Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1

Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract: The present invention relates to methods for the prophylaxis, management and treatment of certain diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD) by the administration of a composition containing as an active ingredient a compound according to Formula I. In particular, the invention relates to methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the administration of a compound which inhibits malonyl-coenzyme A decarboxylase activity. The present invention also includes within its scope the novel process for the preparation of certain compounds.

Abstract: Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)-(A)n —Y, —CH2 —CH(R4)-(A)n—Y, —CO—B1-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.

Abstract: A novel pharmaceutical compound 5-[4-2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione L(+) Tartrate or a solvate thereof, a process for preparing such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.

Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) HMG-Co-A reductase inhibitors or a pharmaceutically acceptable salt thereof; and (ii) ACE inhibitors or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.

Abstract: The present invention provides methods of treating cancers, chemoprevention, selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

Abstract: A methylidene oxazolidinone compound represented by formula (1) or a pharmaceutically acceptable salt thereof, and a preparation method thereof, showing superior antimicrobial activities against gram-positive germs including resistant strains such as methicillic-resistant staphylococcus aureus and vancomycin-resistant enterococcus: 1

Abstract: The present invention relates to epothilon derivatives and to their use.

Abstract: A method for delaying or preventing an increase in prostate gland volume in humans or non-human mammals, which method comprises the administration of an effective, non-toxic and pharmaceutically acceptable amount of an insulin sensitiser or a pharmaceutically acceptable derivative thereof.

Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) 1

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: Compounds of formula (I): 1

Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1

Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a therapeutically effective amount, wherein the compound is present in the form of solid particles, about 25% to 100% by weight of which are smaller than 1 mm. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired. The novel Form I and Form II crystalline forms of celecoxib are described. The crystalline forms have unique chemical and physical properties relative to other solid state forms of celecoxib and are characterized by their powder x-ray diffraction (PXRD) patterns, differential scanning calorimetric (DSC) thermograms, and other physical characterizations.

Abstract: A compound of the formula (I): 1

Abstract: The present invention relates to methods for treating, preventing, managing and/or modifying pain, comprising administering an effective amount of a JNK Inhibitor to a patient in need thereof. Specific embodiments encompass the administration of a JNK Inhibitor, alone or in combination with a second active agent and/or surgery or physical therapy. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: The present invention provides a method of treatment of thrombotic thrombocytopenic purpura (TTP) and hemolytic uremic syndrome (HUS) with protein C. The claimed invention provides a needed therapy for a potentially serious and debilitating disorder while avoiding complications such as bleeding tendency, toxicity and general side effects of plasma exchange or currently available anti-coagulant agents.

Abstract: The present invention is referred as a formula or combination of two compounds, one of them being a non-steroidal anti-inflammatory such as ketorolac, and the other an opiate analgesic known as tramadol, which are formulated in capsules.

Abstract: Use of an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with an other antihypertensive, a cholesterol lowering agent, a diuretic or aspirin, in the manufacture of a medicament for the prevention of cardiovascular events; a method of preventing cardiovascular events comprising administering to a patient in need of such prevention an effective amount of an inhibitor of the renin angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with an other antihypertensive, a cholesterol lowering agent, a diuretic or aspirin; and a combination product containing an an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof and a cholesterol lowering agent.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, 1

Abstract: There is provided amino acid derivatives of formula I, 1

Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: 1

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: The present invention refers to a composition based on monoterpenes with chemopreventive and chemotherapeutic effects in malignant neoplasias of humans and animals containing from 0,03% to 30% of monoterpenes and 99,97% of solvents. Another objective of the present invention is an application of monoterpenes in inhibition of cell growth and metastasis control of primary tumors being applied in vitro and in vivo gliomas cell lines C6 and U 87 and A172. Further another objective of the present invention refers to a specific methods for applying the composition with chemopreventive and chemotherapeutic effects in humans and animals showing malignant neoplasias by inhalation and nebulization treatment, oral and intratumoral, followed or not by radiotherapy with dilutions from 0,03% to 30% of the monoterpene perillyl or its derived metabolites diluted in the solvents specified by the usual techniques.

Abstract: The present invention relates to the use of the drug valproic acid and derivatives thereof as inhibitors of enzymes having histone deacetylase activity. The invention also relates to the use of those compounds for the manufacture of a medicament for the treatment of diseases which are associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect for example by induction of differentiation and/or apoptosis in transformed cells.

Abstract: Therapeutic methods for the prevention and treatment of respiratory diseases or conditions are described, the methods including administering to a subject in need thereof a respiratory disease or condition effective amount of a selective inhibitor of inducible nitric oxide synthase.

Abstract: A compound of formula (I): namely (2S)-2-amino-4-{[2-(etha-nimidoylamino)ethyl]thio}butanoic acid, compound with prosphoric acid, or a solvate or physiologically functional derivative thereof, is useful as a relatively non-hygroscopic selective inhibitor of inducible nitric oxice synthase.

Abstract: Described are 6-substituted indanoyl amino acid conjugates as defined in claim 1 of the present invention as potent plant elicitors and efficient mimics of the phytotoxin coronatine. Also, processes for producing the improved elicitors are provided, which allow a rapid and convenient access to large quantifies of the highly active compounds. Furthermore, there are compositions and plant protecting agents described, comprising as active ingredient a compound of the present invention. The plant protecting agents are useful for inducing resistance to pathogens in plants. The compositions may also be used to selectively induce senescence in fruit of plants.

Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: The present application is directed to a method of treating diseases of the central nervous system (CNS) comprising administering to a individual in need of treatment a therapeutically effective amount of an inhibitor of histone deacetylase. In particular embodiments, the CNS disease is a neurodegenerative disease. In further embodiments, the neurogenerative disease is an inherited neurodegenerative disease, such as those inherited neurodegenerative diseases which are polyglutamine expansion diseases. The individual can be a mammal such as a primate or human.

Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.

Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives.

Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Abstract: Treatment of central nervous system disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine and with (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is also disclosed.

Abstract: The invention relates to the use of an accelerated lymphocyte homing agent, e.g. a 2-amino-1,3-propanediol derivative, in reducing delayed graft function in a recipient of organ or tissue transplant.

Abstract: This invention provides various biquinone and trimeric quinone derivatives. The invention also provides a method for synthesis of a multi-quinone compound including reacting a hydroxyquinone anion with a first quinone possessing a first directing group at a C-2 of the first quinone and a second directing group at a C-3 of the first quinone and obtaining a biquinone having one of the first and second directing groups at a C-3 of a first quinone monomer and a hydroxyl group at a C-3′ of a second quinone monomer. The biquinone can be further reacted to obtain various biquinone derivatives or with a second hydroxyquinone anion to obtain trimeric quinone derivatives, including trimeric naphthoquinone derivatives. The biquinones and trimeric quinones of this invention demonstrate antiviral activity and can be used to treat viral infections, particularly HIV infections.

Abstract: The present invention describes linking a therapeutic agent to a compound which is known to be naturally concentrated in a tissue affected by, or that is causing, a disease, to create a prodrug for treatment of the disease. Embodiments of the present invention include a new class of carotenoid-linked drugs to treat such blinding retinal disease such as age-related macular degeneration, retinoblastoma, and diabetic macular edema. For example, the present invention comprises a method for the treatment of a disorder of the eye comprising linking a therapeutic agent to a xanthophyll carotenoid to create a prodrug, and administering a therapeutically effective amount of the prodrug to an individual in need of treatment. Provided are prodrugs for treatment of retinoblastoma, cystoid macular edema (CME), exudative age-related macular degeneration (AMD), diabetic retinopathy, diabetic macular edema, or inflammatory disorders.

Abstract: In order to replace methyl bromide in all the uses thereof in soil or substrate treatment, the invention relates to the use of at least one sulphur compound having general formula: wherein R represents an alkenyl or alkyl radical, n is equal to 0, 1 or 2, x is a number between 0 and 4 and R′ represents an alkenyl or alkyl radical or, only if n=x=0, a hydrogen or alkali-metal atom. The sulphur compounds (in particular dimethyldisulphide) can be applied according to standard soil treatment methods (by injection, spraying, dripping, sprinkling) and said compounds have no phototoxic effects.

Abstract: A guest host assembly comprising a host assembly formed of calixarene molecules and a guest component located within the host assembly. A crystallographic assembly of layers of the calixarene molecules and stacked along the crystallographic c axis of the assembly in a repeating configuration associated together predominantly by van der Waal forces. The guest component is transferable through the host assembly in a direction normal to the stacked layers. The calixarene molecules are configured in bilayers of adjacent layers along the c axis. The bilayers are shifted along the a or b axis so the assembly, relative to a corresponding assembly of the calixarene molecules without the inclusion of the guest component is shifted. The calixarene are calix(N)arenes in which N is an integer within the range of 4-8. The calixarene molecules are distally substituted with a substituent such as methyl, ethyl, propyl, butyl amyl or phenyl groups.

Abstract: An aerosol composition which is prepared from a biliquid foam, an aqueous phase and a propellant.

Abstract: A stable, aqueous composition containing a substantially crosslinked alkali-swellable acrylate copolymer rheology modifier, a surfactant, an alkaline material, and various compounds therein, as for example substantially insoluble materials requiring suspension or stabilization, such as a silicone, an oily material, or a pearlescent material. Additionally, this invention also relates to the formation of a rheologically and phase stable cationic hair dye composition. The invention further relates to the incorporation of an acidic material after the addition of an alkaline material to reduce the pH of the composition without negatively impacting the viscosity of the composition.

Abstract: The invention relates to soft capsules that consist of a gel from a starch mixture having a reduced branching degree and a swelling agent. The soft capsules are especially useful for pharmaceutical, cosmetic and veterinary uses, but also in food technology.

Abstract: Methods of more rapidly producing aerogel products by means of a rapid solvent exchange of solvent inside wet gels with supercritical CO2 by injecting supercritical, rather than liquid, CO2 into an extractor that has been pre-heated and pre-pressurized to substantially supercritical conditions or above. Preferably, pressure waves are applied to the supercritical CO2 to enhance the solvent exchange. The rapid solvent exchange process is followed by depressurization, optionally with a gas exchange. Preferably, pressure waves are used to speed up the depressurization. The process greatly reduces the time for forming aerogel products.

Abstract: The present invention relates to compositions for use in analyte monitoring devices. These compositions are useful to increase the flux of analyte across skin, tissue or mucosal surfaces. The compositions include hydrogels and collection reservoir systems comprising ionically conductive materials. The present invention also includes methods of making/manufacturing hydrogels or collection reservoir systems, collection assemblies comprising the hydrogels, electrode assemblies in combination with the hydrogels or collection reservoir systems, and methods of using the same.

Abstract: A catalyst composition and a process of using a catalyst composition for preparing high molecular weight hydrocarbons, such as polymethylene, from a fluid containing hydrogen and carbon monoxide are disclosed. The catalyst composition contains ruthenium and a treated silica support component. The treated silica support component is prepared by a process including contacting a silica support component, such as silicon dioxide, and a treating agent, such as a silicon-containing compound.

Abstract: The invention relates to a method for processing contaminated polycondensate materials, especially polyethylene terephthalate (PET). The inventive method is characterized by removing a surface layer of the polycondensate material to be processed before the material is melted and filtered in the melt. Optionally, said method may be followed by a step for increasing the intrinsic viscosity by melt phase or solid phase polycondensation.

Abstract: A method for producing polyisocyanurate insulation foams, the method comprising contacting an A-side stream of reactants that includes an isocyanate with a B-side stream of reactants that include a polyol and a blowing agent, where the blowing agent includes isopentane and n-pentane in a substantial absence of cyclopentane.