Abstract: Novel crystalline forms of anti Pneumocystis carinii compound (2-[4-(4-Chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone) commonly known as Atovaquone and methods for producing the same is disclosed herein. This also provides pharmaceutical compositions comprising the said polymorphs of Atovaquone and method of treating Pneumocystis carinii pneumonia, the method comprising administering to a warm blooded animal an effective amount of a product-by-process composition of matter comprising polymorphic forms of Atovaquone.

Abstract: A combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support, wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed.

Abstract: The present invention provides a system for delivery of an enteric coated active agent generally resistant to disintegration in an neutral environment having one or more active agents encapsulated by a polymer coating formed by chemical vapor deposition of one or more monomers on the one or more active agents to form a chemical vapor deposition polymer coating that controls the release of the one or more active agents in the gastrointestinal tract.

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 ?-hydroxyketones and ?-alkoxyketones of formula (I), to their use as estrogen receptor modulators, and to methods for their preparation.

Abstract: Methods and compositions are described whereby poorly water-soluble beneficial agents such as vitamins and co-factors are formulated into self-emulsifying formulas (SEF) and optionally sorbing the SEF into pores of porous solid particulates, or preparing supersaturated solutions (SSS) and sorbing the SSS into pores of porous solid particulates. These formulations are useful as dosage forms with oral availability.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries.

Abstract: Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating diabetic retinopathy or drusen formation in age-related macular degeneration. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid other than genistein, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.

Abstract: A composition for alleviating symptoms associated with neurotoxicity. The composition may comprise compounds for preventing glutamate mediated neurotoxicity. The composition may include one or more of the following elements: at least one glutamate antagonist, at least one cAMP stimulating agent, at least one antioxidant, vitamin B12, at least one transporter and at least one surfactant. The composition may be used in methods for alleviating tinnitus, Ménière's Disease and/or hearing loss.

Abstract: The invention provides methods and compositions for treating and preventing a skin rash secondary to anti-epidermal growth factor receptor (EGFR) therapy, where the method comprises applying a vitamin K analog or a phosphatase inhibitor to the skin.

Abstract: The present invention relates to two novel and stable crystalline forms of atovaquone, to processes for their preparation and to pharmaceutical compositions comprising them. The present invention also provides crystalline particles of atovaquone having a specific surface area of from about 0.7 m2/g to about 4 m2/g, methods for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles. The present invention further provides an improved and commercially viable process for preparation of atovaquone substantially free of its undesired isomeric impurity, namely cis-2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone.

Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.

Abstract: The therapeutic ultrasound gel is a composition that lubricates the abdomen for ultrasound scanning, that enhances the transmission of sound waves during ultrasound diagnostic imaging, and that has beneficial therapeutic effects in preventing the formation of stretch marks. The composition contains effective amounts of aloe vera (Aloe barbadensis), glycerin, and various agents for preventing the formation of stretch marks, with the balance being sufficient water to adjust the consistency of the composition. The composition may also be formulated for home use, chiefly by the addition of vitamin D3 or, alternatively, vitamin K. Either formulation may contain additional excipients, including surfactants, emulsifiers, humectants, stabilizers, thickeners, pH balancers, preservatives, colorants, and scent, if desired.

Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.

Abstract: The present invention relates to an oily suspension of atovaquone comprising atovaquone particles and a combination of surfactants having HLB more than 10.

Abstract: A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.

Abstract: Novel perfluoroketone compounds of formula [I] and [Ia] are described. Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and/or inflammatory conditions, such as demyelinating (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).

Abstract: A pharmaceutical and nutraceutical product is provided comprising vitamin K2 or a compound within the vitamin K2 class of compounds, optionally and preferably in combination with one or more polyunsaturated fatty acids, either in purified form or as a marine oil (i.e. fish and/or krill oil). Also provided is the use of vitamin K2 or a compound within the vitamin K2 class of compounds, preferably in combination with one or more polyunsaturated fatty acids, either in purified form or as a marine oil, in the treatment or prophylaxis of disorders related to bone, cartilage and the cardiovascular system. Preferred compounds within the vitamin K2 class of compounds are MK-7, MK-8, MK-9 and MK-10, in particular MK-7 or MK-9. The marine oil is preferably krill oil or fish oil.

Abstract: Medications which are derived by combining one or more doses of the agonist, vitamin K, with doses of one or more selected vitamin K antagonists such as the R-isomer of warfarin, the R-isomer of phenprocoumon, or the racemic phenprocoumon are useful in anticoagulant therapy. These products are designed to minimize or circumvent the detrimental impact of newly identified genetic-based variables that currently significantly complicate the therapeutic response of individual patients to anticoagulation therapy.

Abstract: The present invention relates to immediate release pharmaceutical compositions for oral administration comprising micronized atovaquone particles and at least one drug, wherein about 90% of the atovaquone particles have a volume diameter between about 4 ?m to about 8 ?m; and having a uniform release profile after a storage for at least three months at 40° C. and 75% relative humidity.

Abstract: The present invention relates to methods and compositions comprising naphthoquinones such as 2,3-dimethylnaphthalene-1,4-dione, for the use of treating, regulating or preventing a skin condition characterized by oxidative stress or a degenerative process. Methods of preventing, lightening or reducing the appearance of visible and/or tactile discontinuities of the skin resulting from skin pigmentation or skin aging are also disclosed.

Abstract: Agents that inhibit or prevent restenosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on cell proliferation, thrombosis, tissue modeling, and inflammation. Treatment for restenosis is provided using compositions of the invention.

Abstract: The use of phanquinone for the manufacture of a pharmaceutical composition for the prevention or the treatment of Alzheimer's disease is disclosed. Also methods of treatment or prevention of Alzheimer's disease are disclosed.

Abstract: This invention relates to compositions containing a compound of formula (I) shown below: Each variable is defined in the specification. Also disclosed are methods of using these compositions to treat acne, psoriasis, and infective skin ulcer.

Abstract: The present disclosure relates to novel cocrystals and novel methods for cocrystallization. In particular, the disclosure includes cocrystals comprising a salt of an active agent, such as a chloride salt of an active pharmaceutical ingredient. The present disclosure also relates to methods of preparing cocrystals and methods for screening for solid state phases.

Abstract: The inventors have found that vitamin K3 and vitamin K5 which may be used in pharmaceuticals and foods or ACNQ, DHNA, or the like which can stimulate the growth of bifidobacteria can inhibit degranulation of basophil-like cells, exhibit a potent degranulation-inhibiting effect, and are useful anti-allergic agents or foods. The present invention provides an anti-allergic agent containing, as an active ingredient, one or more species selected from among 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-dihydroxy-2-naphthoic acid, 1,4-naphthoquinone, 4-amino-2-methyl-1-naphthol, 2-methyl-1,4-naphthoquinone, 2-amino-3-chloro-1,4-naphthoquinone, and a salt thereof.

Abstract: The present invention relates to novel combinations suitable for the treatment or amelioration of pain of various genesis or aetiology, which comprise, as active ingredients, at least one cannabinoid receptor binding compound, in particular a cannabinoid receptor binding naphthalene derivative, and at least one opioid, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract: The presently-disclosed subject matter provides compositions and methods for treating a cancer by providing a composition comprising a biocompatible polymeric matrix incorporating an effective amount of a phytochemical agent, a combination of phytochemical agents, or a phytochemical agent and a chemotherapeutic agent. Further, provided is a device for uterine cervical insertion for local delivery.

Abstract: The invention provides methods and compositions tor treating and preventing a skin rash secondary to anti-epidermal growth factor receptor (BGKR) therapy, where the method comprises applying a vitamin K analog or a phosphatase inhibitor to the skin.

Abstract: Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.

Abstract: The invention provides methods and compositions for treating and preventing a skin rash secondary to anti-epidermal growth factor receptor (EGFR) therapy, where the method comprises applying a vitamin K analog or a phosphatase inhibitor to the skin.

Abstract: Provided is a substance which is a safer and more commonly-consumed food ingredient that increase the testosterone level. The testosterone enhancer of the invention comprises vitamin K as an active ingredient. The vitamin is preferably menaquinone-4 and/or menaquinone-7. This enhancer is useful as pharmaceutical agents, supplements, health foods or functional foods for the prevention, amelioration and/or treatment of a condition or disease induced by the decreased testosterone level.

Abstract: A pharmaceutical formulation and its use. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimethylsulfoxide (“DMSO”); a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone. The pharmaceutical formulation is used to effectively stimulate bone regeneration and increase osteoblastic activity in a patient.

Abstract: Two-phase preparation for temporally gradual administration comprising a) a phase (A) comprising water soluble vitamins and/or the corresponding provitamins, wherein phase (A) does not contain liposoluble vitamins or provitamins corresponding to liposoluble vitamins, b) a phase (B) comprising vitamins and/or the corresponding provitamins, wherein the quantity of liposoluble vitamin compounds is larger than the quantity of water soluble vitamin compounds.

Abstract: The present invention provides a process for the preparation of atovaquone exhibiting characteristic peaks (expressed in degrees 2?±0.2°?) at approximately one or more of the positions: about 7.0, 9.7, 14.2, 14.8, 17.0, 19.2, 20.4, 22.1, 22.7, 26.9 and 28.7, which comprises: (a) providing a solution comprising atovaquone in an aprotic polar solvent; (b) adding a suitable antisolvent to precipitate atovaquone; and (c) isolating the precipitate.

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 selected from the group consisting of H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, and NHSO2X, wherein X is selected from the group consisting of an alkyl, a substituted alkyl, an aryl, a substituted aryl, an alkylaryl, and a heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

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 provides to methods of preventing, treating or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder utilizing combinatorial therapy. In particular, the present invention provides methods of preventing, treating, or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder comprising administering to a subject in need thereof one or more integrin ?V?3 antagonists and at least one other prophylactic or therapeutic agent. The present invention also provides compositions and articles of manufacture for use in preventing, treating or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder.

Abstract: The invention provides pharmaceutical compositions and methods of treating immunological disorders. The invention also provides pharmaceutical compositions and methods of inducing eosinophil apoptosis, and methods for treating eosinophil-associated disorders comprising inducing eosinophil apoptosis in an individual in need thereof.

Abstract: Disclosed are neuroblastoma tumor-initiating cell inhibiting compositions comprising chemical entities capable of affecting neuroblastoma tumor-initiating cells. Pharmaceutical preparations that include these chemical entities are also provided for the treatment of neuroblastoma. These pharmaceutical preparations are suitable for the treatment of humans, and are particularly suited for the treatment of children of 12 years of age or younger having neuroblastoma. The compositions and pharmaceutical preparations posses reduced normal cell cytotoxicity. The compositions and pharmaceutical preparations may be used alone or together with other conventional neuroblastoma preparations as part of a clinical regimen in the treatment and management of neuroblastoma.

Abstract: A benzoquinone or hydroquinone for use in the topical treatment of a condition which is caused, exacerbated or transmitted by bacterial, in particular staphylococcal or propionibacterial, activity. The condition may be a skin or skin structure condition such as acne. The invention also provides the use of a benzo- or hydroquinone in the manufacture of a medicament for the treatment of such a condition.

Abstract: The present invention relates to the surprising discovery that agents that increase intracellular accumulation of NADH+H+ enhance the anti-cancer effects of angiogenesis inhibitors. Furthermore, treatment of a mammal with a combination of at least one angiogenesis inhibitor and at least one agent that enhances intracellular accumulation of NADH+H+ allows for the enhanced treatment and/or prevention of angiogenic diseases and disorders.

Abstract: The present invention provides an antiprotozoal agent, which is particularly preferred as an antileishmanial agent. Specifically, the present invention is directed to an antiprotozoal agent comprising, as an active ingredient, a compound of Formula (I): wherein R is —H or acyl, a salt thereof, or solvate thereof.

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 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 atovaquone particles having d90 value of about 4-15 ?m. It further relates to a pharmaceutical composition comprising said particles.

Abstract: The present invention is directed to compounds having the structure Formula (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

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.