Abstract: The device allows the pain associated with the insertion of a needle of a syringe into the skin to be reduced. To do this, this device comprises a sleeve, which has a first rear portion to at least partially receive the syringe with the needle and a second front portion fitted with an end part, through which an opening passes for passage of the needle. A front face of the end part is intended to be applied with pressure against the skin of a person before insertion of the needle into the skin. This front face of the end part is arranged to receive an active substance for desensitizing the skin. The active substance can be applied to the skin at the instant the terminal part presses on the penetration site to desensitize the skin.

Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.

Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.

Abstract: The 1-aryl-2-aryloxyethane compounds of Formula 1 in which n and m are zero or equal to 1, provided that n+m=1, R1 and R2 in particular representing hydrogen atoms, R3 and R4 in particular representing hydrogen atoms, halogen atoms, hydroxy or alkoxy groups, and R5 in particular representing hydrogen atoms, hydroxy, alkyl, alkoxy, amino or nitro groups, in cosmetic compositions intended for anti-ageing and/or depigmenting and/or anti-inflammatory and/or wound-healing care.

Abstract: The present invention relates to use of inhibitors of Notch signalling pathway selected from the group consisting of 6-(4-Tert-Butylphenoxy)Pyridin-3-Amine (I3), its derivatives, in treating and/or preventing cancers.

Abstract: Benzonatate resinates of weak acid ion exchange resins having the same distribution of butyl 4-aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210. These resinates, in simulated gastrointestinal dissolution, release essentially the same distribution of butyl-4 aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210.

Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.

Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.

Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.

Abstract: Provided are new functionalized surfactants and methods of their preparation and use. The surfactants are compounds of formula I: wherein R1, R2, and R3 are as defined herein.

Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.

Abstract: Methods to generate doubled haploid plants and plant components using low mammalian toxicity chromosome doubling agents are disclosed. Chromosome doubling agents provide low mortality rates and higher chromosome doubling rate in plants.

Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. A compound of formula (I): and the salts and N-oxides thereof.

Abstract: The present invention provides methods for the design and identification of novel antimicrobial compounds, and provides antimicrobial compounds identified using these methods. These antimicrobial compounds inhibit the binding of a prokaryotic single-stranded DNA binding protein to a polypeptide that binds to the prokaryotic single-stranded DNA binding protein. In some examples, the prokaryotic single-stranded DNA binding protein is prokaryotic Exonuclease I. In one embodiment, the antimicrobial compound has the structure wherein Y is selected from the group consisting of CH2, O, and NH, R1 is selected from the group consisting of H, F, Cl, Br, and I, R2 is selected from the group consisting of H and CF3, R3 is selected from the group consisting of H and CO2H, R4 is selected from the group consisting of H and OH, and R5 is selected from the group consisting of H, alkoxy, and NO2.

Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.

Abstract: Oral dosage forms of benzonatate useful for anti-tussive and anti-tussive/combination applications.

Abstract: Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof.

Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: Stilbene compounds for the prevention and treatment of colon cancer or colon inflammation and methods of using same are provided.

Abstract: Activated polymeric bicine derivatives such as, as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Abstract: Suggested are agrochemical compositions, comprising (a) biocides, and (b) alkoxylation products of di- and/or oligosaccharide esters.

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: A novel polyoxyalkylene derivative represented by the following formula (1), wherein each symbol is as defined in the specification, which has a functional group capable of reacting with various physiologically active substances according to the object is provided.

Abstract: Agrochemical compositions comprising (a) one or more branched alkyl polyglycosides, and (b) one or more biocides are disclosed. The compositions display improved solubility in water, and reduced foam generation.

Abstract: Provided are new functionalized surfactants and methods of their preparation and use. The surfactants are compounds of formula I: wherein R1, R2, and R3 are as defined herein.

Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, mollus and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. A compound of formula (I): and the salts and N-oxides thereof.

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: The present application discloses a method of modifying a macromolecule, the method comprising the steps of (i) providing the macromolecule; (ii) providing a compound of the general formula (I): wherein N is a primary amino group protected with the protecting group P, wherein the protecting group involves both free valences of the primary amino group; m is an integer of 1-12 and n is an integer of 1-2000; R1 and R2 are independently selected from the group consisting of hydrogen and C1-4-alkyl; and X is a reactive group; and (iii) allowing the compound of the general formula (I) to react with the macromolecule so as to form grafts on the macromolecule. Compounds of the general formula (i) and a method for the preparation thereof are also disclosed.

Abstract: A control method against noxious organisms in a field of soybean or corn, which comprises applying one or more PPO-inhibiting compounds selected from the group consisting of flumioxazin, sulfentrazone, saflufenacil, oxyfluorfen and 3-(4-chloro-6-fluoro-2-trifluoromethylbenzimidazol-7-yl)-1-methyl-6-trifluoromethyl-2,4-(1H,3H)pyrimidinedione to soil or weeds in the field where soybean or corn seeds have been sown or where said seeds are to be sown, said seeds being treated with one or more compounds selected from the group consisting of neonicotinoid compounds, azole compounds, strobilurin compounds and metalaxyl compounds.

Abstract: Compounds of formula (I) are described for deterring vermin, wherein R is unbranched or branched C1-C15 alkyl, which is unsubstituted or substituted by halogen, cyano or nitro; R1 and R2 are unbranched or branched C1-C12 alkyl, preferably C1-C6 alkyl, which is unsubstituted or substituted by halogen, cyano or nitro; and X and Y, independently of one another, are a straightchain or branched alkylene bridge with 1 to 20 carbon atoms, preferably an alkylene bridge with 1 to 3 carbon atoms, which is unsubstituted or substituted by halogen, cyano or nitro. Furthermore, an essentially non-therapeutical process for deterring vermin is described, which is based on the usage of these compounds, as well as verminrepellent compositions containing these compounds as the active ingredient, and finally the use of these compounds for producing vermin-deterring compositions and their usage in deterring vermin from animals, humans and objects. New compounds within the scope of formula (I) are also described.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: A series of Z-stilbenes derivatives are disclosed, which have the structure as shown by formula 1. In the structure of formula 1, X is hydrogen, NHR, or nitro group, and R is hydrogen. Y and Z is independently hydrogen, halogen, C1-C10 alkyl, or C1-C10 alkoxyl. Furthermore, A is hydrogen, hydroxyl, or amino group. The compounds of the present invention have both aqueous solubility and anti-tumor activity. The Z-stilbenes derivatives of the present invention can further include a pharmaceutical carrier to form pharmaceutical compositions as potent anti-mitotic agents and anti-cancer agents.

Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

Abstract: Activated polymeric bicine derivatives such as, as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Abstract: Pharmaceutical compositions are provided containing a combination of benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof. Methods of using compositions comprising benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof, provide relief from cough, pulmonary congestion or both. The compositions and methods provide relief to opiate-sensitive individuals, in particular, as well as to infants and other pediatric patients.

Abstract: A series of Z-stilbenes derivatives are disclosed, which have the structure as shown by formula 1. In the structure of formula 1, X is hydrogen, NHR, or nitro group, and R is hydrogen. Y and Z is independently hydrogen, halogen, C1-C10 alkyl, or C1-C10 alkoxyl. Furthermore, A is hydrogen, hydroxyl, or amino group. The compounds of the present invention have both aqueous solubility and anti-tumor activity. The Z-stilbenes derivatives of the present invention can further include a pharmaceutical carrier to form pharmaceutical compositions as potent anti-mitotic agents and anti-cancer agents.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, X1 and X2 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: Materials and methods for treating certain cancers are described, preferably cancers that result from the up-regulation of the RAF-MEK-ERK pathway, and more preferably chronic myelogenous leukemia, and which cancer is preferably resistant to the inhibition of the Bcr-Abl tyrosine kinase, imatinib.

Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.

Abstract: The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: Activated polymeric bicine derivatives such as as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Abstract: The present invention relates to novel pharmaceutical aerosol formulations comprising: (A) salmeterol xinafoate in the form of particles coated by spray-drying with at least one surfactant in the absence of any other coating excipient, in suspension in (B) a liquefied propellant gas which is 1,1,1,2,3,3,3-heptafluoro-n-propane or 1,1,1,2-tetrafluoroethane and mixtures thereof for administration particularly by the pulmonary route and to a process for preparing these formulations. It also relates to novel particles suitable for use in such formulations.

Abstract: Activated polymeric bicine derivatives such as, as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Abstract: Polyacetals comprising a recurring units represented by a formula selected from the group consisting of formula (I) and (II): wherein A comprises at least one acetal group; B is selected from the group consisting of —CH—, —CH(CH3)—, CH2CH—, —CH2C(CH3)—, —CH(CH3)CH—, and —CHCH(CH3)CH(CH3)—; Z is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VU; V is a linker group; U is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, hexadecaamine dendrimer, enhancer, and targeting receptor; R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl; D is a linkage selected from the group consisting of carboxylic amide, carboxylic ester, urea, and urethane; and G is selected from the group consisting of C4 to C20 alkyl, C6-C10 aryl, and —(OCH2CH2)n—, where n is in the range of 1 to about 250, are useful in nucleic acid delivery applications.

Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.

Abstract: An antitumor combination comprising a stilbene derivative and an anticancer compound selected from the group consisting of taxanes, alkylating agents, antimetabolites, vinca alkaloids, platinum compounds, epidophylloptoxins, and antibiotics as the active ingredients is provided. Methods of using these pharmaceutical preparations for the treatment of solid carcinomas and the like are also provided.

Abstract: Biphenyl derivatives are disclosed for use in the treatment of androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, precocious puberty, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and premature male baldness. For example, some preferred compounds having the structure: are formulated together with pharmaceutically acceptable diluent or carrier for topical use in the treatment of acne, hirutism, seborrhea or androgenic alopecia, or for systemic use in the treatment of androgen-dependent prostate cancer.