Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel phosphonic acids derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel phenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing neurodegenerative disorders.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing diabetes mellitis, optionally in combination with a second treatment. Furthermore, the present invention also provides methods of inducing remission of the symptoms of diabetes mellitis in a patient comprising administering a thiazolidinedione analogue and a GLP-1 agonist.

Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing obesity or diabetes, optionally in combination with a second treatment therapy such a diet restriction or an increase in duration or exertion in physical activity.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.

Abstract: The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.

Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Abstract: The present invention relates to the general field of the treatment and prevention of diseases involving an inflammatory condition, namely sepsis or infectious or viral diseases as well as diseases requiring for the of treatment an immunosuppressive activity namely autoimmune diseases and graft rejection. In particular, the invention relates to an inhibitor of the activity or the formation of the PP1/GADD34 complex for the treatment of a condition requiring an immunosuppressive activity or an anti-inflammatory activity.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: A topical skin barrier for protecting and promoting healing of skin, and for providing comfort to a patient, comprises a semi-solid hydrocarbon, a water-absorbing compound, and a pain relief agent. The topical skin barrier effectively adheres to skin, affords protection from moisture and waste, provides transparency in use, and is anhydrous and therefore is preservative-free. Methods of in vitro evaluation are for (i) a composition's protection from moisture and waste, and (ii) a composition's adhesion to skin.

Abstract: A method for treating the symptoms of multiple sclerosis and related neurodegenerative conditions, using a histamine compound that is methylated in vitro prior to being introduced into the body of the patient. The histamine compound is suitably histamine diphosphate, and may be methylated in vitro by mixing in combination with at least one thiol compound in the presence of at least one methyl group donor compound. The thiol compound is suitably L-reduced glutathione and the methyl group donor is suitably betaine hydrochloride. The compounds are mixed vigorous in an acid environment, to create a shearing force that facilitates exchange of the methyl group from the donor compound to the histamine diphosphate. The resulting methylated histamine compound is suitably administered to the patient by transdermal application. The method also provides a medicament for treatment the symptoms of multiple sclerosis and related neurodegenerative conditions, and a method for preparation of such a medicament.

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The invention relates a pharmaceutical composition comprising a combination of (i) the AT 1-antagonist valsartan or a pharmaceutically acceptable salt thereof and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of selected conditions or diseases.

Abstract: Certain substituted benzylamino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, and R4 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: The present invention relates to novel phosphonic acids derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: Methods of treating hypertension, pain, and resuscitative hemorrhagic shock using an adrenergic agent, like centhaquin, are disclosed. The methods treat mammals, including humans.

Abstract: Methods of treating diabetic ketoacidosis are disclosed. The methods utilize an endothelin antagonist to treat diabetic ketoacidosis in mammals, including humans.

Abstract: The present invention relates to the use of a protein phosphatase inhibitor selected from an inhibitor of the catalytic subunit of the protein phosphatase 1 (PP1), an inhibitor of GADD34 and an inhibitor of the PP1/GADD34 complex to prepare a pharmaceutical composition to prevent or treat a cancer in a mammal, wherein the pharmaceutical composition is intended for administration in combination with a product used in a treatment of a cancer.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.

Abstract: Concentrated microemulsions comprising: 1) 10-25 parts by weight of a pesticide with a solubility in water at 20° C. lower than 1% l by weight and having a melting point from 10° C. to 60° C.; 2) 8-25 parts by weight of one or more solvents containing oxygen atoms, having a solubility in water at 20° C. lower than 5% by weight and the Hildebrand solubility parameter in the range 16-21 MPa1/2; 3) 10-20 parts by weight of a polyol; 4) 10-25 parts by weight of one or more non ionic surfactants having a HLB value from 9 to 15; 5) 2-10 parts by weight of one or more anionic surfactants; 6) water up to 100 parts by weight; wherein—the ratio by weight between 2) and 1) ranges from 0.8:1 to 1.5:1;—the ratio by weight between 4) +5) and 1) is in the range 0.5:1-3:1;—the ratio by weight between 4) and 5) ranges from 1:1 to 4.1.

Abstract: A compound having a formula II(a): wherein R1 and R2 are hydrogen lower alkyl, lower aliphatic acyl, or lower alkoxycarbonyl; R4 is C1-C4 alkyl; n is 2 or 3; X is a formula ?N-D, wherein D is hydrogen, C1-C6 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2—, —CH(OH)—CH2— or phenylene; Z is C1-C6 alkylene; R5 is C3-C10 cycloalkyl or C6-C10 aryl; R6 and R7 are hydrogen, lower alkyl, halogeno lower alkyl, lower alkoxy or lower alkylthio; and R10 and R11 are hydrogen or lower alkyl.

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.

Abstract: A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.

Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.