Banyu Pharmaceutical Co. Ltd

Ricoh Company, Ltd.

Toshihiko Satoh

Yoshikazu Iwasawa

Kumiko Kawakami

Sachie Arai

Tetsuya Aoyama

Yoshiaki Monden

Toshio Kamei

Takashi Nomoto

Masahiro Hayashi

Yoshimi Tsuchiya

Mitsuru Ohkubo

Yasufumi Nagata

Hitoshi Masaki

Yumiko Sakuma

Morihiro Mitsuya

Katsumasa Nonoshita

Yoshio Sawasaki

Kohki Isago

Yutaka Tomita

Haruhiko Sakurai

Toshiaki Higashi

Substituted amide derivatives

The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.5 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; R.sup.6 is a lower alkyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group of the formula --NR.sup.b --, the other is a carbonyl group or a group of the formula --CHR.sup.a --, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.

N,N-disubstituted amic acid derivatives

Cyclic amic acid derivatives

The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.5 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group, R.sup.6 is a lower alkyl group, and R.sup.7 is a hydrogen atom or a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group of the formula --NR.sup.b --, the other is a carbonyl group or a group of the formula --CHR.sup.a --, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.

N, n-disubstituted amic acid derivatives

The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2 and Ar.sup.3 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; Q represents a group of the formula --(CH.sub.2).sub.m -- (m is an integer of from 1 to 6) or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p -- (W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; n and p are a integer of from 0 to 3); R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aryl or heteroaromatic ring group which may be substituted; R.sup.2, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.3 and R.sup.4 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; R.sup.5 represents a lower alkyl group; and R.sup.6 represents a hydrogen atom or a lower alkyl group, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.

Substituted heterocyclic derivative having squalene epoxidase inhibition

Substituted amine derivatives represented by the general formula ##STR1## wherein Q is --C--D--E--F--G--M-- or --N--H--I--J--K--L-- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, --CHR.sup.a --, --R.sup.b .dbd. or --NR.sup.c -- (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or --NR.sup.c --]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub.3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.

Substituted amine derivatives having anti-hyperlipemia activity

Substituted amine derivatives represented by the general formula ##STR1## wherein Q is -C-D-E- F-G-M- or -N-H-I-J-K-L- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, -CHR.sup.2 -, -R.sup.b = or -NR.sup.c - (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or -NR.sup.c -]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub. 3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.

Substituted amine derivatives having antihyperlipemia activity

A device for measuring a rate exposed to deleterious materials comprises a heartbeat sensor for sensing heart rates, a deleterious material sensor for sening concentrations of deleterious materials in the air, a memory for storing the conversion values for converting the heart rates into corresponding respiration rates, and an operation unit. The operation unit counts a heart rate based a heartbeat signal received from the heartbeat sensor, calculates a respiration rate corresponding to the heart rate based on a conversion value read out from the memory, and calculates a rate exposed to deleterious material per unit time based on the calculated respiration rate and a signal respresenting a concentration of the deleterious material which signal is received from the deleterious material sensor.

System for determining hazardous substance exposure rate from

Growing community of inventors

Tsukuba, Japan

Toshihiko Satoh