Abstract: Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1??-amide derivative of the formula (II) and a caprazene-1??-ester derivative of the formula (III) from caprazene. Further, there could be synthesized a caprazol-1??-amide derivative of the formula (V) and a caprazol-1??-amide-3??-ester derivative and a caprazol-3??-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol. The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.

Abstract: There are disclosed a novel ?-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.

Abstract: By culturing Lysobacter sp. BMK333-48F3 (deposit number of FERM BP-7477), an antibiotic, tripropeptin Z, tripropeptin A, tripropeptin B, tripropeptin C or tripropeptin D represented by the general formula (I): wherein R is 7-methyl-octyl group, 8-methyl-nonyl group, 9-methyl-dodecyl group, 10-methyl-undecyl group or 11-methyl-dodecyl group, is obtained as antibiotics having excellent antibacterial activities against bacteria and having a novel molecular structure. These tripropeptins each have an excellent antibacterial activity against various bacteria and drug-resistant strains thereof, such as methicillin-resistant strains and vancomycin-resistant strains.

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.

Abstract: Provided are novel processes for the efficient production of L-epi-2-inosose and epi-inositol which are useful either as various medicines or intermediates for the syntheses of various medicines. In the processes, inexpensive myo-inositol is used as a starting compound which is reacted with a gram-negative bacterium capable of converting myo-inositol into L-epi-2-inosose, and thereby producing L-epi-2-inosose by conversion of myo-inositol into L-epi-2-inosose. A biologically pure culture of Pseudomonas sp. AB 10215 strain is also provided which has a characteristic nature of being capable of converting myo-inositol into L-epi-2-inosose.

Abstract: A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents —O— and R represents a hydroxyl group, by using a microorganism belonging to the genus Cunninghamella; and a Cunninghamella sp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents —O— or —CH2—, and R represents a hydroxyl group when X represents —O—, or a hydrogen atom when X represents —CH2—.

Abstract: An antibiotic SF2487 substance having the formula (I) or a salt thereof possesses an antimalarial activity against the proliferation of malarial parasites and is therefore useful as an antimalarial drug.

Abstract: Compounds represented by formula (I) below; a process for producing the compounds by culturing a microorganism belonging to the genus Aspergillus and isolating the above-mentioned compounds from the culture; an angiogenesis inhibitory agent containing as an active ingredient the compounds; and an Aspergillus sp. F-1491 (FERM BP-8288) strain capable of producing the compounds. In formula (I), R represents a methyl group or an ethyl group, R1 represents a hydrogen atom, a chlorine atom, a hydroxyl group or a methoxy group, R2 represents a hydroxyl group, or R1 and R2 taken together form an epoxy ring structure.

Abstract: A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents —O— and R represents a hydroxyl group, by using a microorganism belonging to the genus Cunninghamella; and a Cunninghamella sp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents —O— or —CH2—, and R represents a hydroxyl group when X represents —O—, or a hydrogen atom when X represents —CH2—.

Abstract: A compound of the formula (I): and a compound of the formula (V): as well as a compound of the formula (X): which are each a novel siastatin B derivative having a potent inhibitory activity against a glycosidase, are now synthesized by new processes. The compound of the formula (I), the compound of the formula (V) and the compound of the formula (X) have a potent enzyme-inhibitory activity to a glycosidase, which is particularly N-acetyl-galactosaminidase, galactosidase, glucosidase and mannosidase.

Abstract: Provided are novel processes for the efficient production of L-epi-2-inosose and epi-inositol which are useful either as various medicines or intermediates for the syntheses of various medicines. In the processes, there is used inexpensive myo-inositol as a starting compound. That is, there is now developed a new process which comprises reacting myo-inositol with a gram-negative bacterium capable of converting myo-inositol into L-epi-2-inosose, and thereby producing L-epi-2-inosose by conversion of myo-inositol into L-epi-2-inosose. Further, a novel process is provided, which comprises reacting the so produced L-epi-2-inosose with a reducing agent made of an alkali metal boron hydride or any other alkali metal hydride in an aqueous reaction medium, to produce epi-inositol and myo-inositol, and then isolating epi-inositol from the resulting reaction product composed of the epi-inositol and myo-inositol.

Abstract: There have been obtained, by cultivation of Streptomyces sp. MK730-62F2 (deposit number of FERM BP-7218), antibiotic caprazamycins A to F having by the following general formula (I) wherein R is tridecyl group, 11-methyl-dodecyl group, and others. These caprazamycins have excellent antibacterial activities against various acid-fast bacteria and various bacteria as well as their drug-resistant strains.

Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.

Abstract: A sulphostin analogue represented by the general formula, wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable salt thereof.

Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.

Abstract: Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

Abstract: 20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.

Abstract: Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

Abstract: As novel substances having an activity of inducing an apoptosis even on the apoptosis-resistant cancer cells, there are obtained polyoxypeptin and deoxypolyoxypeptin represented by the following general formula (I) wherein R denotes a hydroxyl group for polyoxypeptin, or R denotes a hydrogen atom for deoxypolyoxypeptin, by cultivation of Streptomyces sp. MK498-98F14 strain. Polyoxypeptin and deoxypolyoxypeptin are physiologically active substances which have an activity of inducing apoptosis on a human pancreatic adenocarcinoma cell, AsPC-1 cell.

Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. wherein y is 0 or 1; R1 represents an unsubstituted C1-C8 alkyl group or others; R2 represents a hydrogen atom, a C1-C5 alkyl group or others; R3 represents a hydrogen atom, a C1-C8 alkyl group or others; R4 represents a hydrogen atom, a C1-C3 alkyl group or others; R5 represents a group —OR42, a group  or others.