Abstract: Compositions and methods useful in the treatment of certain cancers. The methods include administering, to a patient receiving an antifolate anticancer agent, methoxyamine administered in an amount sufficient to enhance or increase the effect of the antifolate anticancer agent. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.

Abstract: Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.

Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.

Abstract: The present invention provides compositions comprising a gas and a gastrointestinal smooth muscle relaxing agent comprising ethyl nitrite in a therapeutically effective amount. The present invention also provides methods of relaxing gastrointestinal smooth muscle, alleviating contraction or spasm of gastrointestinal smooth muscle to facilitate a diagnostic medical procedure and treating or preventing a gastrointestinal disorder using the compositions of the invention.

Abstract: The invention provides methods for treating and preventing a neurodegenerative disease associated with aberrant protein aggregation by modulating the expression and/or activity of XBP-1, IRE-1 alpha, and/or EDEM. The present invention also pertains to methods for identifying compounds that modulate the expression and/or activity of XBP-1, 1RE-1 alpha, and/or EDEM. The present invention further provides methods for determining whether a subject is at risk of developing or has developed a neurodegenerative disease associated with aberrant protein aggregation.

Abstract: The present disclosure provides compositions including a first component including at least one phospholipid possessing at least one vinyl group, a second component including a furanone possessing vinyl and/or acrylate groups, and a third component including a hydroxamate. Compositions, medical devices, and coatings including copolymers and blends of the foregoing components are also provided.

Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris

Abstract: A pharmaceutical preparation containing the active substance glyceryl trinitrate having improved storage stability in a container. The improved storage stability is achieved by the addition of a proton-absorbing substance either as part of the preparation as placed into the container or applied to the surface of the preparation's storage container before the remaining components of the preparation are placed into the container. The preparation can preferably be filled into a plastic bottle having a spray pump.

Abstract: Methods for treating or reducing the risk of transmission of chlamydia to a recipient by topically applying a metalloprotease inhibitor to a site on the recipient which is likely to be exposed to Chlamydia. Topical compositions containing metalloprotease inhibitors are also disclosed for treating or reducing the risk of transmission of Chlamydia, as well as barrier contraceptive devices coated therewith.

Abstract: The present invention relates to physically stable oil dispersions. It also relates to a method for activating bentones that are designed for use with a low polarity organic systems. It also relates to physically stable oil dispersions comprising said activated bentone.

Abstract: Nitric oxide synthase deficiency causes diminished ryanodine receptor S-nitrosylation leading to increased diastolic calcium (Ca2+) and reduced intra sarcoplasmic reticulum calcium (Ca2+) content. Compositions for treatment of cardiac failure and cardiac disorders such as arrhythmias and sudden cardiac death are described.

Abstract: This invention generally relates to improvement of the body and skin appearance, for example enhancing the appearance of sagging, wrinkled, or cellulite-afflicted areas of the skin and body, through the local delivery of a nitric oxide donor, for example, using delivery vehicles such as lotions, creams, liquids, and/or transdermal patches. In some embodiments, a delivery vehicle containing a nitric oxide donor, for example, L-arginine (an important biological precursor) or its derivatives in a sufficient concentration to improve the appearance of a selected area of the body may be applied. In certain cases, one or more agents may also be included that aid in the transfer of the nitric oxide donor into the tissue, which may overcome the resistance to transfer into the skin. Non-limiting examples of suitable agents include agents able to create hostile biophysical environments, for instance, choline chloride, magnesium chloride, and/or sodium chloride.

Abstract: This invention is related to hydroxylamino derivatives of the following general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing the compounds and to pharmaceutical compositions containing them.

Abstract: This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.

Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.

Abstract: The present invention provides an oral care composition Comprising a nitric oxide releasing particle and an orally-acceptable carrier. The nitric oxide releasing particle comprises at least one nitric oxide donor. Another aspect of the present invention provides a device for oral care comprising a nitric oxide releasing particle, wherein the device is configured to expose a targeted site in an oral cavity of a subject to nitric oxide. The present invention also provides methods and uses of providing oral health benefits by using the oral care compositions or devices as described above.

Abstract: Antimycorbacterial compositions are disclosed comprising at least one hydroxamate or at least one hydroxamate and at least one hydroxylamine. The preferred ratio of hydroxamate to hydroxylamines is about 100:1 to about 1:1. A method for inhibiting mycobacterial growth is also disclosed comprising the step of administering the compositions of this invention to an animal including a human.

Abstract: The invention provides a compound of one of the formulae (A), (B), (C), (D), (E), (F) as herein defined, or a salt thereof, for use in the treatment of a condition associated with increased or decreased HIF levels or activity, or a condition in which an increase or decrease in HIF levels or activity may be beneficial.

Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.

Abstract: The present invention relates to the use of beta-naphthoquinone derivatives, and salts thereof, for the prevention and/or the treatment of glutamate cytotoxicity. It further relates to the use of beta-naphthoquinone derivatives, and salts thereof, for preventing and/or treating glutamate induced neurological disorders. Additionally, it concerns the use of beta-naphthoquinone derivatives, and salts thereof, for making drugs exerting an inhibitory effect on the release of glutamate.

Abstract: An object of the present invention is to provide an enhancing agent for effect of anticancer agent for achieving an excellent therapeutic effect on cancer. The enhancing agent for effect of anticancer agent according to the present invention which is a solving means therefor is characterized in that a nitric oxide donor is an effective ingredient. In accordance with the present invention, an excellent therapeutic effect is able to be achieved on non-small cell lung cancer which is still in such a state that no effective therapeutic method has been established yet for a progressive cancer which is not operable and is one of cancers where chemotherapy is most difficult to apply.

Abstract: A hair cosmetic which can impart, to hairs, flexibility, smoothness and oily feeling when the hairs are wetted and smoothness, softness and combing easiness after the hairs are dried are provided, the hair cosmetic comprising an amine represented by the formula (I): Formula (I) (wherein R1 represents a C8-40 alkyl group or alkenyl group or a group represented by the formula R5O-(AO)n—CmH2m—(R5 represents a C8-40 alkyl group or alkenyl group having 8 to 40 carbon atoms, A represents a C2-3 alkylene group, n denotes a number from 0 to 30 in average and m denotes an integer of 2 or 3), R2 represents a C1-5 alkylene group, R3 represents H, a C1-24 alkyl group, alkenyl group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, R4 represents H, a C1-5 alkyl group, alkylene group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, p denotes an integer from 1 to 3, q and r denote integers from 0 to 2 and p+q+r is equal to 3.

Abstract: Compositions and methods are disclosed for treating an illness that is caused or associated with cellular damage or dysfunction which is caused by excessive mitochondrial production of reaction oxygen species (ROS). Compositions which act as mitochondria-selective targeting agents using specific structural signaling features recognizable by cells as mitochondrial targeting sequences are discussed. A method for delivering these agents effectively into cells and mitochondria where they act as electron scavengers by way of certain targeting sequences is also disclosed. Mitochondria dysfunction and cell death by way of apoptosis is inhibited as a result of the ROS-scavenging activity, thereby increasing the survival rate of the patient. In a preferred embodiment, the compositions and methods may be administered therapeutically in the field to patients with profound hemorrhagic shock so that survival could be prolonged until it is feasible to obtain surgical control of the bleeding vessels.

Abstract: A hair cosmetic which can impart, to hairs, flexibility, smoothness and oily feeling when the hairs are wetted and smoothness, softness and combing easiness after the hairs are dried are provided, the hair cosmetic comprising an amine represented by the formula (I): (wherein R1 represents a C8-40 alkyl group or alkenyl group or a group represented by the formula R5O-(AO)n—CmH2m—(R5 represents a C8-40 alkyl group or alkenyl group having 8 to 40 carbon atoms, A represents a C2-3 alkylene group, n denotes a number from 0 to 30 in average and m denotes an integer of 2 or 3), R2 represents a C1-5 alkylene group, R3 represents H, a C1-24 alkyl group, alkenyl group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, R4 represents H, a C1-5 alkyl group, alkylene group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, p denotes an integer from 1 to 3, q and r denote integers from 0 to 2 and p+q+r is equal to 3.

Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.

Abstract: Methods for treating vascular conditions associated with localized imbalance in vascular tone, which are hypothesized to be largely due to elevated endothelin (ET) are provided. The methods involve administration of nitric oxide (NO), agents which are able to provide NO, such as NO donors, agents which activate guanyl cyclase, such as YC-1, or agents which prolong the actions of endogenous NO or cyclic guanosine monophosphate (cGMP; a 2nd messenger molecule), such as phosphodiesterase (PDE) inhibitors. According to the invention, such agents are administered in minimal doses or microdoses by any route known in the art, so as to provide dosages which are about one half to about one twentieth (½ to 1/20) of those known to induce vasodilation in “normal” circulations.

Abstract: To provide a novel compound which inhibits the generation of AGE and an AGE generation inhibitor containing the compound. A compound represented by the following formula or a pharmaceutically acceptable salt thereof, a medicinal composition containing the compound or such a salt thereof, and an additive composition containing the compound.

Abstract: The invention relates to methods and compositions for treating premature ejaculation in a male or prolonging intercourse comprising administering to the male an antidepressant via a route selected from the group consisting of mucosal administration (preferably nasal, buccal or rectal), administration to the lungs (preferably by inhalation), local administration to at least a part of the male genitalia (applied to the penis for example, in the form of a gel) and combinations thereof.

Abstract: A method of treating an autoimmune disease comprising administering to the subject a treatment effective amount of a histone hyperacetylating agent, or a pharmaceutically acceptable salt thereof.

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: N-acylethanolamines (NAEs) that can deliver an ethylene- or cytokinin-like effect to a plant, plant part or fungus are disclosed. Also disclosed are methods of using the NAEs.

Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.

Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.

Abstract: A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with these combinations. Also provided is wood treated by these combinations, and a method of treatment for composite wood.

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: Pulmonary disorders in which the GSNO pool or glutathione pool in the lung is depleted and where reactive oxygen species in lung are increased, are treated by delivering into the lung as a gas, agent causing repletion or increase of the GSNO pool or protection against toxicity and does so independently of reaction with oxygen. Agents include ethyl nitrite, NOCl, NOBr, NOF, NOCN, N2O3, HNO, and H2S. Optionally, N-acetylcysteine, ascorbate, H2S or HNO is administered in addition to other GSNO repleting agent to potentiate the effect of said agent.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: Desensitization of receptors that control disease is prevented by inhibiting G-protein receptor kinases. This has applicability, e.g., for patients with heart failure or on a left ventricular heart device or a heart pump after surgery or about to undergo surgery and at high risk for a cardiac event or on an opiate or addicted to opiate or with cystic fibrosis or rheumatoid arthritis.

Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.

Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.

Abstract: Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic compound comprising a nitrate ester, or a pharmaceutically acceptable salt or ester thereof.

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by ornithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: A method and device are disclosed which prevents the decay and deterioration of wooden objects caused by pests by using a controlled release device. This controlled release device utilizes polymers which incorporate pesticides. In the disclosed method, the controlled release device is placed in contact with the wood of the wooden object. The pesticide is gradually released from the device and absorbed into the wood structure. The pesticide absorbed by the wood creates a barrier or an exclusion zone to penetration by inserts. The controlled release device maintains a minimal effective level of pesticide in the barrier or exclusion zone for a predetermined period of time.

Abstract: Methods for treating CMV and CMV-related diseases are provided that use compounds having the formula: wherein the subscripts m and n are each independently integers from 1 to 2; and the R groups are as defined in the specification.

Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, an

Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.

Abstract: The invention relates to compounds of the general formula (I), as defined, and to pharmaceutical compositions containing them. The compounds of formula (I) are inhibitors of various lipid-related enzymes. They can be used in reducing accumulation of sphingolipids and thus in the treatment of lipid storage diseases. The compounds of formula (I) can also be used for the treatment of cancerous diseases and for killing of wild type and drug-resistant cancer cells.

Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.