Shionogi Company Limited

The University of Tokyo

Tohoku University

Shiro Kida

Sachio Mori

Shozo Takechi

Hiroshi Matsumoto

Masaru Ogata

Takuji Mizui

Teruhisa Ichihashi

Sumio Shimizu

Koji Masuda

Manabu Katou

Naoki Yoshikawa

Nobuyuki Tanaka

Mado Nakajima

Tetsuo Nagano

Akira Kugimiya

Hirotatsu Kojima

Osamu Nureki

Hiroshi Nishimasu

Eiichi Kojima

Yasuhiko Kanda

Katsuya Tawara

Takayoshi Okabe

Ryuichiro Ishitani

Yusuke Tateno

Junken Aoki

Terukazu Kato

Kyohei Hayashi

Mitsuhiro Yonehara

Junji Yamane

Mitsuyasu Kawaguchi

Yoshiyuki Kioi

Kouji Masuda

A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: 

Pyrimidinone derivative having autotaxin-inhibitory activity

Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof,wherein

Acetic acid amide derivative having inhibitory activity on endothelial lipase

A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is &#x2014;O&#x2014; or &#x2014;S&#x2014;, Ris hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, Rand Rare each independently hydrogen, halogen, hydroxy or the like, Ris a group represented by the formula: &#x2014;(CRR)&#x2014;R, Rand Rare each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, Ris carboxy, cyano, substituted or unsubstituted alkyl or the like, Ris halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.

Oxadiazole derivative having endothelial lipase inhibitory activity

An anti-hyperlipemic agent which has a potent activity of reducing LDL and VLDL cholesterols, which are thought to be a risk factor for arteriosclerosis among total blood cholesterols, and which is excellent in the antioxidant activity on LDL, is provided. Additionally, a compound and a pharmaceutically acceptable salt thereof are disclosed, which is represented by Formula (I): ##STR1## �wherein R.sup.1 is a lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl group which is optionally substituted; R.sup.2 is a group represented by the formula: --COOR' (wherein R' is a lower alkyl or aralkyl which is optionally substituted), lower alkyl or halogenated lower alkyl; or R.sup.1 and R.sup.2, together with adjacent carbonyl group, form a cyclohexanone ring represented by the formula: ##STR2## R.sup.3 is a phenyl group optionally being substituted, and, ring A is a benzene nucleus which is optionally substituted, or a heterocyclic ring containing S or O optionally being substituted!.

Lignan analogues, methods of preparation thereof and anti-hyperlipemic

An anti-hyperlipemic agent which has a potent activity of reducing LDL and VLDL cholesterols, which are thought to be a risk factor for arteriosclerosis among total blood cholesterols, and which is excellent in the antioxidant activity on LDL, is provided. Additionally, a compound and a pharmaceutically acceptable salt thereof are disclosed, which is represented by Formula (I): ##STR1## wherein R.sup.1 is a lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl group which is optionally substituted; R.sup.2 is a group represented by the formula: -COOR' (wherein R' is a lower alkyl or aralkyl which is optionally substituted), lower alkyl or halogenated lower alkyl; or R.sup.1 and R.sup.2, together with adjacent carbonyl group, form a cyclohexanone ring represented by the formula: ##STR2## R.sup.3 is a phenyl group optionally being substituted, and, ring A is a benzene nucleus which is optionally substituted, or a heterocyclic ring containing S or 0 optionally being substituted!.

Preparation of compounds of lignan series

An anti-hyperlipemic agent which has a potent activity of reducing LDL and VLDL cholesterols, which are thought to be a risk factor for arteriosclerosis among total blood cholesterols, and which is excellent in the antioxidant activity on LDL, is provided. Additionally, a compound and a pharmaceutically acceptable salt thereof are disclosed, which is represented by Formula (I): ##STR1## [wherein R.sup.1 is a lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl group which is optionally substituted; R.sup.2 is a group represented by the formula: --COOR' (wherein R' is a lower alkyl or aralkyl which is optionally substituted), lower alkyl or halogenated lower alkyl; or R.sup.1 and R.sup.2, together with adjacent carbonyl group, form a cyclohexanone ring represented by the formula: ##STR2## R.sup.3 is a phenyl group optionally being substituted, and, ring A is a benzene nucleus which is optionally substituted, or a heterocyclic ring containing S or O optionally being substituted].

The compounds of the present invention inhibit HMG-CoA reductase, subsequently suppress the synthesis of cholesterol; and are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.

Benzofuran derivative

A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.

Azabicycloalkanes

Novel pyridonecarboxylic acids of the formula: ##STR1## or the pharmaceutically acceptable salts thereof having a more potent and longer lasting antibacterial activities against gram-positive and gram-negative bacteria than known analogues, useful for antibacterial agents at an oral dose of 1-500 mg, preferably 50-100 mg per day to an adult.

Quinolone-carboxylic acids as antibacterial agents

A compound of the formula: ##STR1## (wherein Az is imidazolyl or triazolyl;

Azole type dioxolane derivatives

Growing community of inventors

Osaka, Japan

Shiro Kida