemia, chronic myelocytic leukemia, or acute lymphocytic leukemia in a subject in need thereof.

Histone deacetylases (HDACs) inhibitors

Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed. In one aspect, the invention relates to a compound having the structure or a pharmaceutically acceptable salt, a solvate or hydrate, a prodrug, or a metabolite thereof. In one embodiment of the invention, Ris ethyl; Ris 2-phenylethyl; Ris hydrogen; Ris fluoro; Ris (2E)-3-N-hydroxyamino-3-oxo-propenyl; and Ris hydrogen, or a salt thereof. In another embodiment of the invention, Ris ethyl; Ris 2-phenylethyl; Ris hydrogen; Ris (2E)-3-N-hydroxyamino-3-oxo-propenyl; Ris chloro or fluoro; and Ris hydrogen, or a salt thereof.

Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases. In one aspect, the invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein

Multifunctional quinoline derivatives as anti-neurodegenerative agents

Histone deacetylases inhibitors (HDACIs) and methods for treating cancer in a subject in need thereof are disclosed. The HDACIs comprise a compound of Formula X. or a pharmaceutically acceptable salt thereof. In one embodiment of the invention, Ris ethyl; Ris 2-phenylethyl; Ris hydrogen; Ris fluoro; Ris (2E)-3-N-hydroxyamino-3-oxo-propenyl; and Ris hydrogen, or a salt thereof. In another embodiment of the invention, Ris ethyl; Ris 2-phenylethyl; Ris hydrogen; Ris (2E)-3-N-hydroxyamino-3-oxo-propenyl; Ris chloro or fluoro; and Ris hydrogen.

Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed.

Cyclopropanecarboxylate esters of purine analogues

A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. In one aspect, the invention relates to a compound a compound of Formula A: or a pharmaceutically acceptable salt thereof, wherein:

Indolin-2-one derivatives as protein kinase inhibitors

The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers. 

Benzenesulfonamide derivatives and pharmaceutical composition thereof

A method of treating psychosis in a patient which comprises administering a pharmaceutical composition useful in treating psychosis containing a therapeutically effective amount of 1-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one as an active ingredient.

Method of treating psychosis in a patient

The present invention features proactive antitumor compounds of the following formula: ##STR1## wherein R.sup.1 is COOZ; Z being H, alkali metal, alkaline earth metal, an ammonium group which is optionally substituted with one or more alkyl groups, or a carboxyl protecting group; each of R.sup.2, R.sup.3, and R.sup.4, independently, is OH or OR.sup.a ; R.sup.a being a hydroxyl protecting group; X is benzene or pyridine, optionally substituted with R.sup.b ; R.sup.b being H, C.sub.1-5 alkyl, C.sub.1-5 alkoxy, NO.sub.2, F, Cl, Br, SO.sub.3 H, and CN; R.sup.5 is H or OH; and each of n and m, independently, is 0 or 1; or a salt thereof.

Proactive antitumor compounds

A compound of the formula: ##STR1## wherein X is arylene, heteroarylene, fused arylene, fused heteroarylene, or deleted; Y is sulfonyl, --O--, or deleted; R.sub.1 is aryl, heteroaryl, fused aryl, or fused heteroaryl; R.sub.2 is H, lower alkyl, lower alkoxy, halo, nitro, cyano, haloalkyl, hydroxyl, carboxyl, amido, amino, or aminoalkyl; or a salt thereof are disclosed. Also disclosed are a pharmaceutical composition which contains an excipient and an effective amount of a compound of the above formula and a method of treating cancer which involves the administration of an effective amount of such a compound to a patient in need thereof.

Sulfonyl-N-hydroxyguanidine derivatives

This invention relates to novel optically active 3-substituted methyl-5-methylthio-2,3-dihydroimidazo�1,2-c!quinazoline (I) and 3-substituted methyl-2,3-dihydroimidazo�1,2-c!quinazolin-5(6H)-one (II). This invention also relates to the therapeutical use of these novel compounds ##STR1## wherein: R is halogen, hydrogen, methoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, nitro, acetyl, cyano or hydroxy group; or pharmaceutically acceptable salts thereof.

Optically active 2,3-dihydroimidazo(1,2-C) quinazoline derivatives, the

The present invention provides a novel series of 3-substituted methyl-2,5-dihydroimidazo 1,2-c!quinazoline compounds. These compounds are found useful as an active ingredient for the treatment of hypertension and dysuria.

3-substituted methyl-2,3-dihydroimidazo 1,2-c!quinazoline derivatives,

The present invention provides a novel series of 3-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazoline compounds. These compounds are found useful as an active ingredient for the treatment of hypertension and dysuria.

3-substituted methyl-2,3-dihydroimidazo[1,2-C] quinazoline derivatives,

The present invention provides a novel series of 2-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-ones (-thiones) compounds. These compounds are found useful as an active ingredient for the prophylaxis and treatment of hypertension.

2-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-ones

A process for preparing 3-(1H-tetrazol-5-yl)-4(3H)-quinazolinone ammonium salts of the formula I: ##STR1## wherein: R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, which process comprises: reacting ethyl N-(1H-tetrazol-5-yl) formimidate in an inert solvent with substituted anthranilamide of the formula IV ##STR2## wherein R is as defined above. The process is simpler than prior processes for preparing the same compounds and thus is economically valuable.

Growing community of inventors

Taipei, Taiwan

Ji-Wang Chern