Abstract: [Problems] To provide an antibacterial agent, particularly a novel polypeptide compound having an antifungal action. [Means for Solution] As a result of an extensive study on a novel antifungal agent, the inventors have found that an excellent anti-deep-fungal activity is exhibited by introducing a cyclohexylmethylamino group or a piperidylmethylamino group as a partial structure of a natural polypeptide compound, and completed the present invention. The compound of the present invention has an excellent antibacterial activity and is therefore useful as an agent for preventing or treating various fungal infections.

Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

Abstract: A compound of the formula (I): 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: Novel anthranilic acid derivatives having an inhibiting activity of cGMP-PDE are represented by the formula I where A is a lower alkylene group: 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: 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: Compounds of formula (I) where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R4 is a group CR6R7R8 wherein R6 and R7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R8 is hydrogen; its prodrug and a salt thereof.

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 substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued 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 a quinoline compound of the formula: ##STR1## wherein R.sup.1 is a pyridyl group or aryl, each of which may be substituted with suitable substituent(s),A is --COHN-- or --NHCO--,n is an integer of 0 or 1, and ##STR2## is a group of the formula: ##STR3## In which R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined,and pharmaceutically acceptable salt thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prevention and/or the treatment of bone diseases caused by abnormal bone metabolism in human being or animals.

Abstract: A compound of the formula: ##STR1## in which R.sup.4 is acyl,R.sup.5 is lower alkyl,R.sup.6 is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic-(lower)alkyl,R.sup.7 is lower alkyl or lower alkylthio(lower)alkyl,R.sup.8 is carboxy or protected carboxy,A is lower alkylene,Z is a group of the formula: ##STR2## wherein R.sup.1 is hydrogen, lower alkyl, common amino-protective group or optionally substituted ar(lower)alkyl,R.sup.2 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic-(lower)alkyl, optionally substituted cyclo(lower)alkyl(lower)alkyl, common amino-protective group, amino(or protected amino)(lower)alkyl, optionally substituted heterocyclic-carbonyl or cyclo(lower)alkyl, andR.sup.3 is optionally substituted heterocyclic(lower)alkyl, andm is an integer of 0 to 2,or pharmaceutically acceptable salts thereof, useful as endothelin antagonist.

Abstract: This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.

Abstract: Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,R.sup.2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.6 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension.

Abstract: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.

Abstract: Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,R.sup.2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.6 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is carboxy or pharmaceutically acceptable salts and esters thereof;R.sup.2 is hydrogen, lower alkyl or halogen;R.sup.3 is phenyl, naphthyl, phenyl or naphthyl each substituted by from one to three C.sub.1-6 alkyl groups, mono-, di- or triphenyl (C.sub.1-6)alkyl; or substituted mono-, di- or triphenyl (C.sub.1-6) alkyl;A is lower alkylene which may be substituted by oxo or lower alkenylene,Q is carbonyl or lower alkylene,X is ##STR2## in which R.sup.4 is hydrogen or C.sub.1-6 alkyl, andR.sup.5 is hydrogen, C.sub.1-6 alkyl or Y--Z--R.sup.3,Y is a bond or lower alkylene,Z is lower alkylene ##STR3## in which R.sup.6 is hydrogen, (C.sub.1 -C.sub.6) alkyl, mono-, di- or triphenyl(C.sub.1-10) alkyl, C.sub.1-6 alkyl or lower alkoxycarbonyl substituted mono-, di- or triphenyl(C.sub.1-6)alkyl or pharmaceutically acceptable carboxylic acid acyl, and pharmaceutically acceptable salts thereof. The compound is useful as a testosterone 5.alpha.-reductase inhibitor.