Chinese Academy of Medical Sciences

Bayer Aktiengesellschaft

Taisho Pharmaceutical Co., Ltd.

Institute of Materia Medica

Geng-tao Liu

Liang Huang

Ming-he Yang

Yan-rong Chen

Yan Li

Katsuo Hatayama

Kensei Yoshikawa

Ulrich Benz

Tatsuhiko Sano

Iwao Arai

Er-chang Rao

Shohei Higuchi

Yen-rong Chen

Jin Zhou

Dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxyla te (DDB), a synthetic analogue of Schizandrin C, is a useful chemotherapeutic agent for the treatment of BEL-7402 human hepatocarcinoma when used in combination with 6-mercaptopurine.

DDB as an agent against BEL-7402 human hepatocarcinoma

A process for the preparation of compound of the formula ##STR1## in which R.sup.1 --represents ##STR2## and R.sup.2 --represents hydrogen, fluorine, chlorine or bromine. Comprising cyclizing compounds of the formula ##STR3## and, in a further step, either a) reducing stereo-specifically to give compounds of the formula in which R.sup.1 represents ##STR4## or b), to give compounds of the formula in which R.sup.1 represents ##STR5## or by c) forming compounds of the formula ##STR6## followed by stereoselective reduction to give compounds in which R.sup.1 represents ##STR7##

Process for the preparation of clausenamide and neoclausenamide, and

Processes for the preparation of compounds of the formula ##STR1## in which R and R.sup.1 are identical or different and represent hydrogen or halogen, in the racemic form or in the form of its pure enantiomers by cyclicizing compounds of the formula ##STR2## with 2,6-lutidine or by cyclicizing compounds of the formula ##STR3## with diethyl azodicarboxylate. Compounds where R is halogen are new and are useful as cerebral therapeutics, nootropics or in the reduction of increased glutamine pyruvate transaminase in serum.

Dehydrocycloclausenamide, its preparation and use in treating cerebral

N-substituted amide derivative represented by the formula ##STR1## wherein A is --CH(OH)-- or --C(.dbd.O)--, R.sup.1 is a hydrogen atom or an lkyl group having 1 to 3 carbon atoms, and R.sup.2 is an alkyl group having 1 to 6 carbon atoms, are disclosed. These compounds are useful for prevention and therapy for liver diseases.

N-substituted amide derivatives useful for treating liver diseases

A pharmacologically active .epsilon.-valerolactam has been isolated from the leaves of Clausena lansium. This compound and its derivatives have the formula ##STR1## where R is hydrogen or a C.sub.1 -C.sub.18 -acyl group. It has been found that these compounds are useful in the treatment of hypoxia and as antiamonestics.

Pharmacologically active .epsilon.-valerolactams

Purified Clausenamide of the formula ##STR1## is obtained by extraction of leaves of Clausena lansium followed by purification, Reduction products, ethers, etc. can be produced. The compounds are effective in treating hypoxia and amnesia.

Delta-butyrolactams, thereof, processes for the preparation thereof and

Compounds of the general formula ##STR1## wherein R.sub.1 represents hydrogen, an acyl group having 1 to 18 carbon atoms or both R.sub.1 together the group ##STR2## R.sub.2 represents hydrogen or a methyl group, have been isolated in small amounts from the leaves of Clausena lansium. The new compounds are to be used for the production of compositions for the use of the treatment of acute and chronical viral hepatitis, liver intoxication, hypoxia or amnesia.

2,3-dihydroxy-3-phenyl-N-(2-phenyl-ethyl)-propionic acid amides

A pharmacologically active phenyl-substituted bicyclic lactam has been isolated from the leaves of Clausena lansium. This compound and its derivatives have the formula ##STR1## Where R is hydrogen of a C.sub.1 -C.sub.18 -acyl group. It has been found that these compounds are useful in the treatment of hypoxia and as antiamnestics.

Growing community of inventors

Beijing, China

Geng-tao Liu