Abstract: Compounds of the following formula (I): where A, a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Adjuvants selectes from mon/ionic water/soluble mixed polyalkoxy-lated aliphatic alcohol surfactants, non ionic water soluble ethoxylated aliphatic alcohol surfactants, amine ethoxylates, and micronized polymeric waxes enhance the efficacy of fungicidal triazolopzrimidines of structural formula I. They can be incorporated into formulations of the fungicidal compounds or be added to spray mixtures (tank mix) as separately formualted additives in order to improve the efficacy and spectrum of these fungicides.

Abstract: Compounds of Formula (I) 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: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: A pyrimidine derivative of formula (I) wherein, for example, R1 is hydrogen, (1–6C)alkyl, (3–5C)alkenyl or (3–5C)alkynyl; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bears on any available carbon atom one substituent of formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH— link]; wherein, for example, X is CH2, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH2, (1–4C)alkoxy, (1–4C)alkylthio, —NH(1–C)alkyl, —N[(1–4C)alkyl]2 or —NH—(3–8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may optionally bear other substituents selected, for example, from halogeno, (1–6C)alkyl, cyano and (2–4C)alkenyl; or a pharmaceutically-acceptable salt or in-vivo-hydrolyzable ester thereof; are useful as anti-cancer agents; and processes for heir manufacture and pharmaceutical compositions containing them are described

Abstract: The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.

Abstract: The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.

Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N? atom or a —N(Rb)—, —C(Rb)? or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase mediated diseases or disorders, such as rheumatoid arthritis

Abstract: A compound represented by the formula: [wherein R1 is methoxy, methylthio, ethyl, etc.; R5 and R6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and two of R40, R41 and R42 are C1-6 alkoxy while the remaining one is methoxymethyl, etc.], a salt thereof, or a hydrate of the foregoing. This compound has excellent antagonism against corticotropin-releasing factor receptor.

Abstract: An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.

Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.

Abstract: There is provided an acid addition salt of (?)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (?)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (?)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity that affects the use as a drug or its drug substance, and is very useful as a drug or its drug substance.

Abstract: An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

Abstract: A method for manufacturing a pharmaceutical composition having uniform drug distribution and potency is described which utilizes silicon dioxide to reduce the loss of active ingredient during the manufacturing process. The method is particularly useful for the manufacture of low dosage tablet compositions.

Abstract: The present invention provides intermediates, synthetic methods and novel urea compositions of matter.

Abstract: Process for the synthesis of 5-(3-pyridylmethyl)imidazolidine-2,4-dione, according to which 5-(3-pyridylmethylene)imidazolidine-2,4-dione is subjected to a hydrogenation reaction.

Abstract: Novel compounds that are modulators of PPAR receptors, and pharmaceutically acceptable salts, solvates and hydrates thereof, processes for making the compounds, pharmaceutical compositions containing the compounds, or pharmaceutically acceptable salts, solvates and hydrates thereof

Abstract: This invention provides compounds of the formula: wherein A?, X and Y are defined in the specification. These compounds are useful as antibacterial agents.

Abstract: This invention relates to crystal form II of 2-[2-(1-chlorocyclopropyl)-3-(2-chloropenyl)-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione of the formula to a process for its preparation and to its use for controlling unwanted microorganisms.

Abstract: Novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism, and cancer metastasis include compounds represented by the following general formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof: wherein each of n1, n2, and n3 is an integer of 1; each of R1, R2, R3, R4, R5, and R6 is independently a hydrogen atom; A1 is imidazole; A2 is imidazole or imidazole substituted with an alkyl group; W is a phenyl group or naphthyl group; X is CH2; D is a group represented by -Q-Y—B, wherein Q is NR12 and R12 is a hydrogen atom or an alkyl group; Y is (CH2)m3 and m3 is an integer of 2 to 4; and B is N(R25R26), wherein each of R25 and R26 are independently a hydrogen atom, a C1–C6 alkyl group or a C3–C6 cycloalkyl group.

Abstract: The invention relates to biphenylcarboxamides of the formula (I) in which A, R, Z, X, Y, m and n are each as defined in the disclosure, to a plurality of processes for preparing these substances, to their use for controlling undesirable microorganisms, and to novel intermediates and their preparation.

Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

Abstract: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5?-hydroxymethyl-2?-furyl)indazole (YC-1), and their anti-platelet activity.

Abstract: The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.

Abstract: The present invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione.

Abstract: This invention relates to the methods and pharmaceutical compositions for treating diseases or disorders associated with oxidative stress and/or genomic instability. In particular, the invention relates to methods for treating ataxia-telangeictasia (AT) and such disease states by administering a therapeutically effective amount of a chelating agent to increase genomic stability and/or decrease oxidative stress.

Abstract: The compound of the formula (I): wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together a saturated heterocyclic ring or amino acid residues; and non-toxic salts thereof and acid addition salts thereof.

Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).

Abstract: Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

Abstract: This invention relates to methods and compositions for modulating movement of eukaryotic cells with migratory capacity. More specifically, the invention relates to methods and compositions for modulating movement of CaR receptor expressing cells of hematopoietic, neural, epithelial, endothelial, or mesenchymal origin, in a specific site in a subject. The foregoing are useful, inter alia, in the treatment of conditions characterized by a need to modulate migratory-cell movement associated with specific sites in a subject. Specific sites include sites of inflammation and modulation of migratory-cell movement is movement away from an agent source, or repulsion. The invention also relates to methods for manipulating hematopoeitic progenitor cells and related products.

Abstract: The invention provides a method and compositions for controlling food borne enteric bacterial pathogens in animals. Populations of enteropathogenic bacteria may be substantially reduced or eliminated by treatment of animals with an effective amount of 2-nitropropanol, 2-nitroethane or 2-nitroethanol. The compounds may be administered orally, providing a reduction in the populations of the enteropathogenic bacteria in the alimentary tract of the animal, or they may be applied externally onto the animal to reduce the populations of any such bacteria which may be present as contaminants on the surface of the animal. The method and compositions are particularly useful for the control of Salmonella species, enteropathogenic Escherichia coli, Campylobacter species, and Listeria monocytogenes.

Abstract: Mesoscopically ordered, hydrothermally stable metal oxide-block copolymer composite or mesoporous materials are described herein that are formed by using amphiphilic block polymers which act as structure directing agents for the metal oxide in a self-assembling system.

Abstract: A process for thermochemical conversion of heavy oil and petroleum coke to fluid fuels includes the steps of: providing a fossil fuel selected from the group consisting of heavy oil, petroleum coke and mixtures thereof; and exposing the fossil fuel to an external source of concentrated radiation so as to increase the temperature of the fossil fuel, supply high-temperature heat required for the desired endothermic conversion process, and convert the fossil fuel to a product selected from the group consisting of hydrogen, carbon monoxide, gaseous hydrocarbons and mixtures thereof.

Abstract: A water insoluble interpenetrating polymer network is obtained by independently cross-linking a first polymer derived from a sulfonic acid or phosphonic acid group containing alkenyl monomer and a second polymer polymerized independently of the first polymer and interpenetrating the first polymer, where the second polymer is selectively permeable to water compared to methanol. Through adjustment of the degree of first polymer monomer acidification, polymer ratios and the extent of cross-linking in the at least two interpenetrating polymers, ion conductivity and solvent permeability are controlled. A film produced from such a water insoluble interpenetrating polymer network is well suited as a membrane in a direct methanol fuel cell. The relative degree and mechanism of cross-linking and interpenetrating the first polymer and second polymer are also adjustable parameters that impact on film properties.

Abstract: This invention pertains to inkjet inks, in particular to smear resistant inkjet inks, and even more particularly to smear resistant pigmented aqueous inkjet inks comprising polyurethane dispersion binders and self-dispersing pigments.

Abstract: The invention provides an aqueous ink composition, which comprises at least: 1) an alkali neutralized product of a copolymer containing constituent units of: (i) at least one monomer selected from the group consisting of alkene, styrene, styrene derivatives, vinyl naphthalene, and vinyl naphthalene derivatives; (ii) at least one monomer selected from monomers containing an acidic group that ion dissociate; and (iii) at least one ?,?-ethylenic unsaturated carboxylic acid alkyl ester; 2) a pigment; and 3) an aqueous medium, wherein the alkali neutralized product of the copolymer in the aqueous ink composition forms micelle aggregations with an average diameter being set in the range of 10 nm to 300 nm. A manufacturing method of the aqueous ink composition and an image forming method using the aqueous ink composition are also provided.

Abstract: A non-vinylidene fluororesin powder coating material having blocking resistance and high impact resistance, is provided. A fluororesin powder coating composition comprising a non-vinylidene fluororesin having a Tg higher than 40° C. and a resin having a Tg of from 0 to 40° C.

Abstract: The present invention provides polymeric compositions containing thermoplastic starch and a thermoplastic polymer incompatible with starch, in which the starch constitutes the dispersed phase and the thermoplastic polymer constitutes the continuous phase, selected: A) from compositions comprising an agent with an interfacial effect selected from esters of polyols with mono- or polycarboxylic acids with dissociation constants within certain limits, the esters having specific values of the hydrophilic/lipophilic balance index HLB or being amongst the non-ionic surfactants which are soluble in water but cannot significantly be extracted by water from the compositions which contain them; B) from compositions wherein the thermoplastic polymer is an aliphatic or aliphatic-aromatic copolyester wherein the ratio (R) between the average viscometric molecular weight and the melt index is greater than 25,000 and C) from compositions wherein the thermoplastic polymer is selected from aliphatic-aromatic copolyesters, poly

Abstract: A solid phosphite composite, having at least a portion in amorphous form, which includes at least one, preferably two or more phosphite antioxidants or alternatively at least one phosphite and at least one other polymer additive. The phosphites, at least one of which can initially be a liquid, are generally uniformly distributed since they are melt blended. A desired class of phosphites are the bis(arylalkylphenyl)pentaerythritol diphosphites, at least a portion of which is in amorphous form.

Abstract: A jettable non-curable support material composition useful for three-dimensional ink jet printing comprising at least one fatty alcohol and at least one abietic rosin ester alcohol, wherein the support material has a melting point between about 50° C. to about 65° C. and a freezing point between about 45° C. to about 55° C.

Abstract: Novel sizing compositions, their preparation and use. The compositions contain water-dispersible and/or water-soluble and alkylamine-blocked polyisocyanates, film-forming resins, coupling agents and lubricants. The isocyanates are synthesized from at least one polyisocyanate, at least one ionic and/or potentially ionic and/or nonionic compound, and at least one blocking agent which is at least 20% by weight aralkylamines.

Abstract: The present invention relates to a process for preparing dye-comprising aqueous polymer dispersions by free-radical aqueous emulsion polymerization of ethylenically unsaturated monomers in the presence of free-radical initiators, in which at least some of the monomers are employed in the form of an oil-in-water emulsion E1 whose disperse phase comprises at least one oil-soluble dye, wherein the disperse phase of E1 is formed essentially of dye-comprising monomer droplets having a diameter<500 nm. The present invention relates in addition to dye-comprising formulations which comprise the dye-comprising polymers of the invention and to pigmented formulations which comprise a polymer of the invention comprising optical brightener.

Abstract: Crosslinked polymer compositions comprise a first synthetic polymer containing multiple nucleophilic groups covalently bound to a second synthetic polymer containing multiple electrophilic groups. The first synthetic polymer is preferably a synthetic polypeptide or a polyethylene glycol that has been modified to contain multiple nucleophilic groups, such as primary amino (—NH2)or thiol (—SH) groups. The second synthetic polymer may be a hydrophilic or hydrophobic synthetic polymer which contains, or has been derivatized to contain, two or more electrophilic groups, such as succinimidyl groups. The compositions may further comprise other components, such as naturally occurring polysaccharides or proteins (such as glycosaminoglycans or collagen) and/or biologically active agents.