Takeda Chemical Industries, Inc.

Takeda Chemical Ind., Ltd.

Takeda Chemical Corporation

Kitasato Kenkyushio

Seiichi Tanida

Mitsuko Asai

Eiji Higashide

Masayuki Muroi

Toru Hasegawa

Setsuo Harada

Motowo Izawa

Mitsuhiro Wakimasu

Tsuneaki Hida

Nobuhiro Inatomi

Yasunori Funabashi

Koichi Yukishige

Shigeharu Tanayama

Shuichi Furuya

Tetsuya Aono

Tatsuhiko Kaneko

Haruhide Kimura

Yoshikazu Ohta

Heart muscular cell apoptosis inhibitors and remedies/preventives for heart diseases

This invention relates to a compound of the following formula or a salt thereof, their production and use. ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; R.sup.3 represents hydrogen, halogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; W represents an oxygen atom or sulfur atom; A represents a group forming a nitrogen-containing condensed ring at the 3,4- of a 1,4-thiazine ring; R.sup.1 and R.sup.2 may be combined to form a bivalent hydrocarbon group interrupted by one or more hetero atoms or an alkylene group. The above compound or a salt thereof not only has Th1 and Th2 cell function modulating activity but has splenocyte proliferation response, interleukin-5 production, and interferon-gamma production inhibitory activity and finds application as an effective therapeutic and/or prophylactic agent for allergic or autoimmune diseases or as an effective therapeutic and/or prophylactic agent for graft rejection or graft-vs-host disease.

Condensed thiazine derivatives, their production and use thereof

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 invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof. The compound or salt thereof of the present invention possesses immunoenhancing activity and platelet reduction recovery activity, and can be used as a prophylactic/therapeutic agent for leukocytopenia in cancer chemotherapy or radiotherapy, as an immunoenhancing agent in bone marrow transplantation therapy and the treatment of osteomyelodysplasia and aplastic anemia, and as a prophylactic/therapeutic agent for thrombocytopenia.

Thioglycerol derivatives

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

A compound of the formula: ##STR1## wherein each R.sup.1, R.sup.2 and R.sup.3 is an aliphatic acyl group, X is an amino acid sequence consisting of 1 to 5 amino acid residues which contain at least one acidic amino acid residue, n is an integer of 0 to 4, provided that when n is 0, X has glutamyl-glycyl at its N-terminal and when n is 1 or 2, the acidic amino acid residue is an acidic amino acid residue other than D-glutamyl, or a salt thereof has an activity of remarkably improving anhematopoiesis and is useful as an immuno-stimulating agent having a leukocyte-increasing activity.

TAN-1511, its derivatives, production and use thereof

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

A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl and X is ##STR2## provided that when R.sub.1 is hydrogen, R.sub.2 is hydrogen or methyl and X is ##STR3## and when R.sub.1 is methyl, R.sub.2 is methyl and X is ##STR4## is produced by cultivating a a microorganism belonging to the genus Streptomyces in a culture medium. Said compound is useful as an antimicrobial agent and so forth.

Antibiotic TAN-420

Macbecin derivatives are produced by cultivating a microorganism of the genus Actinosynnema in a culture medium. The Macbecin derivatives are useful as antibacterial, antifungal or antiprotozoal agent.

Macbecin derivatives and their production

Novel antibiotic C-15003 PHM, which is produced by cultivating a microorganism belonging to the genus Nocardia and being capable of producing antibiotic C-15003 PHM, and novel C-15003 PHM acylate, which is produced by subjecting C-15003 PHM thus obtained to acylation reaction with an acylating agent, have antiprotozoan and antitumor activities.

Antibiotic C-15003 PHM and production thereof

Macbecin derivatives

A novel antibiotic C-14482 A.sub.1 is produced by cultivating a microorganism belonging to the genus Nocardia and capable of producing Antibiotic C-14482 A.sub.1 is a culture medium, whereby Antibiotic C-14482 A.sub.1 is elaborated and accumulated in the culture medium and recovering the same antibiotic. Antibiotic C-14482 A.sub.1 is useful as a germicide or disinfectant.

Culture of Nocardia ATCC 31309

A novel Antibiotic C-15003 is produced by cultivating a microorganism of the genus Nocardia. The Antibiotic C-15003 is useful as an antifungal agent or an antiprotozoan agent.

Process for preparing maytansinol

Maytansinoids

Novel Antibiotic C-15003PND, which has the formula: ##STR1## wherein R represents hydrogen, --CO--CH.sub.3, --CO--CH.sub.2 --CH.sub.3, ##STR2## is produced by cultivating a microorganism of the genus Nocardia. The Antibiotic C-15003PND wherein R is acetyl, propionyl, isobutyryl or isovaleryl is useful for an antifungal, antiprotozoal or antitumor agent and Antibiotic C-15003PND wherein R is hydrogen is useful for an intermediate thereof.

Growing community of inventors

Kyoto, Japan

Seiichi Tanida