Abstract: The invention provides certain 5 and/or 8 substituted benzopyran, pyranopyridine or tetrahydroquinaline compounds having C.sub.4 -amide substituent and processes for making them. The compounds described are useful in treating and/or preventing certain disorders.

Abstract: A cosmetic or pharmaceutical composition including, as the active ingredient, a compound of general formula (I), wherein 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 selected from --H, --OH, --OCH.sub.3 and a glucosyl radical, or a pharmaceutically acceptable salt thereof.

Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.

Abstract: A method of promoting lean body mass in an individual is disclosed, comprising administering to the individual a lean body mass promoting effective amount of forskohlin. A method of treating a mood disorder is also disclosed, comprising administering to a patient in need thereof a mood disorder treating effective amount of forskohlin. Compositions suitable for promoting lean body mass and/or treating a mood disorder are also disclosed, the composition comprising about 1 to about 40% forskohlin in combination with at least one physiologically acceptable carrier or excipient. A method of preparing a forskohlin composition from a forskohlin extract of Coleus Forskoli plant is further disclosed, as well as a forskohlin composition prepared by the method.

Abstract: A phototoxic insecticidal composition includes at least one photoactive dye, an attractant bait composition and/or feeding stimulant and at least one adjuvant, whereby the adjuvant interacts with the photoactive dye and insect membranes to alter the toxicity of the composition once ingested by the insect. More specifically, the composition is directed to killing the Mexican fruit fly.

Abstract: The present invention relates to novel pharmaceutical use of forskolin derivatives represented by the general formula: ##STR1## wherein R.sup.1, R.sup.2 and Ac are as defined later ##STR2## (wherein R.sup.3 and R.sup.4 are each hydrogen or lower alkyl group, or R.sup.3 and R.sup.4 may be combined to represent lower alkylene group which may have oxygen or nitrogen atom in the linking chain, and n is an integer of 1 to 5); R.sup.2 represents hydrocarbon group having 2 to 3 carbon atoms; and Ac represents acetyl group.The above-mentioned forskolin derivative or a physiologically acceptable salt thereof can be used as a platelet aggregation inhibiting or controlling agent, spasmolytic agent, therapeutic agent for skin ulcer, peripheral circulation improving agent for limbs and differentiation inducing and promoting agent.

Abstract: A broad class of photosensitive compounds having enhanced in vivo target tissue selectivity and versatility in photodynamic therapy. Many furocoumarin compounds, such as psoralens, exhibit cytostatic activity when photoactivated but exhibit little in vivo specificity for selectively accumulating in any particular target tissue such as atheromatous plaques. Reactive Oxygen Producing Photosensitizers ("ROPPs") are photoactivatable compounds having an affinity for hyperproliferating cells (such as atheromatous plaque cells), which when photoactivated, produce cytotoxic reaction products. The photoactivity of a ROPP, such as a porphyrin, may be reduced by metalating the porphyrin while the selective affinity of the metalized ROPP for hyperproliferating tissue remains substantially unchanged.

Abstract: A method of administering photodynamic therapy begins with administering to an animal an effective amount of a photosensitizing agent which is less than about one half of the usual clinical dose for the photosensitizing agent. Then, following a post injection interval which is less about one quarter of the usual post injection interval, an effective dose of light which is less than about one half of the usual clinical dose of light used in conjunction with the photosensitizing agent is administered to the animal.

Abstract: A redox, hydrogen-acceptor compound, having utility in treating inflammation, is a 1,4-dioxonaphthalene or 1,4-dilminon aphthalene having either a 2,3-double bond, in which cast there are 2 and 3-substituents, or a 2,3-single bond. Examples of such compounds are menadione epoxide and water-soluble derivatives or menadione such as menadione bisulphite.

Abstract: Aglucone isoflavone enriched vegetable protein extract and isolate and processes for producing and recovering are disclosed. The aglucone isoflavone extract is made by extracting a vegetable protein material comprising glucone isoflavones with an aqueous extractant having a pH above about the isoelectric point of the protein material to produce an aqueous extract, and reacting the glucone isoflavones with a sufficient amount of beta-glucosidase enzyme or esterase enzyme for a time period, temperature, and pH sufficient to convert at least a majority of the glucone isoflavones in the extract to aglucone isoflavones and thereby produce the aglucone isoflavone enriched extract. The aglucone isoflavone enriched isolates are produced by adjusting the pH of the reacted extract to about the isoelectric point of the vegetable protein material to precipitate the protein material, and separating the protein material to produce an aglucone enriched protein isolate.

Abstract: Disclosed herein is a method of treating amyotrophic lateral sclerosis with topiramate and related compounds.

Abstract: This application relates to the use of topiramate and related sulfonamides for the treatment of manic-depressive bipolar disorder.

Abstract: Compounds of general Formula I in which the substituents of R.sub.1 -R.sub.7 are hydrogen, hydroxy group, C.sub.1-6 alkyl group, C.sub.1-6 alkoxy group, or epoxypropoxy, but at the most, six of the substituents can simultaneously be hydrogen, methoxy group, or hydroxy group, or epoxypropoxy group for activity against hepatoma. There are also described processes for the preparation of the novel compounds and useful intermediates. Substitute benzophenones are described.

Abstract: A method destroys or impairs target cells that have selectively accumulated a photosensitizing agent. The target cells are in the bloodstream of an intact animal, which bloodstream and animal further contain non-target cells. Radiation is applied transcutaneously to at least a portion of the intact animal at an intensity effective to impair or destroy selectively the target cells and to leave non-target cells relatively unimpaired. Target cells include leukemia cells, virus-containing cells, parasite-containing cells, and microorganisms such as bacteria, parasites and free viruses.

Abstract: The present invention is directed to compounds that are analogs of the natural product suksdorfin. Compounds of the present invention include those having Formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined herein. The invention is also directed to methods of making these compounds, pharmaceutical compositions including these compounds and methods of using the compounds to inhibit retroviral infections in cells and tissues of animals. A method for stereoselectively preparing compounds within the scope of the invention by catalytic asymmetric dihydroxylation is also disclosed.

Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations exhibiting insulin resistent non-impaired glucose tolerance (IRNIGT) in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed.

Abstract: A method of administering photodynamic therapy begins with administering to an animal an effective amount of a photosensitizing agent which is less than about one half of the usual clinical dose for the photosensitizing agent. Then, following a post injection interval which is less about one quarter of the usual post injection interval, an effective dose of light which is less than about one half of the usual clinical dose of light used in conjunction with the photosensitizing agent is administered to the animal.

Abstract: The primary etiology of antibiotic-associated diarrhea (which may lead to pseudomembranous colitis) has been recognized as Clostridium difficile. It is believed that the indigenous microflora of a healthy individual suppresses the normally present C. difficile. However, when the indigenous microflora are disrupted (e.g., during antibiotic treatment) overgrowth of C. difficile may occur causing diarrhea and colitis. Treatment of C. difficile with antibiotics has proven effective, but many times relapse occurs. The present invention involves a non-antibiotic approach to the treatment and/or prevention of C. difficile--associated diseases. A therapeutically effective amount of an indigestible oligosaccharide inhibits the infection of mammals by C. difficile when administered enterally.

Abstract: A phototoxic insecticidal composition includes at least one photoactive dye present in the amount of between 0.025%-4.0% of the composition, an attractant compound and/or feeding stimulant and at least one adjuvant, whereby the adjuvant interacts with the photoactive dye and insect membranes to alter the toxicity of the composition once ingested by the insect.

Abstract: A method is provided for preventing or reducing the risk of onset of a cardiovascular event by administering an HMG CoA reductase inhibitor such as pravastatin, to a patient which has one or more risk factors for a coronary and/or cerebrovascular event such as hypercholesterolemia.

Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagen-like substances or the biosynthesis of Cl.sub.q.

Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarius are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.

Abstract: The present invention contemplates methods of decontaminating human fluids prior to processing in the clinical laboratory. The techniques handle large volumes of human serum without impairing the testing results. Novel compounds for photodecontaminating biological material are also contemplated which are compatible with clinical testing, in that they do not interfere with serum analytes.

Abstract: Disclosed are reconstituted lyophilized formulations for the treatment of mammalian tumors comprising a thioxanthenone antitumor agent in combination with mannitol or sucrose as a stabilizer in a lactate buffer.

Abstract: A composition for increasing synthesis of melanin in a human melanocyte thereby enhancing pigmentation of the human skin. Use of this composition promotes tanning of the human skin and increases photoprotection from ultraviolet radiation. An organ culture system comprising viable human foreskin samples which may be used to test the effects of agents on human skin, including pigmentation enhancers on human skin.

Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.

Abstract: The present invention relates to the use of compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moieties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms, in the reduction of coagulation time in mammals.

Abstract: The present invention relates to organic molecules capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such molecules to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such molecules to treat various disease states including diabetes mellitus.

Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.

Abstract: Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moieties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms.The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I.Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.

Abstract: This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of phospholipase A.sub.2. This invention also provides a series of compounds which are useful as inhibitors of phospholipases A.sub.2, especially cytosolic phospholipase A.sub.2.

Abstract: The present invention provides a method for inhibiting endometriosis comprising administering to a woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is hydrogen or methyl;R.sup.1 and R.sup.2 each are methyl or ethy, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group; andX is bromo, chloro, fluoro, or hydrogen; or a pharmaceutically acceptable salt thereof.

Abstract: There are provided novel compounds of the formulae I and II: ##STR1## and their physiologically acceptable salts. The compounds according to the present invention and their physiologically acceptable salts exhibit an antiallergic activity and are useful for treating allergic diseases.

Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarins are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.

Abstract: The novel compounds 3,6-Disubstituted xanthen-9-one of formula I ##STR1## in which R is a C.sub.3 -C.sub.8 linear, branched or cyclic alkyl and R.sub.1 is linear, branched C.sub.1 -C.sub.8 alkyl or cyclic C.sub.3 -C.sub.8 alkyl or --OR in which R is as defined hereinabove, exhibit bone resorption inhibiting activity. Pharmaceutical compositions are described.

Abstract: A method for inhibiting smooth muscle cell proliferation in an injured blood vessel includes the steps of administering a photoactivatable psoralen to a patient in an amount to achieve local arterial tissue levels of psoralen suitable for light-dependent inhibition of smooth muscle cell growth, and delivering radiation in the visible wavelength range to the injured region of the blood vessel at a level sufficient for photoactivation of the psoralen. The psoralen is preferably 8-methoxypsoralen and can be delivered systemically or locally. The method of the invention can be used for preventing restenosis in a blood vessel following transluminal angioplasty. Both the psoralen and the visible light can be delivered with a laser balloon catheter having a porous balloon. The method of the invention may also be used for inhibiting proliferation of other undesired cell types in a patient's body.

Abstract: This invention relates to certain hydroxy derivatives of 3,4-dihydro-2,5,7,8-tetraalkyl-2H-1-benzopyran-2-carboxylic acids and the lactones thereof, to the processes and intermediates useful for their preparation and to their use as free radical scavengers useful in the treatment of tissue damage implicated with free oxygen radicals.

Abstract: The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.

Abstract: The present invention provides the fumarate salt of 4-(diethyl-3-(1-methyloctyl)-7,8,9,10-tetrahydro-6,6,9-trimethyl-6H-dibenz o[b,d]pyran-1-ol, 4-diethyl-amino)butyric acid ester, i.e. the compound having the following structure (I): ##STR1## and methods of treatment, particularly treatment of glaucoma, and pharmaceutical compositions that utilize or comprise the fumarate salt (I).

Abstract: A method destroys or impairs target cells that have selectively accumulated a photosensitizing agent. The target cells are in the bloodstream of an intact animal, which bloodstream and animal further contain non-target cells. Radiation is applied transcutaneously to at least a portion of the intact animal at an intensity effective to impair or destroy selectively the target cells and to leave non-target cells relatively unimpaired. Target cells include leukemia cells, virus-containing cells, parasite-containing cells, and microorganisms such as bacteria, parasites and free viruses.

Abstract: This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of phospholipase A.sub.2. This invention also provides a series of compounds which are useful as inhibitors of phospholipases A.sub.2, especially cytosolic phospholipase A.sub.2.

Abstract: Synthetic media formulations are disclosed for use with blood preparations intended for in vivo use, including synthetic media formulations to be employed in conjunction with the photodecontamination of platelets using 8-methoxypsoralen.

Abstract: The invention relates to a process for the solubilization in a non-ionic surface-action agent of from between about 0.001 mg and about 1 mg of forskolin, to the pharmaceutical compositions based on such solubilized forskolin and to the use of these in the treatment of various diseases and disorders and maladies in mammals, including humans. Forskolin is 7-beta-acetoxy-8,13-epoxy-1-alpha,6-beta,9-alpha-trihydroxylabd-14-en-11-o ne.

Abstract: The occurrence of restenosis following percutaneous transluminal coronary angioplasty is prevented or inhibited using a photopheresis treatment method, In accordance with the photopheresis treatment method, a photoactive compound such as 8-methoxypsoralen is administered to the patient's blood or affected tissue, or some fraction thereof, in vitro or in vivo using conventional administration routes. A portion of the patient's blood or affected tissue is then treated (preferably, extracorporeally) using photopheresis, which comprises subjecting the blood or affected tissue to electromagnetic radiation in a wavelength suitable for activating the photoactive compound, such as ultraviolet light, preferably long wavelength ultraviolet light in the wavelength range of 320 to 400 nm, commonly called UVA light. The treated blood or affected tissue, or a fraction thereof, is returned to the patient (in the case of extracorporeal photopheresis) or remains in the patient (following in vivo photopheresis).

Abstract: A composition for the treatment or prevention of osteoporosis, is disclosed, which comprises:(a) 75 to 200 parts of one or more phytoestrogen compounds;(b) 0 to 100 parts of dried licorice root extract;(c) 300 to 600 parts of calcium contained in a biologically acceptable calcium salt;(d) 70 to 280 parts of magnesium contained in a biologically acceptable magnesium salt;(e) 4 to 25 parts of zinc contained in a biologically acceptable zinc salt;(f) 5 to 20 parts of beta-carotene;(g) 0.005 to 0.010 parts of Vitamin D as cholecalciferol; and(h) 6 to 12 parts of Vitamin E,in admixture with a biologically acceptable inert carrier. The new compositions are administered to a mammalian subject as either a pharmaceutical or as a dietary supplement.

Abstract: Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moleties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms.The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I.Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.

Abstract: A compound of the formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, a lower alkyl group, a hydroxy group or a lower alkoxy group,R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.11 are as defined in the description.Medicaments.

Abstract: A pharmaceutical formulation comprising 5-methoxy psoralen, which is useful in the treatment of psoriasis and other skin disorders, is disclosed herein. 5-methoxy psoralen may be synthesized from phloroglucinol by a five step process which is also disclosed.

Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.

Abstract: This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are variables.