Chugai Seiyaku Kabushiki Kaisha

Wisconsin Alumni Research Foundation

Isao Matsunaga

Minoru Shindo

Kiyoshige Ochi

Yusuke Harada

Haruki Ogawa

Nobuhiro Oi

Hiroshi Okazaki

Teizo Shinozaki

Takao Noto

Kanji Moro

Toshiyuki Nebashi

Bunya Aoki

Takao Kimura

Hisao Endo

Noboru Kubodera

Hiroyuki Nagano

Shun-ichi Hata

Kazushige Sakai

Chikara Kaneko

Hiroyuki Nabata

Tamotsu Yamazaki

Yasuhiro Ohba

Katsuhito Miyamoto

Mitiro Takagi

Eigoro Murayama

Yasumi Uchida

Yoshikazu Hinohara

Hector Floyd Deluca

Masayuki Ishikawa

Takashi Mori

Sakae Takaku

Koji Mizuno

Takashi Matsuno

Toshichika Ogasawara

Shun-Ichi Hata

Eiichi Hoshino

Shigeru Takanashi

Yugo Ikeda

Morio Kakimoto

Shin-ichi Kaiho

Yasuo Fujimura

Toshio Kuroki

Mitsuru Tanemura

Hiroki Mitsui

Sadao Tanaka

Yasuyuki Shiraki

Masahiko Matsumoto

Tatsuo Kujirai

Shigeru Sugano

Kana Kojima

Yumiko Tsuruma

Mitsura Tanemura

Masami Saitou

Rokuro Kaifu

Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed. The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.

Vitamin D derivatives, process for producing the same and their use in

Benzoic acid derivatives of the formula: ##STR1## wherein n is an integer of 0 to 2; R.sub.1 to R.sub.3 which may be the same or different each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or nitro group; R.sub.4 is a hydroxyl group or the group --NHZ (Z is hydrogen atom or a lower alkyl group), or an alkali metal salts thereof are useful as an infection control agent. These derivatives excepting compounds of the formula above wherein n is 0 or 1; any one of R.sub.1 to R.sub.3 is 5-chloro, 5-methoxy or 5-nitro and the remainder is a hydrogen atom; and R.sub.4 is a hydroxyl group; and compounds of the formula wherein n is 0 or 1; two of R.sub.1 to R.sub.3 are 3,5-dichloro or 3,5-dinitro and the remainder is a hydrogen atom; and R.sub.4 is a hydroxy group) are novel, and they were first prepared in this invention.

Benzoic acid derivatives

A method of diminishing appetite, in turn preventing and treating obesity, by administration of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and selected from a hydrogen atom or an acetyl group, or its pharmaceutically acceptable acid addition salt, and a pharmaceutical composition containing as an active ingredient the compound represented by the above formula.

Method of preventing and treating obesity

A 1.alpha.-hydroxy vitamin D.sub.3 derivative of the formula: ##STR1## where R.sub.1 is a hydroxyl group, an amino group or the group: OR' (where R' is a lower alkyl group having 1 to 7 carbon atoms that may or may not be substituted by a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group having 1 to 3 carbon atoms, an amino group, or an acylamino group); R.sub.2 is a hydrogen atom or a hydroxyl group), and a process for preparing the same are disclosed. The compound represented by the formula above has the calcium control action and the ability to induce differentiation in tumor cells and, therefore, are useful as an antitumor agents and a medicine for treating calcium dysbolism-caused diseases.

vitamin D.sub.3 derivatives having a substituent at 2-position

Complexes of pentaerythritol derivatives such as sulfuric acid ester of pentaerythritol or dipentaerythritol with a basic polyaluminum chloride and process for preparing the same are disclosed. The complex is novel and has a good anti-pepsin activity and therefore it is useful as an anti-ulcer agent. The complex is prepared by reacting pentaerythritol or dipentaerythritol with a sulfating agent and then reacting the resulting sulfate with a basic polyaluminum chloride.

Pentaerythritol derivative

Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.

Phenyliperazine derivatives

Compounds of the formula ##STR1## (wherein R.sub.1 is a lower alkyl group, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group or a lower alkoxycarbonyl group; two adjacent groups of R.sub.2, R.sub.3 and R.sub.4 may combine to form a methylenedioxy group; n is an integer of 2 to 6) or salts thereof, are disclosed. These compounds are useful as agents for treating circulatory diseases because they have hypotensive action and are capable of increasing the cerebral blood flow, decreasing the heart rate and suppressing ventricular arrhythmia due to myocardial ischemia.

Method for treating circulatory diseases by using (2-lower

An anti-peptic ulcer agent which contains as an active ingredient aminobenzoic acid compounds of the formula ##STR1## (wherein R.sub.1, R.sub.2, and R.sub.3 which may be the same or different represent a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group but they do not represent a hydrogen atom at the same time) or pharmaceutically acceptable salts thereof and a method of preventing or treating a human in need of said prevention or treatment an effective amount of said active ingredient are disclosed.

Anti-peptic ulcer agent

An agent for treating diseases in circulatory organs which comprises a piperazine compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are as defined hereunder, or a salt thereof and a pharmaceutically acceptable carrier.

Compositions and methods for treating diseases in circulatory organs

Novel uracil derivatives of the formula ##STR1## (wherein R.sub.1, R.sub.2 R.sub.3 and X are defined in the description) and their pharmaceutically acceptable salts, process for preparing the same and pharmaceutical composition containing the same are disclosed. The uracil derivatives have good antitumor activity and, therefore, are useful as antitumor preparation.

Novel uracil derivatives, process for preparing the same and a

Novel pyrazoloindazole derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxyl group or benzyloxyl group; R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or phenyl group (provided R.sub.1 and R.sub.2 are not hydrogen at the same time); and X.sup..crclbar. is a halide ion, a hydroxide ion, a methanesulfonate ion, a p-toluene sulfonate ion, a sulfate ion, a nitrate ion, a carbonate ion, an acetate ion, a benzoate ion or a salicylate ion, a process for preparing the derivatives, and a pharmaceutical composition containing the same are disclosed. The derivatives have good bronchodilating action for human without exhibiting substantially bad effects on the functioning of heart, and therefore, they are useful as a drug.

Pyrazoloindazole derivatives and bronchodilating composition

.alpha.-Substituted ureido-benzylpenicillanic acids of the formula ##STR1## (wherein R.sup.1, X and Y are as defined in the description) and pharmaceutically acceptable salts thereof, and a bactericidal composition comprising the above penicillanic acid or the salt and a pharmaceutically acceptable carrier are disclosed. The acids and salts thereof have high antibacterial activities against Gram-positive and Gram-negative bacteria, particularly those of the genus Pseudomonas.

.alpha.-Substituted ureido-benzylpenicillanic acids

Cephalosporin derivatives which have an excellent antibacterial action particularly against bacteria belonging to genus Pseudomonas or Serratia and are represented by the formula: ##STR1## wherein R.sub.1 R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n are as defined in the specification, and salts thereof; a process for preparing the same; and an antibacterial preparation containing the same as an active ingredient are disclosed.

Cephalosporin derivatives

Cephalosporin derivatives which have an excellent antibacterial action particularly against bacteria belonging to genus Pseudomonas or Serratia and are represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n are as defined in the specification, and salts thereof; a process for preparing the same; and an antibacterial preparation containing the same as an active ingredient are disclosed.

Growing community of inventors

Tokyo, Japan

Isao Matsunaga