Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: The present invention provides an improved method for treating lung cancer, preferably non-small cell lung cancer, by orally administering UFT to postoperative lung cancer patients.

Abstract: The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: The present invention relates to substituted dihydropyrimidine inhibitors of calcium channel function having formula I where A, a, J, R1, R2 R3, R4, and R5, are defined herein; pharmaceutical compositions comprising said compounds; and methods of treating calcium channel-dependent disorders, including hypertension.

Abstract: A compound of formula: wherein Ar, Ar1, Ar2, R3–R6, R13, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopiperazine Compound”); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.

Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.

Abstract: Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.

Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) Wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions such as autoimmune diseases like transplant rejection or rheumatoid arthritis in a warm-blooded animal.

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

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: A compound of general formula 1 wherein R1, R5, R6, A, B, Y, i, j and m are defined as in the description and claims. It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.

Abstract: The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.

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

Abstract: Compounds of Formula (I), and their N-oxides and suitable slats, are disclosed which are useful as invertebrate pest control agents, wherein A and B are independently O or S; E is C or N; J is a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; K is taken together with the two contiguous linking carbon atoms to form a 5- or 6-membered nanoaromatic carbocyclic or heterocyclic ring optionally including one or two ring members selected from the group consisting of C(?O), SO or S(O)2, each ring optionally substituted with 1 to 4 R4; and R1, R2, R3, R4 and R5 are as defined in the disclosure.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

Abstract: Compounds of formula I: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's disease

Abstract: A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof Wherein X1 represents O or S; R1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3–5 membered cycloalkyl ring; R3 and R4 independently represent H, halogen, —CH3 and —OCH3; R5 represents H or C1-6 alkyl X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted.

Abstract: The present invention is directed to compositions comprising pramipexole and the use of such compositions to treat neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). As shown in FIG. 6B the mean +/? SEM serum 2,3-DHBA levels for the 12 ALS participants decreased significantly after pramipexole treatment.

Abstract: Novel isothiazolecarboxamides of the formula in which R is as defined in the description, a plurality of processes for preparing the novel compounds and their use for protecting plants against attack by undesirable microorganisms and animal pests.

Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.

Abstract: A method of modulating, sodium channels in warm-blooded animals in need thereof by administering a compound of the formula Wherein the substituents are defined as in the specification and compounds of the formula wherein the substituents are as defined in the specification.

Abstract: Process for the synthesis of compounds of formula (I): wherein R represents hydrogen or a protecting group. Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

Abstract: Process for the synthesis of compounds of formula (I): wherein R1 represents hydrogen, alkyl or benzyl and R2 represents a protecting group for the amine function. Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ----- represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1-WB- (in which, WA is substituted or unsubstituted aryl, etc., A1 is —NR1—, single bond, —C(O)—, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, —NH—, —OCH2—, alkenylene, etc., X is —C(O)—, —CH2—, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents —CH2—O—, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same.

Abstract: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.

Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.

Abstract: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: This invention provides estrogen receptor modulators having the structure where R1–R5 are as defined in the specification; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification.

Abstract: The present invention discloses methods of making a mixture of theaflavin, theaflavin-3-gallate, theaflavin-3?-gallate and theaflavin 3,3?-digallate, pharmaceutical compositions of the above mixture of theaflavins, diet supplement compositions of the above mixture of theaflavins and methods for using the above mixtures of theaflavin and pharmaceutical compositions thereof to treat or prevent various diseases. The present invention also discloses methods of making theaflavin, theaflavin-3-gallate, theaflavin-3?-gallate and theaflavin 3,3?-digallate, each as a separate compound, pharmaceutical compositions of the above compounds, diet supplement compositions of the above compounds and methods for using the above compounds to treat or prevent various diseases.

Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, SO2NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection

Abstract: Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.

Abstract: The objects of this invention are to prevent or ameliorate hypertension to improve physical constitution and finally to provide feeds, drinks, foods, health food supplements and pharmaceuticals which may be led to the prophylaxis or amelioration of life style related diseases. A prophylactic or ameliorating agent of hypertension comprising conjugated fatty acids (e.g., conjugated linoleic acid) as effective ingredients. A feed, food and drink, and health food supplement comprising the conjugated fatty acids described above. A pharmaceutical comprising the conjugated fatty acids described above. A method for prophylactic or ameliorating of hypertension in a mammal, which comprises administering to the mammal an effective amount of a conjugated fatty acid for preventing or ameliorating of hypertension in the mammal. Use of a conjugated fatty acid for preparing a pharmaceutical for prophylactic or ameliorating of hypertension.

Abstract: A method of stimulating or enhancing an ornithine-urea cycle in ruminant gut tissues, which entails either feeding to a ruminant an effective amount of a ruminant feed or feed supplement containing an effective amount of a compound which stimulates activity of one or more enzymes required in the ornithine-urea cycle.

Abstract: The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO2, CH2, C?O or COO; YZ represents a group of formula CH(R25)—CH(R26) or CH(R27)?(R28), and R1 to R28, identical or different, represent independently of one another, a hydrogen or halogen atom or an alkyl, cycloalkyl, CN, NO2, hydroxy, aryl, aralkyl, alkoxy, aryloxy, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, arylalkylamino, diarylamino diarylalkylamino, trihalogenoalkyl or trihalogenoalkoxy group, provided that in the group A1, at least one of the radicals R1, R2, R3, R4 or R5 represents the hydrogen atom when the other four do not represent the hydrogen atom and in the group B1, at least one of the radicals R13, R14, R15, R16 or R17 represents the hydrogen atom when the other four do not represent the hydrogen atom, and their salts with a pharmaceutically acceptable acid, in the form of racemic mixtu

Abstract: Preferred compositions used to inhibit the growth of bacteria, fungi and yeast include perillyl aldehyde as an active ingredient. Other active ingredients include perillyl alcohol. The compositions are formed as gels, creams, liquids and dry formulations.

Abstract: Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoprotein; and S-nitroso-immunoglobulin. The invention also relates to therapeutic use of S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body.

Abstract: Fischer-Tropsch process for the conversion of carbon monoxide and hydrogen to C5+ hydrocarbon mixtures in which process use is made of Fischer-Tropsch catalyst particles and fluid catalytic cracking (FCC) catalyst particles. The FCC catalyst can be a fresh FCC catalyst, or an equilibrium catalysts (E-cat).

Abstract: This invention relates to a polymerizable dental barrier material and method of making same including at least one high molecular weight polymer with reactive end groups having a concentration ranging from about 50 to about 99 percent by weight and a polymerization system.

Abstract: An antibacterial, antifouling paint for construction materials contains a coating resin composition and powdery metal-modified apatite. Part of metal atoms in the apatite crystal structure is provided by an optically catalytic metal. Preferably, the metal-modified apatite is a calcium hydroxyapatite which has part of its Ca atoms substituted by Ti.

Abstract: Systems and methods for providing smudge resistant and durable ink-jet images having good optical density are provided. Specifically, a system for printing durable ink-jet ink images can comprise a set of two ink-jet pens, preferably thermal ink-jet pens. The first ink-jet pen contains an ink-jet ink, wherein the ink-jet ink comprises a first liquid vehicle, from 0.5% to 6% by weight of a pigment colorant, and from 0.2% to 15% by weight of an anionic or neutral latex-containing colloidal suspension. The second ink-jet pen contains a fixer composition, wherein the fixer composition comprises effective amounts of second liquid vehicle, and from 0.2% to 15% by weight of a cationic polymer such as poly(vinyl pyridine) salts, polyalkylaminoethyl acrylates, polyalkylaminoethyl methacrylates, poly(vinyl imidazole); or preferably, polyethyleneimines, polybiguanides, and/or polyguanides.

Abstract: Novel, rapidly drying, low volatile organic compound (VOC), minimal dot gain coatings, (including lithographic ink and varnish systems) are herein described. These systems dry sufficiently rapidly, that their usage eliminates ink drying speed as the rate limiting factor in most lithographic printing applications. In addition to providing enhanced drying rates as compared with their conventional counterparts, the rapid drying, low/no VOC lithographic coating systems of the instant invention can provide the user with significant improvement in dried film rub resistance.

Abstract: A resin composition comprising a cyanate compound (A) having 2 or more cyanato groups in the molecule; a phenol compound (B); a silicone polymer (D) having at least one siloxane unit selected from the group consisting of a tri-functional siloxane unit represented by the formula RSiO3/2 and tetra-functional siloxane unit represented by SiO4/2, polymerization degree of 7,000 or less, and at least one terminal functional group reactive with hydroxyl group; and inorganic filler (E).