Abstract: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.

Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.

Abstract: The present invention relates to a hydrazine derivative represented by the formula (I): ##STR1## (wherein each of Ar.sup.1 and Ar.sup.2 is a substituted or unsubstituted phenyl group, a substituted or unsubstituted heteroaryl group, or the like, R.sup.1 is an alkyl group or the like, and A is a divalent radical having --C.dbd.N--N-- or --CH--NH--N-- as a fundamental skeleton), which is a useful compound as an agricultural and horticultural insecticide.

Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.

Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.

Abstract: A novel benzhydrazone derivative has a general formula [I]: ##STR1## (wherein R.sup.1 is a lower alkyl group, R.sup.2 and R.sup.3 are same or different halogen atoms and Z is a chlorine atom or an amino group) and is useful as an intermediate for the production of a triazole derivative having the following general formula [II]: ##STR2## (wherein R.sup.1, R.sup.2 and R.sup.3 are the same as mentioned above and X is a chlorine atom located at 2- or 6-position).

Abstract: Compounds having the structural formula ##STR1## where X, Y, R and Z are defined in the specification are disclosed. The compounds of this invention are effective for controlling mites, nematodes, rice planthopper, tobacco budworm, and southern corn rootworm. Methods for making these compounds are also set forth.

Abstract: There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular disorders with the compounds. The active components of the pharmaceutical compositions are compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain alkyl and olefinic groups, which may be unsubstituted or substituted; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic group; and R.sub.3 is a pharmaceutically acceptable organic group selected from alkyl and olefinic groups which may be unsubstituted or substituted, acyl, a sulfonyl, sulfinyl, sulfenyl, carbonate, or carbamate derivative; or R.sub.3 is a group of the formula--(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2, wherein n is 2-8, and R.sub.1 and R.sub.2 are as described above. Novel compounds are disclosed wherein at least one of R.sub.1, R.sub.2 and R.sub.

Abstract: Amidinophenylalanine derivatives, a process for their preparation, their use and pharmaceutical compositions which contain these compounds are described.

Abstract: Novel antineoplastic 1-alkyl-2-acyl-1,2-disulfonylhydrazine having the following formula and methods of therapy using those antineoplastic compounds: ##STR1## where R.sub.1 and R.sub.2 are (independently) alkyl, cycloalkyl, aryl, aralkyl or heteroaryl. X is an acyl group, and Z is an alkyl or a haloalkyl group.

Abstract: Disclosed herein are N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives of the formula (I): ##STR1## wherein R.sup.1 and CF.sub.3, COOH or CCl=CClCOOH, R.sup.2 is H, Cl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.4 alkoxycarbonyl; Z is CH or N; X.sup.1 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxyl or Cl; and X.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxyl, a process for the preparation thereof, and herbicidal compositions containing the N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives as active ingredients.

Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-disubstitutedhydrazines, methods of using such compositions and N'-substituted-N, N'-disubstitutedhydrazines. Specifically, the invention relates to insect growth regulating compositions, and methods of using such compositions, which include compounds having a nucleus of the formula ##STR1## where A', B', D and J are independently any atom or group of atoms; where E is a tertiary carbon containing organic radical, a haloalkyl having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen, and is attached to the nitrogen shown in the formula by a carbon-to-nitrogen single bond; where one G.sub.1 is C, N, O and S, and both G.sub.2 's and the other G.sub.1 are carbon; or one G.sub.2 is S or P, and both G.sub.1 's and the other G.sub.

Abstract: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl. Such methylating agents are useful as antitrypanosomal and anticancer agents.

Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.

Abstract: Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, NH.sub.2 CH.sub.2 --, --CH(Me)NH.sub.2, --CH(NH.sub.2)CHMe.sub.2, --CH(NH.sub.2)CH.sub.2 CHMe.sub.2, --CH(NH.sub.2)CH(Me)CH.sub.2 Me, 2-pyrrolidinyl residues wherein the R.sup.1 CO-- constitutes an .alpha.-aminoacyl group, N-acetylaminoacyl derivatives and the corresponding dipeptidyl radicals wherein R.sup.1 CO-- is a dipeptidyl residue containing two amino acid residues of the formula where R.sup.1 is --CHR.sup.7 NHCOCHR.sup.8 NH.sub.2, R.sup.6 NHCHR.sup.5 --, ##STR2## and R.sup.6 NHCH.sub.2 CHR.sup.5 --; R.sup.2 is selected from the group consisting of H, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, and cycloalkyl;R.sup.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.

Abstract: There are disclosed compounds of the formulaR.sup.1 -XwhereinR.sup.1 is alkyl of 8-22 carbon atoms;X is ##STR1## R.sup.2 is --(CH.sub.2).sub.n NR.sup.4 R.sup.5 ; R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or lower alkyl;R.sup.5 is hydrogen or lower alkyl; andn is 0-7, with the proviso that when X is ##STR2## n is 6-7; and their use in the prevention and/or treatment of conditions such as allergic rhinitis, allergic bronchial asthma and other naso-bronchial obstructive air-passageway conditions, other immediate hypersensitivity reactions such as allergic conjunctivitis and various inflammatory conditions.

Abstract: Compounds of the formula ##STR1## where R is methyl or 2-chloroethyl, and R.sup.1 and R.sup.2 are each an aromatic hydrocarbon, ring substituted aromatic hydrocarbon moiety, or an alkyl moiety. The compounds have been found to be alkylating agents having antineoplastic activity.

Abstract: Propionic acid amides of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are as defined hereinafter, processes for their preparation, herbicidal compositions containing these amides and methods of use of the herbicidal compositions are disclosed.

Abstract: The use of arylsulphonyl hydrazones corresponding to the following general formula:Ar (SO.sub.2 --NH--N.dbd.R).sub.x (I)whereinAr represents a benzene, naphthalene, diphenyl, diphenyl ether, diphenyl sulphone or diphenylene oxide radical which may be substituted by methyl and/or chlorine;R represents the radical of an aldehyde or ketone without the carbonyl oxygen atom; andx represents 1 or 2;as blowing agents for the production of cellular or porous plastics articles.

Abstract: Color-forming para-sulfonamidodiphenylamines and their corresponding sulfonimide dyes are useful in imaging materials. The color-forming sulfonamidodiphenylamines are prepared by condensation reactions. The corresponding sulfonimide dyes are formed by oxidation of the color-forming sulfonamidodiphenylamines by means of a suitable oxidizing agent, such as the oxidized form of a cross-oxidizing silver halide developing agent.

Abstract: Sulphonanilides of formula ##STR1## and salts thereof, wherein R.sup.1 represents alkyl or certain other groups;R represents alkylene or alkenylene;A represents --COR.sup.12 or a carbonyl derivative or addition compound thereof, where R.sup.12 represents hydrogen, alkyl or certain other groups; andR.sup.2 -R.sup.6 represent hydrogen, alkyl, halogen or certain other groups;are pesticides and plant growth regulants, especially herbicides and fungicides.

Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.

Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.

Abstract: A di- or tri-sulphonic acid hydrazide of an alkylated diphenyl ether, said hydrazide being of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and represent halogen or a lower alkyl radical and R.sub.1 and R.sub.2 can denote hydrogen,R.sub.3 denotes a lower alkyl radical andn represents the number 1 or 2.A process for the preparation of such hydrazides and the use of such hydrazides as chemical blowing agents in the production of foams from foamable compositions, especially rubbers and thermoplastic resins.

Abstract: Sulphonanilides of formula ##STR1## and salts thereof, wherein R.sup.1 represents alkyl or certain other groups;R represents alkylene or alkenylene;A represents --COOH, --COO alkyl, --CSSH, CN or certain related groups; orR-A represents a group of formula ##STR2## where R.sup.14 represents hydrogen, alkyl or aryl, B represents oxygen or ##STR3## R.sup.15 represents hydrogen or alkyl, and n represents 0, 1 or 2; and R.sup.2 -R.sup.6 represent hydrogen; alkyl, halogen or certain other groups,are pesticides and plant growth regulants, especially herbicides and fungicides.

Abstract: New process for the preparation of acetylenic macrocyclic ketones, which compounds represent useful intermediates for the synthesis of valuable perfuming ingredients, viz. muscone and EXALTONE.RTM. (cyclopentadecanone).

Abstract: There is provided a process for preparing amides which comprises reacting an amine, or an amide, and an acid halide, or anhydride, in suitable molecular proportions, in an inert organic diluent, in the presence of an effective amount of a molecular sieve, until the reaction is completed, separating the molecular sieve, and recovering the amide from the organic mother liquor.