Abstract: This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.

Abstract: The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, X and n are the same as defined in the specification.

Abstract: Dihydroxyhexanoic acid derivatives of the general formula are useful to treat inflammation and other immune disorders.

Abstract: The subject invention provides a compound having the structure: or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A3 adenosine receptor by administering a therapeutically effective amount of the compound.

Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group

Abstract: A compound of the formula (I) or a pharmacologically acceptable salt, ester or other derivative thereof: R1 is H or NHOH. R2 is H, optionally substituted alkyl, cycloalkyl or a group —AR6. A is an alkylene which may be optionally interrupted by O, —S(O)m— or —N(R9). R6 is a group (II), (III), (IV) X is O, S, —N(R10)—, —C(R11)(R12)—. Y is O, CO, —S(O)n—, —N(R10)—, —C(R11)(R12)—. Each of R7 and R8 is H, alkyl, COOH, optionally substituted alkyl, etc. Each of R9, R10, R11, and R12 is H, alkyl, etc. Each of m and n is 0 to 2. R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl. R4 is optionally substituted (hetero)arylene. R5 is optionally substituted alkyl, optionally substituted (hetero)aryl. These compounds have matrixmetalloproteinase—13 inhibitory activity and aglycanase inhibitory activity.

Abstract: The present invention relates to novel stable solution formulations comprising oxaliplatin alone or in combination with irinotecan (CPT-11), an effective stabilizing amount of lactic acid and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method for manufacturing such formulations ready for administration and their use in the antitumor therapy are also within the scope of the invention.

Abstract: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from a solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline Forms I and II in a solvent at a temperature below about 30° C.

Abstract: Methods for increasing graft survival time comprising administering the combination of a compound that inhibits the production of nitric oxide and a compound that is a tricyclic macrolide, such as tacrolimus.

Abstract: To provide a pharmaceutical composition comprising a macrolide compound, such as tricyclic compound (I) or its pharmaceutically acceptable salt, a dissolution/absorption promoter, a pharmaceutical base, and optionally a compatibilizing agent and/or a thickener. It is satisfactory in stability and absorption kinetics and/or a low irritation potential.

Abstract: The present invention relates to a compounds of formula I, wherein A is olefin, diol, or acetonide; which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: The present application describes imidazo-heterobicycles of formulas I and III: or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Disclosed are 1H-Pyrrolo[3,2-b]pyridine-3-carboxylic acid amides that bind to the benzodiazepine site of GABAA receptors. Such compounds can be used to modulate ligand binding to GABAA receptors in vivo and in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals.

Abstract: An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.

Abstract: This invention provides a method of identifying and reversing multidrug resistance in a multidrug resistant tumor comprising administering a multidrug resistance reversing amount of any of the compounds as defined herein.

Abstract: The present invention relates to methods useful for the treatment of neoplastic diseases, tumor cells, and the treatment of cancer delivering compounds of the formula The invention provides various methods of delivering such compounds, combinations of treatments, and altering such compounds to enhance their effectiveness.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is CH or N and, A, E, M, G, X2, X3, X4, R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: Compounds of general formula (I), in which m is 0-8, q is a 0-8, a is 0-4, A signifies a single or double bond, R1, R2 signify hydrogen or lower alkyl and, when m signifies 2-8, R1 and R2 in the group CR1═CR2 can have various significances within the following sequence, R3 signifies hydrogen or lower alkyl, X signifies hydrogen or —(CH2)b—COR4 with b=0-4, Y signifies hydrogen, —COR4, phenyl or indolyl residue R4 signifies hydroxyl, lower alkoxy or the NR1R2 residue, W signifies an optionally mono- or polysubstituted saturated or unsaturated mono-, bi- or tricycle which can contain hetero atoms, as well physiologically compatible salts, esters, optically active forms, racemates, tautomers, and derivatives which can be metabolized in vivo to compounds of general formula (I).

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.

Abstract: The present invention relates to novel compounds of Formula I, and pharmaceutically acceptable salts thereof, as antibacterial agents. The compounds of the present invention are nitric oxide releasing derivatives of proton pump inhibitors (NO-releasing PPIs). In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above. The invention also relates to new intermediates for use in the preparation of the novel compounds. Additionally the present invention relates to co-administration of NO-releasing PPIs with other known medicaments.

Abstract: The invention relates to novel compounds of the general formula: in which R1 is hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl or unsubstituted or mono- to pentasubstituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different; R2 is hydrogen, C1-C6alkyl, (C1-C6alkylene)phenyl, pyridyl, COOR6, CONR7R8, COR6, allyl or CH2—O—R6; R3 is unsubstituted or substituted heterocyclyl, where the substituents are in each case selected from the group consisting of unsubstituted or substituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different, benzyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano, hydroxyl, ami

Abstract: Nitrogen heterocycles that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds.

Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: Disclosed is a method for treating a pituitary tumor in a mammal, employing the administration of a peroxisome proliferator activated receptor gamma ligand (also known as “peroxisome proliferating-activator receptor gamma” or “PPAR-&ggr;”). In some embodiments, the peroxisome proliferator activated receptor gamma ligand is a thiazolidinedione compound. Also disclosed are methods for preventing the formation of a pituitary tumor in a mammal and for preventing the recurrence of a pituitary tumor in a mammal. Further disclosed is a method for treating a mammal exhibiting one or more symptoms of Cushing's syndrome.

Abstract: Compounds of the formula inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) —C(O)H or —C(O)R6; (h) —CO2H or —CO2R6; (i) —SH, —S(O)nR6, —S(O)m—OH, —S(O)m—OR6, —O—S(O)m—R6, —O—S(O)mOH or —O—S(O)m—OR6; (j) —Z4—NR7R8; or (k) —Z4—N(R11)—Z5—NR9R10; and the remaining symbols are as defined in the specification.

Abstract: Urazole compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective as anti-inflammatory or immunosuppressive agents, wherein L and K are O or S; Q is a linker such as —O—, —S—, C(═O), and so forth, R1 is an aryl or heteroaryl group, and R3, R4a, R4c, Z, r, s and t are as defined in the specification.

Abstract: An improved method of treating skin diseases comprises applying to the skin of a patient suffering such a skin disease an allantoin-containing composition in a therapeutically effective quantity. The allantoin-containing composition is a water-in-oil emulsion that includes allantoin and an emulsifier system that includes at least one emulsifier that is either an anionic emulsifier or a nonionic emulsifier. If the emulsifier is an anionic emulsifier, the emulsifier system can include beeswax. The nonionic emulsifiers used can include at least one nonionic emulsifier that is an ethoxylated ether or an ethoxylated ester whose carbon chain length ranges from 8 to 22 carbon atoms. Alternatively, the emulsifier system can include an acidic anionic polymer such as carboxypolymethylene and an anionic emulsifier. In another alternative, the emulsifier system can include the acidic anionic polymer and a nonionic emulsifier, or the acidic anionic polymer alone.

Abstract: The present invention provides methods of treating or preventing fungal infections in a host comprising administering a treatment effective or treatment effective amount of a yeast NAD synthetase inhibitor compound. The invention further provides a method of killing yeast comprising administering a yeast NAD synthetase compound that selectively binds to catalytic sites in yeast whereby the yeast is killed.

Abstract: The invention provides new and useful analogs of 2-phthalimidinoglutaric acid. These analogs include DL-2-methyl-2-phthalimidinoglutaric acid and hydroxylated analogs of 2-phthalimidinoglutaric. The invention also provides processes for making these analogs. The invention also provides the two individual enantiomers of DL-2-methyl-2-phthalimidinoglutaric acid, (R)-(+)-2-methyl-2-phthalimidinoglutaric acid and (S)-(−)-2-methyl-2-phthalimidinoglutaric acid, and processes for separating these individual enantiomers from the racemate. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering one or more of these compounds.

Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Abstract: The present invention provides novel antiviral compounds, refered to as calanolides, related compounds, and their derivatives, which may be isolated from plants, or derived from compounds from plants, of the genus Calophyllum in accordance with the present inventive method. The compounds and their derivatives may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2.

Abstract: The instant invention provides methods for preventing or reducing the risk of developing atherosclerosis, as well as for halting or slowing the progression of atherosclerotic disease once it has become clinically evident, comprising the administration of a therapeutically effective amount of an HMG-CoA RI in combination with folic acid or a pharmaceutically acceptable salt or ester thereof to a person who is at risk of developing atherosclerosis or who already has atherosclerotic disease.

Abstract: The invention provides a method of determining whether a compound alleviates vasoconstriction-independent nerve pain mediated by endothelin-1 (ET-1). The method involves (i) determining whether the compound has the ability to inhibit a vasoconstriction-independent ET-1 action, and, if the compound has the inhibitory ability, then ii) determining whether the compound reduces vasoconstriction-independent nerve pain by testing the compound in human patients suffering from pain mediated by the vasoconstriction-independent ET-1 action. The invention also includes a method of determining whether a compound alleviates pain caused by nerve injury in human patients. The method involves (i) determining whether the compound has the ability to inhibit an inflammatory leukocyte response, and, if the compound has the inhibitory ability, then (ii) testing the compound in human patients suffering from pain caused by nerve injury to determine whether the compound alleviates the pain.

Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases in which high blood platelet aggregations occur.

Abstract: A viscous gel for delivering minor effective amounts of active substances through the nasal membrane into the body.

Abstract: A vehicle for applying chemical compounds to wood comprises the following components in the indicated approximate percentages by weight of the total: toluene (40-70%), xylene (6-40%), benzophenone (3-18%), butyl glycol (2-9%), cetyl acetate (1-7%) and methanol (0.3-4%). The vehicle has a high wood penetration index and can be used for preparing compositions containing one or more chemical compounds useful for treating wood, for example insecticides and/or fungicides, for the purpose of treating or preventing damage caused by the attack of biological agents harmful for wood.

Abstract: A novel solid, crystalline and non-hygroscopic substance consisting of acetyl L-carnitine acid fumarate and a process for preparing same are disclosed.

Abstract: A novel salt of O-desmethyl venlafaxine is provided, O-desmethylvenlafaxine succinate. Pharmaceutical compositions, dosage forms and methods of use are also provided.

Abstract: Acylcarnitines, such as L-acetylcarnitine (I) were found to have marked antitumour activity, which can be further increased by simultaneous administration of somatosstatin.

Abstract: Disclosed is the use of metabolites produced from arachiconic acid by the catalytic action of lipoxygenase as capsaicin-channel or- receptor agonists. The lipoxygenase metavolites of arachidonic acid and their derivatives can activate the capsaicin channel to excite pain nerves, causing serious pain. In contrast, the capsaicin channel activation of the pain nerves, so that an analgesic effects are brought about. The lipoxygenase metabolites of arachidonic acid can be used as an analgesic and in searching for and developing analgesics.

Abstract: The present invention relates to a composition of topical preparation containing alprostadil alkyl ester, and more particularly, comprising an alprostadil alkyl ester, an oily vehicle, a skin permeation enhancer and an anti-irritant agent.

Abstract: A method of treating onychomycosis is described which includes administration of an effective amount of urea in a topical formulation to an infected area around a nail of a patient.

Abstract: Methods for treating diseases or disorders of the skin which are characterized by angiogenesis have been developed using curcumin and curcumin analogs. Based on the results obtained with curcumin, it has been determined that other angiogenesis inhibitors can also be used to treat these skin disorders. It has further been discovered that curcumin acts to inhibit angiogenesis in part by inhibition of basic fibroblast growth factor (bFGF), and thereby provides a means for treating other disorders characterized by elevated levels of bFGF, such as bladder cancer, using curcumin and other analogues which also inhibit bFGF.

Abstract: A warming composition which produces an excellent warming effect of long duration with no or little skin irritation, a fragrance composition comprising the warming composition, and cosmetics, toiletries, bath additives, and pharmaceuticals containing the warming composition or the fragrance composition.

Abstract: An integrated process for producing hydrocarbon products and energy includes reforming a hydrocarbonaceous gaseous feed stock to synthesis gas, and exothermally reacting the synthesis gas at elevated temperature and pressure, and in the presence of a Fischer-Tropsch catalyst, to produce a range of hydrocarbon products of differing carbon chain lengths. The reaction temperature is controlled by indirect heat exchange of a reaction medium, comprising synthesis gas and hydrocarbon products, with water, with the water being converted to steam (‘FT steam’). The process includes burning a combustible gas in a combustion chamber of a gas turbine generator, to form combusted gas, and expanding the combusted gas through an expansion chamber of the gas turbine generator to form hot flue gas. The gas turbine generator generates electrical energy. The FT steam is superheated by means of hot flue gas, thereby producing superheated FT steam.

Abstract: This invention relates to methods of minimizing catalyst degradation during the handling of a catalyst used in a slurry phase reactor. The methods include catalyst handling steps such as catalyst loading into a slurry phase reactor, slurry phase reactor start-up, slurry phase reactor shut-down, and slurry phase reactor unloading when catalyst reloading is envisaged. In the method of loading the slurry phase reactor, a slurry of wax and catalyst is formed in a loading vessel. Clean molten wax is formed in the reactor, syngas is pumped through the clean molten wax in the reactor, and the slurry from the loading vessel is transferred to the reactor.

Abstract: The present invention relates to a method of removing water immiscible porogens from macroreticular copolymers comprising distilling said porogen in water soluble organic solvent.

Abstract: The present invention provides a process for manufacturing a cross-linked expanded safety support having a cellular structure comprising closed cells. The process involves kneading by thermomechanical working a rubber composition comprising a diene elastomer having a molar ratio of diene units (defined as units resulting from dienes) of less than 15%, water in an amount of from 3 to 6 phr (phr=parts by weight per 100 parts elastomer), a blowing agent, such as azobisformamide, that provides for formation of the cellular structure and a vulcanization system. The rubber composition so prepared is then formed, e.g. by injection or extrusion, into cross-linkable blank, which is then cured in a mold and then demolded. The demolded blank is then expanded by decomposition of the blowing agent and vulcanized to produce the cross-linked expanded elastomeric support.