Abstract: Halo active aromatic sulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to releaser active halogen ions has been utilized in a range of biocidal and fungicidal applications. The most widely used sulfonamide organic compound for these applications has been Chloramine T. This invention deals with nearly discovered halo active aromatic sulfonamide organic compounds and uses of these compounds as biocides, odor control agents, bovine teat cleaners, drugs for cultured fish, soap biocides, stain removal agents, and paint fungicides.

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer.

Abstract: Methods for treatment of antibiotic-resistant and multi-drug resistant bacterial infections are provided. The methods comprise administration of compositions which mimic plasmid incompatibility in bacteria, resulting in their sensitization to previously resistant drugs. Also provided herein are methods for screening compositions for the ability to mimic plasmid incompatibility by inhibiting Rep protein or by destabilizing RNA/RNA stem loop “kissing” structures. The invention also encompasses compositions identified by the screening methods disclosed herein.

Abstract: The present invention relates to microbial multidrug resistance and, in particular, to compounds that microbial drug transporters of the ABC protein superfamily. The invention also relates to methods for selecting or designing compounds for the ability to inhibit drug transporter proteins and to methods of inhibiting drug transporter proteins. The invention concerns the new use of opioid receptor antagonists in the treatment of multidrug resistant microbial infections.

Abstract: A therapeutic and/or prophylactic agent for nervous system disorder comprising as the active ingredient substances having an effect of improving calcium ion uptake of cardiac sarcoplasmic reticulum and/or an effect of inhibiting overaccumulation of intracellular calcium ions is offered. Preferably, the therapeutic and/or prophylactic agent for disease selected from the group consisting of cerebrovascular disease, traumatic head injury and postencephalitis and the therapeutic and/or prophylactic agent for disease selected from the group consisting of dementia and neuronal degeneration disease are offered.

Abstract: Provided is a topical pharmaceutical composition for the treatment of inflammatory dermatoses, including acne vulgaris, together with methods for its use. The composition and methods involve the topical use of an active agent effective in the treatment of inflammatory dermatoses plus a permeation-enhancing base that, in one embodiment, gives the composition a pH of about 8.0 to about 13.0, preferably about 8.0 to 11.5, and most preferably about 8.5 to 10.5.

Abstract: Topical compositions which include urea and an antimicrobial agent, particularly sulfacetamide, are described. Sulfacetamide compositions further including sulfur are also described. Methods for treating dermatological disorders using the compositions are also described.

Abstract: A palatable antimicrobial drug concentrate comprising: (a) a sulfonamide and/or sulfonamide salt in aqueous solution; (b) a 2,4-diaminopyrimidine in stable suspension within said solution; and (c) a suspending agent. The invention has a long room temperature shelf life and is sufficiently stable to be administered via the drinking water of animals.

Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: This application relates to a stable pharmaceutical composition and methods for the cleansing of skin to facilitate the prevention, treatment, and management of skin conditions, such as seborrheic dermatitis, psoriasis, folliculitis, rosacea, perioral dermatitis, acne, impetigo and other inflammatory skin conditions, and the like, including a sufficient amount of an acidic component of a hydroxyacid or tannic acid, or a pharmaceutically acceptable salt thereof, to exfoliate a portion of the skin, a sufficient amount of stabilized hydrogen peroxide to facilitate cleansing of the skin without substantial irritation thereof, and an antimicrobial agent including at least one of an antibacterial agent, antimicrobial agent, antiviral agent, anthelmintic, or a combination thereof, in an amount sufficient to inhibit or reduce microorganisms on the skin.

Abstract: Combinations of a cyclooxygenase-2 inhibitor and a leukotriene B4 receptor antagonist are described for treatment of inflammation and inflammation-related disorders.

Abstract: Compounds of formula (I) are inhibitors of the bacterial enzyme S aureus methionyl tRNA synthetase and are of use in treating bacterial infections.

Abstract: Disclosed herein is the discovery that an allosteric receptor site exists on the intracellular surface of Shaker class voltage-gated potassium ion channels that is distinct from the pore and is involved in regulating gating of the pore. A class of compounds has been identified that binds to this allosteric site and modulates the length of time the channel remains open. Based on these discoveries, novel methods of modulating the activity of Shaker class voltage-gated potassium ion channels and assays for determining which compounds are modulators of these ion channels are reported herein.

Abstract: Disclosed are pharmaceutical compositions and formulations comprising the compound: wherein: (a) R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, or optionally substituted alkyl, aryl, vinyl, alkyl(aryl), vinyl(aryl), amine, amide; or at least one of R1 and R2, together, and R3 and R4, together, form an optionally substituted ring system, wherein the ring system is optionally interrupted by at least one heteroatom; (b) X is hydrogen, NO2, CN, halogen, OH, SO2, alkyl, alkoxy, or vinyl; and (c) wherein when R1, R2, R3, and R4 are alkyl, aryl, vinyl, alkyl(aryl), vinyl(aryl), amine or amide, R1, R2, R3, and R4 are optionally interrupted with at least one heteroatom, or a salt thereof; and a pharmaceutically acceptable carrier or diluent. Also disclosed are methods of inhibiting microbial replication and treating microbial infections, comprising administration of a pharmaceutical composition or formulation of the invention.

Abstract: Both a process and a method of using peracid compositions, especially mixed peracid systems, to treat field or greenhouse grown plant tissue, seeds, fruits, and growing media and containers. The peracid can lower the natural, plant pathogen and human pathogenic microbial load resulting in less waste to molding, spoilage, and destruction because of pathogenic poisons.

Abstract: Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclooxygenase II ##STR1##

Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.

Abstract: Disclosed herein are parenteral solutions containing 7-halo-1,2,3, 4-tetrahydro-3-aryl-6-quinazoline sulfonamide in Tris or Bis-Tris or Tris buffer useful in the treatment of hypertension, heart disease and heart failure and renal disease. Also disclosed are methods for preparing such solutions.

Abstract: The present invention relates to novel compounds of formula (I): ##STR1## or a physiologically functional derivative thereof, pharmaceutical formulations containing them, processes for their preparation and their use in therapy for the prophylaxis or treatment of HIV infection or inflammation are disclosed.

Abstract: Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in Tris or Bis-Tris or Tris buffer useful in the treatment of hypertension, heart disease and heart failure and renal disease. Also disclosed are methods for preparing such solutions.

Abstract: A cyano compound useful as an insecticide, of the formula (I) ##STR1## wherein the radicals are defined in the claims.

Abstract: The antibacterial substance baquiloprim (2,4-diamino-5-[8-dimethylamino-7-methyl-5-quinolylmethyl]pyrimidine) is shown to be active against protozoal infections, e.g. toxoplasmosis. Preferably the baquiloprim is administered together with a sulphonamide.

Abstract: The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Abstract: The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Abstract: Disclosed are substituted bis(4-aminophenyl-sulfonees of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.

Abstract: A compound of formula I ##STR1## wherein R.sub.1 is of formula II ##STR2## wherein R.sub.4 and R.sub.5, which may be the same or different, are bromo, chloro, iodo or alkylsulphonyl;R.sub.2 is of formula III ##STR3## wherein R.sub.6 and R.sub.7, which may be the same or different, are H, alkyl, aryl, carboxy, hydroxy or amino and n is 0-10; andR.sub.3 is hydroxy or a group capable of being cleared and replaced by a radical having an antigen binding site or R.sub.3 is a radical having an antigen binding site.

Abstract: The present invention relates to the use of sulphonamide derivatives for the treatment of diseases caused by viruses, especially caused by enclosed viruses such as, e.g., herpes simplex, as well as to an antiviral agent having a content of these sulphonamide derivatives as active substance, optionally together with pharmaceutically acceptable carriers and/or auxiliaries.

Abstract: A method of preparing aqueous pharmaceutical compositions containing a synergistic combination of trimethoprim and sodium sulfacetamide is described. The method results in a significant improvement in the aqueous solubility of trimethoprim due to a favorable interaction between the trimethoprim and sodium sulfacetamide which is dependent on a mildly acidic pH.

Abstract: Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.

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: The present invention concerns compounds of the formula: ##STR1## where R.sub.1 is an alkyl or alkenyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3 to 7 carbon atoms, an aralkyl, aralkenyl or aryl radical in which the aryl radical or moiety can be substituted one or more times by halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.12 -dialkylamino, C.sub.1 -C.sub.6 -acylamino, C.sub.1 -C.sub.16 -acyl, C.sub.1 -C.sub.6 -alkylsulphenyl, -sulphinyl or -sulphonyl or by azido, R.sub.2 is hydrogen atom or a C.sub.1 -C.sub.6 -alkyl, aralkyl, aralkenyl or acyl radical, A and B are saturated or unsaturated alkylene chains containing up to 10 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.

Abstract: The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.

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: Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is H, methyl, ethyl, or chloro and R.sup.2 is hydrocarbyl of 1-12 C are useful as antifungal agents. Compounds of this series wherein R.sup.2 is 7-12 C are novel. A new synthetic method for the compounds is also described.

Abstract: The present invention provides gamma-glutamyl-4-azoanilides, processes for their preparation and their use as substrates for gamma-glutamyl transferase determination, of the formula ##STR1## wherein X is alkyl, --(CH.sub.2).sub.m --COOH or --O--(CH.sub.2).sub.n --COOH wherein m is 0-4 and n is 1-4; R is optionally substituted p-nitrophenyl; an optionally substituted thiophene residue; an optionally substituted thiazole residue; an optionally substituted benzothiazole residue; an optionally substituted benzoisothiazole residue; an N-alkylthiazole residue; or an optionally substituted 1,3,5-thiodiazole residue; as well as the alkali metal, alkaline earth metal and ammonium salts thereof.

Abstract: The invention relates to new medicaments having lipid regulating properties nd processes for their preparation.The medicaments according to the invention contain as active principle at least one compound, (or its corresponding optical isomer) of the arylsulfonamide type corresponding to the formula: ##STR1## in which: Ar prepresents an aromatic ring which may if necessary be substituted;n+m+1 is comprised from 3 to 11, being preferably equal to 3, 5 or 10;R.sub.5 and R.sub.6 represent independently of one another, particularly an alkyl radical;R.sub.4 represents the hydroxy group, the radical OR.sub.7 in which R.sub.7 is particularly an alkyl group, the radical NR.sub.8 R.sub.9 in which R.sub.8 and R.sub.9 are identical or different, and represent in particular a hydrogen atom, and form with the nitrogen a nitrogenous heterocyclic ring with 5 or 6 links.

Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.

Abstract: Compounds of the formula: ##STR1## wherein R is aryl of 6 to 12 carbon atoms or aralkyl of 7 to 14 carbon atoms either optionally substituted with 1 to 3 substituents independently selected from lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, lower alkylsulfinyl of 1 to 6 carbon atoms, lower alkylsulfonyl of 1 to 6 carbon atoms, halogen, trihalomethyl, nitro, cyano or carboxyl; alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 halogen atoms; lower alkoxyalkylene; lower alkylene carbalkoxy; lower alkylthioalkylene; lower alkylsulfinylalkylene; or lower alkylsulfonylalkylene; R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl of 1 to 6 carbon atoms, aryl of 6 to 12 carbon atoms, or thienyl, or taken together form an alkylene bridge to give a cycloalkyl group of 3 to 10 carbon atoms; and R.sup.

Abstract: The present invention provides a novel method for treating osteoporoses, joint and dental diseases and increasing the rate of bone healing by orally administering certain prostaglandins. Further provided are novel compositions employing these prostaglandins.

Abstract: A combination tablet containing metolazone and triamterene is useful in diuretic therapy and the treatment of hypertension. The composition is advantageous in the prevention of hypokalemia, a common side effect of diuretic therapy and possesses enhanced dissolution properties. Proper selection of the excipient formulation permits preparation of the tablets by direct compression.

Abstract: An insecticidal composition which comprises as an active ingredient a compound of the formula: ##STR1## wherein X is a hydrogen atom or an acyl group, Y is a hydrogen atom, a lower alkyl group or a halogen atom and R.sub.1 and R.sub.2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cyclo(lower)alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group or an acyl group, provided that R.sub.1 and R.sub.2 are not simultaneously a hydrogen atom or an acyl group.