Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: Acetaminophen conjugates are provided, which have an acetaminophen moiety covalently linked to a second moiety. The conjugates provided may have one or more advantageous properties, including increased water solubility as compared to acetaminophen, reduced toxicity profile as compared to acetaminophen and an altered pharmacokinetic profile. Formulations comprising the conjugates are also provided, as are methods of using the conjugates and kits comprising the conjugates.

Abstract: The present invention relates to a transdermal therapeutic system for administering an active substance through the skin, comprising: a) a cover layer, b) a reservoir present on the cover layer, comprising a polymer matrix comprising the active substance, c) an adhesive layer present on the reservoir comprising a contact adhesive, and d) a removable layer present on the adhesive layer, the active substance being rivastigmine, a physiologically compatible salt, hydrate, solvate or derivative thereof, characterized in that the polymer matrix of the reservoir comprises neither hydroxyl groups nor carboxyl groups.

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.

Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The present invention relates to a transdermal therapeutic system for administering an active substance through the skin, comprising: a) a cover layer, b) a reservoir present on the cover layer, comprising a polymer matrix comprising the active substance, c) an adhesive layer present on the reservoir comprising a contact adhesive, and d) a removable layer present on the adhesive layer, the active substance being rivastigmine, a physiologically compatible salt, hydrate, solvate or derivative thereof, characterized in that the polymer matrix of the reservoir comprises neither hydroxyl groups nor carboxyl groups.

Abstract: Methods and compositions for treating underactive bladder and/or symptoms thereof are disclosed, wherein the composition including an effective amount of a therapeutic agent and a pharmaceutically acceptable lipid vehicle is locally administered to the bladder, thereby treating the underactive bladder and/or symptoms thereof.

Abstract: The invention relates to a transdermal or transmucosal non-occlusive, semi-solid pharmaceutical formulation that includes at least one systemically active agent that acts on the Central Nervous System (CNS) of a mammal; and a permeation enhancing solvent system present in an amount sufficient to solubilize the at least one active ingredient.

Abstract: A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.

Abstract: The present invention provides transdermal therapeutic systems for dispensing a pharmaceutical product, in particular a pharmaceutical product with a low tendency to spontaneously crystallize. The matrix layer or at least one of the matrix layers in said systems contains a silicone hot-melt adhesive, a pharmaceutical product, and particles made of crosslinked polyvinylpyrrolidone. The invention also relates to a method for producing said transdermal therapeutic systems.

Abstract: The invention provides a method of diagnosing Alzheimer's Disease in a subject, by determining the level of at least one miRNA in a sample derived from the subject, wherein a change in the level of the at least one miRNA relative to a suitable control is indicative of Alzheimer's Disease in the subject. Methods for monitoring the course of Alzheimer's Disease, methods of treating a subject having Alzheimer's Disease, and kits for diagnosing Alzheimer's Disease are also provided.

Abstract: It has been found that phenyl carbamates, in particular Rivastigmine, can be formulated as a stable TTS by using a monolayer poly alkyl (meth)acrylates, wherein the poly alkyl (meth)acrylates are substantially free of free carboxylate groups.

Abstract: A transdermal patch for the treatment of Alzheimer's disease includes: a backing, a rivastigmine-containing layer, a pressure-sensitive adhesive layer, and a release liner. In the transdermal patch, the rivastigmine-containing layer contains rivastigmine and an alkyl (meth)acrylate resin, the pressure-sensitive adhesive layer is composed of an acrylic pressure-sensitive adhesive containing a (meth)acrylic acid ester having a hydroxy group, and neither the rivastigmine-containing layer nor the pressure-sensitive adhesive layer contains an anti-oxidizing agent.

Abstract: The present invention provides a transdermal drug delivery system comprising rivastigmine or its pharmaceutically acceptable salt and method of making the same.

Abstract: Described are transdermal drug delivery systems for the transdermal administration of tertiary amine drugs, such as rivastigmine, fentanyl or rotigotine, comprising a polymer matrix comprising a free base form of the drug and at least one carboxyl group-containing compound. In some embodiments, the systems include a rate-controlling membrane and a skin-contacting face adhesive apart from the polymer matrix.

Abstract: Acetaminophen conjugates are provided, which have an acetaminophen moiety covalently linked to a second moiety. The conjugates provided may have one or more advantageous properties, including increased water solubility as compared to acetaminophen, reduced toxicity profile as compared to acetaminophen and an altered pharmacokinetic profile. Formulations comprising the conjugates are also provided, as are methods of using the conjugates and kits comprising the conjugates.

Abstract: The present invention relates to an injectable pharmaceutical composition with gelling properties containing: -an active principle; a hydrophobic and bio-compatible organic liquid; and an organogelling substance, the molecules of which have the capacity to bind together via bonds of low energy, wherein the organogelling substance is chosen among L-tyrosine derivatives responding to the following formula (I) wherein: R1 is an alkyl group containing 1 to 3 carbon atoms, linear or branched; and R2 is a hydrophobic group chosen among aliphatic saturated or unsaturated fatty chains or aryl or arylalkyl groups. Its use as a vector for the release of active principles, as well as its process of preparation.

Abstract: Provided is an adhesive patch which has excellent rivastigmine storage stability and an increased skin permeability of rivastigmine to such an extent that the amount of percutaneous absorption required for treating Alzheimer's disease is obtained. This adhesive patch includes a backing and an adhesive layer containing rivastigmine and an alkyl(meth)acrylate-based copolymer that does not contain any acrylic monomer component having a carboxy group, the adhesive layer being laid on one side of and integrated with the backing.

Abstract: The present invention relates to a rivastigmine-containing patch having improved storage stability and proper release property.

Abstract: The present invention relates to the use of compounds of the invention for treatment and/or prevention of fatigue, including fatigue associated with diseases or treatments.

Abstract: The present invention relates to Transdermal Therapeutic Systems having a silicone adhesive layer, to Transdermal Therapeutic Systems providing specific plasma concentrations, to their manufacture and use.

Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.

Abstract: The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.

Abstract: The present invention is directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a salicylanilide or salicylanilide derivative, disclosed herein, alone or in combination with one or more other active or excipient pharmaceutical substances. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein, further comprised of one or more active or excipient pharmaceutical substances.

Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: Disclosed is a percutaneous absorption preparation for treatment of dementia that comprises rivastigmine or its pharmaceutically acceptable salt as an active ingredient, a styrene-isoprene-styrene block copolymer, a tackifier resin, and a plasticizer, which preparation contains a small amount of rivastigmine but allows a sufficient amount of the active ingredient penetrated into the skin to achieve an effective treatment of dementia.

Abstract: The present invention relates to Transdermal Therapeutic Systems having a silicone adhesive layer, to Transdermal Therapeutic Systems providing specific plasma concentrations, to their manufacture and use.

Abstract: The present invention relates to a transdermal therapeutic system for administering an active substance through the skin, comprising: a) a cover layer, b) a reservoir present on the cover layer, comprising a polymer matrix comprising the active substance, c) an adhesive layer present on the reservoir comprising a contact adhesive, and d) a removable layer present on the adhesive layer, the active substance being rivastigmine, a physiologically compatible salt, hydrate, solvate or derivative thereof, characterized in that the polymer matrix of the reservoir comprises neither hydroxyl groups nor carboxyl groups.

Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: The invention concerns a transdermal therapeutic system with a carbamate cholinesterase inhibitor for the treatment of mild to moderate Alzheimer's disease dementia and/or Parkinson's disease dementia.

Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).

Abstract: A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.

Abstract: The present invention relates to the cosmetic, dermatological or pharmaceutical (therapeutic) use of compounds of formula (I) or a cosmetically acceptable salt of a compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that a 3 to 8 membered ring is formed, for the lightening of skin and/or hair. The invention further relates to compositions and cosmetic, dermatological or pharmaceutical preparations (compositions) comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.

Abstract: A stable transdermal adhesive composition comprising: an adhesive comprising a washed polymerization reaction product of at least two ethylenically unsaturated monomers; and at least one pharmaceutically active compound which is susceptible to oxidative degradation; wherein the at least two ethylenically unsaturated monomers, if present in the adhesive as unreacted monomers, are present at a level of less than 200 ppm of total unreacted monomer, based upon the total weight of the adhesive, methods of making the composition, a transdermal drug delivery device using the composition, methods of making the device, and methods of delivery the pharmaceutically active compound are provided.

Abstract: The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and/or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

Abstract: Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).

Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.

Abstract: The invention discloses particulate complexes composed of chitosan, poly-glutamic acid, and at least one bioactive agent, wherein equal moles of the positively charged chitosan and the negatively charged poly-glutamic acid substrate form an electrostatic network enabling improved loading the bioactive agent.

Abstract: Amorphous, polymorphic, and solvated forms of 17-amino geldanamycin are disclosed. These compounds are particularly useful for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and inhibiting Heat Shock Protein 90 (“Hsp90”).

Abstract: Disclosed is a pharmaceutical composition containing rivastigmine. Specifically, disclosed is a transepidermal drug delivery system including a rivastigmine-containing drug layer and a supporter adhered to one surface of the drug layer to support the drug layer, wherein the drug layer contains 10 to 40 parts by weight of a rubber, 20 to 80 parts by weight of a rosin ester resin and 0.1 to 10 parts by weight of an acrylic adhesive and the drug layer has a thickness of 40 ?m to 100 ?m.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: The present invention is directed to triclosan derivatives and nanoparticles comprising said derivatives together with an organic or an inorganic carrier. The present invention is also directed to uses of the triclosan nanoparticles for preventing or inhibiting bacterial growth.

Abstract: The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.

Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.

Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.

Abstract: The present invention relates to a compound of the general formula (I) where: X?S, SO or SO2; and one of the radicals R1 and R2 is a hydrogen atom and the other is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6alkoxy group(s); or a COR3 or CONHR3, but not simultaneously, where R3 is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6alkoxy group(s); an aralkenyl, optionally substituted by one or more C1 to C6 alkoxy groups and/or one or more OH group(s); or an aryl radical, optionally substituted by one or more C1 to C6 alkoxy group(s).

Abstract: The present invention discloses novel uses of specific menthol-derivative compounds of Formula 1, and compositions thereof, for methods of providing oral and systemic health care benefits, and methods of up-regulating or down-regulating periodontal disease metabolites: Formula 1 wherein, X is an oxygen atom or an NH radical; and R is an unsubstituted or substituted aryl or aliphatic radical. In some embodiments, the oral and systemic health care benefits include biofilm anti-attachment, anti-inflammation, anti-oxidant, anti-bone loss, and anti-microbial benefits. In some embodiments, the periodontal disease metabolites correspond to healthy and/or diseased oral status and allow differential diagnosis of oral health.