Abstract: A method for preparing N.sup.2 -(3-(a hydrogen atom or a lower alkyl)-8-quinolinesulfonyl)-N.sup.G -nitro-L-arginine which comprises the step of condensing N.sup.G -nitro-L-arginine and 3-(a hydrogen atom or a lower alkyl)-8-quinolinesulfonyl chloride. The method achieves an extremely efficient and high yield preparation of N.sup.2 -arylsulfonyl-L-arginineamides that are useful as active ingredients of medicaments. Also provided is a novel N.sup.2 -(3-(a hydrogen atom or a lower alkyl)-8-quinolinesulfonyl)-N.sup.G -nitro-L-arginine compound which can be used as synthetic intermediate for the manufacture of (2R,4R)-4-methyl-1-?N.sup.2 -(3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl!-2-piperidine -carboxylic acid.

Abstract: Disclosed herein is a fibrinolysis-enhancing agent comprising, as an effective ingredient, an N.sup.2 -arylsulfonyl-L-arginine amide represented by the general formula (I): ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## where R.sup.3 is an alkyl group having 3 to 5 carbon atoms or an alkoxyalkyl group having 2 to 4 carbon atoms and R.sup.4 is an alkyl group having 1 to 3 carbon atoms; and R.sup.2 is a group of the formula: ##STR3## where R.sup.5 and R.sup.6 are independently hydrogen atom, methyl group or methoxy group provided that they cannot be hydrogen atoms simultaneously, and R.sup.7 is an alkyl group having 1 to 3 carbon atoms; or a salt thereof. The agent is used in combination with a plasminogen activator.

Abstract: A method of suppressing vasoconstriction in a warm-blooded animal which comprises administering to said warm-blooded animal an effective amount of a serotonin antagonist compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen, halo, C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.6 dialkyl amino;R.sup.2 is hydrogen, halo or C.sub.1 -C.sub.5 alkoxy;R.sup.3 is hydrogen, hydroxy, --O--(CH.sub.2).sub.n --COOH or --O--CO--(CH.sub.2).sub.l --COOH, wherein n is an integer of 1-5, and l is an integer of 1-3;R.sup.4 is ##STR2## wherein R.sup.5 and R.sup.6 are each independently hydrogen or C.sub.1 -C.sub.8 alkyl, and A is C.sub.3 -C.sub.5 alkylene or C.sub.3 -C.sub.5 alkylene substituted with carboxy; andm is an integer of 0-5,or a pharmaceutically acceptable salt thereof. The use of the compound (I) for the preparation of a pharmaceutical formulation useful as a serotonin antagonist is also provided.

Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.

Abstract: Novel arginine derivatives represented by the general formula ##STR1## wherein R.sup.1 stands for a naphthalenesulfonyl, a naphthalenecarbonyl, a 1,2,3,4-tetrahydronaphthalenesulfonyl, a 1,2,3,4-tetrahydronaphthalenecarbonyl, a dioxa b-6,7-naphthalenesulfonyl, a dioxa b-6,7-naphthalenecarbonyl, a 1,2,3,4-tetrahydro-8-quinolinesulfonyl, a 1,2,3,4-tetrahydro-8-quinolinecarbonyl, a dibenzofuransulfonyl, a dibenzofurancarbonyl, a fluorenesulfonyl, a fluorenecarbonyl, a dibenzothiophenesulfonyl or a dibenzothiophene, and R.sup.2 stands for a piperidino or a piperazino are disclosed. These arginine derivatives and their pharmaceutically acceptable salts have trypsin-inhibiting activity and useful as a pancreatitis remedy.

Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.

Abstract: A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention.

Abstract: This invention relates novel thieno[2,3-d]pyrimidine derivatives represented by the following general formula (I): ##STR1## or salts thereof; wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen or alkyl group having 1 to 6 carbon atoms; or R.sup.1 and R.sup.2 may concatenate to form a cycloalkylene group having 5 or 6 ring carbon atoms; R.sup.3 and R.sup.4 independently represent hydrogen or alkyl group having 1 to 6 carbon atoms; R.sup.5 represents a member selected from(1) hydrogen or alkyl having 1 to 6 carbon atoms,(2) ##STR2## in which m is an integer of from 1 to 3 and X represents halogen, or (3) ##STR3## in which R.sup.6 represents alkyl group having 1 to 6 carbon atoms; Ar represents substituted or unsubstituted phenyl, or 2- or 3-thienyl group; and n is 2 or 3. The derivatives of the invention can be used in the treatment of the various depression disease or the higher dysfunction of the brain.

Abstract: Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.

Abstract: Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.

Abstract: N.sup.2 -dansyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the group consisting of (1) alkoxy, alkenyloxy, alkynyloxy, and cycloalkoxy, respectively, containing not more than 10 carbon atoms, aralkyl of not more than 15 carbon atoms, tetrahydrofurfuryloxy, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms, halogen or nitro; (2) ##STR2## wherein R.sub.1 and R.sub.

Abstract: A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention.

Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

Abstract: 2-Substituted-1-(omega-aminoalkoxy)benzenes are prepared and found useful as pharmaceutical agents, particularly as antidepressants.

Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

Abstract: Piperazinylalkoxyindanes and their pharmaceutically acceptable acid addition salts which have anti-anxiety activity and are effective as sedatives.

Abstract: 2-(4-aminobutoxy)stilbenes are prepared and found useful as pharmaceutical agents, particularly as anticonvulsants and skeletal muscle relaxants.

Abstract: 2-(4-aminobutoxy)stilbenes are prepared and found useful as pharmaceutical agents, particularly as anticonvulsants and skeletal muscle relaxants.

Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.

Abstract: N.sup.2 -dansyl-L-arginine esters and amides or the acid addition salts thereof with a pharmaceutically acceptable acid have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.