Abstract: Benzodiazepine derivatives of the formula: 1

Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substituted amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.

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: This invention relates to an antimycotic composition comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and an allylamine-series antimycotic agent as active ingredients, which composition has a potent antimycotic action as compared with its component drugs used each independently and is not only of great use in the treatment of dermatophytosis such as tinea, tinea imbricata, tinea favosa, tinea profunda, etc. and fungal infections such as candidiasis of cutaneous mucosa, candidiasis profunda, etc. but also useful from the standpoint of alleviation of side effects and improvement in the patient's compliance.

Abstract: A compound of the formula: wherein R1 is amino or protected amino; R2 is hydrogen, lower alkyl or hydroxy protective group; R3 is carboxy or protected carboxy; R4 is an unsubstituted 5, 6 or 7-membered heteromonocyclic group containing two nitrogen atoms as heteroatoms, and which optionally further contains one oxygen or sulfur atom; or R4 is said 5, 6 or 7-membered heteromonocyclic group substituted by 1 to 4 groups selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyclo(lower)alkyl, cyclo(lower)alkenyl, halogen, amino, protected amino, protected hydroxy, cyano, nitro, carboxy, hydroxy(lower)alkyl, amino(lower)alkyl, and carbamoyloxy; and n is 1 or 2.

Abstract: A compound of the formula (I): 1

Abstract: A compound of the following formula (II) and a process for preparing of the compound of the following formula (I) its preparation wherein R1 is carboxy or protected carboxy; R2 is lower alkoxy or higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane, or a salt thereof. The process comprises, reacting a compound of the formula (III): wherein R1, R2, A1 and A2 are each as defined above or a salt thereof, with an acid ammonium salt to give a compound of the formula (II).

Abstract: 1

Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R 1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R 2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R 3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino, R 4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group, R 5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R 10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: 1

Abstract: Providing an oral formulation of a macrolide compound where the dissolution of the macrolide compound is under sustained release; and a sustained-release formulation containing a composition in solid solution, where the macrolide compound is present at an amorphous state in a solid base.

Abstract: The present invention provides a cyclic lipopeptide acylase which may effectively deacylate the acyl side chain of a cyclic lipopeptide compound, specifically FR901379 Substance or its analog thereof shown by the following general formula [I], and a process for production of a cyclic peptide compound which comprises the use of said acylase.

Abstract: Oxazole compounds of formula (I), wherein R1 is aryl which may be substituted with halogen(s), R2 is aryl which may be substituted with halogen(s), X is single bond, (a) or SO2, R3 and R4 are independently hydrogen or suitable substituent, (wherein X is (a), neither R3 nor R4 is hydrogen), R3 and R4 may be linked together to form (b), (b) is N-containing heterocyclic group which may be substituted with one or more suitable substituent(s), R5 is hydrogen, etc., A1 is lower alkylene or single bond, (c) is cyclo(C3-C9)alkane or cyclo(C5-C9)alkene, or a pro-drug thereof, or a pharmaceutically acceptable salt thereof, which are useful as medicament.

Abstract: Heterobicyclic derivatives of the formula: 1

Abstract: Heterobicyclic derivatives of the formula: wherein R1 is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected carboxy(lower)alkyl, acyl(lower)alkyl, heterocyclic group or heterocyclic(lower)alkyl which may have suitable substituent(s), R2 is aryl which may have suitable substituent(s) or heterocyclic group, and R3 is hydrogen, lower alkoxy or arylthio, and a pharmaceutically acceptable salt thereof which are useful as a medicament.

Abstract: The invention provides a composition for improving an action of an immunosuppressant, comprising insulin-like growth factor I or its analog as an active ingredient.

Abstract: Administration of a decoy, i.e. a compound which specifically antagonizes the nucleic acid domain to which NF-&kgr;B is bound, is effective in the treatment and prevention of diseases caused by the transcriptional regulatory factor NF-&kgr;B, such as ischemic diseases, inflammatory diseases, autoimmune diseases, cancer metastasis and invasion, and cachexia.

Abstract: A sulfonamide compound of the formula (I):

Abstract: This invention provides &bgr;-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a &bgr;-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and/or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

Abstract: A process for producing a compound of the general formula (I): (wherein R1 represents hydrogen, a lower alkanoyl group or a lower alkyl group; R2 and R3 each represents hydrogen or a lower alkanoyl group) characterized in that a compound of the general formula (II): (wherein R1, R2 and R3 are respectively as defined above) is reacted with a culture of a strain of microorganism belonging to the genus Fusarium or its cells harvested by filtering the broth.