Abstract: This invention relates to a method of treating cancer, and particularly a method including the steps of administering to a mammal in need of such treatment, either simultaneously or sequentially, (i) a compound selected from a paclitaxel and docetaxel, and (ii) a compound of the formula 1

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: Nucleic acid-imaging compositions and methods for noninvasive imaging of a nucleic acid introduced into somatic tissues of an animal or human are disclosed. The noninvasive imaging enables quantitative assessment of the biodistribution of the introduced nucleic acid. The disclosed imaging compounds include a base-binding moiety, a phosphate-binding moiety, and a metal-binding moiety. A chelated metal is non-invasively detected for imaging by radioactivity or magnetic resonance.

Abstract: First-pass effective substances derived from citrus.

Abstract: 5′-substituted, 4′,5′-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. Also described are 2-substituted mercurimethyl-2-3-dihydro-benzofurans of forumla (7): Also reported are versatile direct syntheses through a hitherto unknown compounds such as 3-R-4,8-dimethyl-4′,5′-dihydro-5′-bromomethylpsoralen or a 3-R-4,8-dimethyl-4′, 5′-dihydro-5′-iodomethylpsoralen to prepare a structurally diverse array of partially reduced psoralens and benzofurans. The presence of a permanent ammonium charge in these psoralens precludes membrane passage and the mono-unsaturation precludes the cross-linking of nuclear DNA, thereby minimizing the mutagenic/carcinogenic side effects long associated with psoralen-derived therapies.

Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect.

Abstract: A non-steroidal compound suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. The compound can have the general formula A wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of O, S, NH, a substituted N, CH2 or a substituted C.

Abstract: Compositions and methods for the prevention and treatment of neoplastic diseases are described. Individuals at a high risk of developing or having neoplasia undergoing conventional therapies may be treated with an effective dose of triterpene derivatives in limonoids, polyphenolic flavonoid compounds, tocotrienols or a combination of these agents.

Abstract: The present invention relates to methods for preventing or treating skin disorders using flavonoid compounds. The present invention also relates to methods for regulating skin condition.

Abstract: The present invention involves a combination therapy of administering a cholesterol reducing agent, such as a 3-hydroxy-3-methylglutaryl coenzyme a (HMG-CoA) reductase inhibitor and a platelet aggregation inhibitor for treating, preventing or reducing the risk of developing cardiovascular and cerebrovascular events and disorders in a mammal.

Abstract: Anticonvulsant derivatives useful in treating essential tremor are disclosed.

Abstract: A method is provided for preserving tissues during removal, storage and implantation into a subject by enhancing cell viability in a population of graft cells during the transplantation procedure. The method includes selecting an effective dose of a polycylic phenolic compound in a physiologically acceptable formulation and exposing at least the population of graft cells to the formulation containing the compound within a time that is effectively proximate to the transplantation procedure so as to confer cytoprotection on the population of graft cells.

Abstract: Methods and compositions for treating pathogens in material are described, including methods of decontaminating human fluids prior to processing in the clinical laboratory and methods for decontaminating blood products prior to in vivo use. The techniques handle large volumes of human serum without impairing the testing results.

Abstract: The invention relates to 4′-substituted-4′,5′-dihydropsoralen compounds of formula(V): In the formula R is hydrogen, a halogen, CN or an acyl group; T is a halogen, CN, a carboalkoxy group NR1R2, or (N+R1R2R3)X−, R1 and R2 are independently a C1-C6 alkyl, or R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring, or when T is (N+R1R2R3)X−, R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring or heterocyclic aromatic ring; R3 is hydrogen, a C1-C12 alkyl, or, when R1 and R2 together with the nitrogen form a heterocyclic aromatic ring, R3 is a double bond within the heterocyclic aromatic ring; X− is a halide. In another embodiment, the invention relates to processes for preparing 4′-substituted-4′,5′-dihydropsoralen compounds described above.

Abstract: Viral and bacterial contaminants present in biological solutions are inactivated by mixing one of a novel class of photosensitizer with said solution and irradiating the mixture.

Abstract: The present invention provides a composition and methods for inhibiting cytochrome P450 enzyme activity and in particular, inhibiting the activity of the cytochrome P450 3A sub-family of enzymes, specifically, CYP3A4. The present invention provides 6',7'-dihydroxybergamottin, a furanocoumarin, as the compound primarily responsible for the inhibitory effects of grapefruit juice on cytochrome P450 enzyme activity. The present invention also provides a novel synthesis scheme for 6',7'-dihydroxybergamottin.

Abstract: The present invention provides novel assay methods for identifying compounds that may have both estrogen agonist and antagonist properties. In particular, the assay use cells comprising promoters having an AP1 site linked to a reporter gene. Compounds capable of inducing or blocking expression of the reporter gene can thus be identified. The compounds may be further tested for the ability to modulate the standard estrogen response, as well.

Abstract: A novel ophthalmic preparation containing menthol together with sodium cromoglycate and an antihistaminic is provided, which alleviates the unpleasant irritating eye-ache induced by sodium cromoglycate at the time of instillation and enhances the prompt antipruritic effect of the antihistaminic to strongly suppress itchiness of eyes immediately after instillation.

Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.

Abstract: The invention provides a method to inhibit the formation of neovasculature while maintaining viability of the underlying tissue by subjecting a subject in which angiogenesis is to be inhibited to sublethal photodynamic therapy. The invention also provides a model for assessing sublethal PDT protocols to inhibit angiogenesis in particular target tissues.

Abstract: The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow.

Abstract: The composition is characterized in that it contains an extract of Chrysanthellum indicum with low concentration comprising 0.0001% to 0.05% of equivalent dry extract of Chrysanthellum indicum. It is both applicable to natural ageing and to phenomena of accidental ageing of the skin caused by the numerous assaults to which the skin is subjected daily.

Abstract: Diabroticite insects, in particular the corn rootworm, are major pests of corn as well as a variety of other agricultural crops. The invention describes an aqueous composition which is effective as an insecticide for the control of Diabroticite insects and contains a photoactive xanthene dye, such as phloxine B, as a toxicant and a cucurbitacin-containing feeding stimulant. Additives such as a starch thickener and an adherent may also be included in the composition.

Abstract: The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which is not substituted, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which has substituent(s), or a group represented by --Y--R.sup.3 (provided that when R.sup.2 is a hydrogen atom, R.sup.1 is not a methyl group or an acetyl group; when R.sup.2 is an acetyl group, R.sup.1 is not a methyl group), an antifungal agent containing it as an active ingredient and an antifungal composition containing it and an azole type antifungal agent.

Abstract: A sulphamate compound suitable for use as an inhibitor of both oestrone sulphatase activity and aromatase activity. The compound can have the general formula (II) wherein F represents a phenolic ring structure (the first ring structure), J represents the third ring structure; I represents a phenolic ring structure (the second ring structure), G is an optional double bond, H is a link joining the second ring structure to the third ring structure, and Y represents a suitable second group; wherein any one of ring structures F, J and I has bound thereto a sulphamate group.

Abstract: A compound selected from those of formula (I): ##STR1## in which A, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the Specification, and pharmaceutical compositions containing the same, which are useful for treating a mammal afflicted with a disorder of the melatoninergic system.

Abstract: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for inhibiting the first pass effect.

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: The present invention provides an antifeedant and a contact insecticide using the components contained in Cyperaceae species. In particular, the present invention provides an insect antifeedant and a contact insecticide comprising as an active ingredient at least one compound selected from the group consisting of scabequinone, remirol, cyperaquinone and the derivatives thereof.

Abstract: Novel iridoid derivatives represented by general formula (I): and a vascularization inhibitor having for its active ingredient said derivative are disclosed. This vascularization inhibitor has remarkable vascularization inhibitory effects unaccompanied by serious adverse side effects, which is useful for the treatment and prevention of various diseases accompanied by abnormal acceleration of vascularization.

Abstract: Aglucone isoflavone enriched vegetable protein extract and isolate and process 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: This invention relates to benzofuran/pyran derivatives of a new tricyclic amide compound, their composition and method of use for treating disorders of the melatoninergic system.

Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.

Abstract: A method of treating inflammatory disorders of the bowel and inflammatory disorders of the urinary bladder are disclosed. A method of modulating the function of monocytes is also disclosed. The method involves the treatment of a patient's blood with a photoactivatable compound followed by ultraviolet light-activation of the photoactivatable compound. The blood treated as such is returned to the patient in a process known as extracorporeal photopheresis.

Abstract: The present invention offers a safe and effective drug for heart diseases and a safe and effective method for treating heart diseases such as ischemic heart disease and cardiac arrhythmia. The method comprises administering a pathologically effective amount of a benzopyran derivative expressed by the following general formula (I): ##STR1## wherein R.sup.1 is an alkyl group or an alkenyl group, R.sup.2 is a hydrogen atom, an alkyl group, an alkyl group having at least one hydroxyl group, an alkenyl group, an acyl group or a glycosyl group; or physiologically acceptable salts thereof.

Abstract: Diabroticite insects, in particular the corn rootworm, are major pests of corn as well as a variety of other agricultural crops. The invention describes an aqueous composition which is effective as an insectide for the control of Diabroticite insects and contains a photoactive xanthene dye, such as phloxine B, as a toxicant and a cucurbitacin-containing feeding stimulant. Additives such as a starch thickener and an adherent may also be included in the composition.

Abstract: The invention relates to topically applied pharmaceutical compositions containing 5-methoxypsoralen in a concentration of 60 ppm to 100 ppm, and more particularly 65 to 95 ppm, and preferably 75 ppm, in a pharmaceutically acceptable oleaginous formula, as well as the use of these compositions in the treatment of psoriasis.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: Methods of using phytoestrogens, in particular, isoflavones in the prevention and treatment of endometriosis and related disease conditions in females. One method comprises administering a therapeutically effective dosage of a phytoestrogen to females with endometriosis, females having symptoms related to endometriosis, or to females at risk of developing or suffering recurrence of endometriosis. In another method, at least one phytoestrogen may be administered singly or in combination with at least one hormonal therapeutic agent such as GnRH analogs, androgens, progestins, estrogens or any combination thereof. The therapeutically effective dosage of the phytoestrogen or the combination therapeutic ranges between about 25 and about 250 mg/day.

Abstract: Disclosed is how to make and to use a genistin-enriched fraction from soy meal. The fraction is prepared by acetone extraction of soy meal, followed by ice-water precipitation. The resulting composition is useful as a pharmaceutical or a dietary supplement for the treatment or prevention of cancer, cardiovascular disease, osteoporosis, or adverse symptoms of menopause in a human.

Abstract: The present invention concerns photochemical labelling reagents comprising a digoxigenin derivative and a furocoumarin derivative bound via a spacer. The labelling reagent can be used in gene diagnostic.

Abstract: An antifungal composition, containing a synergistic mixture, containing the compound of the formula (I): ##STR1## wherein R is acetyl or lower alkyl; or a pharmaceutically acceptable salt thereof; and an azole antifungal agent selected from the group consisting of an imidazole compound and a triazole compound, as an active ingredient.

Abstract: The invention provides a method of treating or preventing a fungal infection comprising administering to a plant having a fungal infection a composition comprising an effective amount of a compound of formula I, wherein said compound is the following or an agriculturally acceptable salt of the following: ##STR1## The invention further provides such compounds and related methods.

Abstract: The present invention relates to the use of forskolin and of the extracts containing it for the treatment of alcohol addiction.

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.

Abstract: An aglucone isoflavone enriched vegetable protein whey, whey protein material, high genistein material, high daidzein material, and aglucone isoflavone material are provided, as well as a process for producing the same from a vegetable protein whey. Isoflavone conjugates in a vegetable protein whey are converted to isoflavone glucosides by treating the whey at a temperature and a pH for a period of time sufficient to effect the conversion. The isoflavone glucosides are converted to aglucone isoflavones by enzymatic reaction to produce an aglucone isoflavone enriched vegetable protein whey. Aglucone isoflavone whey protein material is recovered from the aglucone isoflavone enriched vegetable protein whey. A high genistein content material, a high daidzein content material, and an aglucone isoflavone material are produced from an alcohol extract of the aglucone isoflavone whey protein material.

Abstract: The present invention provides novel cyclopropachromen-carboxylic acid derivatives having an antagonistic activity against metabotropic glutamate receptors and its pharmaceutically acceptable salts. Cyclopropachromen-carboxylic acid derivatives and its pharmaceutically acceptable salts represented by the following general formula (1): ##STR1## ?wherein A denotes an oxygen atom, hydroxyimino group, an alkyloxyimino group having 1 to 5 carbon atoms, or the group .dbd.N--O--(CH.sub.2).sub.n -NR.sup.1 R.sup.2 (where n represents an integer of 2 to 8, and each of R.sup.1 and R.sup.2 independently represents a hydrogen atom or alkyl group having 1 to 5 carbon atoms, respectively); B denotes the group --COOR.sup.3 (where R.sup.3 represents a hydrogen atom or alkyl group having 1 to 5 carbon atoms) or the group --CONR.sup.4 R.sup.5 (where R.sup.4 and R.sup.5 independently represent a hydrogen atom, alkyl group having 1 to 5 carbon atoms, alkenyl group having 2 to 5 carbon atoms and an aminoalkyl group.

Abstract: The invention relates to pyran-chromenone compounds, their synthesis and anti-HIV activity. Methods of synthesis are disclosed; the compounds have activity against reverse transcriptase. Biological compositions containing the compounds and method of treating patients are also disclosed.

Abstract: A compound selected from those of formula (I): ##STR1## in which A, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description, and a medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.