Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.

Abstract: The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N;Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene;Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.

Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

Abstract: These compounds correspond to the following general formula: ##STR1## where: n is 0, 1, or 2,m is are 1, 2, or 3,R, R.sub.1, R.sub.2, and R.sub.3, whether identical or different, represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,R.sub.1 and R.sub.2, or R.sub.2 and R.sub.3 taken together can form a 5- or 6-group cycle,X and Y, whether identical or different, represent a nitrogenous aromatic heterocycle in position 2,Z.sub.1, Z.sub.2, and Z.sub.3, whether identical or different, represent an atom of hydrogen, a linear or branched alkyl radical at C.sub.1 -C.sub.4, the radical --OR.sub.4 or --NR.sub.4 R'.sub.4,R.sub.4 and R'.sub.4 represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,and the metallic salts and complexes thereof.Use in pharmaceutical and cosmetic compositions to protect the organism from oxidizing stress situations linked to certain pathological states.

Abstract: A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents;W represents optionally substituted thiazolyl or quinoxalinyl;X is hydrogen, hydroxy or lower alkyl; andT is hydrogen, halogen, hydroxy, nitro, amino or alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.

Abstract: This invention relates to novel heterocycle compounds including but not limited to 3-?3-?3-(imidazolin-2-yl amino)propyloxy!isoxazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-pro pionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of the formula ##STR1## where R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are H or lower alkyl of 1 to 10 carbons; R.sub.5 is lower alkyl of 1 to 10 carbons, fluoro, chloro, bromo, iodo, nitro, or fluoroalkyl having 1 to 10 carbons; m is an integer having the value of 1-4; n is an integer having the value of 0-4; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl, said Y group being optionally substituted with one or more R.sub.5 group; A is (CH.sub.2).sub.p where p is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.

Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention relates to substituted thiazole derivatives of the following general formula, the substituent groups of which are as defined in the specification herein: ##STR1## These compounds are useful as inhibitors of platelet aggregation and inhibitors of adhesion molecules and may be provided in pharmaceutical compositions and in methods of treating reperfusion thrombosis injury in patients. Also included are novel intermediates for preparing the compounds of the invention.

Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.

Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Abstract: A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.

Abstract: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.

Abstract: The invention concerns compounds of the formula I: ##STR1## in which R.sub.1 to R.sub.5 are as defined in claim 1. These compounds find their application in the treatment of pathologies involving CRF.

Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.

Abstract: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.

Abstract: There is disclosed an iminothiazoline derivative of the general formula: ##STR1## wherein R.sub.1 is (halo)alkyl, (halo)alkenyl, (halo)alkynyl or the like; R.sub.2 is (halo)alkyl, optionally substituted aryl, formyl, cyano or the like; R.sub.3 is hydrogen, (halo)alkyl or the like; and Q is a group of the particular general formula. Also disclosed are a herbicide containing a herbicidally effective amount of the iminothiazoline derivative and a method for controlling unfavorable weeds, which includes applying a herbicidally effective amount of the iminothiazoline derivative to an area where the unfavorable weeds grow or will grow.

Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.

Abstract: A novel imidazole derivatives of formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, or optionally substituted aryl; R.sup.2 is alkyl, optionally substituted aryl optionally substituted aralkyl, or optionally substituted hetero ring group; R.sup.3 is hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted hydroxyalkyl; R.sup.4 is hydrogen, alkyl, halogen, acyl, optionally substituted hydroxyalkyl, optionally esterified or amidated carboxyl group, hydroxy group, aryl or arylthio; X is S, SO, SO.sub.2, CH.sub.2, or Se; n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, said derivative having anti-HIV activity and being useful for the treatment of HIV infections.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is a specified linking group; and A, B and E, which may be the same or different, are H, hydroxy, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; except that when Z is unsubstituted phenyl and X and K are oxygen, A, B and E are not all hydrogen.

Abstract: The invention relates to the derivatives of formula I: ##STR1## in which R.sub.1 represents a phenyl or naphthyl radical (optionally substituted), R.sub.2 represents a hydrogen or halogen atom or an alkyl, hydroxymethyl or formyl radical, R.sub.3 represents an alkyl, cycloalkyl, alkenyl, cycloalkylalkyl or phenyl radical, R.sub.4 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl radical, R.sub.5 represents an alkyl, cycloalkyl, cycloalkylalkyl or alkenyl radical or a radical of formula B: ##STR2## (p=0, 1, 2 or 3), R.sub.6 represents a phenyl, pyridyl, imidazolyl, pyrrolyl, thienyl or furyl radical, optionally substituted, or a cycloalkyl radical,m and n, which may be identical or different, each represent 0 or 1,their possible stereoisomers and their addition salts.

Abstract: There is disclosed a process of producing a 2-iminothiazoline derivative of the general formula [II], characterized in that a thiourea derivative of the general formula [I] is treated with an acid. Also disclosed are a process of producing an N-substituted N-arylcyanamide derivative of the general formula [VI], characterized in that an N-arylcyanamide derivative of the general formula [IV] is reacted with an allyl halide derivative of the general formula [V] in an aprotic polar solvent in the presence of an iodide and an alkali metal carbonate; and a process of producing an N-substituted N-arylthiourea derivative of the general formula [VII], characterized in that an N-substituted N-arylcyanamide derivative of the general formula [VI] obtained as described above is further reacted with a chemical species which generates sulfide ion or hydrogensulfide ion.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y.sub.m and Y'.sub.n are herein defined.

Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: Bifunctional aromatic compounds which are capable of linking metal ions to biologically useful molecules. The bifunctional compounds are characterized as having a hydrazine or hydrazide group and a protein reactive group. The hydrazine or hydrazide group may be protected as a lower alkyl hydrazone. Conjugates of the bifunctional compounds with macromolecules are also described and labelled macromolecules comprised of the conjugates and metal ions are provided. Additionally, a method is provided for forming a labelled macromolecule by reacting a conjugate with a metal species. The compounds and method of this invention are particularly useful in the fields of biology and medicine for imaging and/or therapy.

Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Abstract: An azole compound represented by the formula (I): ##STR1## wherein X is a nitrogen atom; Ar is a phenyl group substituted by halogen or a halogenated C.sub.1-4 alkyl group; R.sup.1 and R.sup.2 independently are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; n denotes an integer of 0 to 2; and R.sup.7 is a hydrogen atom, a hydroxyl group which may be optionally acylated by an acyl group selected from acetyl, propionyl, butyryl, isobutyryl, phenylacetyl and benzoyl, or may form a bond together with R.sup.1 ; or a salt thereof.

Abstract: Disclosed are a polyfluorinated thiazoline compound represented by the following formula (I): ##STR1## wherein Q represents a phenyl group; a phenyl group substituted by a halogen atom, a halo-lower alkyl group, a nitro group, a cyano group, a formyl group, a lower alkoxycarbonyl group or a benzoyl group; a pyridyl group; or a pyridyl group substituted by a halogen atom, a halo-lower alkyl group, a nitro group, a cyano group, a formyl group, a lower alkoxycarbonyl group or a benzoyl group; andR represents a hydrogen atom, a lower alkyl group or an acetyl group,and a chemical for controlling noxious organisms containing the same as an active ingredient.

Abstract: 3,4-Diaryl-4,5-dihydro-1H-pyrazole compounds having a selected 5- or 6-membered aromatic heterocyclic moiety in the 4-position and an optionally substituted phenyl moiety in the 3-position, such as 4,5-dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2-pyridinyl)-1H-pyrazo le were prepared as intermediates in the preparation of insecticidal 3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds. The 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds can be prepared from appropriate 1,2-diarylethanone compounds by successive treatments with N,N,N',N'-tetramethyldiaminomethane in dichloromethane in the presence of acetic anhydride (to form a Mannich adduct) and hydrazine in the presence of a catalytic amount of trifluoroacetic acid.

Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

Abstract: 4-Isoxazolyl-imidazole derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated, as well as their production and use in pharmaceutical agents, are described.

Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.

Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.

Abstract: The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group of an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pyridino group.

Abstract: The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.

Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.

Abstract: Bifunctional aromatic compounds which are capable of linking metal ions to biologically useful molecules. The bifunctional compounds are characterized as having a hydrazine or hydrazide group and a protein reactive group. The hydrazine or hydrazide group may be protected as a lower alkyl hydrazone. Conjugates of the bifunctional compounds with macromolecules are also described and labelled macromolecules comprised of the conjugates and metal ions are provided. Additionally, a method is provided for forming a labelled macromolecule by reacting a conjugate with a metal species The compounds and method of this invention are particularly useful in the fields of biology and medicine for imaging and/or therapy.

Abstract: The compounds of the formula: ##STR1## (wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is carbocyclic or heterocyclic ring, unsubstituted or substituted by R.sup.3 s; R.sup.3 is halogen, trihalomethyl, hydroxy, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfornyl, cyano, nitro, or group of the formula: --C.sub.6 H.sub.4 --R.sup.4, --NR.sup.5 R.sup.6, --CO--R.sup.7, --COOR.sup.8, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6 or --NHCO--R.sup.7, in which R.sup.4 is hydrogen, halogen, trihalomethyl, hydroxy, alkyl or alkoxy, R.sup.5 and R.sup.6 are each hydrogen or alkyl, R.sup.7 is alkyl or phenyl substituted by R.sup.4 and R.sup.8 is hydrogen or alkyl; Z is hydrogen or group of the formula: --COR.sup.9, ##STR2## in which R.sup.9 is alkyl or phenyl substituted by R.sup.10, in which R.sup.10 is hydrogen, halogen, trihalomethyl, alkyl or alkoxy, R.sup.11 and R.sup.12 are each hydrogen, alkyl or phenyl substituted by R.sup.10, or R.sup.11 and R.sup.

Abstract: There is described a new process for the preparation of substituted 3-aminoacrylic esters of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and n have the meaning given in the description.The 3-aminoacrylic esters of the formula (I) are obtained by reacting acetic esters of the formula (II)R.sup.1 --(X).sub.n --CH.sub.2 --COOR.sup.