Abstract: The present invention provides insecticidal polypeptides related to Bacillus Cry2 polypeptides. Nucleic acids encoding the polypeptides of the invention are also provided. Methods for using the polypeptides and nucleic acids of the invention to enhance resistance of plants to insect predation are encompassed.

Abstract: A pharmaceutical composition comprising peptide HA3G76 Tyr-Leu-Ser-Lys-Gly-Arg-Leu-Val-Phe-Ala-Leu-Gly (SEQ ID NO:8).

Abstract: Novel pseudopeptide analogs of the insect allatostatin neuropeptide family which possess biological activity mimicking that of the naturally occurring neuropeptides are disclosed. By addition of a hydrophobic moiety to an active portion of the allatostatin peptides, analogs are produced which exhibit an overall amphiphilic nature and which are capable of penetrating the insect cuticle while still retaining biological activity. Furthermore, by substituting sterically hindered amino acids or aromatic acids for any or all of the first, third or fifth amino acid residues of the allatostatin C-terminal pentapeptide, analogs may be produced which are resistant to degradation by insect peptidases while still retaining biological activity. The analogs may be used for insect control by disrupting critical reproductive and/or developmental processes normally regulated by allatostatins in insects.

Abstract: The subject invention provides methods and compositions for the treatment of benign tumors, cancers, neoplasias, and/or other inflammatory disorders or diseases. In the practice of the subject invention, and anti-convulsant agent, such as topiramate, is administered to an individual.

Abstract: Immunostimulatory polynucleotide-immunomodulatory molecule conjugate compositions are disclosed. These compositions include a polynucleotide that is linked to an immunomodulatory molecule, which molecule comprises an antigen and may further comprise immunomodulators such as cytokines and adjuvants. The polynucleotide portion of the conjugate includes at least one immunostimulatory oligonucleotide nucleotide sequence (ISS). Methods of modulating an immune response upon administration of the polynucleotide-immunomodulatory conjugate preparation to a vertebrate host are also disclosed.

Abstract: The present invention provides a peritoneal dialysis solution that contains heat stable osmotic agents such as D-glucitols, gluconic acids and alkylglycosides produced the reduction, oxidation or glycosylation of icodextrins respectively. As a result, osmotic agents that are stable under autoclaving or heat sterilization conditions are provided which reduces the amount of bioincompatible materials in the sterilized peritoneal dialysis solutions. Methods of preparing the D-glucitols, gluconic acids and alkylglycosides are disclosed.

Abstract: A fluid gel obtainable by a process which comprises subjecting a solution comprising a mixture of xanthan and one or more non-gelling polysaccharides selected from galactomannans or glucomannans in a solvent to shear while cooling the solution from a temperature above the gelation temperature of the mixture, and recovering the resulting continuous gel. The gel is useful in cosmetic and pharmaceutical compositions where it may, for instance, be generated in situ.

Abstract: The present invention relates to methods of use of aminodiphosphonate to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease states.

Abstract: A compound of formula (I):

Abstract: Polymeric delivery agents, delivery agent compounds and compositions comprising them which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: A method of making 1?-hydroxy-2-methylene-19-nor-homopregnacalciferol. The method includes the steps of condensing a bicyclic ketone with an allylic phosphine oxide to produce a protected 19-nor-pregnacalciferol analog, thereafter cleaving the protecting group to form 22-alcohol, converting the alcohol to an ester, reducing the ester to 17?-isopropyl-19-nor-vitamin D analog, and finally deprotecting the 17?-isopropyl derivative to form the desired compound.

Abstract: The present invention provides a crystalline halobetasol propionate selected from the group consisting of halobetasol propionate having crystalline Form I characterized by power X-ray diffraction peak positions and intensities as set forth in Table 1 herein, halobetasol propionate having crystalline Form II characterized by power X-ray diffraction peak positions and intensities as set forth in Table 2 herein, halobetasol propionate having crystalline Form III characterized by power X-ray diffraction peak positions and intensities as set forth in Table 3 herein, halobetasol propionate having crystalline Form IV characterized by power X-ray diffraction peak positions and intensities as set forth in Table 4 herein, halobetasol propionate having crystalline Form V characterized by power X-ray diffraction peak positions and intensities as set forth in Table 5 herein, and halobetasol propionate having crystalline Form VI characterized by power X-ray diffraction peak positions and intensities as set forth in Table 6

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).

Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.

Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens

Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.

Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R1–R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.

Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases , inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.

Abstract: The present invention provides piperazine derivatives of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in the description. They can be used for the treatment of obesity.

Abstract: A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Abstract: The present invention is directed to compounds 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: The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

Abstract: The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X1–X5 and R1–R5 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.

Abstract: In one aspect, the present invention provides a method of modulating an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with a modulator of the Edg-3 receptor sufficient to modulate the Edg-3 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating an Edg-3 receptor mediated biological activity in a subject. A therapeutically effective amount of a modulator of the Edg-3 receptor is administered to the subject. In yet another aspect, compounds and composition useful for modulation of the Edg-3 receptor are presented.

Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzoyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract: Benzotriazoles of formula I in which R1 to R8 have the abovementioned meanings and process for their preparation are described. The compounds show an inhibitory effect on hormone-sensitive lipase.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g.

Abstract: The present invention relates to compounds of formula I wherein R1, R2 and R3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.

Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor cells.

Abstract: The present invention relates to the new use of bradycardiac substances such as a Ca++ channel blocker, beta-receptor blocker or if channel blocker, the if channel blockers being preferred, optionally in combination with a cardioactive substance for inducing the regression of myocardial diseases accompanied by hypertrophy, particularly for the treatment of idiopathic hypertrophic cardiomyopathies (HCM) in humans and domestic pets.

Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.

Abstract: The present invention relates to fungicidally active compound combinations of a fluorobenzothiazole derivative of the formula (I) and at least one of the compounds listed in the disclosure.

Abstract: A microbicidal composition containing: (a) 2-methyl-4-isothiazolin-3-one; and (b) 2,2-dibromo-3-nitrilopropionamide.

Abstract: The present invention provides benzodifuran imidazoline derivatives and benzofuran imidazoline derivatives for lowering intraocular pressure and providing ocular neuroprotection.

Abstract: Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

Abstract: A compound having a xanthine oxidase inhibitory activity, such as 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid and the like, can be a drug for preventing cancer including colon cancer and the like, as an agent for suppressing tumorigenesis.

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: Methods of treating, managing or preventing psoriatic arthritis are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione alone or in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms are also disclosed.

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, a method of antagonizing endothelin, methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.

Abstract: The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.

Abstract: The invention includes a pesticidal compound comprising at least one organic phenolic compound and at least one salt comprising a divalent cation. Preferably, the organic phenolic compound is chosen from Carvacrol, thymol or combinations thereof; and is derived from a natural source, preferably extracted from a member of the family Labiatae or Verbenacea. Preferably the divalent cation is a transition metal salt and more preferably is zinc chloride or zinc sulfate. The invention also includes methods of eradicating, repelling or preventing infestations of pests, including such pests as insects, mites, ova, fungus, or parasites. The methods comprise the steps of preparing a pesticidal compound, combining it with a carrier, and applying it to the affected area.

Abstract: The present invention provides ethyl (?)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent ?3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Abstract: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC3,4.21.31) of the aryl guanidine type.

Abstract: Methods and compositions for preventing or treating Syndrome X are provided. The method includes administering a therapeutically effective amount of conjugated linoleic acid.

Abstract: The therapeutic agent for hepatitis, containing alanine and glycine, has only a slight toxicity and it can be administered either orally or intravenously to improve the liver function.