Kureha Chemical Industry Company, Limited

Kureha Kagaku Kogyo Kabushiki Kaisha

Michihito Ise

Mikiro Yanaka

Hiroyuki Enari

Fuyuhiko Nishijima

Toru Yamazaki

Toshikazu Dewa

Hiroshi Takahashi

Shigeru Suzuki

Yasuo Uehara

Mikio Sugano

Hideo Hayashi

Hiroshi Maruoka

Naohiro Sonobe

Hideyuki Yamato

Haruhisa Hayashi

Satoshi Mitsuhashi

Susumu Morimoto

An adsorbent for an oral administration, comprising a porous spherical carbonaceous substance wherein a diameter is 0.01 to 1 mm, a specific surface area determined by a BET method is 700 m /g or more, a volume of pores having a pore diameter of 20 to 15000 nm is from not less than 0.04 mL/g to less than 0.10 mL/g, a total amount of acidic groups is 0.30 to 1.20 meq/g, and a total amount of basic groups is 0.20 to 1.00 meq/g, is disclosed.

Adsorbent for oral administration

Benzimidazole derivative

Cardiac diseases improving method

This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly, this invention relates to cardiac diseases improving agents composed of effective ingredients of aromatic compounds or pharmacologically acceptable salts thereof shown by below mentioned general formula. ##STR1## (wherein, substituents thereof typically include, R.sup.1, R.sup.4, R.sup.13 representing hydrogen atom, an alkyl group, a haloalkyl group and so forth, R.sup.8 representing --CO--, --SO.sub.2 -- or single bond, R.sup.2 representing a 3-7 membered aliphatic cyclic amino group having at least one nitrogen atom, R.sup.7 representing --CO-- or --SO.sub.2 --, and R.sup.12 representing N-substituted valeramido group.)

Cardiac diseases improving agents

An aromatic compound of the formula (I): ##STR1## specifically, for example, 3-��(4-carboxyphenyl)methyl!valeramido!-4-dimethylaminobenzoic acid 4'-methylpiperazide, or a salt thereof, and a pharmaceutical composition comprising said aromatic compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent which provides sufficiently effective alleviation of renal dysfunction without affecting blood pressure at a low blood concentration.

Aromatic compound and pharmaceutical composition

A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH; R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, or --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.

Benzene derivatives and pharmaceutical composition

A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O) (CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O) R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH; R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, or --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.

A pyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or --NHR.sup.11 group; R.sup.2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, --(CH.sub.2).sub.m C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.12, --NH(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH(CH.sub.2).sub.p C.sub.6 H.sub.4 --OR.sup.13, --N(R.sup.14)(CH.sub.2).sub.q C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.15, --NHC(.dbd.O)(CH.sub.2).sub.r C.sub.6 H.sub.5, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --OR.sup.16, or --O(CH.sub.2).sub.s C.sub.6 H.sub.5 group; R.sup.3 is --COOH, --COOR.sup.17, hydroxyl, --OR.sup.18, --NH.sub.2, --N(R.sup.19).sub.2, --NHR.sup.20, azole, or sulfonic acid group; R.sup.11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, and R.sup.20 are independently alkyl of 1 to 6 carbon atoms; m is 0 or an integer of 1 to 6; n is 0 or an integer of 1 to 6; p is 0 or an integer of 1 to 6; q is 0 or an integer of 1 to 6; r is 0 or an integer of 1 to 6; and s is 0 or an integer of 1 to 6, or a salt thereof, and a pharmaceutical composition comprising said pyrimidine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.

Pyrimidine derivatives and pharmaceutical composition

An agent for reducing nephrotoxicity due to a platinum complex compound, comprising an activated spherical carbon as an active ingredient is disclosed.

Agent for reducing nephrotoxicity due to medicine

The disclosure describes a method of treating a patient suffering from hemorrhoidal diseases, comprising orally administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a spherical activated carbon having a particle size of 0.05 to 2 mm.

Method for the treatment of hemorrhoidal diseases

The disclosure describes a method of treating a patient suffering from stoma-peripheral inflammation diseases, comprising orally administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a spherical activated carbon having a particle size of 0.05 to 2 mm.

Method of treatment for stoma-peripheral inflammation diseases

The disclosure describes a method of treating a patient suffering from inflammatory bowel diseases, comprising orally administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a spherical activated carbon having a particle size of 0.05 to 2 mm.

Method for the treatment of inflammatory bowel diseases

There is disclosed an enhancer for the antianemia effect of erythropoietin using a spherical carbon as an active ingredient in an amount effective for treating anemia in combination with erythropoietin. The enhancer is orally administered. The antianemia effect of erythropoietin can be remarkably enhanced, the dosage of erythropoietin can be remarkably decreased, and side effects from erythropoietin can be remarkably reduced. There is further disclosed a method of augmenting the antianemia effect of erythropoietin by administering to a patient an effective amount of a spherical carbon in combination with a portion of an effective amount of erythropoietin for treating anemia.

Enhancer for the antianemia effect of erythropoietin and method of

An antidiabetic agent containing a spherical carbon (e.g., an activated spherical carbon or a spherical carbonaceous adsorbent) as an active ingredient. The antidiabetic agent can be used for treating diabetes, preferably by using the agent internally as an oral medicine and will not be painful to a patient at an injection site, unlike conventional injections of insulin. Moreover, unlike conventional antidiabetic agents, the antidiabetic agent of the present invention will not induce hypoglycemia.

Growing community of inventors

Saitama, Japan

Michihito Ise