Abstract: The present invention is directed to novel G protein-coupled receptors that are found predominantly in the dorsal root ganglia. The invention encompasses both the receptor proteins as well as nucleic acids encoding the proteins. In addition, the present invention is directed to methods and compositions which utilize the receptors.

Abstract: New antifibrillogenic agents and compositions containing same, methods of using the antifibrillogenic agents and compositions for inhibiting amyloid fibril formation, and effective therapeutics for preventing or delaying the progression of, e g., Alzheimer's disease and diabetes.

Abstract: Disclosed are glycosides, orthoester glycosides and glycuronamides of fluoxetine and analogs thereof to treat conditions and diseases such as depression.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic

Abstract: The present invention relates to the use of peracylated N-acyl-mannosamine derivatives for the preparation of a medicament for stimulating neurite growth.

Abstract: Methods of treating an individual who has a disease or disorder associated with one or more genetic mutations or undesirable alleles in genomic DNA of the individual, or preventing an individual from developing a disease or disorder associated with one or more genetic mutations or undesirable alleles in genomic DNA of the individual, by replacing a segment of genomic DNA that has a mutated sequence or undesirable allele with a corresponding segment of DNA that has a non-mutated sequence or desirable allele, are disclosed. Methods of inducing tolerance and preventing transplant rejection in a recipient, methods of inducing tolerance and or reducing allergies are disclosed and method of increasing fertility in a woman are disclosed. Each of the methods comprises replacing a segment of genomic DNA in an individual with a corresponding segment of DNA from another. An apparatus for doing large scale PCR preparations is disclosed.

Abstract: Dendritic cells play a critical role in antigen-specific immune responses. Materials and methods are provided for treating disease states, including cancer and autoimmune disease, by facilitating or inhibiting the migration or activation of antigen-presenting dendritic cells. In particular, chemokines are used to initiate, amplify or modulate an immune response. In one embodiment, chemokines are used to attract dentritic cells to the site of antigen delivery. An increase number of dendritic at the site of antigen delivery means more antigen uptake and a modified immune response.

Abstract: An intracellular calcium concentration increase inhibitor containing as the active ingredient (1) a boron compound represented by the formula (I). The compound represented by the formula (I) inhibits the increase of the intracellular calcium concentration, and therefore it is deemed to be useful as an agent for the prophylaxis and/or treatment of platelet aggregation, ischemic diseases in hearts and brains, immune deficiency diseases, allorgosis, bronchial asthma, hypertension, cerebrovascular spasm, various renal diseases, pancreatitis, Alzheimer's disease, etc.

Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.

Abstract: The present invention provides 8-(2-hydroxyphenoxy)octyldiethanolamine) and salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same. The delivery agents of the present invention are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals.

Abstract: The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.

Abstract: The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the treatment of Parkinson's disease.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the ihibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

Abstract: There is provided substantially crystalline forms of 4-({3-[7-(3,3-dimethyl-2-oxobutyl) -9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]propyl}amino)benzo-nitrile; tert-butyl 2 -{7-[3-(4-cyanoanilino)propyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate; tert-butyl 2-{7-[4-(4-cyanophenyl)butyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl}ethylcarbamate; or tert-butyl 2-{7-[2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cardiac arhythmias.

Abstract: The invention relates to Tetracyclic Benzamide Derivatives; compositions comprising a Tetracyclic Benzamide Derivative; and methods for treating or preventing an inflammatory disease, a reperfusion disease, an ischemic condition, renal failure, diabetes, a diabetic complication, a vascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Benzamide Derivative.

Abstract: Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.

Abstract: The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R1 to R3 and n are defined as in claims 1 to 8, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various GSK-3-mediated disorders, such as diabetes and Alzheimer's disease.

Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds-are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.

Abstract: Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain

Abstract: Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.

Abstract: Methods of inducing immune tolerance by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed: Additionally methods of suppressing an immune response by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed. Further disclosed are methods for treating autoimmune diseases by administering an immunosuppressive agent and a compound represented by Formula (I). The variables of Formula (I) are described herein.

Abstract: The present invention relates to 1,3,8-triara-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.

Abstract: The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Abstract: An objective of the present invention is to provide compounds having Rho kinase inhibitory activity. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: Het—X—Z??(I) wherein Het represents a monocyclic or bicyclic heterocyclic group containing at least one nitrogen atom, for example, pyridyl or phthalimide; X represents group (i) —NH—C(?O)—NH—Q1-, group (ii) —NH—C(?O)—Q2-, wherein Q1 and Q2 represent a bond, alkylene, or alkenylene, or the like; and Z represents hydrogen, halogen, a monocyclic, bicyclic, or tricyclic carbocyclic group, a heterocyclic group or the like, for example, optionally substituted phenyl.

Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.

Abstract: The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: —C(W)?C(R3A)—N(R3)—, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting ?3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.

Abstract: Disclosed herein is compound 1 or a pharmaceutically acceptable salt, or a prodrug thereof. Compound 1 is useful for treating or preventing a variety of diseases or conditions. Results presented herein also demonstrate that Compound 1 is a prostaglandin D2 antagonist, and as such is useful in the treatment or prevention of prostaglandin D2 mediated conditions or diseases. A method comprising administering a prostaglandin D2 antagonist to a mammal suffering from a disease or condition selected from the group consisting of the gastrointestinal tract disorders or diseases, hyperalgesia, allodynia, abdominal cramping, glaucoma, ocular hypertension, and ocular hypotension is also disclosed herein. Pharmaceutical compositions and products comprising compound 1 are also disclosed.

Abstract: The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them.

Abstract: A novel class of 3-oxo-3H-benzo[d]isoxazole carboxamide compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases.

Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

Abstract: Substituted indoles of the formula I, a process for the production of such compounds, pharmaceutical preparations containing these compounds and the use of these compounds for alleviating pain.

Abstract: The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula: Wherein substitutions at R1, R2, R3—R12, and Y are set forth in the specification.

Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.

Abstract: ACE inhibitor nitroderivatives of formula (I): A—(X1—ONO2)s ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating cardiovascular and renal diseases and inflammatory processes.

Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate cancer.

Abstract: The invention, at least in part, is directed to methods for enhancing delivery of therapeutic agents, such as macromolecules and drugs, into the interior of tissues, such as solid tissues or tumors. The method initially uses an apoptosis inducing agent, such as paclitaxel, in doses which create channels within the tissues, and enhance the penetration of therapeutic agents to the interior of the tissue. Current methods of treating tissues are often not effective because the therapeutic agents are not delivered to the interior of the tissue. By using the methods and the compositions of the current invention, therapeutic agents can be delivered to the interior of the tissue.

Abstract: The invention provides compounds for use in photochemotherapy or diagnosis, said compounds being branched alkyl esters or substituted alkyl esters of 5-aminolevulinic acid, or derivatives or pharmaceutically acceptable salts thereof. In particular, the invention provides compounds of formula (I): R22N—CH2COCH2CH2CO—OR1 (wherein R1 represents an optionally substituted branched alkyl (e.g.

Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.

Abstract: Disclosed are multibinding compounds which are ?2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Carbonyl scavengers, which have been recognized for their ability to react with reactive carbonyl species, have been implicated as agents that can accelerate or induce the death of abnormal cells without having a parallel effect on normal cells. As such, they are useful therapeutic agents in cases where the acceleration or induction of cell death is desirable, such as in cells where the normal apoptotic pathways have been disrupted and where hyperproliferative cell growth occurs.

Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: Fischer-Tropsch synthesis is performed using a compact catalytic reactor unit (10) defining channels in which is a gas-permeable catalyst structure (16), the channels extending between headers (18). The synthesis occurs in at least two stages, as the reactor unit provides at least two successive channels (14, 14a) for the Fischer-Tropsch synthesis connected by a header, the gas flow velocity through the first channel being sufficiently high that no more than 65% of the carbon monoxide undergoes conversion. The gases are cooled (25) in the header between the two stages, so as to condense water vapor, and then pass through the second channel at a sufficiently high gas flow velocity that no more than 65% of the remaining carbon monoxide undergoes conversion. This lowers the partial pressure of water vapor and so suppresses oxidation of the catalyst.

Abstract: Sulphonic fluorinated ionomers crosslinked by radical crosslinking of: A) crosslinkable sulphonic fluorinated ionomers, having equivalent weight 380–1300 g/eq and comprising: from 48% to 85% by moles of monomeric units deriving from tetrafluoroethylene (TFE); from 15% to 47% by moles of fluorinated monomeric units containing sulphonyl groups —SO2F; from 0.01% to 5% by moles of monomeric units deriving from a bis-olefin of formula: wherein: m=2–10, preferably 4–8; R1, R2, R5, R6, equal to or different from each other, are H or C1–C5 alkyl groups; B) a fluorinated compound as crosslinking radical initiator; C) a fluorinated bis-olefin of structure (I) as crosslinking agent; the radical crosslinking being carried out at a temperature in the range 250° C.–310° C., preferably 260° C.–300° C.

Abstract: A curable ink for jet-ink recording comprising a white pigment and a polymerizable compound, wherein the polymerizable compound is a compound selected from the group consisting of: (a) oxetane compounds; (b) pyrrole or substituted pyrroles; (c) aniline or substituted anilines; and (d) thiophene or an substituted thiophenes, provided that when the polymerizable compound is the oxetane compound, the curable ink further comprises an epoxy compound or a vinyl ether compound.