Abstract: The present invention provides a compound of formula (I): wherein R1–R5, R25, R26, Y and X2 are as defined herein. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and are useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.

Abstract: The present invention relates to compounds of the formula wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.

Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed.

Abstract: The present invention relates to compounds of general formula R—Z1—Z2—Z3—R1, ??(I) wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same.

Abstract: Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein.

Abstract: The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.

Abstract: The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

Abstract: A new crystalline Form III of moxifloxacin monohydrochloride and processes for making the crystalline form as well as compositions, pharmaceutical compositions, and methods utilizing the crystalline form are described.

Abstract: The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.

Abstract: The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of an inflammatory or immunoregulatory disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

Abstract: Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nito, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.

Abstract: A 1,2,4-triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: wherein: R1 represents naphthyl, indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, benzooxazolyl, quinolinyl, or isoquinolinyl; wherein, R1 is optionally substituted at a substitutable position with one or more radicals independently selected from halogen, hydroxy, nitro, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, cyano, amino, monoalkylamino, and dialkylamino; R2 represents methyl or amino; and A, B, E, and D each independently represent carbon or nitrogen.

Abstract: The present invention relates to compounds of formula I: which are antagonists of 5-HT6 receptor.

Abstract: Pharmaceutical compositions and single unit dosage forms of thalidomide and pharmaceutically acceptable prodrugs, salts, solvates, hydrates, or clathrates are disclosed. Also disclosed are methods of treating and preventing diseases and conditions such as, but not limited to, leprosy, chronic graft-vs-host disease, rheumatoid arthritis, sarcoidosis, an inflammatory condition, inflammatory bowel disease, and cancer using the novel dosage forms disclosed herein.

Abstract: Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention provides pharmaceutical formulations suitable for intravenous injection comprising a lyophilized anti-ulcerative agent reconstituted in isotonic solutions suitable for intravenous administration, such as 5% dextrose or 0.9% sodium chloride. The solutions are brought to a pH of between about 9 and about 12, preferably between about pH 10 and 11, by a glycine-sodium hydroxide buffer. Such formulations are chemically and physically stable, and do not significantly change color, for at least between about 6 and about 12 hours at room temperature, and are stable to color change for from between about 24 and 48 hours if kept at 5° C.

Abstract: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.

Abstract: Water-soluble salts of pioglitazone especially pioglitazone sulfate are useful in pharmaceutical applications.

Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.

Abstract: This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.

Abstract: A compound having Formula I R1—Z—R2Formula I wherein R1 is an optionally substituted phenyl ring; R2 is or comprises an optionally substituted aromatic ring; and Z is —X—Y—L— or —Y—X—L— wherein either X is selected from —S(?O)(?O)— and —C(?O)—; and Y is —NR3—; or X is selected from —S(?O)(?O)— and —S—, and Y is —C(R4)(R5)—; L is an optional linker; and R3, R4 and R5 are each independently selected from H and hydrocarbyl; and wherein when R2 comprises the following structural moiety wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1—C(?O)—NR3—L—R2; R1—S(?O)(?O)—C(R4)(R5)—L—R2; R1—S—C(R4)(R5)—L—R2; R1—NR3—S(?O)(?O)—L—R2; R1—NR3—C(?O)—L—R2; R1—C(R4)(R5)—S(?O)(?O)—L—R2; and R1—C(R4)(R5)—S—L—R2.

Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.

Abstract: The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5?, R6, a, b, c, d, and u are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.

Abstract: A triazole compound of the formula (I) or a pharmacologically salt thereof: wherein X represents a group of formula X—OH which has antifungal activity, L represents an -(adjacently substituted C6-C10 aryl)-CH2 group and R represents a —P(?O)(OH)2 group.

Abstract: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.

Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: Compositions, methods, etc. for addressing the first-pass effect.

Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection

Abstract: The present invention relates to fatty acid analogues of the general formula (I): R1-[xi-CH2]n—COOR2 wherein R1 is; a C1–C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C1–C24 alkyne, and/or a C1–C24 alkyl, or a C1–C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1–C4 alkoxy, C2–C4 alkylthio, C1–C5 acyloxy or C1–C4 alkyl, and wherein R2 represents hydrogen or C1–C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and with the proviso that if R1 is an alkyne or alkene, then the carbon-carbon triple bond or double bond is positioned between the (?-1) carbon and the (?-2) carbon, or between the (?-2) carbon and the (?-3) carbon, or between t

Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

Abstract: The present invention provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like; R1 is halogen, lower alkyl, halo-lower alkyl, CN and the like; R3 is hydrogen and the like; R4 is hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, —CONR7(R8), —S(O)mR9, —SO2NR7(R8) and the like; R5 is hydrogen, halogen, alkyl, substituted alkyl and the like; A is —N(R6)CO—A1—COR10 and the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor ?.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: Compositions and methods for controlling an arthropod pest population that include an eremophilane sesquiterpene pest control agent (such as, nootkatone or 13-hydroxy-valencene) and a dialkyl-substituted phenol pest control agent (such as, carvacrol) are disclosed. The compounds present in the compositions may be isolated from natural sources, semi-synthesized from naturally occurring compounds, or completely synthesized. The pest control compositions may be applied directly to a pest or the locus of a pest, and function as topical or ingestible pest toxins.

Abstract: The invention relates to methods for prevention of and recovery from a catalyst bed slumping in a gas-agitated multiphase hydrocarbon synthesis reactor, while the reactor is either under non-reactive conditions or under reaction promoting conditions when syngas is converted to products. The reactor contains a catalyst bed comprising catalyst particles and a gas injection zone suitable for injecting a reactor gas feed. A method for preventing bed slumping comprises supplying a supplemental gas to the gas-agitated multiphase reactor to prevent the catalyst bed from slumping due to insufficient reactor gas feed flow. The method may include recycling some or all of the supplemental gas to the reactor. The method may further comprise separating the gas injection zone from the catalyst bed with a porous plate so as to prevent migration of catalyst particles into the gas injection zone and to minimize plugging of gas distributor(s) present in said zone.

Abstract: The present invention relates to improved catalyst compositions, as well as methods of making and using such compositions to prepare synthesis gas and ultimately C5+ hydrocarbons. In particular, preferred embodiments of the present invention comprise catalyst systems comprising a core and an outer region disposed on said core, wherein a substantial amount of the catalytic metal is located in the outer region of the catalyst support matrix. In addition, the catalyst systems are able to maintain high conversion and selectivity values with very low catalytically active metal loadings. The catalyst systems are appropriate for improved syngas, oxidative dehydrogenation and other partial oxidation reactions, including improved reaction schemes for the conversion of hydrocarbon gas to C5+ hydrocarbons.

Abstract: A polyurethane and/or polyisocyanurate foam is made using expandable microspheres which encapsulate a primary blowing agent. By expanding during the foam making process, the microspheres function as a blowing agent. The foam preferably has at least 10% by weight expandable micro spheres which encapsulate a non-halogenated hydrocarbon chemical or a non-halogenated hydrocarbon chemical blend and less than 2% by weight of any non-encapsulated blowing agents.

Abstract: The present invention relates to a method for the continuous mixing of at least one polyol component and at least one isocyanate component and optionally additives to form a polyurethane reaction mixture in a stirrer mixer with an axially conveying stirrer.

Abstract: Fluoropolymers are made by admixing tetrafluoroethylene, hexfluoropropylene, and vinylidene fluoride; reacting the reaction admixture to generate a set of fluoropolymeric oligomers; irradiating the fluoropolymeric oligomeric precursor admixture (preferably with electron beam radiation) to form free radical sites on individual fluoropolymeric oligomers of the set and generate thereby a set of free radical oligomer derivatives in the fluoropolymeric oligomeric precursor admixture; and reacting the fluoropolymeric oligomeric precursor admixture to derive the fluoropolymer compound from the free radical oligomer derivatives. In a second approach, fluoropolymers are made by admixing tetrafluoroethylene, hexfluoropropylene, and vinylidene fluoride and irradiating the admixture.

Abstract: Orthopedic compositions are provided that include a homogeneous mixture of a biocompatible polymer and a bioactive particulate ceramic wherein the ceramic has an average particle size of not more than 500 nm are provided. The compositions may be used to form bone cement or various spinal implants, including spinal spacers, interbody fusion cages, bone plates and bone screws. Methods for stabilizing a spine, for correcting a bone defect, and for promoting fusion of adjacent vertebrae are also provided.

Abstract: High concentrations of dye may be prepared in combination with thermoplastic polymers and used in optical polymers as monomeric and dimeric molecular solutions. The method of preparing high concentration levels allows the control over the aggregation of dye molecules that is required to maintain effective nonlinear operation. The present invention is applicable to many systems and is essential to the successful production of working optical limiting devices and other optically transparent polymeric devices, as well as other photonic applications, such as nonlinear optics.

Abstract: The present invention relates to a bituminous composition, comprising a bituminous component and a block copolymer, wherein the block copolymer comprises at least two terminal poly(vinyl aromatic) blocks and at least one poly(conjugated diene) central block, wherein said poly(conjugated diene) central block(s) is (are) obtained by substantially random copolymerization of butadiene and isoprene a molar ratio between butadiene and isoprene in the range or from 1:2 to 9:1; wherein the poly(vinyl aromatic) content (PSC) is in the range of from 20 to 30 wt %, wherein the content of a possibly accompanying diblock comprising a poly(vinyl aromatic) block and a poly(butadiene/isoprene) block is at most 25 mole %, wherein the 1,2-addition (vinyl content) of the polymerized conjugated dienes is in the range of from 10 to 80%, and wherein the apparent molecular weight of the complete block copolymer is in the range of 310,000 to 380,000.

Abstract: The instant invention pertains to a thermoplastic organic polymer containing a conventional flame retardant and a hydroxylamine ester, in particular a tetraalkyl piperidine hydroxylamine ester. Further aspects of the invention are the use of hydroxylamine esters as flame retardants and a method for improving flame retardancy of a thermoplastic organic polymer.

Abstract: A hydrophilic polymer composition is described comprising thermoplastic of thermoset polymer, and a fluorochemical additive dispersed therein. The hydrophilic composition is useful, for example, in medical and surgical drapes.

Abstract: The invention provides intimate physical mixtures of macrocyclic polyester oligomer (MPO) and filler, as well as methods for their preparation and use. Improved dispersion of filler in a polymer matrix is achieved upon polymerization, and larger amounts of filler with high aspect ratio can be used. In one aspect, the invention provides mixtures of MPO with magnesium silicate. In another aspect, the invention provides a mixture of MPO, filler, and polymerization catalyst as a one-part, ready-to-polymerize material with a long shelf life. The one-part material can be used, for example, in the manufacture of parts without modification of existing processing equipment.

Abstract: A golf ball comprising a single-layer core having a diameter of 0.10 inches to 1.50 inches, a PGA compression of 110 or less and, and comprising a copolymer of ethylene and an ?,?-unsaturated carboxylic acid, the acid being 100% neutralized by a salt of an organic acid, a cation source, or a suitable base of the organic acid; and a thermoplastic or thermoset cover comprising polyurethane, polyurea, epoxy resins, polyamides, polyesters, polycarbonates, or a copolymer comprising urethane and urea segments.

Abstract: A flame-retardant composition is described, containing a thermoplastic resin component which includes polyphenylene ether (PPE), along with a low-melting glass having a glass transition temperature (Tg) of less than about 500° C. The low-melting glass contains phosphate, and at least one of RO; R?2O; Al2O3; B2O3; or SO3, where R is a bivalent metal, while R? is an alkali metal. Related articles are also described.

Abstract: The present invention relates to curable elastomer compositions and deformable thermoplastic compositions which are reshapable subsequent to cure or solidification. In particular, the present invention relates to compositions and articles of manufacture which are prepared from curable elastomeric or deformable thermoplastic matrices having distributed therein polymeric powders which have a melting point below the degradation of the matrix and which are present in shape-holding amounts to permit reshaping subsequent to elastomer cure.