Abstract: MC4-R binding compounds of the formula: B—Z—E  (I) wherein B is an anchor moiety, Z is a central moiety, and E is a MC4-R interacting. moiety are discussed. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also discussed.

Abstract: Fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of (a) at least one azolopyrimidine of formula I  in which R1, R2, L1, L2 and L3 have the meaning given in claim 1; and (b) at least one fungicidal active ingredient selected from benomyl, carboxin, captan, chlorothalonil, copper oxychloride, cyprodinil, dimethomorph, dithianon, dodine, famoxadone, fenhexamid, fenpiclonil, fenpropimorph, fluazinam, mancozeb, metalaxyl, pyrimethanil, quinoxifen, sulfur, triforine, vinclozolin, a fungicidal triazole derivative, and a synthetic strobilurine derivative. The invention also provides a method of controlling the growth of phytopathogenic fungi at a locus by applying synergistically effective amounts of at least one azolopyrimidine of formula I and at least one fungicidal active ingredient (b) to the locus.

Abstract: Cascade esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment are also described.

Abstract: Compound of formula (I): wherein: n is 0, 1 or 2, R1 represents (C3-C11)cycloalkyl or (C3-C11)cycloalkylalkyl, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81, and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group.

Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I and salts thereof with pharmaceutically acceptable acids. Also disclosed are methods for making the derivative, and pharmaceutical compositions comprising the derivative. Methods for treating pain, migraine, and various other diseases using the pharmaceutical composition are also disclosed.

Abstract: Imidazonaphthyridine compounds that are unsubstituted at the 2-position induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract: The present invention provides phenyl urea and phenyl thiourea derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors, of formula (I) in which: Z represents oxygen or sulfur; and R1 to R7 represent various substituent groups; and pharmaceutically acceptable salts thereof. In particular, these compounds are of potential use in the treatment of obesity including obesity observed in Type 2(non-insulin-dependent) diabetes patients and/or sleep disorders.

Abstract: This invention relates to the compounds represented by the general formula [I], [in which A—D signify optionally substituted methine group(s) or nitrogen atom; E signifies oxygen or sulfur atom; signify optionally substituted mono- or bi-cyclic aliphatic nitrogen-containing heterocyclic group(s); R1 signifies lower alkenyl, lower alkynyl, cyclo(lower alkyl), lower alkanoyl, lower alkoxycarbonyl, optionally substituted lower alkyl and the like; and R2 signifies lower alkyl].

Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.

Abstract: Paroxetine is adsorbed on a carrier to form a free-flowing powder useful for capsule filling or for tablet formulation; and used in therapy to treat depression.

Abstract: The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I) wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each independently of the others, carbon or nitrogen atoms, the radicals Z denote, each independently of the others, a hydrogen atom, a halogen atom, a pseudohalogen, an optionally substituted alkyl, alkenyl, alkynyl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloaralkyl, cycloaralkenyl, cycloaralkynyl, aryl or alkoxy radical or an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and/or at least two of the radicals Z may be part of an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and to pharmaceutical compositions comprising at least one of the above-mentioned compounds, optionally in combination with carriers and/or adjuvants and/or excipients customary per se.

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: Disclosed herein are methods, kits, combinations, and compositions for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibiting agent (PPI) and a buffering agent in a pharmaceutically acceptable carrier.

Abstract: The present invention provides store operated calcium influx inhibitor compounds, pharmaceutical compositions, and methods of use. The compounds are useful for treating an inflammatory disease or treating an inflammatory reaction. Preferably, compounds, compositions and methods of this invention are used for treatment of inflammatory skin, pulmonary, musculoskeletal, and gastrointestinal diseases, as well as autoimmune disorders, transplantation treatment, and osteoporosis.

Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.

Abstract: The present invention relates to small molecules according to formula (I) that are potent inhibitors of &agr;L&bgr;2 mediated cell adhesion and which could be useful for the treatment of inflammatory diseases:

Abstract: A method for reducing post-ischaemic injury of the heart and/or improving the functional recovery of the heart following myocardial ischaemia which method comprises administration of an effective, non-toxic amount of a glucose uptake enhancer to a human or non-human mammal in need thereof.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2 , R3 and R4 are as defined herein.

Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: The present invention discloses a novel and improved pharmaceutical salt, nicotinate, of amlodipine having the following formula: The present invention also discloses methods for preparing and using the same.

Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of inflammatory bowel disease.

Abstract: The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.

Abstract: This invention provides compounds having the structure wherein A is OR5, or R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, R2 is H, alkyl, or aryl; R3 and R4 are halo, H, alkyl, aryl, trifluoromethyl, alkoxyaryl, nitro, amino, carboalkoxy, carbamide, carbamate, urea, alkylsulfonamide, —NR7(CH2)mCO2H, arylsulfonamide, cycloalkyl, or a heterocycle; R5 is H, alkyl, —CH(R8)R9, —CH2(CH2)nCO2R10, —C(CH3)2CO2R10, —CH(R8)(CH2)nCO2R10, —CH(R8)C6H4CO2R10, or —CH2-tetrazole; R6 is H, alkyl, halo, alkoxy, trifluoroalkyl or trifluoroalkoxy; R7 is H or alkyl; R8 is H, alkyl, aryl, arylalkyl, cycloalkyl, phthalic acid, R9 is CO2R12, CONHR12, tetrazole, or PO3R12; R10 is H, alkyl, aryl, or aralkyl; R11 is alkyl; R12 is H, alkyl, aryl, or aralkyl; X is O, or S; Y is O, N, or S; Z is C, or N; Q is O, N, or S; m=1-3; n=1-6, or a pharmaceutically acceptable salt thereof, which

Abstract: Group A streptogramin derivatives of formula (I) and salts thereof: Group A streptogramin derivatives of formula (II) and salts thereof: and Group A streptogramin derivatives of formula (III) and salts thereof: as well as processes for preparing such streptogramins, and pharmaceutical compositions comprising such streptogramins, alone or combined with at least one group B streptogramin derivative.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.

Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.

Abstract: Hydrophilic and lipophilic silibinin pro-forms and pharmaceutical compositions thereof, and methods of using compositions of silibinin pro-forms for topical or oral administration for treatment of disorders of cell proliferation, oxidative stress, sebaceous gland activity, and cardiovascular activity.

Abstract: The present invention relates to an antitumor derivative of double dicarboxylic acid diaminoplatin complex of formula (I): wherein R1 and R2 have the meanings defined in the specification, also relates to a process for preparation thereof, to an antitumor pharmaceutical composition containing the same, and further to application of the derivative in making antitumor pharmaceutics. The composition is a new generation of safe and effective antitumor drug, which has advantages such as low toxicity, broad antitumor spectrum, high antitumor activity, good solubility in water and fine stability in aqueous solution, selective killing of cancer cells without damaging normal cells, etc.

Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.

Abstract: This invention provides a means for preparing a monohydrate of the lithium salt of cis 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylate which is a novel composition of matter.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: This invention provides pharmaceutical compositions containing lipoxin compounds and therapeutic uses for the compounds in treating or preventing a disease or condition associated with columnar epithelial inflammation. The invention also discloses methods for screening for compounds useful in preventing columnar epithelial inflammation.

Abstract: A method of reducing exertion related muscle discomfort in a mammal is provided, in which a supplement containing a lactic acid salt is administered a specified period of time before exercising. A method of marketing a lactic acid salt supplement is also provided.

Abstract: A novel antimicrobial composition is disclosed including from about 60 to 95% of a lipophilic polar solvent such as propylene glycol, ethylene glycol, glycerol, or isopropanol and from about 0.5 to 5% of a mixture of C8 to C14 fatty acids. Other constituents of the present invention may include water, an alcohol (such as ethanol or propanol) or a mixture thereof. Also disclosed is a novel method of killing harmful microbes on the udder of a milk-producing animal using the above-mentioned composition.

Abstract: Methods and formulations for inducing substantially safer local anesthesia in a patient are provided. The methods comprise administering, to a patient in need thereof, a substrate containing a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material to safely obtain a reversible nerve blockade when implanted or injected in a patient.

Abstract: The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: A process is provided for the preparation of cyclohexene derivatives of general formula I or II: in which the substituents R1 and R2 independently of one another are defined as follows: R1 is R2 is OH or a protective group convertible to a hydroxyl group by hydrolysis; R3 and R4 are hydrogen or C1-C4-alkyl; and R5 is hydrogen or C1-C4-acyl, by the reduction of alkyne compounds of general formula III or IV: in which the substituents R1 and X are as defined above, wherein the reducing agent used is a mixture of zinc and at least one compound B selected from the group consisting of ammonium salts, copper salts and alkali metal and alkaline earth metal salts.

Abstract: A method for preparation of a semitransparent colloidal solution of bismuth sodium tartrate generally comprises producing an aqueous solution of bismuth sodium tartrate; extracting a magma of bismuth sodium tartrate from the aqueous solution at a pH of approximately 2.2; and then dissolving the magma into a salting-in mixture. It is critical that the magma be extracted at a pH of at least 2.2 but not more than 2.3. As a result, the magma is extracted by washing with a wash liquor comprising an addition of distilled water; allowing the magma to settle out of the wash liquor; measuring the pH of the wash liquor after the magma has settled; and then decanting the wash liquor from the magma. This process is then repeated as necessary to arrive at a magma within the critical pH range, whereafter the magma is air dried in preparation for salting-in. After addition of preservative and strength testing, the base solution is diluted to an elixir strength.

Abstract: The present invention relates to a process for preparing novel, monodisperse anion exchangers having strongly basic functional groups either in the center of the resin particle or in the shell of the resin particle, as well as to their use.

Abstract: A water-repellent composition for foaming process of a hydrophobic textile, comprising (A) a dispersion of a fluorine-containing polymer, (B) a foaming agent, and (C) a wetting agent is suitable for water-repellent treatment of the hydrophobic textile and can give easy generation of sufficient foaming.

Abstract: Disclosed are formulations adapted to form a foamed cementitious composition, the foamed cementitious composition itself, a method of forming a hydraulic binder foam, and a method of conveying and applying the resulting foam to a substrate. A pumpable cementitious slurry is formed, the slurry is mixed with a gas such as air, and is subjected to mechanically created turbulence to generate gas bubbles and create a foam, which preferably is stabilized by a foam stabilizing agent such as polyvinyl alcohol present in the slurry. The foam is then conveyed to a nozzle or other suitable dispense point from which it is applied, for example sprayed, preferably uniformly, onto a substrate to be coated. Prior to dispensing, a set accelerator is preferably injected, which causes the foam to gel, which in turn improves the hangability of the product on a substrate. The spray material adheres to the substrate and hardens to form an insulative coating on the substrate.

Abstract: Rigid polyurethane foams that can be produced at component volumes ratios of less than 4:1 are prepared from an isocyanate component that contains certain polyfunctional (meth)acrylate compounds. These isocyanate components are mixed with a polyol component to produce rigid foams. The foams are particularly suitable for foam-in-place applications, such as for reinforcing structural members of automobiles.

Abstract: The present invention relates to low impact resilience polyurethane form that has excellent deodorization property, hygroscopicity and contained carbon powder does not fall because the carbon powder of wide scope grading is dispersed and maintained in low impact resilience polyurethane form, and suitable producing of this low impact resilience polyurethane form; producing of low impact resilience polyurethane form that low impact resilience polyurethane form that carbon powder is dispersed and maintained, isocyanate ingredient and polyol ingredient that carbon powder which has over 1 &mgr;m particle diameter is dispersed previously are molded after blended, heated and foamed, and producing of low impact resilience polyurethane form that isocyanate ingredient, polyol ingredient and carbon powder which has 0.01˜1 &mgr;m particle diameter are molded after blended simultaneously, heated and foamed.

Abstract: An organopolysiloxane composition is provided including: (A) an organopolysiloxane with hydroxyl groups at both terminals of the molecular chain; (B) an organosilicon compound represented by the general formula shown below: wherein, R2 represents a hydrogen atom, a phenyl group or a halogenated phenyl group, R3 represents a hydrogen atom or a methyl group, R4 represents a monovalent hydrocarbon group, X represents a hydrolysable group, Z1 represents —R5—, —R5O— or —R5(CH3)2SiO— (wherein R5 represents a bivalent hydrocarbon group), Z2 represents an oxygen atom or a bivalent hydrocarbon group, m represents 0, 1 or 2, and n represents 0, 1 or 2; (C) a condensation curing catalyst; and (D) a photopolymerization initiator.

Abstract: Polypropylene having improved long chain branching increased melt strength obtained by irradiating polypropylene with an electron beam having an energy of at least 5 MeV and with a radiation dose of from 5 to 100 kGray in the presence of a grafting agent, the branching index of the obtained polypropylene being lower than 0.7.

Abstract: A method of manufacturing a polishing substrate is disclosed. The method includes disposing into a mold a reaction mixture of dibasic acid and a hydroxylated polymer, and applying a pressure and a temperature to the reaction mixture that are sufficient to cause polymerization and substrate formation in the mold. The dibasic acid is preferably adipic acid. Before pressure and temperature are applied to the reaction mixture, the reaction mixture is capable of being fortified with a polishing agent and/or a filler for controlling modulus and/or the coefficient of expansion.

Abstract: There is provided a rubber composition whose run-flat durability is improved and in which precipitation of sulfur and a vulcanization accelerator on the rubber surface before vulcanization is prevented. Sulfur in an amount of 2 to 8 parts by weight and two or more vulcanization accelerators in a total amount of at least 5 parts by weight based on 100 parts by weight of a rubber component are used, at least one of the accelerators being a sulfen amide accelerator.

Abstract: Polymers having increased hydrophilicity are made by adding to the polymer an effective amount of an additive which is a di-C10-12 fatty acid ester of polyethylene glycol.