Taipei Medical University

Other

Industrial Technology Research Institute

National Science Council

Syn-tech Chem. & Pharm. Co., Ltd.

Department of Health the Executive Yuan, Republic of China

Angiorx Corporation

Standard Chemical & Pharmaceutical Co., Ltd.

Hui-po Wang

On Lee

Che-Ming Teng

Jih-Hwa Guh

Chin-Tsai Fan

Jia-Shuai Lee

Chun-Li Wang

Yu-Wen Cheng

Shiow-Lin Pan

Oliver Yoa-Pu Hu

Eric I C Li

Ming-Cheng Tsai

Hsiao-Hwa Lu

Ya-Lan Chen

Ya-Bing Fan

Huei-Ting Chen

Jin-Yuh Shew

Hsiao Che-Chih

Feng-Shuo Chang

Jang-Feng Lian

Yuan-Yi Wang

Wen-Lin Luo

Tung-Shing Bai

Shui-Jane Lee

Che-Chih Hsiao

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

This invention relates to compounds of the following general formula: The variables are defined herein. Also disclosed is a method for treating mucositis or cancer using these compounds.

Histone deacetylase inhibitors

This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each ofand, independently, is a single bond or a double bond; A is H or CH(RR) whenis a single bond, or C(RR) whenis a double bond; Z is CH(RR) whenis a single bond, or C(RR) whenis a double bond; each of Rand R, independently, is H, C(O)R, C(O)OR, C(O)NRR, or SOR; and each of R, R, R, R, R, and R, independently, is H, C-Calkyl, aryl, heteroaryl, C-Ccycloalkyl, or C-Cheterocycloalkyl; or Rand Rtaken together are C-Ccycloalkyl, C-Cheterocycloalkyl, aryl, or heteroaryl; or Rand Ror Rand Rtaken together are C-Ccycloalkyl, C-Cheterocycloalkyl, aryl, or heteroaryl; provided that one of Rand Ris aryl or heteroaryl.

A novel anti-oncogenic azatyrosine analogues of formula (I) ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, benzyl, or (C.sub.1-6 alkyl)carbonyl; R.sub.2 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, or C.sub.1-6 alkoxyl; and R.sub.3 is CONR.sub.4 R.sub.5, CONHNR.sub.4 R.sub.5, or COOR.sub.6, wherein each R.sub.4 and R.sub.5 independently is a hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, or C.sub.3-6 cycloalkyl, or R.sub.4 and R.sub.5 taken together with the nitrogen attached thereto form a C.sub.3-8 heterocyclic group; R.sub.6 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or benzyl. Also disclosed is a method of preparing such a novel anti-oncogenic azatyrosine analogues, as well as a pharmaceutical composition containing a compound of formula (I).

Azatyrosine analogues

A series of di- and tri-peptide mimetic dopamine prodrugs are synthesized in which D-phenylglycine or D-p-hydroxyphenylglycine is attached as tools for delivery of L-dopa through the intestine via the intestinal dipeptide-mediated carrier transport system. These compounds are found useful as an active ingredient for the treatment of Parkinson's disease.

Di-and tri-peptide mimetic compounds for Parkinson's disease

A series of 2-amino-6-alkyl-5-(4-substituted-1-piperazinyl)pyrimidin-4-ones that have selective cytotoxicity on human CNS tumor cells.

2-amino-6-alkyl-5-(4-substituted-1-piperazinyl) pyrimidin-4-ones, the

Novel anticholesteremic compounds capable of reducing blood cholesterol levels. Also included in this invention are (i) intermediates from which the abovementioned anticholesteremic compounds can be prepared, and (ii) methods for preparing both the intermediates and the anticholesteremic compounds.

Anticholesteremic compounds

A method for preparing cephalosporm derivatives by reacting cephalosporin alkaline metal salts with organic halide in the presence of quaternary ammonium salts catalyst is disclosed. .DELTA..sup.3 .fwdarw..DELTA..sup.2 isomerization, a side reaction commonly reported in preparation of cephalosporin derivatives was successfully eliminated. The desired .DELTA..sup.3 was obtained as a sole product in the reaction.

Method for preparing cephalosporin derivatives

Novel 3-substituted derivatives of 2,2-dimethyl-5-substituted phenoxy-pentanoic acids of formula (I) are prepared. These compouds are prepared from 2,2-dimethyl-5-substituted phenoxy-3-hydroxy-pentanoic acid-.beta.-lactones (formula II). The .beta.-lactones are prepared by condensing relevant phenoxypropanals with dimethylketene.

Derivatives and preparation of 2,2-dimethyl-5-substituted

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Taipei, Taiwan

Hui-po Wang