Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: A scleral lens solution comprising an aqueous mixture that includes sodium, potassium, calcium and magnesium cations and a pH in a range from about 6.5 to about 8.7.

Abstract: The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: A floral fragrance composition for use as a replacement for 3-(4-tertbutylphenyl)-2-methylpropanal (LILIAL®) that is a primary perfuming ingredient composition that includes a first perfuming ingredient of (2,5-dimethyl-2,3-dihydro-IH-inden-2-yl) methanol (LILYFLORE®) in an amount of 5 to 25% by weight; a second perfuming ingredient of a dimethyl-5-indanyl propanal compound in an amount of 0.2 to 10% by weight; and one or more secondary perfuming ingredients including at least one of 3-methyl-5-phenylpentanal, decanal, octanal, cuminic aldehyde, cuminic alcohol, carvone, tetrahydro-2-isobutyl-4-methyl-4(2H)-pyranol, or cis-7-P-menthanol.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: An object is to provide a novel therapeutic drug for adult T-cell leukemia having an ATL cell specific antitumor effect. The therapeutic drug for adult T-cell leukemia according to the invention is characterized by containing a compound represented by the formula I or a prodrug thereof, wherein R1 is H, OH, an alkoxy group, an acyl group, or a thioacyl group, R2 is an acyl group, a thioacyl group, CONR7R8, or CSNR7R8 (R7 and R8 being each independently H, an alkyl group containing 1 to 3 carbon atoms, or a phenyl group), or R1 and R2 together may form a ring, X1 and X2 may be the same or different and are each —CR3R4—, —SiR3R4— or oxygen, and R3 and R4 may be the same or different and are each an alkyl group containing 1 to 6 carbon atoms.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.

Abstract: An ecologically compatible anti-microbial-adhesion agent is described, which is particularly suitable for use in anti-fouling paints, preferably for boats, characterized in that it comprises a compound selected from eugenol, vanillin, benzaldehyde substituted with one or two substituents selected from the groups —OH (hydroxy) and —OCH3 (methoxy), or any combination thereof. An anti-fouling paint is also described, particularly for boats, comprising the anti-microbial-adhesion agent mentioned above and other components selected from conventional biocides, solvents, resins, pigments, charges and fillings, and combinations thereof.

Abstract: The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.

Abstract: The present invention provides a biomarker for selecting a patient for treatment with gossypol, wherein the biomarker comprises an elevated expression level of c-Myc, Mcl-1, or combination thereof, relative to the normal expression level of c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for targeting patients for treatment with gossypol, wherein the patient has a disease, condition, or disorder that overexpresses c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for treating or ameliorating a disease, condition, or disorder in a patient comprising determining the expression level of c-Myc, Mcl-1, or combination thereof in the patient and administering gossypol to the patient. In certain embodiments of the invention, the disease is cancer, and the cancer cells show elevated expression levels of c-Myc compared to non-cancerous cells.

Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.

Abstract: Provided are a triterpene derivative represented by a general formula (I), a pharmaceutically acceptable salt thereof, and an agent for preventing or treating chronic hepatitis C comprising the triterpene derivative or the salt as an active ingredient: [in the formula (I), R1 represents a carboxyl group, a hydroxymethyl group, —CH2OSO3H, or and R2 represents —OR3 or —O— (CH2) m-OR4, where R3 represents a benzyl group which may be substituted with a hydroxymethyl group, a dimethylaminomethyl group, a phenylaminomethyl group, a morpholinomethyl group, a carboxyl group, or a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a hydroxy C1-6 alkyl group, R4 represents a phenyl group which may be substituted with a carboxyl group, and m represents an integer of 1 to 3, with the proviso that a case where R1 is —CH2OH, and R3 is a C1-6 alkyl group, a C2-6 alkenyl group, or a benzyl group is excluded].

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: An object is to provide a novel therapeutic drug for adult T-cell leukemia having an ATL cell specific antitumor effect. The therapeutic drug for adult T-cell leukemia according to the invention is characterized by containing a compound represented by the formula I or a prodrug thereof, wherein R1 is H, OH, an alkoxy group, an acyl group, or a thioacyl group, R2 is an acyl group, a thioacyl group, CONR7R8, or CSNR7R8 (R7 and R8 being each independently H, an alkyl group containing 1 to 3 carbon atoms, or a phenyl group), or R1 and R2 together may form a ring, X1 and X2 may be the same or different and are each —CR3R4—, —SiR3R4— or oxygen, and R3 and R4 may be the same or different and are each an alkyl group containing 1 to 6 carbon atoms.

Abstract: The disclosure describes an animal model for simulating cardiac arrhythmia. Methods of discovering new anti-arrhythmia drugs using the model are described. Novel anti-arrhythmia agents are provided, as are pharmaceutical compositions made from the agents. Methods of inhibiting spontaneous mechanical activity in myocardially-derived biological systems, and methods of treating and preventing cardiac arrhythmia based on novel anti-arrhythmia agents are described. Kits for performing the above methods are also described.

Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.

Abstract: The present invention relates to use of Bcl inhibitors for the prevention of fibroproliferation resulting in the growth of visible or disfiguring scar tissue on human skin, including without limitation keloids and hypertrophic scars. In particular, the present invention relates to the new use of small molecule inhibitors of the Bcl-2/Bcl-XL family of anti-apoptotic proteins for the treatment of cutaneous wounds, burns and abrasions during the healing phase.

Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.

Abstract: Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.

Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulation angiotensin activity to stimulate or activate the formation of new nerve cells.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: The present invention relates to compounds of general formula (1): in which, independently of each other, R1 and R2 represent: —OH, or —CH2—O—R3, or —CH2—S—R3, or R3, R4, R5 and R6 representing, independently of each other, —H or a carbon-containing group with 1 to 10 carbon atoms, saturated or unsaturated, optionally substituted with one or more heteroatomic groups. The invention also relates to pharmaceutical compositions containing these compounds, and their uses, in particular in the context of the treatment of cancer.

Abstract: The present invention relates to new compounds of formula (I) and to their use as medicaments. Preferably, the said compounds are used in the preparation of a medicament or food supplement intended for the treatment and/or prevention of ailments or pathologies ensuing from a disorder of the reuptake of the following neurotransmitters: dopamine, serotonin and/or noradrenaline.

Abstract: Phenylboronic acid and water soluble derivatives thereof and related boronic acid compounds are used for treating fungal and bacterial infections.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.

Abstract: The present invention relates to the use of a Eucalyptus for preparation of a drug or a dietary supplement intended for treatment and/or prevention of affections or pathologies caused by neuromediator recapture disorder. The present invention also relates to a new enriched extract of Eucalyptus characterized in that it contains at least one compound having the formula (I) or any one of its diastereoisomers in which R1 forms a C?CH2 substituent with the carbon to which it is joined, a formula (II) substituent and R2 which represents an isobutyl, ?-isobutyl or ?-isobutyl substituent; and the method of preparation thereof.

Abstract: A compound comprising a Schiffs base of an aldehydic musk aromachemical with a substantially nonvolatile, odorless amine, wherein the imine moiety of said Schiffs base compound is stable against oxidation to a carboxyl group or a mixture of said compounds; said Schiffs base compound being biodegradable over time to said aldehydic musk and said nonvolatile, odorless amine; as well as compositions, products, preparations or articles having improved aroma, fragrance or odor characteristics containing as active ingredient such compound or mixture of compounds; the aldehydic musks themselves, and methods for the preparation of the Schiff bases and methods of imparting fragrance characteristics to substrates.

Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g.

Abstract: The present invention relates to a therapeutic agent or prophylactic agent for a disease accompanying an abnormality in an amount of insulin or insulin response, an insulin-mimetic action agent, a food, beverage, or feed, an agent for enhancement of glucose uptake into a cell, and an agent for inducing differentiation into an adipocyte, each comprising as an effective ingredient at least one compound selected from the group consisting of specified compounds having an insulin-mimetic action, derivatives thereof, and pharmacologically acceptable salts thereof.

Abstract: The present invention relates to a composition for the prevention and the treatment of cardiovascular disease containing extracts of T. nucifera or abietane diterpenoid compound or terpenoid compound isolated from the same as an effective ingredient. T. nucifera extracts or abietane diterpenoid compound or terpenoid compound isolated from the same of the present invention not only shows excel lent anti-oxidative activity to LDL but also effectively inhibits ACAT activity. Further, T. nucifera extracts of the present invention reduce blood LDL cholesterol and total cholesterol. Therefore, the composition of the present invention can be effectively used for the prevention and the treatment of cardiovascular diseases including hyperlipidemia and atherosclerosis caused by the LDL oxidation and the synthesis and accumulation of cholesteryl ester.

Abstract: 6-methoxy gossypol and 6,6?-dimethoxy gossypol were isolated from cottonseeds. Bioactivities of these two gossypol derivatives and gossypol were investigated regarding their antioxidant activities, DNA damage prevention ability, anti-cancer, and anti-trypanosomal activities. Both methoxy compounds had nearly equivalent bioactivities, but gossypol showed greater bioactivities than either methoxy derivative on free radical scavenging activity, reducing power, and DNA damage prevention ability. Gossypol and its methoxy derivatives inhibited growth of three cancer cell lines, i.e., SiHa (cervical cancer), MCF-7 (breast cancer) and Caco-2 (colon cancer) cells, in a dose dependent manner. These three compounds also significantly inhibited growth of trypanosome T. brucei, the cause of African Sleeping Sickness, which affects thousands in western and central Africa.

Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.

Abstract: The invention relates to novel aldolase-inhibiting compounds that can be advantageously used as medicaments (in therapeutic doses), especially for treating certain cancers, due to the inhibition efficacy thereof. An inventive compound corresponds to general formula (I) wherein the aldehyde group (—CHO) and the phenol group (—OH) are linked to two carbon atoms adjacent to the same aromatic chain, i.e., the first aromatic chain, and R is a phosphate group or a phosphate group mimetic linked to a carbon atom of the second aromatic chain.

Abstract: This invention relates to compositions comprising co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract: This invention relates to compositions comprising co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract: The topical administration of statins for the treatment of bone disorders is disclosed.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention includes the use of pelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP 1 activity. This invention also provides novel terpene compounds capable of modulating SHIP 1 activity and methods of synthesis thereof.

Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g.

Abstract: A method of treating osteoporosis in warm-blooded animals comprising administering to warm-blooded animals in need thereof an effective amount to treat osteoporosis of a compound selected from the group consisting of a compound of the formula: wherein the substituents are defined as in the Specification.

Abstract: Low concentrations of gossypol and related phyllophage toxins from cotton improve the effectiveness of insecticidal agents against social insects, including cockroaches, and particularly termites and ants. Levels of gossypol and other cotton phyllophage toxins which are sufficiently low as to be non-biocidal to social insects alone, will significantly increase the control efficacy of other insecticidal agents. Consequently, use of these low levels of these cotton phyllophage toxins allows the levels of insecticidal agents necessary for effectively controlling the insects to be significantly reduced relative to applications without cotton phyllophage toxins. Furthermore, insecticidal agents which are normally ineffective for control of social insects when used alone, may be effective when used in conjunction with the cotton phyllophage toxins.

Abstract: This invention also provides a method to inhibit neovascularization in tissue by delivering to the cell or tissue an effective amount of gossypol, or a pharmaceutically acceptable salt, derivative or prodrug thereof. Also provided herein is a method for treating a disease associated with hyproliferation of endothelial cells and/or neovascularization by administering to a subject an effective amount of gossypol, or a pharmaceutically acceptable salt, derivative or prodrug thereof. Kits to treat patients are provided as well.

Abstract: A triterpene derivative useful for the treatment of hepatic disorders is disclosed. This compound comprises as an active ingredient a triterpene derivative represented by the following formula (I) or a salt thereof: wherein R1 represents a hydroxyl group, arylmethyloxy, lower alkoxy, or lower alkanoyloxy, R2 represents lower alkyl, lower alkenyl, —CH2OR5, formyl, —COOR6, or —CH2N(R7)R8, or R1 and R2 may combine with each other to form —O—C(R9)R10—O—CH2—, R3 and R4, which may be the same or different represent a hydrogen atom, a hydroxyl group, lower alkyl, lower alkenyl, aryl, hydroxymethyl, —N(R11)R12, formyl, —COOR6, or —OR13, or R3 and R4 may combine with each other to form oxo, hydroxyimino, or alkylidene and X represents O, CH2, or NH.

Abstract: A method for treating cancer in a human, which comprises administering to the human subject an anti-cancer effective amount of a compound selected from gossypol, gossypol acetic acid, gossypolone, metabolites thereof, or physiologically acceptable salts thereof. Also included is a method for treating cancer in a human which comprises administering to the human subject an anti-cancer effective amount of any of the compounds listed above in combination with an anti-cancer effective amount of other conventional chemotherapeutic agents. Finally, the invention also encompasses a pharmaceutical composition comprising an anti-cancer effective amount of gossypol, gossypol acetic acid, or gossypolone, and an anti-cancer effective amount of a conventional chemotherapeutic agent, or combinations of the latter.