Abstract: A method of inhibiting effects of growth hormone comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically accepatable salt of solvate thereof.

Abstract: The present invention relates, in general, to methods of treating disorders of the eye, and, in particular, to methods of preventing or treating elevated eye pressure and glaucoma by administering to a patient in need thereof a non-sulfhydryl reactive derivative of phenoxyacetic acid (eg indacrinone or ticrynafen) that increases aqueous humor outflow. The invention further relates to compounds and compositions suitable for use in such methods.

Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.

Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.

Abstract: This invention relates to benzyl and naphthalenylmethyl thiophenones and cyclopentenones, some of which are novel, which have oral antihyperglycemic activity in diabetic mice, a genetic animal model of non-insulin dependent diabetes mellitus. These compounds are represented by the formula ##STR1## wherein: R.sup.2 and R.sup.3 are independently selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl or R.sup.2 together with R.sup.3 forms a benzo ring fused to the phenyl ring and optionally substituted with one or two substituents independently selected from C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifiuoromethyl;R.sup.1 is selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl;andR.sup.4 is selected from the group consisting of: ##STR2## wherein R.sup.5 is H or C.sub.1-6 alkyl or a pharmaceutically acceptable salt thereof.

Abstract: Substituted amine derivatives represented by the general formula ##STR1## wherein Q is --C--D--E--F--G--M-- or --N--H--I--J--K--L-- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, --CHR.sup.a --, --R.sup.b .dbd. or --NR.sup.c -- (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or --NR.sup.c --]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub.3 an acetoxy group, a lower alkyl group or a lower alkoxy group.

Abstract: There are disclosed compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl, cycloalkyl, arylalkyl, --(CH.sub.2).sub.r CH.dbd.CH.sub.2, --(CH.sub.2).sub.s OY, --(CH.sub.2).sub.t CH(OZ)CH.sub.3, or Ar;X is O, S, or NR.sup.2 ;Y and Z are each, independently, hydrogen, alkyl, or --COR.sup.3 ;R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, or arylalkyl;Ar is an aryl radical that may be optionally substituted;m=1-5;n=0-1;p=1-9;r=0-6;s=2-6; andt=0-6or a pharmaceutically acceptable salt thereof which are useful as antiinflammatory agents.

Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.

Abstract: Compounds of formula ##STR1## Ar is selected from (a) phenyl, (b) phenyl substituted with one or more groups selected from halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl, (c) furyl, (d) furyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (e) pyridyl, (f) pyridyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (g) thienyl, and (h) thienyl substituted with one or more groups selected from halogen, alkyl, and alkoxy; L is selected from alkylene of one to three carbon atoms, alkenylene of two to three carbon atoms, and alkynylene of two to three carbon atoms, and ##STR2## wherein p is an integer of 1 to 4, inclusive, and R.sup.4 is selected from the group consisting of hydrogen, alkyl of one to four carbon atoms, halogen, haloalkyl of one to four carbon atoms, and alkoxy of one to six carbon atoms;R.sup.1 is alkyl; R.sup.2 is hydrogen or alkyl; m is 1 or 2; Z is oxygen or CHOR.sup.

Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

Abstract: Disclosed are compounds of Formula I useful in the treatment of cyclooxygenase mediated diseases such as pain, fever and inflammation of a variety of conditions including rheumatic fever, symptoms associated with influenza or other viral infections, common cold, low back and neck pain, dysmenorrhea, headache, toothache, sprains and strains, myositis, neuralgia, synovitis, arthritis, including rheumatoid arthritis degenerative joint diseases (osteoarthritis), gout and ankylosing spondylitis, bursitis, burns, injuries.

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; and R.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: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.

Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.

Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.

Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted aralkyl, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.1, --CONR.sup.2 R.sup.3, or --COR.sup.

Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is O, S or NR;R is hydrogen or lower alkyl;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;m is 0-15;n is 0-20;p is 0-15,where m+p.ltoreq.15;and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.

Abstract: 3-Alkyloxy-, aryloxy-, or arylalkyloxybenzo[b]-thiophene-2-carboxamides are described as agents which block leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of preparation are also described.

Abstract: 3-Thio or amino substituted benzo[b]thiophene-2-carboxamides and 3-oxygen, thio, or amino substituted benzofuran-2-carboxamides are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of manufacture are also described.The same benzo[b]thiophene and benzofuran-2-carboxamides also inhibit the activation of human immunodeficiency virus (HIV), latent in infected mammals.

Abstract: Angiotensin converting enzyme inhibitors have the formula Z(CH.sub.2).sub.n CHR.sub.1 COOCHR.sub.2 COOHin which Z is --SR.sub.3, --COCHR.sub.4 NHCOR.sub.5, ##STR1## or --NHCHR.sub.7 COOH, R.sub.4, R.sub.5, R.sub.6, and R.sub.7, which may be the same or different, are each phenyl or alkylphenyl C.sub.7-12,R.sub.4 is hydrogen, alkyl C.sub.1-6, NHR.sub.8 or (CH.sub.2).sub.p R.sub.9,R.sub.2 is (CH.sub.2).sub.m XR.sub.10, alkyl C.sub.1-6 optionally substituted by a saturated 5- or 6-membered carbocyclic or heterocyclic ring, alkylhalo C.sub.1-6, alkylcyano C.sub.1-6, or alkyl phenyl C.sub.7-12, the phenyl being optionally substituted by NO.sub.2 or NH.sub.2,X is O, S(O).sub.q, C.dbd.O or NR.sub.11, andR.sub.10 is alkyl C.sub.1-6, alkylhalo C.sub.1-6, alkoxy C.sub.1-6, alkoxy C.sub.1-6 substituted by halogen, alkanoyl C.sub.1-6, S(O).sub.r R.sub.12, NR.sub.13 R.sub.14, phenyl, alkylphenyl C.sub.

Abstract: The invention is concerned with novel antioxidants, namely the [R] and, respectively, [S] compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 together represent the --S(O)-- group and R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together represent the --S(O)-- group and R.sup.1 and R.sup.2 represent hydrogen.

Abstract: New aryloxy-alkylamine derivatives of the general formula I ##STR1## in which A signifies a benzene or thiophene ring, R and R.sub.1, independently of one another, each hydrogen, alkyl, halogen, CF.sub.3 or alkoxy, R.sub.2 alkyl, cycloalkyl, alkenyl, alkynyl, alkaryl or saturated or unsaturated aliphatic or aromatic acyl, R.sub.3 and R.sub.4 in each case hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl with, in each case, up to 8 C-atoms, whereby R.sub.3 and R.sub.4 can be the same or different but are not simultaneously hydrogen or R.sub.3 and R.sub.4, together with the nitrogen atom connecting them, form a 5- to 7-membered saturated ring or a saturated heterocyclic ring which can possibly contain an oxygen or nitrogen atom as a further heteroatom in the ring, whereby an additional nitrogen atom can be substituted by an alkyl radical with up to 3 C-atoms, and their acid-addition salts possess interesting pharmaceutical properties and are especially suitable as anti-arrhythmics.

Abstract: There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.

Abstract: Substituted amine derivatives represented by the general formula ##STR1## wherein Q is -C-D-E- F-G-M- or -N-H-I-J-K-L- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, -CHR.sup.2 -, -R.sup.b = or -NR.sup.c - (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or -NR.sup.c -]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub. 3 an acetoxy group, a lower alkyl group or a lower alkoxy group.

Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.

Abstract: Use as microbicides of thioacryloyl compounds of the formula ##STR1## Compounds and compositions are also disclosed.

Abstract: The present invention provides novel carbonic anhyrase inhibitors represented by the structural formula: ##STR1## wherein R.sub.1 and R.sub.2 are, for example, independently (a) hydrogen; or(b) OR.sub.4, wherein R.sub.4 is hydrogen or C.sub.1-7 alkyl; or(c) NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are independently hydrogen, or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen or OR.sub.4 ; or(d) --COR.sub.7, wherein R.sub.7 is hydrogen, C.sub.1-7 alkyl, or NR.sub.5 R.sub.6 ; or(e) --SR.sub.8, wherein R.sub.8 is hydrogen or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 ; or(f) C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 or NR.sub.5 R.sub.6 ; or(g) R.sub.1 and R.sub.2 are together(i) .dbd.O, or(ii) .dbd.NOR.sub.8 or(iii) .dbd.S;and R.sub.3 is(h) C.sub.1-7 alkyl or C.sub.1-7 substituted with one or more halogen, OR.sub.4 or NR.sub.5 R.sub.6.

Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.

Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.

Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is --CH.sub.2 R;R is ##STR2## and further when Y=S, R may also be --(CH.sub.2).sub.e CH.sub.3 ; Y is --O--or --S--;R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl;R.sup.3 is indolyl, furyl, phenyl or phenyl optionally mono- or disubstituted independently by alkyl of 1-7 carbon atoms, --C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 CH.sub.3, haloloweralkyl, perfluoroalkyl, lower alkoxy, aryl alkoxy, halo or nitro;R.sup.4 and R.sup.5 are, independently, --COCH.sub.2 R.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, geranyl or CH.sub.2 R.sup.3 ;R.sup.6 is hydrogen or lower alkyl;R.sup.7 is geranyl and any moiety selected from R other than ##STR3## A and B are, independently, --O--, --S-- or --NR.sup.6 --; and a is 0-8;b is 1-10 when Y=S, and 2-10 when Y=O;c is 1-3;d is 0-9; ande is 3-18;which by virtue of their ability to inhibit PLA.sub.

Abstract: Disclosed are the use of hexamethylenetetramine as a stabilizer for 3-isothiazolones under basic conditions, i.e. above pH 7.0, and compositions comprising HMT and 3-isothiazolones.

Abstract: Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl (C.sub.1 -C.sub.6) alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.

Abstract: Described are caffeic acid derivatives represented by the following formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a group --CO.sub.2 R.sup.4, or a group --CONR.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 being either a hydrogen atom or a particular group, and the other is the group --CO.sub.2 R.sub.4 or the group --CONF.sup.5 R.sup.6, or R.sup.1 and R.sup.2 are coupled together to represent a 5-membered ring so formed, Y represents a particular group or atom, X represents a substituted or unsubstituted C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl, heterocyclic or heterocyclic ring-alkyl group, m and n stand for particular integers, and R.sub.3 represents a hydrogen atom, a hydroxyl group, a group --OCO.sub.2 R.sup.7, R.sup.7 being a hydrogen atom or a particular group, or a group --OCONR.sup.8 R.sup.9, R.sup.8 representing a C.sub.1 -C.sub.6 alkyl group and R.sup.9 representing a hydrogen atom or a C.sub.1 -C.sub.

Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

Abstract: Administration of a folate binding protein binding agent in conjunction with use of an antitumor agent which is an inhibitor of glycinamide ribonucleotide transformylase or other antifolate reduces the toxic effects of such agent and provides an enhanced therapeutic index.

Abstract: This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.

Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.

Abstract: Substituted imidazoles attached through a methylene bridge to novel substituted phenyl thiophene or phenyl furan derivative of the Formula I are useful as angiotensin II antagonists.

Abstract: An aquatic antifouling composition comprising (A) at least one 4-isothiazolin-3-one compound represented by the general formula: ##STR1## where X.sub.1 and X.sub.2 respectively represent a hydrogen atom or a halogen atom, and (B) at least one insoluble dithiocarbamic acid derivatives possessing a dithiocarbamyl group ##STR2## selected from the group consisting of divalent and higher heavy metal (zinc, manganese, copper, iron, and nickel) salts of ethylenebisdithiocarbamic acid, linear or branched propylenebisdithiocarbamic acid, linear or branched butylenebisdithiocarbamic acid, N-substituted ethylenebisdithiocarbamic acid, N,N'-substituted ethylenebisdithiocarbamic acid, N-substituted propylenebisdithiocarbamic acid, N,N'-substituted propylene-bisdithiocarbamic acid, N-substituted butylenebisdithiocarbamic acid, and N,N'-substituted butylenebisdithiocarbamic acid.

Abstract: Compounds of the structure ##STR1## where M is a pharmaceutically acceptable cation or a metabolically cleavable group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted alkyl, cycloalkyl, carbocyclic aryl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Abstract: Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5- and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.

Abstract: Novel 4-chloro-4,4-difluorothiobutyric acid derivatives of the formula I ##STR1## in which R.sub.1 and R.sub.2 are, independently of one another, hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 halogenoalkyl and R.sub.3 is hydrogen or an organic radical can be employed as pest-control agents. Control of insects and arachnids is possible and preferable.

Abstract: Certain N-aryl, N-heteroaryl-, N-arylalkyl-, N-heteroarylalkyl-, N-arylcyclopropyl- and N-heteroaryl-cyclopropyl-N'-hydroxyurea compounds are inhibitors of lipoxygenase enzyme activity and are thus useful agents in treating disease states such as asthma, arthritis, allergy, psoriasis, inflammatory bowel disease, gout, adult respiratory distress syndrome, endotoxin shock, and other inflammatory conditions in which the products of the arachidonic acid cascade are implicated.

Abstract: Retinoid like activity is exhibited by compounds of the formula ##STR1## R.sub.1 -R.sub.3 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and A.sub.1 independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR.sub.4 or OR.sub.4 where R.sub.4 is lower alkyl, cycloalkyl or lower alkenyl; Y is selected from a group consisting of thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; E is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl, or is characterized by the formula (CH.sub.2).sub.n where n is 0-5, and Z is H, OH, OR.sub.5, OCOR.sub.5, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH, CH.sub.2 OR.sub.6, CH.sub.2 OCOR.sub.6, or --CHO, CH(OR.sub.7).sub.2, CHOR.sub.8 O, or COR.sub.9, CR.sub.9 (OR.sub.7).sub.2, CR.sub.9 OR.sub.8 O where R.sub.5 is lower alkyl, phenyl or lower alkylphenyl, R.sub.6 is lower alkyl, phenyl or lower alkylphenyl, R.sub.7 is lower alkyl, R.sub.

Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.