Abstract: The present invention provides processes for preparing co-precipitates of non-crystalline, solid drug substances, such as (E)-4-(1,3-bis(cyclohexylmethyl)-1,2,3,6 -tetrahydro-2,6-dioxo-9H-purin-8-yl)cinnamic acid nonaethylene glycol methyl ether ester and solvates thereof.

Abstract: Disclosed herein are pyrido[2,3-d]pyrimidines having the structure wherein R1, and R2 are independently selected from nitro and amino; wherein R3 is selected from alkyl (C1-C10) and cycloalkyl (C3-C8); wherein R4 is selected from hydrogen, benzyl, alkyl (C1-C10), cycloalkyl (C3-C8), arylalkyl (C4-C8), and aryl (C3-C8); wherein R5 and R6 are independently selected from hydrogen, benzyl, alkyl (C1-C10), cycloalkyl (C3-C8), arylalkyl (C4-C14), and aryl (C3-C8); wherein R3 and R4 may form a ring; wherein R5 and R6 may form a ring or a heterocyclic structure; and wherein R5 and R6 are independently unsubstituted or substituted, wherein each substituent is independently selected from halogen, amino, alkyl (C1-C6), haloalkyl (C1-C6), alkoxy(C1-C6), alkylenedioxy, aryl, heteroaryl, and cycloalkyl (C3-C8). Also disclosed are methods for the preparation of compounds of Formula I and various intermediates. These compounds are useful as NAD+-dependent DNA ligase inhibitors.

Abstract: The invention concerns quinazoline derivatives of Formula (I); wherein each of Q<1>, Q<2>, Z, R<1>, R<2>, R<3>, and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.

Abstract: Disclosed are huperzine A prodrugs and method of synthesis thereof. The invention further relates to methods of treating, preventing or reversing neurodegenerative diseases, such as, Alzheimer's Disease and neuronal dysfunctions, such as, memory impairment using a pharmaceutical composition comprising a huperzine A prodrug as disclosed herein.

Abstract: The present teachings relate to the field of anti-inflammatory substances, and more particularly to the preparation of compounds that act as antagonists of the mammalian adhesion proteins known as selecting. In some embodiments, the present teachings provide methods for preparing compounds for treating selectin-mediated disorders that have the formula VI: wherein R1, R2, R3, p, and q are defined herein.

Abstract: The invention provides improved processes for the preparation of hydrated form of (S)-(+)-Clopidogrel bisulfate as well as improved processes for the preparation of form-I and form-II of (S)-(+)-Clopidogrel bisulfate.

Abstract: A method for the preparation of montelukast acid sodium salt thereof in amorphous form has been described. The method comprises of following steps: (a) generating the dilithium dianion of 1-(mercaptomethyl)cyclopropane acetic acid, by reacting with alkyl lithium, (b) coupling the said dianion with wet mesylate to get montelukast acid in crude form, (c) obtaining DCHA salt in crude form by adding dicyclohexylamine (DCHA) to crude acid obtained in the above step (b), (d) purifying and converting the said DCHA salt in crude form, to montelukast acid in pure form, and (e) reacting the pure montelukast acid in a polar protic solvent with a source of sodium ion followed by evaporating the solvent and triturating of the residue with non-polar water immiscible solvent.

Abstract: A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid and S-(?)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.

Abstract: A piperidine derivative of the formula (I) is found to bind specifically with the NR1/NR2B receptor and usable as an analgesic (pain treatment drug). wherein X is OH or lower alkylsulfonyloxy; Ar is optionally substituted aryl or optionally substituted heteroaryl; n is an integer of 1 to 4; m is an integer of 0 to 1; R1 is hydrogen; R2 is OH or R1 and R2 taken together may form a single bond; excluding that 1) n is 2; m is 0; R1 and R2 taken together may form a single bond; and Ar is optionally substituted phenyl and 2) n is 3; m is 0; R1 and R2 taken together may form a single bond; and Ar is phenyl.

Abstract: A method for treating anxiety disorders and other disorders using cholinesterase inhibitors including donepezil and its pharmaceutically acceptable salts.

Abstract: Chemical syntheses and medical uses of novel inhibitors of the gastric H+, K+-ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by gastric acid secretion and/or psoriasis are described.

Abstract: The invention provides a pharmaceutical composition, pharmaceutical product or kit comprising a first active ingredient which is a P2X7 receptor antagonist, and a second active ingredient which is a nonsteroidal anti-inflammatory drug, for use in the treatment of inflammatory disorders.

Abstract: Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of the derivatives for the treatment of pain.

Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, T, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting dipeptidyl peptidase IV or for treating Type II diabetes with such a compound.

Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.

Abstract: The invention discloses compounds which are substituted 4-aryloxy and 4-arylsulfanyl-phenyl-2-aminothiazoles with anti-cancer activity. The invention futher discloses methods of preparing compounds of the invention. The invention also discloses methods of inhibiting cell proliferation and tumor growth in a subject by administering compounds of the invention to the subject.

Abstract: A method for disinfecting or sanitizing a surface by applying an antimicrobial composition comprising a metal-polymer complex.

Abstract: The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA A ?5 mediated diseases, including Alzheimer's disease.

Abstract: The present invention relates to synergistic combinations of the compounds of formula (I) such as compounds of the xanthenone acetic acid class such as 5,6dimethylxanthenone-4-acetic acid (DMXAA) and a selective COX-2 inhibitor, in particular rofecoxib, which have anti-tumour activity. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical formulations containing said combinations.

Abstract: A new polymorphic crystalline form of bicifadine hydrochloride, designated form B, which is more thermodynamically stable than the previously known polymorphic form of bicifadine hydrochloride, designated as form A, methods for preparing said crystalline form B and pharmaceutical compositions containing said crystalline form B.

Abstract: The present invention provides novel compositions and methods for treating symptoms associated with neuropathic disorders such as hyperalgesia, allodynia, and parasthesias, using a 1-aryl-3-azabicyclo[3.1.0] hexane. The invention further relates to the use of 1-aryl-3-azabicyclo[3.1.0] hexanes in pharmaceutical compositions and methods for treating neuropathic disorders and related symptoms in mammals. Patients amenable to treatment according to the invention include those suffering from diabetic neuropathies, post-herpetic neuralgia, trigeminal neuralgia, chronic lower back pain, sciatica, idiopathic and post-traumatic neuropathies, HIV-associated neuropathic pain, among many other neuropathic disorders and related symptoms.

Abstract: The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

Abstract: A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2?±0.2°) of 19.1° in a powder X-ray diffraction.

Abstract: The present invention relates generally to the prevention or delaying of retroviral infection by use of agents that prevent the clustering of retroviral receptors associated with cell membrane raft domains. The present invention relates more specifically to the prevention or treatment of HIV-1 infection through the use of agents that inhibit Rho-A activation by affecting GTPase activity or protein isoprenylation. The present invention relates also to the prevention or delay of HIV-1 infection through the displacement of cytokine receptors from cell membrane raft domains.

Abstract: The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HCl and 4[-2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride usingS methanolic ammonia and glacial acetic acid to obtain highly pure Glimepiride Form I (I) having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.

Abstract: A catechin is modified in at least one position (most preferably in the 3-position of the C-ring) to increase its lipophilicity. Contemplated catechins are demonstrated to have significantly improved antibacterial properties, likely due to catastrophic membrane damage.

Abstract: Pharmaceutical formulations comprising discodermolide in the form of an infusion concentrate, and methods of administration of discodermolide in suitable form for parenteral administration.

Abstract: Methods are disclosed for treating or preventing disorders such as mental diseases, inflammation and pain by inhibiting the enzyme anandamide amidohydrolase. A therapeutically effective level of an anandamide amidohydrolase inhibitor is administered such as a therapeutically effective level of a haloenol lactone. Preferably, the haloenol lactone is of the formula: wherein R is hydrogen, R1 is a halogen, and R2 is selected from the group consisting of aryl, aryloxy, and heteroaryl radicals, derivatives of said haloenol lactones, and mixtures thereof. The haloenol lactone, E-6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyrane-2 -one, is most preferred.

Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.

Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.

Abstract: A highly effective, safe agent for preventing and treating language disorders containing at least one member selected from the group consisting of icosapentaenoic acid and its salt and ester as an effective component is provided. The agent exhibits remarkable therapeutic effects for language disorder with no adverse side effects.

Abstract: The present invention relates to a process for preparing vitamin A acetate by reacting ?-vinylionol with triphenylphosphine in the presence of sulfuric acid in a solvent mixture consisting of 60 to 80% by weight methanol, 10 to 20% by weight water and 10 to 20% by weight aliphatic, cyclic or aromatic hydrocarbons having 5 to 8 carbon atoms to give ?-ionylideneethyltriphenylphosphonium salts and subsequent Wittig reaction with 4-acetoxy-2-methylbut-2-enal.

Abstract: The present invention relates to heparin-binding calixarene compounds of general Formula (I) in which R, R1, L and n have the meanings indicated in the description and their use in the biomedical field.

Abstract: The present invention provides compositions, useful as pharmaceuticals, comprising 3-biphenyl-4-yl-(2S)-[(4?-trifluoromethyl-biphenyl-4-carbonyl)-amino]-propionic acid. Also disclosed are methods for preparing the compositions and methods for using the compositions.

Abstract: The present invention concerns the use of L-dopa, its derivatives or physiologically compatible salts thereof for the prophylaxis of psychotic disorders and for the treatment of diseases which are caused by disrupted tyrosine transport or disrupted tyrosine decarboxylase. In addition, the invention concerns pharmaceutical compositions which contain L-dopa, its derivatives or physiologically compatible salts thereof for the prophylaxis of psychotic disorders, in addition to pharmaceutically compatible adjuvants and additives.

Abstract: Cannabinoid derivatives are known for their functions in the central as well as peripheral nervous system. The present invention describes some novel (+)-cannabidiol (CBD) derivatives, and their selective activity in the peripheral and not in the central nervous system. Thus, it is an object of the invention to provide the use of (+)-CBD derivatives as analgesics, anti-inflammatory and anti-diarrheal agents.

Abstract: The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.

Abstract: The invention relates to a novel use of 1-amino-alkylcyclohexane NMDA receptor antagonists such as neramexane in the treatment of pain hypersensitivity and neuropathic pain.

Abstract: The invention provides adamantane derivatives of formula (I), a process for the their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).

Abstract: Propargylamine, propargylamine derivatives including N-propargyl-1-aminoindan and analogs thereof, and pharmaceutically acceptable salts thereof, are useful for prevention or treatment of renal failure.

Abstract: A method for producing high-active titanium dioxide anatase hydrosol by using metatitanate as precursor, is characterized in comprising the following steps in order: (1) Wash process: adding alkali to wash so as to remove sulfate ion; (2) Dispersion process: adding acid to disperse the filter cake and obtaining a uniform suspension; (3) Peptization process: peptizing the suspension obtained in dispersion process according to the method of (a), (b) or (c). When producing transition metal or rare earth doped anatase hydrosol, transition metal or rare earth salt solution with a predetermined concentration is first prepared, and then added into the metatitanate suspension which has not been washed by alkali. Subsequently, the resulting suspension is filtered and washed until no sulfate ion is present. When producing precious metal deposited anatase hydrosol, precious metal solution is added into prepared pure anatase hydrosol, and then, the resulting solution is irradiated with ultraviolet light for 0.

Abstract: A process of producing expandable styrene resin particles, wherein in suspension polymerization of styrene monomers, the concentration of oxygen in a reaction vessel is kept low at least in a late stage of the polymerization, and the resulting styrene resin particles are impregnated with an expanding agent before or after completion of the polymerization. Preferably, at a polymerization rate of 60% or higher, the concentration of oxygen in the reaction vessel is kept at 7 vol % or lower. When additional styrene monomers are added during the polymerization, they are added and adsorbed to styrene resin particles in the course of polymerization while the concentration of oxygen is kept low. By this method, the particles whose internal portion has a low molecular weight and surface portion has a high molecular weight are obtained. A foamed article produced from the particles has high strength and a good appearance.

Abstract: The invention concerns blowing agents mixtures containing at least a partially fluorinated hydroncarbon and the usual auxiliaries and additives, in which the inert gas content, measured in the vapour phase of the blowing agent or blowing agent mixture, should not exceed 1.5% by volume. The blowing agent mixture can be used to manufacture foam products from thermnoplastics, especially foamed polystyrene.

Abstract: A resin composition for a foam is composed of a branched rubbery olefin based soft resin (C) obtained by kneading and reacting an organic peroxide crosslinking type olefin based copolymer rubber (A) and an organic peroxide decomposing type crystalline olefin resin (B), in which the organic peroxide crosslinking type olefin based copolymer rubber (A) is present as a continuous phase as well as the organic peroxide decomposing type crystalline olefin resin (B) is present as a discontinuous phase in its microaggregation structure. This resin composition enables to provide foamed articles which can be used for interior parts for automobiles, have high to low foaming magnifications and a recycling property, and are soft and excellent in cushion property, thermal insulating property and in-mold foam molding property.

Abstract: An ink having infrared (IR) absorptivity includes an ink vehicle and an IR absorptive pigment having low visible color. According to one exemplary embodiment, the IR absorptive pigment includes an antimony-containing tin oxide.

Abstract: Disclosed are environmentally friendly, substantially all solids coating compositions which are curable using ultra violet and visible radiation. In addition, methods for coating surfaces, or at least a portion of the surfaces, and curing of the coated surface to obtain partially or fully cured coated surfaces are also disclosed. Furthermore, articles of manufacture incorporating fully cured coated surfaces are disclosed, in particular motor vehicles and motor vehicle parts or accessories.

Abstract: It is an object of the present invention to provide a novel photo-curing composition which can be cured by light of a wide wavelength region including ultraviolet light or visible light, has such high sensitivity that it can be sufficiently cured by exposure to a small amount of light, can favorably form a fine pattern when used as a resist and provides a cured product having excellent heat resistance and insulating properties, and a negative photoresist composition using the photo-curing composition. It is another object of the present invention to provide a process for highly accurately and easily producing a polyimide thin film used for a medical instrument, and a medical instrument having the polyimide thin film. The photo-curing composition of the present invention comprises (A) a carbon cluster and/or its derivative, having a photosensitizing function, (B) a compound having plural heterocyclic rings in a molecule, and if necessary, (C) a photo-insensitive resin.

Abstract: Photopolymerizable polymer composites based on dimethacrylate systems have been increasingly utilized as dental restorative materials. One of the biggest drawbacks of current dental resin systems is the volume shrinkage and shrinkage induced stresses that arise during the polymerization. Other major problems include incomplete double bond conversion and insufficient wear resistance. This invention involves the development of an entirely novel approach to the photopolymerization process that utilizes thiol-ene systems as low shrinkage and ultra-low shrinkage stress dental restorative materials. Compared with the traditional dimethacrylate dental resins, these novel photopolymerizations have demonstrated a dramatically decreased volume shrinkage, extremely rapid polymerization, abilities to photopolymerize ultrathick materials and achieve much higher conversion, lack of oxygen inhibition and ultra-low shrinkage stress due to low volume shrinkage and drastically delayed gel point conversion.

Abstract: A radiation curable waterborne composition is disclosed. Said composition comprises at least one amphiphilic dendritic polymer, at least one non-amphiphilic radiation curable oligomer or polymer, water and optionally at least one initiator initiating and/or promoting radiation curing. Said at least one amphiphilic dendritic polymer is build up from a polyhydric dendritic core polymer having terminal hydroxyl groups and at least one carboxylic acid and at least one adduct, obtainable by addition of a monoalkylated polyethylene glycol to a dicarboxylic acid or anhydride, each bonded to at least one terminal hydroxyl group in said polyhydric dendritic core polymer.

Abstract: The invention provides a photocurable polymer composition having a fluorine-containing polymer and a fluorine-free polymer, and preferably further having a polymerizable double bond-containing compound and a photopolymerization initiator. The fluorine-containing polymer preferably includes a fluorosilsesquioxane skeleton.