Abstract: Method and composition for treating painful conditions of the body, particularly the anal region. The compositions include a combination of nitroglycerin and sucralfate or a combination of nitroglycerin, lidocaine and sucralfate. The compositions may be included in a petrolatum base along with a water soluble lubricant. These compositions have been found effective in treating painful conditions in the anal region, such as anal fissures, inflamed or recently thrombosed hemorrhoids, and other chronic anal pain.

Abstract: The present invention is directed to polymeric- prodrug transport forms of the formula: ##STR1## wherein: B is a leaving group, OH, a residue of a hydroxyl-containing moiety or ##STR2## wherein B.sub.1 is a leaving group, OH or a residue of a hydroxyl-containing moiety;Y.sub.1-2 are independently O or S;M is selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2); R.sub.2-5 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls and substituted C.sub.1-6 heteroalkyls;(m) is zero or one;(n) is a positive integer;(p) is zero or a positive integer;Z is an electron withdrawing group; andR.sub.

Abstract: A number of new therapeutic uses have been found for compounds such as known local anesthetics which are quite different from the present therapeutic uses of these drugs. The uses include, for example; modulating lymphocytes, macrophages and other immune cell functions, or PMN functions; inhibiting the cytotoxic effect of polymorphonuclear neutrophils leucocytes; providing a protective effect on plasma cell membranes; and providing an antidote against intoxication by an intoxicants.

Abstract: The use of compound 1 and/or 2 of the formulae ##STR1## and of physiologically tolerable salts of compound 2 for the treatment of rejection reactions of the organ recipient to the transplanted organ is described.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: A tachykinin receptor antagonist is useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity, in a patient.

Abstract: Method and composition for treating painful conditions of the anorectal region. The compositions include a combination of an .alpha.-adrenergic blocker and sucralfate, a combination of .alpha.-adrenergic blocker and lidocaine, and a combination of an .alpha.-adrenergic blocker, lidocaine, and sucralfate. Alternatively, the composition may contain only an .alpha.-adrenergic blocker. Additional active ingredients for reduction of anal pain may be added to the composition, particularly capsaicin. The compositions may be included in a petrolatum base along with a water soluble lubricant. These compositions have been found effective in treating painful conditions in the anal region, such as anal fissures, inflamed or recently thrombosed hemorrhoids, and chronic anal pain.

Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.

Abstract: The object of the present invention is to provide a novel bioactive substance of value as a therapeutic agent for mycosis, and the like.This invention relates to the bioactive substance TKR1785 of the following general formula (A): ##STR1## (wherein R represents --CH(CH.sub.3).sub.2 or --CH(CH.sub.3)C.sub.2 H.sub.5).

Abstract: Anesthetic compositions that achieve enhanced anesthesia of the peripheral nerves located in the mouth region of a subject or patient are provided. Such anesthetic compositions comprise water, a local anesthetic agent, and a sugar alcohol at a concentration of at least 0.1 moles/L i.e., at least 0.1 M. A method of anesthetizing a peripheral nerve of the mouth region is also provided. The method comprises: providing an anesthetic composition comprising water, a local anesthetic agent, and a sugar or, preferably, a sugar alcohol at a concentration of at least 0.1 M; and administering said anesthetic composition to a site proximate to said peripheral nerve.

Abstract: The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.

Abstract: The present invention is directed to N-benzyl-2-amino-3-methoxypropionamide and stereoisomers the use thereof anti-convulsant and an intermediate in the preparation of other anti-convulsants.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: .beta.-alethine is identified as an anti-tumor agent.

Abstract: This invention provides novel cationic lipids, particularly guanidino lipids, and methods for their preparation. Also provided are polyanionic-lipid complexes comprising the lipids of the invention, their preparation and use to deliver biologically active substances, particularly nucleic acids to cells.

Abstract: A method for increasing the effectiveness of a microbicide is described, wherein a microbicide and an N-alkyl heterocyclic compound are applied to a substrate or aqueous system subject to the growth of microorganisms. The N-alkyl heterocyclic compound is applied in an amount effective to increase the microbicidal activity of the microbicide. The N-alkyl heterocyclic compound has the formula: ##STR1## The variable "In" ranges from 5 to 17, and the heterocyclic ring defined by ##STR2## is a substituted or unsubstituted ring having four to eight members. Microbicidal compositions are described where the microbicide and the N-alkyl heterocyclic compound are present in a combined amount effective to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms on various substrates and in various aqueous systems are also described.

Abstract: The invention is directed to a novel pharmaceutical composition comprising one or more local anaesthetics in oil form, one or more surfactants, water and optionally a taste masking agent. The novel composition is advantageously used as a local anaesthetic for pain relief within the oral cavity.

Abstract: A composition for local anesthesia which comprises (A) lidocaine, (B) a catecholamine such as epinephrine in an amount of, for example, 1/200,000 (g/ml) based on the volume of the composition, and (C) one or more amino acids such as glycine, glutamic acid, and L-glutamic acid-L-lysine or one or more hydroxycarboxylic acids such as lactic acid, glycolic acid, and citric acid, which has a duration suitable for short-time dental operations such as tooth extraction and excellent storage stability.

Abstract: The present invention describes the ability of synthetic cationic amphiphilic molecules to bind and sequester bacterial lipopolysaccharides and other microbial products that share structural and/or physical-chemical properties with those of LPS. Such cationic amphiphilic molecules have a molecular structure comprised of a linear or branched backbone derived from polymethylenes or alkylamines which bear at the termini two or more protonatable positively charged groups derived from primary-amino. imidazolinium, or N, N'-unsubstituted amidinium or guanidium functions. They also possess one or more lipophilic groups derived from fatty acids or hydrocarbon substituents, attached to the backbone via amide, ester, carbamate, or urethane linkages. The use of these compounds provide low cost, effective therapeutic method for the treatment of sepsis and septic shock.

Abstract: There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.

Abstract: The present investigation relates to the use of a local anesthetic for the manufacture of a medicament for use against infertility or for increasing fertility. It also relates to a pharmaceutical composition comprising a pharmaceutically effective dose of a local anesthetic together with a pharmaceutically acceptable excipient. It also relates to a process for increasing fertility in a woman with said pharmaceutical composition.

Abstract: Mammalian hair growth is reduced by inhibiting the activity of a matrix metalloproteinase in the skin.

Abstract: N-substituted fatty acid amides which sufficiently inhibit LRAT or ARAT catalyzed esterification of retinol into inactive retinyl esters, have the same effect on keratinocytes as retinoic acid. Thus, effects of the retinol or retinyl esters in combination with N-substituted fatty acid amides are analogous to treatment with retinoic acid.

Abstract: A non-stinging styptic composition in the form of a water soluble resin coated cast pencil, for stopping bleeding from cuts and nicks received during shaving. The composition comprises aluminum sulfate, aloe, glycerine, lidocaine and polyethylene glycol 400.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: A topical anesthetic includes about 1-10% by weight lidocaine hydrochloride, about 0.01-0.10% by weight adrenaline, and about 0.25-4% by weight tetracaine hydrochloride, preferably in an aqueous base with about 2% benzyl alcohol or in a gel including about 3% hydroxyethyl cellulose. The topical anesthetic has been found to be at least as effective as TAC (tetracaine hydrochloride, adrenaline, cocaine), but with fewer harmful side effects and at a greatly reduced cost (about 1/10 of the cost of TAC).

Abstract: Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.

Abstract: The migraine-treating effectiveness of a local anesthetic drug is significantly enhanced by coadministering dextromethorphan or dextrorphan.

Abstract: Described are the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions; compositions containing these compounds; and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 --C(.dbd.X.sub.2)X.sub.3 R.sub.11, n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, X.sub.2, X.sub.3, Y and Z are independently, O, NH, or S.

Abstract: A method for the protection of trees of the families Musaceae or Plantanginaceae from destructive pests whereby the trees to be protected share a common root system.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: The present invention deals with the composition of matter and the utilization of certain novel amido amine salts of meadowfoam amido propyl dimethyl amine. These materials are useful in personal care applications.

Abstract: A new pharmaceutical preparation comprising one or more local anaesthetic agents, a polar lipid, a triacylglycerol and optionally water. The new pharmaceutical preparation is excellent for topical treatment of pain.

Abstract: The present invention deals with the composition of matter and the utilization of certain amine oxides of meadowfoam amido propyl dimethyl amine. These materials are useful in personal care applications.

Abstract: The present invention pertains to the field of pain management in medicine. Methods for treating reflex sympathetic dystrophy (including causalgia) are provided, in which a haloalkylamine a adrenergic blocking agent and a local anesthetic are administered to the affected limb by intravenous regional block. Formulations which can be used in these methods are also provided. In a preferred embodiment, phenoxybenzamine and either lidocaine or procaine are administered to the affected limb using a Bier block procedure.

Abstract: A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.

Abstract: The present invention relates to a method and pharmaceutical composition for treating fever blisters or cold sores in mammals, and particularly in humans, by topically administering a pharmaceutical composition comprising ethyl alcohol in a concentration of at least 85% W/V and lidocaine in a concentration of 0.5-10% W/V at a periodicity of at least 10 to 12 times daily.

Abstract: A pharmaceutical composition of the eutomer of a chiral drug is disclosed whereby the eutomer has a clearance value greater than that of the racemic mixture of the chiral drug. The pharmaceutical compositions of the present invention allow the delivery of therapeutically effective levels of drugs at doses much lower than would be required when the drug is delivered by conventional injection methods.

Abstract: The present invention is directed to a compound of the following formula: ##STR1## pharmaceutical compositions containing the same and the use thereof as an anticonvulsant.

Abstract: The present invention provides amide-based oligomeric cationic lipids. The present invention further provides compositions of these amide-based cationic lipids with anionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

Abstract: New combination of a .beta.-receptor blocker, an enantiomer thereof, and a local anesthetic, administered simultaneously or sequentially, giving excellent pain relief. Also comprised in the invention is the use of a non-selective .beta.-receptor blocker alone, especially a non-selective .beta.-receptor blocker giving pain relief.

Abstract: A composition containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin can be used to treat many types of discomforts, including arthritis pain, hemorrhoid pain and itching, and poison ivy itching, without the discomfort normally associated with the topical application of capsaicin.

Abstract: The present invention provides compositions comprising a local anesthetic and emu oil. The compositions are useful in a method of anesthetizing cornified skin comprising topically administering the subject compositions. The present compositions and methods permit rapid and effective anesthesia of cornified skin, such that various surgeries and interventions can be performed without the need for subcutaneous injections of local anesthetics. The present invention further provides a compartmentalized kit having a first container providing emu oil and a second container providing an aqueous solution of a local anesthetic.

Abstract: Now are provided (R)-3,6-diamino-N-(.omega.-aminoalkyl)-hexanamides which are novel compounds having the general formula (I): ##STR1## wherein n stands for 2-5, and which may be for example, (R)-3,6-diamino-N-(2-aminoethyl)hexanamide (n=2) and (R)-3,6-diamino-N-(3-aminopropyl)hexanamide (n=3). Their preparation process is also provided. These novel compounds and acid addition salts thereof have activities inhibitory against Gram-positive bacteria, Gram-negative bacteria and AIDS virus, as well as tumor cells and are chemically stable.These novel compounds and their salts are useful as chemotherapeutic agents for diseases caused by these bacteria or virus and also as antitumor agent.

Abstract: Compositions and methods for alleviating pain (in particular, neuropathic pain) in a mammalian patient, wherein an effective amount of a physiologically-acceptable salt of a compound of the general formula ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of hydrogen, hydroxyl, acyl, alkoxyl, alkyl, aryl, alkylaryl, arylalkyl, hydroxyalkyl, hydroxyaryl, alkoxyalkyl, alkoxyaryl and NR.sup.8 R.sup.9, in which each of R.sup.8 and R.sup.9 is independently selected from the group consisting of hydrogen, alkyl, aryl, acyl, alkylaryl, arylalkyl, hydroxyalkyl, hydroxyaryl, alkoxyalkyl and alkoxyaryl, with the proviso that at least one of R.sup.1, R.sup.2 and R.sup.3 is hydroxyl;each of R.sup.4 and R.sup.5 is independently selected from the group consisting of hydrogen, halogen and lower alkyl;A is --C(.dbd.O)O-- or NR.sup.10 C(.dbd.O)--, in which R.sup.

Abstract: A composition for topical therapy of headaches, which contains a topical carrier system for intact mammalian skin of forehead or temples or both, which contains a therapeutically effective dose of a local anesthetic for delivery to a skin surface underneath the topical carrier system.

Abstract: A therapeutic method is provided to treat an eosinophil-associated pathology, such as bronchial asthma, by administering to a mammal in need of such treatment, an effective amount of at least one topical anesthetic, such as lidocaine, with an effective amount of one or more glucocorticoids, or the pharmaceutically acceptable salts thereof.

Abstract: Disclosed is a method of inhibiting the growth of marine organisms on a marine structure, by applying onto or into the marine structure a phenylamide compound. These compounds may be directly incorporated into the marine structure during manufacture, directly applied to the structure, or applied to the structure by means of a coating.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention relates to novel amino acid derivatives, to a process for their preparation and to their use as pesticides, in particular as fungicides, and as intermediates for preparing known substituted amino acid derivatives with fungicidal activity.