Abstract: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.

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: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: The present invention relates to methods for modulating the inflammatory response of respiratory tract cells using an agent that increases ceramide levels in the cells of the respiratory tract.

Abstract: A family of peptides and peptidomimetic compounds useful as GHS analogs according to either formula (I) or (II) as depicted below: or a pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification.

Abstract: Compounds, methods, uses, compositions, kits and packages for the treatment of imbalance between bone resorption and bone formation, based on uses of 4-phenyl-2 propionamidotetralin (4-P-PDOT) and analogs, derivatives, prodrugs, precursors thereof, and salts thereof, are described.

Abstract: Short-chain 2- to 3-carbon alcohols are used as solvents for cooling agents in the preparation of topical therapeutic and cosmetic formulations. Some of these alcohols, especially ethanol, inhibit the ability of the cooling agent to activate its target receptor. In one embodiment of this invention, (R)-1,2-propanediol is used as an alcoholic solvent for the topical delivery of cooling agents to biological surfaces. This propanediol enantiomer has a minimum inhibitory effect on cooling with respect to standard 2- to 3-carbon alcoholic solvents, and functions to substantially protect the agent's cooling activity from inhibition when in the presence of a short-chain alcohol.

Abstract: Embodiments of the present invention are directed to articles of manufacture, spheres having a diameter of 50 to 500 nanometers which contain poorly soluble drugs and methods of making such spheres. Embodiments of the present invention have particular application for the following drug candidates and closely related poorly soluble derivatives of such candidates: (i) indole hydrazinecarbothioamide [NSC 73306]; (ii) fenretinide (4HPR) [NSC 374551]; (iii) safingol [NSC 714503]; (iv) 17-allylamino demethoxygeldanamycin (17-AAG) [NSC 330507]; and (v) an aminoflavone drug [NSC 686288].

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: Control or repellency of bed bugs by bringing the bed bugs into contact with a bed bug control formulation containing at least one compound selected from the group consisting of certain alkyl ketones and cyclic ketones wherein the total number of carbon atoms in the alkyl ketones and cyclic ketones is from 10 to 16 carbon atoms and method for achieving such control or repellency.

Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumors, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumors, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.

Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.

Abstract: Methods and compositions are provided for treating proliferative disorders, wherein the composition comprises at least one compound according to Formula I: wherein R1 is selected from the group consisting of —OH, —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and an anthracycline, e.g. doxorubicin, or a pharmaceutically acceptable salt thereof, or a platin, e.g. oxaliplatin, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are polar, hydrophilic stimulant prodrug compositions comprising at least one stimulant chemically attached to a polar hydrophilic ligand, a salt thereof, a derivative thereof, or a combination thereof. Also disclosed are non-standard amino acid conjugates of amphetamine. Methods of making and using the same are also disclosed.

Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.

Abstract: The present invention relates to a new medical use of fenretinide or bioactive derivatives thereof, particularly to the use of fenretinide or bioactive derivatives thereof in the preparation of a medicament for eliminating or killing tumor stem cells in a subject or for treating and/or preventing a tumor disease originating from tumor stem cells in a subject.

Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.

Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.

Abstract: Compounds that cause reversible night blindness may be used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods and compositions using such compounds and their derivatives to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions. Such compounds and their derivatives may be used as single agent therapy or in combination with other agents or therapies.

Abstract: Stable non-toxic pesticide composition having fungicidal and insecticidal properties including a pesticide that is nontoxic to mammals; one or more disinfectants; a vegetable oil; and one or more stabilizing agents. In one example, one or more stabilizing agents are selected and are present in an amount in combination with the selection and amount of a pesticide, one or more disinfectants, and a vegetable oil to provide the composition with stability upon application to a substrate effective to allow lethality against one or more target pests.

Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.

Abstract: The present invention has discovered that amide compounds represented by Formula I set forth below have unexpected and advantageous flavor enhancement and modification properties: wherein R and R? is independently selected from the group consisting of H and C1-C10 linear, branched, or cyclic alkyl, alkenyl, alkynyl or aromactic groups. Thus, the amide compounds of the present invention can be used to enhance or modify the flavor of orally consumable compositions, such as foodstuff, chewing gums, dental and oral hygiene products, and medicinal products.

Abstract: To provide a drug, quasi-drug, food or drink that can act as a gastric acid secretion suppressant or a potassium channel inhibitor by including a composition that can be safely used and can be inexpensively produced. Each of these products contains one or more cooling sensation compositions that are compounds providing cooling sensation in an amount sufficient for exhibiting the efficacy thereof in a living body to which the product is administered.

Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.

Abstract: Mutated PYR/PYL receptor polypeptides and methods of making and using mutated PYR/PYL receptor polypeptides are described.

Abstract: The invention provides uses and methods for reducing nephropathy in persons with diabetes mellitus (particularly Type 2 diabetes), in persons with metabolic syndrome, in persons with triglyceride levels over 215 mg/dL, and in persons with a cholesterol level over 200 mg/dL, by administering an inhibitor of soluble epoxide hydrolase (“sEH”). Optionally, a cis-epoxyeicosantrienoic acid (“EET”) can be administered with the sEH inhibitor. The invention further provides for using EETs in conjunction with one or more sEH inhibitors to reduce hypertension, and for compositions of EETs coated with a material insoluble in an acid of pH 3 but soluble in a solution with a pH of 7.4 or higher.

Abstract: Disclosed is the use of merocyanine derivatives of formula Q is hydrogen; C1-C22alkyl; —OH; —OR7; —NR7R8; or —N?R9; R1 is hydrogen; C1-C22alkyl; —OR7, —SR7; —NR7R8; C1-C22alkyl; C2-C12 alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C6-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C3-C12cycloheteroalkyl; C6-C10aryl; C1-C12alkoxy-C6-C10aryl; or C1-C9heteroaryl; R6 is hydrogen; C1-C22alkyl; C1-C22alkoxy; or COR7; R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(C

Abstract: The present invention relates to cis-1,2-substituted stilbene derivatives, or their pharmaceutically acceptable salts, glucosides or solvates, a pharmaceutical composition comprising the compound, and use of said compound for preparation of a drug for treatment and/or prevention of diabetes or improvement of diabetic complications.

Abstract: This invention relates to a group of compounds for repelling blood-feeding ectoparasitic arthropods, and a method of deterring their landing and feeding on animals including humans, by applying in one or more formulations compounds that incorporate one or more sulfide and one or more hydroxyl groups to the skin, clothing or environment of animals, including humans. A method of repelling and deterring landing and feeding by blood-feeding arthropods on an animal by applying in effective amount one or more compounds that incorporate alkyl sulfide and alcohol moieties, or alkyl sulfide and amide moieties, or alkyl sulfide and amide moieties to the skin, clothing or environment of an animal.

Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Abstract: Compositions for treating or preventing fat maldistribution or hyperlipidemia resulting from anti-retroviral treatment of HIV-1 infection are disclosed. The compositions contain a conjugated fatty acid or alcohol and at least one member selected from the group consisting of a thiol-containing compound and a bioavailable form of trivalent chromium. Methods of treating a subject suffering from HIV-associated fat maldistribution or hyperlipidemia by administering a composition that includes a conjugated fatty acid or conjugated fatty alcohol and at least one member selected from the group consisting of a thiol-containing compound and a bioavailable form of trivalent chromium are similarly provided.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(?X) group; n=1 or 2; X=O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.

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: An aerosol paint composition includes an alkyd resin; one or more solvents; an organoclay; an anti-settling wax; a dispersing agent; one or more pigments; a drying agent; an anti-skinning agent; a fragrance; and a fungicide.

Abstract: The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract: The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.

Abstract: Antimicrobial compositions which can be used wherever disinfecting compositions are needed, such as in a hospital, healthcare industry, workplace, recreational facility, home or similar environment. The antimicrobial compositions are particularly useful as a topical application for a substrate, such as skin and can be used as a hand sanitizer or pre-surgical scrub. The compositions comprise a synergistic combination of a simple aliphatic alcohol and an activity enhancing substance, wherein the composition provides, heretofore unexpected, persistent activity against a broad range of microorganisms, including gram-negative organisms, while moisturizing the skin.

Abstract: The invention broadly relates to the use of ?, ?-unsaturated fatty acids to inhibit the filamentous growth of fungi and yeasts and to a method for producing same. In particular the invention relates to the use of optionally substituted C8 to C15 ?, ?-unsaturated fatty acids or salts, esters or amides thereof for inhibiting or retarding the yeast-to-mycelium transition of organisms having a dimorphic life cycle.

Abstract: A medicament for preventive and/or therapeutic treatment of a physical dysfunction such as motor dysfunction caused by nerve damage resulting from an accident, cerebral crisis and the like, which comprises as an active ingredient a compound or a salt thereof represented by the following general formula (I): wherein R1 to R5 represents hydrogen atom, an alkyl group, or an alkyl-substituted silyl group, X represents —CONH— or —NHCO—, and A represents a carboxylic acid-substituted aromatic group which may be substituted or a tropolonyl group which may be substituted.

Abstract: The present invention provides a new pharmaceutical application of a 15,15-difluoroprostaglandin F2? derivative. As a result of intensive studies in order to find a new pharmaceutical application of a 15,15-difluoroprostaglandin F2? derivative, it was found that, in a European Phase III clinical trial for tafluprost, one of the 15,15-difluoroprostaglandin F2? derivatives, with patients with open-angle glaucoma or ocular hypertension, tafluprost has actions of growing eyelashes, making eyelashes thicker, and changing the color thereof, that is, has an effect of promoting the growth of hair (eyelashes). Therefore, a 15,15-difluoroprostaglandin F2? derivative is useful as a hair growth promoting agent, and is expected to be useful as an active ingredient of a preventive or therapeutic agent for a disease associated with hair such as alopecia and a hair care product or a hair cosmetic product for regrowing hair, growing hair, increasing hair density, nourishing hair, or the like.

Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-increasing retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) compounds selected from the groups consisting of (i) a non-18 carbon chain length L-threo-sphinganine(s) or pharmaceuticeutically acceptable salt thereof, (ii) glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor(s), and (iii) sphingomyelin or dihydrosphingomyelin synthase inhibitor(s). Preferred L-threo-sphinganines are of carbon chain length 17 carbons, 19 carbons and 20 carbons. A preferred glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingomyelin or dihydrosphingomyelin synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol.

Abstract: The invention relates to using neurotoxic substances which in particular are toxic to the axons and to the nociceptive nerve endings in the preparations of agents treating joint pains.

Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.

Abstract: Provided herein is a stable pharmaceutical product comprising a dry powder inhalation device, and a pharmaceutical composition that comprises R,R-Formoterol L-tartrate salt, in particular crystalline R,R-formoterol L-tartrate; and ciclesonide.

Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.

Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.