Taisho Pharmaceutical Co., Ltd.

Kuraray Co., Ltd.

Chinese Academy of Medical Sciences

Tatsuhiko Sano

Kensei Yoshikawa

Katsuo Hatayama

Yutaka Ohuchi

Takehiro Amano

Takashi Nishida

Yoshiji Fujita

Manzo Shiono

Michihiro Ishiguro

Yan Li

Kaoru Sota

Tohru Tanami

Yasuji Yamada

Jiro Sawada

Liang Huang

Chihiro Yokoo

Tomomi Ota

Geng-tao Liu

Yoshimoto Nakashima

Sadakazu Yokomori

Kazuto Sekiuchi

Toshihisa Ogawa

Shoichi Ito

Hisaya Wada

Iwao Arai

Keiko Saijo

Er-chang Rao

Shohei Higuchi

Jin Zhou

Hidemichi Mitome

Yoshinori Shiobara

To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.

Steroid derivatives

Naphthothiopyranone derivatives

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

Novel styrene derivatives of the general formula ##STR1## wherein X is hydrogen or halogen, X.sup.1 is halogen, R is hydrogen or methyl, Y is hydroxymethyl, carboxyl, --COOR.sup.1 or --COR.sup.2 wherein R.sup.1 is prenyl, geranyl, farnesyl, cyclohexyl, phthalidyl, straight or branched chain alkyl having 1 to 6 carbon atoms, or said alkyl substituted with hydroxy, methoxy, pyridyl or alkanoyloxy having 2 to 16 carbon atoms, and R.sup.2 is amino, hydroxyamino mono-(or di-)alkylamino in which the alkyl moiety contains 1 or 2 carbon atoms, ethoxycarbonylmethylamino, carboxymethylamino, thiazolylamino, cyclohexylamino, pyridylamino, morpholino, N-methylpiperazino, phenylamino, phenylamino substituted with one or two of halogen, hydroxy, methyl, methoxy, trifluoromethyl or carboxyl at the phenyl ring, and the pharmaceutically acceptable salts thereof when Y is carboxyl are disclosed. These compounds exhibit high and long-lasting anti-inflammatory, analgesic and anti-pyretic activity.

Novel styrene derivatives of the general formula

A process for producing 1-(p-prenylphenyl)ethanol, which comprises reacting p-chloroprenylbenzene with magnesium at a temperature between 100.degree. C. and 150.degree. C. to form a Grignard reagent, and then reacting it with acetaldehyde.

Process for producing 1-(p-prenylphenyl)ethanol

A process for producing an .alpha.-arylalkanoic acid ester represented by the general formula ##STR1## wherein Ar represents an aryl group which may optionally be substituted, and R.sup.1 and R.sup.2, independently from each other, represent a lower alkyl group, which comprises reacting a Grignard reagent prepared from an aryl halide of the general formula

Process for producing .alpha.-arylalkanoic acid ester

A novel carboxylic acid ester having the following general formula ##STR1## wherein R is alkoxyalkyl having 2 to 6 carbon atoms, cycloalkyl having 5 or 6 carbon atoms, tetrahydrofurfuryl, or alkyl having 1 to 6 carbon atoms optionally substituted with 1 or 2 hydroxyl groups, is a useful anti-inflammatory and analgesic agent.

Esters of the carboxylic acid

Growing community of inventors

Ohmiya, Japan

Tatsuhiko Sano