Abstract: The subject invention pertains to compounds which are useful as anti-inflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate to the anti-neurogenic inflammatory properties of the disclosed compounds. Specifically exemplified herein is the use of manzamines A, B, C, D, E, and F, and their salts, analogs, and derivatives.

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with a lysosomal storage disorder by administering a competitive inhibitor of the enzyme in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds.

Abstract: A nalmefene transdermal delivery system useful for the treatment of human patients suffering from opioid addiction.

Abstract: The specification discloses the treatment of malaria through the use of tetrandrine and its derivatives.

Abstract: Compositions comprising antimuscarinic compounds that have been modified to render them substantially irreversible, such as by quaternization of the heterocyclic ring nitrogen, have improved properties when administered intravesically for treatment of bladder diseases, particularly urinary incontinence. Pharmaceutical compositions and methods of treatment using these improved compounds or improved routes of administration re disclosed.

Abstract: This invention provides an antipruritic comprising an ipoate &kgr; receptor agonist as an effective component, a new morphian quaternary ammonium salt derivative and a new morphian-N-oxide derivative which are useful in treating pruritus complicated with some diseases.

Abstract: Compounds of the formula 1

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: The subject invention pertains to compounds which are useful as anti-inflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate to the anti-neurogenic inflammatory properties of the disclosed compounds. Specifically exemplified herein is the use of manzamines A, B, C, D, E, and F, and their salts, analogs, and derivatives.

Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.

Abstract: Method fore enhancing in a mammalian cell the activity of an enzyme associated with a lysosomal storage disorder by administering a competitive inhibitor of the enzyme in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds.

Abstract: A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules of interest, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters. The compound may be used in a method of treating cancer, and in a method of imaging opioid receptors either inside or outside of the central nervous system.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Lymphoproliferative syndrome, including such diseases as malignant lymphoma, chronic lymphocytic leukemia, Hodgkin's lymphoma, and non-Hodgkin's lymphoma, is treated in human patients by the administration by a pharmacologically effective mode or route of an essentially pure opiate receptor antagonist, typified by Naltrexone and Naloxone, exerting substantially higher blocking action for Mu opiate receptor sites than against Delta opiate receptor sites at a low dose concentration which produces therapeutic results corresponding to those obtained by the administration of Naltrexone at a low dosage level in the range of 1.0 mg. to 10 mg. and at which Delta receptor blocking activity is at most small and Mu receptor blocking activity is significant and most preferably substantially exclusive. Naltrexone is suitable for oral administration and is preferred.

Abstract: Methods for optimally regulating dopamine homeostasis in persons addicted to, then chemically detoxified from, opioid agonist analgesics, which generally include prolonged controlled administration of nalmefene, with or without the addition of a centrally acting medicinal agent which further enhances dopamine regulation.

Abstract: This invention provides an antipruritic comprising an opiate &kgr; receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated with some diseases.

Abstract: Manzamines, administered either intraperitoneally or orally, have been found to prolong survival and inhibit parasitemia in erythrocytic stage malaria. Thus, manzamines can be used for both prophylaxis and treatment. Manzamine A is a preferred compound for use in prophylaxis or treatment.

Abstract: The present invention provides compounds of formulae (I) and (II), where X in formula (I) represents a group cleavable by a nitroreductase or carboxypeptidase enzyme. Enzymatic activation of the compounds provide pharmaceutical compounds which may be used for the treatment of neoplastic disease.

Abstract: The present invention relates an agent for the treatment of infections, which comprises as the active ingredient at least one member selected from the group consisting of aconite-alkaloids, aconite tuber and an extract thereof, gingerol and analogues thereof, and rhizomes of ginger and a substance therefrom. The agent of the present invention has significant infection-protective and recovery effects and is useful to treat and prevent a variety of infections such as virus infections, fungal infections, opportunistic infections, etc.

Abstract: Compounds of formula I ##STR1## wherein X.sub.1 and X.sub.2 are C.dbd.O, C.dbd.NH or CH.sub.2, X.sub.3 is CH.sub.2, CO, CHOH, ##STR2## wherein n=2 or, 3 or C.dbd.N(R.sub.9) wherein R.sub.9 is hydroxy or amino-aryl, and each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are hydrogen, halogen or an organic residue, are useful in the treatment of amyloidosis. A process for their preparation and pharmaceutical compositions containing them are also described.

Abstract: Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders.

Abstract: A method for treating skin conditions, such as rosacea and sensitive skin, that manifest as a tendency towards flushing and blushing is provided. Also provided herein, are compositions for the treatment of rosacea and sensitive skin that are comprised of at least one antioxidant selected from the following groups of antioxidants: (a) phenolic compounds that contain at least one hydroxyl group connected directly to a benzene ring and to another unsaturated chemical grouping, (b) sulfur-containing compounds that contain at least one sulfhydryl groups or sulfur-containing compounds that contain at least one disulfide group, or (c) polyene compounds that have conjugated systems of double bonds.

Abstract: The invention provides a method for treating acute and severe diarrhea such as that which accompanies chemotherapy and rapid narcotic detoxification. The method includes administering octreotide in an amount sufficient to alleviate the diarrhea without precipitating clinically significant bradycardia. In a preferred embodiment an anticholenergic is administered together with octreotide to further reduce the possibility of significant bradycardia. The invention also provides a method for rapidly detoxifying a patient addicted to narcotics. Acute and severe diarrhea is eliminated during detoxification by administering octreotide in according to the above-described method.

Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.

Abstract: Tetrazole derivatives of the formula ##STR1## wherein R is a substituted or unsubstituted phenyl group, heterocyclic group, or benzo-fused heterocyclic group,which exhibit activity as insecticides and acaricides.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: Methods whereby the narcotic antagonist 17-(cyclopropylmethyl)-4,5alpha-6-methylenemorphinan-3,14-diol,hydrochlori de salt and other narcotic antagonists are used for chemically precipitating a withdrawal response in human beings addicted to exogenous narcotics and who are currently using exogenous narcotics.

Abstract: This invention provides for a method of raising extracellular brain acetylcholine levels to improve cognition by the administration to a warm-blooded animal of a pharmaceutical composition comprising an effective amount of a dopamine D.sub.1 agonist.

Abstract: There is provided a composition for inhibiting the production or secretion of tumor necrosis factor effective for the treatment of cachexia, septic shock, multiple organ failure, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, osteoarthritis, Behcet disease, systemic lupus erythematosus (SLE), graft versus host disease (GvHD), malaria, acquired immune deficiency syndrome (AIDS), meningitis, hepatitis and Type II diabetes mellitus. The composition comprises a pharmaceutically effective amount of a compound of formula (1).

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: A rupununine, either in purified form or a derivative in which one or both of the hydroxyl groups is substituted, the rupununine having the formula: ##STR1## where R.dbd.--H or --CH.sub.3.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: The invention relates to the method of synthesis of bicyclic hexahydroaporphine compounds which may provide improved therapy for diseases characterized by an increase in intraocular pressure. More specifically, the present invention relates to the preparation of agents which may provide for improved treatment of patients with glaucoma or ocular hypertension. The present invention describes the intraocular pressure lowering capabilities of several of the bicyclic hexahydroaporphine structures.

Abstract: A method for inducing apoptosis in target cells employs designed enediynes which are triggered to become chemically reactive when bound to target cells. Conversely, a method for inhibiting the induction of apoptosis employs compounds which compete with the above compounds which induce apoptosis, but which are chemically unreactive with respect to the target cells.

Abstract: 6,11'-Cyclyl-1,2,3,4,5,6,11,11a-octahydrobenzo[b]quinolizine derivatives, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: 6,11-Substituted-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: Biphenylyl compounds of formula ##STR1## wherein the variables R.sub.1, R.sub.2, R.sub.3, p, q and X and the rings A and B are as defined in claim 1, in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as active ingredients in medicaments.

Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, representing various parasitic diseases, apparently by reversing the glycoprotein "pumps" associated with such cells.

Abstract: The compounds of formula (I) ##STR1## wherein R is selected from the group hydroxymethyl and carboxy, have been identified as metabolites of 5.alpha.-23-methyl-4-aza-21-nor-chol-1-ene-3,20-dione and are believed to be active as testosterone 5.alpha.-reductase inhibitors and would thus be useful for treatment of acne, seborrhea, female hirsutism or benign prostatic hypertrophy.

Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.

Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

Abstract: Liquefiable powder compositions are disclosed for the delivery of fragrances. In particular, microporous cellulosic powders, such as cellulose acetates or nitrates, are disclosed as high liquid content vehicles for the delivery of fragrance preparations dissolved or dispersed in a liquid carrier. The resulting powders permit the application of the fragrance preparations by simply rubbing or otherwise applying the formulation onto the skin in such a manner that the powder liquefies and appears to vanish. Upon application, the frangible liquid loaded cellulosic powders break up into minute particles that do not pass easily beyond the initial layers of the skin, but do permit the slow release of the fragrance agent.

Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.

Abstract: A tetrahydroquinoline alkaloid compound named "aspernomine" has been isolated from the sclerotia of the fungus Aspergillus nomius. Aspernomine has the structure: ##STR1## and is effective for controlling Lepidopteran insects.

Abstract: Novel antitussive and anesthetic liquid compositions of matter for oral use comprising an effective oral antitussive drug and dyclonine; and method of using same.

Abstract: Benzolactam compounds of the general formula ##STR1## or isomers thereof as well as salts thereof inclusive of hydrates and/or solvates forms thereof, and benzolactam compounds of the general formula ##STR2## wherein each of the symbols is as defined in the specification. The compound (I) exhibit antiamnesic activity, and are useful as brain function-improving drugs. The compounds (a) and (b) are useful as an intermediate for said compounds (I). Futher, the compound (a) show diuretic or antiulcer activity, and are useful as a diuretic or antiulcer agent.

Abstract: The specification discloses the treatment of malaria through the use of tetrandrine and its derivatives.

Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.

Abstract: This invention relates to antitumor alkaloid compositions, a process of producing the compositions and a method for inhibiting tumors utilizing the compositions. More particularly, the compositions are antitumor alkaloids which are derived from marine organisms, i.e., the marine sponge Xestospongia, sp.

Abstract: This invention relates to antitumor alkaloid compositions, a process of producing the compositions and a method for inhibiting tumors utilizing the compositions. More particularly, the compositions are antitumor alkaloids which are derived from marine organisms, i.e., the marine sponge Amphimedon sp.