Takeda Chemical Industries, Inc.

Fuji Photo Film Company, Limited

Senju Pharmaceutical Co., Ltd.

Hamari Chemicals, Ltd.

Kanji Meguro

Yutaka Kuwada

Hiroyuki Tawada

Hitoshi Ikeda

Takeshi Fujita

Hideaki Natsugari

Yoshiaki Sato

Kohei Nishikawa

Akinobu Nagaoka

Takeshi Fugono

Chitoshi Hatanaka

Satoru Ooi

Morio Yagihara

Yoshio Inagaki

Takashi Sohda

Hiroyuki Mifune

Shoji Ishiguro

Yujiro Yamamoto

Takao Matsuo

Shirou Maeda

Toshiko Kita

Shiro Maeda

The present invention relates to an antibacterial agent, which comprises, as an active ingredient, a compound represented by the following general formula (1): or a pharmaceutically acceptable salt thereof.

2,4-diamino-1,3,5-triazine derivatives

A quinoline derivative of the formula (I): ##STR1## wherein each phenyl ring of A and B can have one or more substituents; X is ##STR2## (R.sup.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group) or ##STR3## (R.sup.2 is a hydrogen atom or a lower alkyl group); Y is --(CH.sub.2).sub.m --(m is 0, 1 or 2) or --CH.dbd.CH--, Z is a group of the formula: ##STR4## wherein each phenyl ring of C and D can have one or more substituents, R.sup.3 and R.sup.4 are each a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, R.sup.5 is a halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, R.sup.6 and R.sup.7 are each a hydrogen atom or a lower alkyl group, and n, o and p are each 1 or 2; l is 0 or 1; or its salt, which is useful as a drug for atherosclerosis.

Quinoline derivatives, their production and use as ACAT inhibitors

Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

Tricyclic heterocyclic compounds, their production and use

Chromene derivatives, their production and use

Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen, an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

Certain 2-oxo-tetrahydro-cycloalkyl-benzopyran-3yl ureas having

Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.

Thienopyridine derivatives which are intermediates

Quinoline derivatives of the formula: ##STR1## , wherein R is hydrogen, alkyl or aralkyl; m and n are 0 or 1, and each of rings A, B and C can have substituents, which are useful as inhibitors for acyl-CoA:Cholesterolacyltransferase.

Quinoline derivatives, their production and use

A quinoline derivative of the formula (I): ##STR1## wherein each phenyl ring of A, B and C can have one or more substituents, X is ##STR2## (R.sup.1 is a hydrogen atom or a lower alkyl group) or ##STR3## (R.sup.2 is a lower alkyl group or a lower alkoxy group), and n is 0 or 1, or its salt, which possesses an inhibitory action against acyl-CoA: cholesterol acyltransferase.

Thienopyridine derivatives and their pharmaceutical use

A compound of the formula: ##STR1## (wherein R.sup.1 is hydrogen or a lower alkyl) can be produced advantageously by (1) reacting a compound of the formula: ##STR2## (wherein R.sup.1 has the meaning given above) with a halogenating agent or sulfonyl halide to give a compound of the formula: ##STR3## (wherein R.sup.1 has the meaning given above and X is a halogen or an alkyl- or aryl-sulfonyloxy), (2) reacting the resulting compound with a compound of the formula: ##STR4## to give a compound of the formula: ##STR5## (wherein R.sup.1 has the meaning given above), (3) reacting the resulting compound with a compound of the formula: ##STR6## to give a compound of the formula: ##STR7## (wherein R.sup.1 has the meaning given above), and (4) subjecting the resulting compound to catalytic reduction.

Pyridine and thiazolidinedione derivatives

Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is alkyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; R.sup.4 and R.sup.5 are the same or different and each is hydrogen, halogen, nitro, trifluoromethyl, alkyl, cycloalkyl, alkoxy, cyano, alkoxycarbonyl or alkylthio; R.sup.6 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a pyridyl; X is oxygen, sulfur, vinylene, azomethine or a group of the formula ##STR2## A is alkylene; Ar is aryl or a pyridyl; m is an integer of 1 to 3; n is an integer of 0 to 2.

Substituted heterocyclylalkyl esters of

A compound of the formula: ##STR1## (wherein R.sup.1 is hydrogen or a lower alkyl) can be produced advantageously by (1) reacting a compound of the formula: ##STR2## (wherein R.sup.1 has a meaning given above) with a halogenating agent or sulfonyl halide to give a compound of the formula: ##STR3## (wherein R.sup.1 has a meaning given above and X is a halogen or an alkyl- or aryl-sulfonyloxy), (2) reacting the resulting compound with a compound of the formula: ##STR4## to give a compound of the formula: (wherein R.sup.1 has the meaning given above), (3) reacting the resulting compound with a compound of the formula: ##STR5## to give a compound of the formula: ##STR6## (wherein R.sup.1 has the meaning given above), and (4) subjecting the resulting compound to catalytic reduction.

Method for producing thiazolidinedione derivatives

1,4-Benzoxazine derivatives representable by the general formula; ##STR1## wherein R.sup.1 and R.sup.2 independently stand for hydrogen, halogen atom, nitro group, an optionally substituted lower alkyl group, an optionally substituted amino group, an optionally substituted hydroxyl group, a lower alkoxycarbonyl group, or when R.sup.1 and R.sup.2 are adjacent to each other,

1,4-benzoxazine derivatives and pharmaceutical use

A thiazolidinedione derivative of the general formula: ##STR1## wherein X is an oxygen or sulfur atom, R.sup.1 and R.sup.2 each independently is hydrogen or a hydrocarbon residue which may optionally be substituted and R.sup.1 and R.sup.2 may jointly, together with the oxazole or thiazole ring, form a condensed ring and A is a lower alkylene group; or a salt thereof, are novel compounds, which exhibit in mammals blood sugar- and lipid-lowering activity, and are of value as a therapeutic agent for diabetes and/or therapeutic agent for hyperlipemia.

Growing community of inventors

Nishinomiya, Japan

Kanji Meguro