Abstract: To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-O-(2,6-dideoxy-2-fluoro-3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-.alpha.-L-talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-O-(3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetrafluoro-.alpha.-L-talopyra nosyl- or -2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:General formula (I) ##STR1## General formula (II) ##STR2## wherein either one or both of A.sup.1 and A.sup.2 is or are an .alpha.-amino acid residue or an .omega.-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine-containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.

Abstract: 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.

Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group.

Abstract: An aqueous solution of kasugamycin or its salt is either mixed with a strongly acidic ion-exchange resin of the H.sup.+ -form in a reaction vessel, or is brought into contact with a strongly acidic ion-exchange resin of the H.sup.+ -form in a column containing said resin, followed by heating said aqueous solution and the resin under an atmospheric pressure or an elevated pressure, thereby to effect hydrolytic reaction of kasugamycin. By this reaction, an acidic reaction solution containing D-chiro-inositol is produced. This acidic reaction solution containing D-chiro-inositol is separated from the strongly acidic ion-exchange resin. Subsequently, D-chiro-inositol is recovered from the reaction solution. For this recovery, the acidic reaction solution is passed successively through a column of a strongly acidic ion-exchange resin of the H.sup.+ -form and through a column of a strongly basic ion exchange resin of the OH.sup.- -form, so that a neutral aqueous eluate containing D-chiro-inositol is obtained.

Abstract: Desalaninebenanomicin A has been synthesized by chemical conversion of benanomicin A. Amino acid derivatives of desalaninebenanomicin A having the general formula (Ia): ##STR1## where R.sup.a represents a hyhrogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group have been synthesized by condensing the 2-carboxyl group of desalaninebenanomicin A with a variety of amino acids. Among the derivatives of the formula (Ia) having antifungal activities, such desalaninebenanomicin A derivatives in which R.sup.a is a C.sub.2-5 alkyl group, a C.sub.2-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group are novel semi-synthetic antibiotics having antifungal activities.

Abstract: D-.beta.-Lysylmethanediamine represented by the formula (I) ##STR1## or a salt or a hydrate thereof has now been found to have an activity of inhibiting the infection with AIDS virus (a virus causative of acquired human immunodeficiency syndrome), mamely HIV. A pharmaceutical composition comprising the above compound or a salt or hydrate thereof as active ingredient is provided and expectable as one of remedial agents for treating AIDS which is now thought to be difficult to cure.

Abstract: A recess-gate type static induction transistor having a high breakdown voltage is provided, which includes an n-type channel region provided over an n.sup.+ -type drain region, p.sup.+ -type elongated gate regions provided in grooves of the channel region, n.sup.+ -type elongated regions formed on the channel region so as to be arranged in parallel with the gate regions, each of which is disposed between the gate regions, and a p.sup.+ -type guard ring region provided in the channel region and arranged to surround the gate regions. The elongated gate regions are coupled to the guard ring region at both edges. In addition, the outer-most elongated gate regions are coupled to the guard ring region along the longitudinal direction, respectively, thereby increasing the breakdown voltage of the device.

Abstract: As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Abstract: A compound of the following formula is provided: ##STR1## wherein A represents a carbonyl group which may be protected; B represents an aldehyde group which may be protected; R.sup.1 represents a hydroxyl group which may be protected; R.sup.2 represents a hydrogen atom or acyl group; W represents a hydrogen atom, hydroxyl group, lower alkanoyloxy group or substituted sulfonyloxy group; Y represents a hydrogen atom, halogen atom, hydroxyl group or substituted sulfonyloxy group; and broken line "-------" represents a double bond or single bond. This compound is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antimicrobial agent.

Abstract: A semiconductor device includes a substrate crystal of a type for epitaxial growth thereon. The substrate crystal has a (111)A face and a (111)B face. Also provided are at least two semiconductor regions of different conductivity types deposited by way of epitaxial growth on the (111)A face of the substrate crystal according to metal organic chemical vapor deposition, thereby providing a structure having a source and a drain. A gate side includes the (111)B face of the substrate crystal. A gate insulating layer is deposited by way of epitaxial growth on the gate side according to molecular layer epitaxy. Alternatively, the at least two semiconductor regions may be deposited on the (111)B face of the substrate crystal according to molecular layer epitaxy, and the gate insulating layer may be deposited on the (111)A face of the substrate crystal according to metal organic chemical vapor deposition.

Abstract: As new compounds are now synthetized 5-deoxy-5,5-difluoro derivatives of aminoglycosidic antibiotics of neamine, kanamycin A-series, kanamycin B-series, gentamicin-series and seldomycin-series. Further, the 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives are synthetized from 5-deoxy-5,5-difluorokanamycins A and B, as well as their analogues now obtained. The 5-deoxy-5,5-difluoro derivatives of the aminoglycosidic antibiotics now provided according to this invention have such antibacterial activities enhanced much more than or equal to those of the respectively corresponding parent aminoglycosidic antibiotics, while these 5-deoxy-5,5-difluoro derivatives exhibit values of the 50% lethal dosage (LD.sub.50) which are improved remarkably better when they are intravenously administered to mice, so that they have remarkedly reduced toxicities to mammals.

Abstract: As new antibiotics are obtained delaminomycins A, B and C having a formula (I) or (I') shown below, or salts thereof. Delaminomycins preferentially inhibit T cells and are useful as immunosuppressants, antineoplastic agents and antibacterial agents. ##STR1## wherein X is a hydroxyl group for delaminomycin A, a methoxy group for delaminomycin B and a hydrogen atom for delaminomycin C.

Abstract: The present invention is concerned with the zinc tranexamate represented by the formula: ##STR1## or its pharmacologically acceptable organic acid salts. The zinc compounds of the present invention, when given in smaller doses than tranexamic acid and cetraxate hydrochloride, exhibit anti-inflammatory and anti-ulcer activities, and are tasteless and odorless, thus being easy to be administered; in particular, the organic acid salts are water-soluble and can be processed into the liquid dosage forms of injectable solution and liquid preparations for external uses.

Abstract: As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Abstract: A semiconductor device has an n.sup.+ source region, a first n.sup.- channel region, a barrier layer, a second n.sup.- channel region, a pair of n.sup.+ drain regions, an insulating film, and a pair of metal electrodes over the respective n.sup.+ drain regions, all successively disposed on an upper surface of an n.sup.+ crystal substrate. The drain regions and the metal electrodes jointly provide a storage electric capacitance. A source electrode is disposed on the lower surface of the n.sup.+ crystal substrate. Bit information can be written and read at a high speed by tunneling through the barrier layer. According to a method of manufacturing the above semiconductor device, the n.sup.+ source region, the first n.sup.- channel region, the barrier layer, the second n.sup.- channel region, the n.sup.+ drain regions, the insulating film, and the metal electrodes are successively deposited on the n.sup.+ crystal substrate in a growing apparatus.

Abstract: A body of water is purified by filtering its water both physically and biologically through a filter layer preferably consisting of a floating filter layer, and by contacting aerobic bacterial flocks, which are formed in the filter layer in time, with the mud in the river bottom typically placed in an anaerobic condition so that denitrification of the river water by denitrifying bacteria may be promoted. Thus, the present invention assists the natural biological purification process, and can improve The transparency of the water, reduce BOD and COD, promote denitrification to a sufficient extent to make the water liveable for fish, and trap low concentration toxic chemical substances such as insecticides and herbicides into the bacterial flocks.

Abstract: The present invention relates to a 2-aminoethanesulfonic acid zinc complex represented by the following formula: ##STR1## (wherein M is an alkali metal atom), to a process for producing the said complex from 2-aminoethanesulfonic acid and to use of the said complex as an anti-hepatitis agent, liver function improving agent and anti-ulcer agent. The said complex exhibits not only improved physiological activities such as anti-hepatitis activity, suppressory activity against liver-function disorder and anti-ulcer activity but also protective and restorative activity for the digestive tract.

Abstract: A static induction thyristor has a first semiconductor area having a high impurity concentration of a first conductivity type. A second semiconductor area having low impurity concentration is formed adjacent to the first semiconductor area. A third semiconductor area having a high impurity concentration of a second conductivity type which is the conductivity type opposite to the first conductivity type is formed on a part of a surface of the second semiconductor area so located as to form a fourth semiconductor area located within the third semiconductor area. A fifth semiconductor area having a high impurity concentration of the first conductivity type is formed on the part of the surface of the second semiconductor area in spaced relation to the forth semiconductor area.

Abstract: A semiconductor device having a source region, a drain region and a channel region which are formed in a surface portion of a semiconductor substrate, and a gate formed with a material having a relatively high built-in voltage relative to the source region. This semiconductor device may further include, in the semiconductor substrate to extend along the channel region, a highly-doped region having a conductivity type opposite to that of the source region. This highly-closed region may have an impurity concentration gradient which is greater toward its portion facing the abovesaid surface of the substrate. These arrangements serve to prevent extinction of memory due to current leakage during absence of bias voltage which otherwise would develop in semiconductor devices having short-channel and thin gate oxide layer, and due to irradiation of alpha-particle onto the device.