Abstract: Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I) wherein R1 is aryloxy, or aryl which is optionally substituted with suitable substituent(s); R2 is lower alkyl; R3 is hydroxy or protected hydroxy; and -A- is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.

Abstract: There is described antifungal combination use of known antifungal agents such as the azoles or polyenes in combination with a lipopeptide compound antifungal agent. More particularly, the invention relates to antifungal combination use of azoles such as fluconazole, voriconazole, itraconazole, ketoconazole, miconazole, ER 30346 and SCH 56592; polyenes such as amphotericin B, nystatin, liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or nikkomycin X; other chitin inhibitors; elongation factor inhibitors such as sordarin and analogs thereof; mannan inhibitors such as predamycin, bactericidal/permeability-inducing (BPI) protein products such as XMP.97 or XMP.127; or complex carbohydrate antifungal agents such as CAN-296; with a lipopeptide compound [I] as described herein.

Abstract: This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.

Abstract: Without requiring ejection of air or the like, the amount and area of irradiation of excited species to a workpiece surface can be increased, the whole surface can be uniformly irradiated, and the loss of effective excited species can be suppressed, whereby the treatment performance and the treatment efficiency can be remarkably improved.

Abstract: A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

Abstract: The present invention relates to a therapeutic agent for soft tissue sarcoma (particularly synovial sarcoma), which contains a histone deacetylase inhibitor (particularly compound A) as an active ingredient.

Abstract: A brain-protective agent containing an NF-?B decoy. In brain diseases, the brain can be particularly effectively protected against brain disorders (for example, cerebral vasospasm following a subrachnoidal hemorrhage and apoptosis of the nerve cells following a cerebrovasucular accident or serious head injury) caused by the undesired activation of cytokines or cell adhesion factors which are regulated by NF-?B by administering the brain-protective agent containing an NF-?B decoy, i.e., acompound antadonistic specifically to a nucleic acid to which NF-?B binds.

Abstract: The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.

Abstract: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R is -A-R6 wherein A is bond, —NHCO—(CH2CO)n—, lower alkylene, —NH—CO—CO— or the like, and R6 is wherein R7, R8, R9 and R10 are independently amino, guanidino, amidino or the like; R4 is carboxy or protected carboxy; and R5 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

Abstract: This invention relates to new polypeptide compound represented by the general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on ?-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystic carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.

Abstract: Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprises a solid base which is a water-soluble or water-insoluble polymer. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. The formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune disease. In addition, a solid dispersion composition is provided. The solid dispersion comprises tacrolimus or its hydrate in a mixture containing water-soluble or water-insoluble polymer and an excipient.

Abstract: This invention relates to new polypeptide compound represented by general formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on ?-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.

Abstract: A method for separating a lactone-containing high-molecular weight compound comprising subjecting a mixture of a lactone-containing high-molecular weight compound having, as its side-chain, at least one of a lower alkenyl group and a lower alkoxy group and its analogous compound(s) to either one or both steps in any order of a step (A) for adsorbing the mixture to a nonionic adsorption resin and eluting with an aqueous solvent containing silver ions, and a step (B) for adsorbing the mixture to a basic active alumina and eluting with an organic solvent to separate each of the compounds.

Abstract: This invention provides a novel industrial process for preparation of an anhydride of 2-(2-aminothiazole-4-yl)-2-hydroxy compound.

Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-? mediated diseases.

Abstract: There is described antifungal combination use of known antifungal agents such as the azoles or polyenes in combination with a lipopeptide compound antifungal agent. More particularly, the invention relates to antifungal combination use of azols such as fluconazole voriconazole, itraconazole, ketoconazole, miconazole, ER 30346 and SCH 56592; polyenes such as amphotericin B, nystatin, liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or nikkomycin X; other chitin inhibitors; elongation factor inhibitors such as sordarin and analogs thereof; mannan inhibitors such as predamycin, bactericidal/permeability-inducing (BPI) protein products such as XMP.97 or XMP.127; or complex carbohydrate antifungal agents such as CAN-296; with a lipopeptide compound (I) as described herein.

Abstract: The present invention relates to an antitumor agent containing a histone deacetylase inhibitor and a topoisomerase II inhibitor in combination, and an enhancer of antitumor effect of topoisomerase II inhibitor, which contains a histone deacetylase inhibitor as an active ingredient. The present invention provides an antitumor agent having superior antitumor activity, which is associated with a fewer side effects.

Abstract: The present invention provides novel benzimidazole derivatives of the following formula (I) and salts thereof: wherein R1 represents a lower alkyl group or a lower alkyloxy-lower alkyl group; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an aryl group, and such; R3 represents a lower alkyl group, a lower alkenyl group, an aryl group, a lower alkylaryl group, an aryl-lower alkenyl group, a halothienyl group, a lower alkylamino group, or an aryl-lower alkylamino group; A represents a benzene ring, a naphthalene ring, or a pyridine ring; and X represents a halogen atom. The derivatives and their salts have blood sugar level-depressing activity or PDE5-inhibiting activity, and are useful as pharmaceutical preparations.

Abstract: The compounds of formula I, have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.

Abstract: A compound of the formula (I): wherein X1 is bond or —OCH2—; X2 is —(CH2)n—, in which n is 1, 2 or 3; X3 is bond, —O—, —S—, —OCH2—, or —NH—; R1 is phenyl or pyridyl each of which may have one or two substituent(s) selected from the group consisting of hydroxy, halogen, etc.; R2 is hydrogen, (lower)alkoxycarbonyl, etc.; R3 is hydroxy(lower)alkyl; halo(lower)alkyl, etc.; R4 is aryl or unsaturated heterocyclic group, each of which may have one or two substituent(s) selected from the group consisting of lower alkyl, hydroxy, carbamoyl, halogen, lower alkoxy, etc.; and a salt thereof which is useful as a medicament.