Kissei Pharmaceutical Co., Ltd.

Ono Pharmaceutical Co., Ltd.

Hiromu Harada

Kinji Iizuka

Tetsuhide Kamijo

Satoshi Akahane

Ryoji Yamamoto

Nobuyuki Tanaka

Tetsuro Tamai

Harunobu Mukaiyama

Takehiro Ishikawa

Junichi Kobayashi

Arao Ujiie

Yukihiko Hotei

Koji Kamata

Kiyoshi Kasai

Hidetoshi Isawa

Masahiko Uchida

Atsushi Tsubaki

Akira Iyobe

Toshiaki Yamaguchi

Yoshinori Nonaka

Junichi Sonehara

Naoyuki Tsutsumi

Hideo Nagata

Humiyasu Satoh

Hiroshi Kusama

Mitsuhiro Ichihara

Hideki Hujikura

Tetsuhide Kamino

The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has &#x3b2;3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates 

Intermediates in producing phenoxyacetic acid derivatives and method of using the same

Intermediates in producing phenoxyacetic acid preventives and method of using the same

The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has &#x3b2;3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates. 

The present invention provides ethyl (&#x2212;)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent &#x3b2;-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Crystals of hydroxynorephedrine derivative

Polyphenylene ether resin

Piperidino-3,4-dihydrocarbostyril compounds represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy group or an acyloxy group having 2 to 11 carbon atoms; one of R.sup.2 and R.sup.3 represents a nitro group, a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 3 carbons atoms, or a halogen atom, and the other represents a hydrogen atom; and pharmaceutically acceptable salts thereof, exhibit platelet aggregation inhibiting activity and thus being useful as therapeutic agents for the prevention or treatment of cerebral ischemic disorders and arterial ischemic disorders.

Piperidino-3,4-dihydrocarbostyril compounds

Benzofuro[3,2-c]quinoline compounds of the general formula: ##STR1## wherein (1) each of R.sup.1 and R.sup.2 is the same, and represent a group of the formula of --OR.sup.3 in which R.sup.3 represents a carbamoyl group, an N-mono-alkylcarbamoyl group, an N,N-dialkylcarbamoyl group, an alkylsulfonyl group, a formyl group or an aliphatic acyl group which may have an alkoxycarbonyl group as a substituent; m represents zero, 1 or 2; n represents zero or 1; with the proviso that n is not zero when m is zero,

Acylated benzofuro[3,2-c]quinoline compounds with utility as treatments

The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound. Illustrative of the process is the reaction of 3,4-dimethoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of piperidine to provide an intermediate salt precipitate, and the salt is treated with an acidic reagent to yield N-(3,4-dimethoxycinnamoyl)anthranilic acid product.

Method for the production of nuclear substituted cinnamoylanthranilic

The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound. Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.

Process for the production of nuclear substituted cinnamoylanthranilic

1,3-Disubstituted imidazoles of the general formula (I): ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, Y is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or an dialkoxymethyl group having 3 to 13 carbon atoms, Z is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, n is zero or 1. The said compounds are intermediates for producing the imidazole derivatives of the general formula (V) above which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutical agents for treatment of diseases caused by thromboxane A.sub.2.

1,3-Disubstituted imidazoles

The imidazole derivatives of the general formula: ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, D is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or a dialkoxymethyl group having 3 to 13 carbon atoms, Q is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, Z is ##STR2## (wherein E is a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms, Y is an oxygen atom or a sulfur atom and may be connected with either A or B), n is zero or 1, with the proviso that n is 1 when Y connects with B. These compounds are novel compounds and are useful as intermediates in producing 1-substituted imidazole derivatives which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutically active agents for treatment of diseases caused by thromboxane A.sub.2.

Imidazole derivatives

Growing community of inventors

Nagano, Japan

Hiromu Harada