Takeda Chemical Industries, Inc.

Takeda Chemical Ind., Ltd.

Takeda Chemical Corporation

Kitasato Kenkyushio

Setsuo Harada

Hideo Ono

Shigetoshi Tsubotani

Mitsuko Asai

Seiichi Tanida

Susumu Shinagawa

Yukimasa Nozaki

Yasunori Funabashi

Tsuneo Kanamaru

Hirotomo Masuya

Nobuhiro Inatomi

Takashi Iwasa

Shigeharu Tanayama

Michihiko Ochiai

Shinji Terao

Mitsuhiro Wakimasu

Hideaki Natsugari

Katsumi Itoh

Akinobu Nagaoka

Toru Hasegawa

Kazuaki Kitano

Takenori Ishimaru

Hideo Shirafuji

Kouichi Yoshioka

Tsuneaki Hida

Akira Imada

Nozomi Katayama

Toyokazu Kishi

Toshiyuki Yamazaki

Koichi Yukishige

Taiki Kusaka

Junya Okada

Disclosed are (1) a structurally novel 6,9-hemiacetal- erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions br a salt thereof, which has an excellent gastrointestinal function promoting effect and is low in toxicity; (2) a process for preparing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which comprises reacting a 6,9-hemiacetal-erythromycin derivative or a salt thereof with an organism-derived oxidase; and (3) a gastrointestinal function promoting agent containing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof.

15-hydroxy 6,9-hemiacetal erythromycin compounds

A compound of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen or aliphatic acyl, A is amino which may be protected, X is an amino acid sequence consisting of 1 to 10 amino acid residues which contain at least one amino acid residue having a water-solubility enhancing group, or a salt thereof has an activity of remarkably improving hematopoietic disorder and is useful as an immuno-stimulating agent or an agent for treating thrombocytopenia.

2-amino-6,7-dihydroxy-4-thiaheptanoic acid derivatives, production and

Disclosed are (1) a structurally novel 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which has an excellent gastrointestinal function promoting effect and is low in toxicity; (2) a process for preparing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which comprises reacting a 6,9-hemiacetal-erythromycin derivative or a salt thereof with an organism-derived oxidase; and (3) a gastrointestinal function promoting agent containing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof.

14 and/or 15-hydroxy 6,9 hemiacetal erythromycin derivatives

TAN-1251 compounds and their production from penicillium thomii

A compound having the formula (I) or (II) ##STR1## wherein R.sup.1 is a hydrogen atom or an organic residue bonded via a carbon atom, R.sup.2 is a hydrogen atom or a N-protecting group, --COR.sup.3 is an optionally esterified or amidated carboxyl group, R.sup.4 and R.sup.5 are the same or different and respectively a hydrogen atom or an acyl group or a chain or alicyclic hydrocarbon group optionally having an aryl substituent, R.sup.6 is NOH or O, n is an integer of 0 to 3, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom may form a ring or an optionally substituted benzylidene amino group, which is useful therapeutics of brain dysfunction.

Cerebral function ameliorating agents related to Tan-950 A

Novel antibiotics TAN-1057 represented by the formula: ##STR1## wherein, the absolute configuration at (A) is R or S; R.sub.1 is hydrogen and both R.sub.2 and R.sub.3 taken together form a chemical bond, or R.sub.3 is hydrogen and both R.sub.1 and R.sub.2 taken together form a chemical bond; were produced by microorganisms belonging to the genus Flexibacter. TAN-1057 strongly inhibit the growth of pathogenic microorganisms and malignant tumors, thus being useful as therapeutic agents of infectious diseases or antitumor agents.

Antibiotics TAN-1057

A compound of the formula: wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.

Derivatives of .beta.-amino-.gamma.-trimethylammonio-butyrate and their

A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.

Antibiotic tan-749, its derivatives, production and use thereof

The compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, amino, isonitrile or an organic residue bonded through nitrogen; R.sup.2 is carboxy or a group derivable therefrom; X is hydrogen, methoxy, formylamino, alkyl which may be substituted, alkylthio in which the sulfur atom may be oxidized or azido, or forms a double bond together with the adjacent carbon atom; provided that when R.sup.1 is acetylamino or amino and X is hydrogen, R.sup.2 is not para-nitrobenzyloxycarbonyl or benzhydryloxycarbonyl, or a pharmaceutically acceptable salt thereof, exhibit excellent antimicrobial activity, and are utilized as antimicrobial agents.

Antibiotic derivatives, their production and use

As the novel antibiotic TAN-950A having the structural formula ##STR1## and salt thereof of the present invention show antimicrobial action against fungi, they can be used in the therapeutics of fungal infections, in human and other animals etc. by oral, parenteral or external administration.

Antibiotic TAN-950A, its production and use

The iron-containing biologically active peptide TAN-866 produced by microorganisms belonging to the genus Pseudomonas and its iron free compounds have antibacterial activity mainly against gram-negative bacteria. These peptides can be used as a therepeutic agent for bacterial infections in mammals, domestic fowl, etc., caused by Pseudomonas aeruginosa. Further, TAN-866 and its deacyl compounds are also promising as the starting materials and intermediates for the synthesis of novel products.

Biologically active peptides TAN-866

Hygromycin, epihygromycin and a mixture thereof have potent inhibitory activity against Treponema hyodysenteriae and are useful for treatment of swine dysentery.

Method for treatment of swine dysentery

A compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.

Derivatives of beta-amino-gamma-trimethylammonio-butyrate and their

A compound of the formula: ##STR1## wherein R.sup.1 is ##STR2## HOOC--(CH.sub.2).sub.3 --CO-- or hydrogen, or a salt thereof, is useful as an intermediate for the production of cephem compounds, and some of them are useful as antimicrobial agents.

Cephem compounds

A compound of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or formylamino, R.sup.2 is a residue of amino acid selected from the group consisting of serine and alanine, or a peptide of at least one of these amino acids, or hydrogen, R.sup.3 stands for --NH--C(.dbd.NH)--NH.sub.2 or --CH.sub.2 NH.sub.2, or its salt, which can be produced by cultivating a microorganism belonging to the genus Xanthomonas, is useful as a therapeutic agent against infectious disease caused by bacteria.

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Kawanishi, Japan

Setsuo Harada