Abstract: The disclosure provides a process for the preparation of 3-(4?-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.

Abstract: 2-Hydroxy-isocaproic acid (HICA), or an ester or amide derivative, an enantiomer or a pharmaceutically acceptable salt thereof, for use in prevention and/or treatment of a disease or condition involving degradation of cartilage and/or disruption of cartilage homeostasis and/or integrity is disclosed.

Abstract: Methods and apparatuses for the therapeutic delivery of nicotine for smoking cessation, harm reduction and/or substitution. Furthermore, the devices and methods herein are useful as an alternative, general nicotine delivery system in place of tobacco combustion or high temperature (over 150 degrees C.) products. In addition, the methods and devices herein are useful for the therapeutic delivery of a drug, for reducing the cumulative drug dose and hence its potential toxic side effects, while increasing its neurophysiological and/or physiological effects. Moreover, the devices and methods herein are useful for addiction treatment or reduction. In certain embodiments, the methods are adaptable to a medicament delivery device that determines a sequence of drug doses to be delivered. Dose information may be used to control operation of the device.

Abstract: A method of treating a subject for reducing the risk of QT space prolongation associated with the intake of a drug known to prolong QT space includes administering to the subject at least one specific inhibitor of mitochondrial ROS production selected from among anethole trithione (ATT), 4-OH-anethole trithione (ATX), and an ATX ester, and administering to the subject the drug known to prolong QT space.

Abstract: Disclosed herein is a therapeutically active agent usable in the treatment of pulmonary arterial hypertension (PAH), for use in the treatment of pulmonary arterial hypertension, as well as methods of treating PAH, said treatment and methods comprising administering such an active agent and effecting pulmonary artery denervation in the subject. In some aspects, a sub-therapeutically effective amount of the active agent is administered. In some aspects, the method is devoid of administering such an active agent for at least one month subsequent to the denervation. Further disclosed is a method of treating PAH comprising determining a responsiveness of the subject to at least one therapeutically active agent usable in treating PAH; and effecting pulmonary artery denervation in a subject responsive to the active agent(s).

Abstract: The subject invention provides materials and methods that effectively support innate immunity and/or disperse pathogenic biofilms using readily available, nontoxic, natural substances, while supporting restoration of normal microbiotic homeostasis. In one embodiment, the subject invention provides anti-biofilm compositions comprising one or more probiotic organisms, anti-microbial honey, and other ingredients such as prebiotic compounds, other hive products, green tea derivatives, other plant derivatives, and vitamin D3.

Abstract: The present disclosure relates to certain chiral diaryl macrocyclic derivatives of the formula I pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.

Abstract: The present invention relates to compounds of formula I: for use in treating pulmonary arterial hypertension and associated conditions, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl, -alkylaryl or -alkylheteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more pyrethroid compound(s) selected from Group (A) shows an excellent controlling activity on a pest.

Abstract: The present invention relates to compounds comprising the general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms; Y and Z, which may be identical or different, are selected from the group comprising —H, —OH, —COOH, —OR3, —CH(OR3)COOH, in which R3 is selected from H, phenyl, benzyl, —CF3 or —CF2CF3, vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.

Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating chronic pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.

Abstract: Disclosed herein are therapeutic regimens for treating or ameliorating a visual disorder associate with an endogenous retinoid deficiency in a subject by administering a therapeutically effective amount of a synthetic retinal derivative or a pharmaceutically acceptable composition comprising a synthetic retinal derivative according to the therapeutic regimen which leads to local recovery of visual functions such as visual fields, visual acuity and retinal sensitivity, among others.

Abstract: A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.

Abstract: The present invention aims at provision of a method for inhibiting remnant lipoprotein production and a remnant lipoprotein production inhibitor, which includes administering a compound having a CETP inhibitory activity to an administration subject. The remnant lipoprotein production inhibitor of the present invention contains a compound having a CETP inhibitory activity as an active ingredient.

Abstract: A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ?-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Abstract: The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.

Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.

Abstract: A lipid composition comprising racecadotril, at least one surfactant and a lipid.

Abstract: The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.

Abstract: The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.

Abstract: The present invention relates to adamantyl derivatives and their anti-cancer activity. Compounds of formulae I and II are provided as well as related methods of treatment and methods of synthesis.

Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl] 2-methylthiopropionate which is useful as a pharmaceutically active compound.

Abstract: Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.

Abstract: The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ?-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Abstract: A method for inhibiting the autophagy of motor neurons in a subject is provided. The method comprises administrating to the subject an effective amount of an active ingredient selected from the group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable ester of the compound and combinations thereof: wherein A is a C1-C5 alkyl optionally having one or more unsaturated bonds and optionally being substituted by one or more substituents selected from a group consisting of —OH, ?O and C1-C3 alkyl; X is H, —OH, Y is O or S and can optionally combine with A to form a five-membered ring; and R1 is H or a substituted or unsubstituted C1-C20 alkyl, wherein one or more —CH2— of the C1-C20 alkyl are optionally being replaced by —NH— or —O—.

Abstract: A lipid composition comprising racecadotril, at least one surfactant and a lipid.

Abstract: A liquid composition comprising racecadotril and cyclodextrin.

Abstract: Methods of treating Parkinson's Disease comprising administering compounds that up-regulate cystine-glutamate exchange (system Xc?) and/or increase glutathione levels in the brain cells. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.

Abstract: A plant disease control composition comprising, as an active ingredient, a compound of formula (I) or a salt thereof, and one or more anilinopyrimidine compounds selected from the group consisting of 4,6-dimethyl-N-phenyl-2-pyrimidinamine, 4-methyl-N-phenyl-6-(1-propynyl)-2-pyrimidinamine and 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine has an excellent plant disease control effect.

Abstract: The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen, diclofenac, licofelone, or HTB, and one or more antioxidants.

Abstract: The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen, diclofenac, licofelone, or HTB, and one or more antioxidants.

Abstract: The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.

Abstract: The present invention relates to adamantyl derivatives and their anti-cancer activity. Compounds of formulae I and II are provided as well as related methods of treatment and methods of synthesis.

Abstract: An anhydrous color cosmetic composition comprising at least one resveratrol derivative and particulates; and an anhydrous emulsion skin care composition.

Abstract: The present invention provides a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which includes: a soft gelatin capsule shell including gelatin and sugar alcohol as a plasticizer, and a mixture including a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.

Abstract: Methods of treatment of diseases that include or are characterized by inappropriate or pathological neovascularization are disclosed. These diseases include diseases of the eye, such as diabetic retinopathy, retinopathy of prematurity, and choroidal neovascularization which can occur in age-related macular degeneration (AMD). Disclosed methods include administering agents that cause directly or indirectly upregulation of the ABCA1 transporter protein in macrophages. These agents include, without limitation, LXR agonists. In some embodiments, inhibitors of CETP expression or activity can also be effective. Administration routes can include, without limitation, intraocular, periocular, or systemic administration.

Abstract: A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ?-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.

Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.

Abstract: A process for controlling the crystallization of certain hydrophobic active pharmaceutical ingredients (APIs) from a supercooled liquid state by hot-melt extrusion processing is described. Also described is a pharmaceutical composition comprising a solid crystalline dispersion of a cholesterol ester transfer protein inhibitor in a hydrophilic excipient matrix. In the process of the present invention, the API is fed to an extrusion system in a crystalline state contemporaneously with carrier excipients where it is first converted to a non-crystalline state by the application of heat and then subsequently recrystallized in-situ by the removal of heat and application of shear. Recrystallization of the API is controlled by carrier formulation design and the hot-melt extrusion process parameters; i.e. barrel temperature profile, feed rate, etc.

Abstract: Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.

Abstract: The present invention relates to a novel stable S-[2-([[1-(2-ethylbutyl)-cyclohexyl]-carbonyl]amino)phenyl]2-methylpropanethioate liposomal composition, a process for the preparation thereof and its use in the treatment of diseases.

Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.

Abstract: The present invention relates to a hygroscopic matrix based formulation, a process for the preparation thereof and its use in the treatment of diseases.