Abstract: This invention relates to novel thiazolylbenzofuran derivatives of formula (I) wherein R.sup.1 is lower alkyl, L is single bond or lower alkylene optionally substituted with aryl, oxo or hydroxy, and Q is a heterocyclic group optionally substituted with one or more suitable substituent(s); or lower alkoxy substituted with aryl which is substituted with one or more suitable substituent(s) and at least one of which is lower alkoxy optionally substituted with cyano, protected carboxy, carboxy, lower alkylene, a heterocyclic group optionally substituted with oxo, or amidino optionally substituted with hydroxy or lower alkoxy, or its salt, which possess activities as leukotriene and SRS-A antagonists or inhibitors.

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 Tachykinin-mediated diseases in human beings or animals.

Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.

Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.

Abstract: A method of making a peptide compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is lower alkyl or halogen,R.sup.3 is hydrogen, lower alkyl or halogen,R.sup.4 is lower alkyl,R.sup.5 is ar(lower)alkyl,R.sup.6 is amino or optionally protected hydroxy, andX is O, S or N--R.sup.7, in which R.sup.7 is N,N-di(lower)alkylamino(lower)alkyl,which is useful as tachykinin antagonist.

Abstract: Disclosed herein are compounds of the following formula: ##STR1## wherein R.sup.1 is a group of the formula ##STR2## "X" is CH.sub.2 or N, "Z" is O, S, or N--R.sup.6, "A" is an amino acid residue, and Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are substituent variables as defined herein.The compounds are antagonists of tachykinin, and as such are useful for alleviation of pain and for treatment of disorders including asthma, bronchitis, rhinitis, conjunctivitis, dermatitis, arthritis, and urticaria.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is aryl, or a group of the formula: ##STR2## wherein X is CH or N, and Z is O or N--R.sup.5,in which R.sup.5 is hydrogen or lower alkyl,R.sup.2 is hydroxy or lower alkoxy,R.sup.3 is hydrogen or lower alkyl which may have suitable substituent(s),R.sup.4 is ar(lower)alkyl which may have suitable substituent(s),A is carbonyl or sulfonyl, andY is a bond or lower alkenylene,and pharmaceutically acceptable salt thereof. The disclosed compounds are useful for treating respiratory diseases such as bronchaedema.

Abstract: A substance P antagonistic peptide of the following formula is disclosed: ##STR1##

Abstract: A tachykinin-antagonistic compound of the following general formula:R.sup.1 --A.sup.1 --D--Trp(R.sup.2)--A.sup.2 --R.sup.3[whereinR.sup.1 is hydrogen or amino-protective groupR.sup.2 is amino-protective groupR.sup.3 is ar(lower)alkoxy or N-(lower)alkyl or N-ar(lower)alkylaminoA.sup.1 is single bond or one amino acid residueA.sup.2 is one amino acid residue other than Phe.]or the salt thereof.

Abstract: The present invention relates to DTrp-Phe containing tripeptides and pharmaceuticals, which possess tachykinin antagonism activity as well as processes of making such peptides.

Abstract: Peptide compounds having Substance P antagonism of the formula: ##STR1## wherein R.sup.1 is lower alkyl, aryl, arylamino, pyridyl, pyrrolyl, pyrazolopyridyl, quinolyl, or a group of the formula: ##STR2## wherein the symbol of a line and dotted line is a single bond or a double bond; X is CH or N; Z is O, S or NH; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen or hydroxy; R.sup.4 is lower alkyl which may have suitable substituent(s); R.sup.5 is ar(lower)alkyl which may have suitable substituent(s) or pyridyl(lower)alkyl, or R.sup.4 and R.sup.5 are linked together to form benzene-condensed lower alkylene; A is an amino acid residue excepting D-Trp, which may have suitable substituent(s); and Y is bond, lower alkylene or lower alkenylene;and their pharmaceutically acceptable salts are disclosed.

Abstract: Peptides of the following formulae:H-THR-LYS-GLU-LYS-LEU-LYS-SER-GLU-LEU-VAL-ALA-ASN-OH, H-GLU-LEU-LYS-SER-GLU-LEU-VAL-ALA-ASN-OH, H-LYS-LEU-LYS-SER-GLU-OH,are effective in the treatment of bacteria viral infection.

Abstract: This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as intermediates for the synthesis of other azetidinone compounds having antimicrobial activity.

Abstract: This invention relates to cephalosporin analogues and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

Abstract: The invention deals with Cephalosporin Analogues of the formula: ##STR1## wherein R.sup.1 is amino or amino substituted with a pharmaceutically acceptable carboxylic acyl protective group for the amino substituents in cephalosporin compounds or with benzyl, phenethyl or trityl, andR.sup.2 is carboxy or a pharmaceutically acceptable ester of said carboxy group employed in cephalosporin compounds, and pharmaceutically acceptable salts thereof, and their use as antimicrobial agents.

Abstract: Compounds of the formula ##STR1## wherein X is --O--or --S--;R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group; and the heavy solid line means single or double bond; the compounds are useful in the treatment of infectious diseases particularly fungal infection, in human beings and animals.

Abstract: Cephalosporin analogues represented by the formula ##STR1## wherein R.sup.1 is amino or a substituted amino,R.sup.2 is carboxy or a protected carboxy, andR.sup.3 is hydrogen or lower alkoxy, processes for making the same, azetidinone intermediates and pharmaceutical compositions comprising said cephalosporin analogues as active ingredients.

Abstract: Novel carbonic acid esters are disclosed which are useful in a process for introducing esterified carboxy-type protective groups on amino and/or imino groups in amino and/or imino group - containing compounds for the temporary protection of said amino and/or imino groups. Additionally, processes for preparing said esters are also disclosed.

Abstract: Carbonic acid esters of the formula substituent(s) substituents(s)R'.sub.1 OCOOR'.sub.2wherein R'.sub.1 is lower alkyl which may have substituent)s) selected from the group of halogen, lower alkoxy and aryloxy, or ar(lower)-alkyl which may have substituents)s) selected from the group of lower alkoxy, halogen, nitro and cyano, andR'.sub.2 is benzotriazolyl which may have halogen; or a group represented by the formula: ##STR1## wherein Y' and Z' are each cyano, nitro, carbamoyl, esterified carboxy, lower alkanoyl, aroyl or disubstituted carbamoyl; provided that whenR'.sub.2 is a group represented by the formula: ##STR2## wherein Y' and Z' are each cyano, nitro, carbamoyl or esterified carboxy, R'.sub.1 is ar(lower) alkyl having substituent(s) selected from the group of lower alkoxy, halogen, nitro and cyano.A process for the protection of amino and/or imino groups in compounds containing them by reacting them with the aforementioned esters is also disclosed.

Abstract: Novel carbonic acid esters are disclosed which are useful in a process for introducing esterified carboxy-type protective groups on amino and/or imino groups in amino and/or imino group-containing compounds for the temporary protection of said amino and/or imino groups. Additionally, processes for preparing said esters are also disclosed. .Iadd.