Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

Abstract: The present invention relates to a class of compounds having specific quaternized amine based upon a dimer acid amido amine linked to specific phosphate esters. Dimer acid is a C-36 diacid having a cyclic structure and two amine groups that allow for the synthesis of a high molecular weight material quaternary compound which is extremely substantitive to human skin and are well tolerated by human tissue making them suitable for use preparation of barrier products for personal care applications.

Abstract: Disclosed is a porous film made of a resin composition containing (I) (i) a propylene-ethylene copolymer or (ii) a polypropylene-based resin mixture containing a propylene-ethylene copolymer, each having an ethylene content of 3.0 to 7.0 wt. % and an MFR measured at 230° C. of 2.0 to 4.0 g/10 min and (II) a ?-crystal nucleating agent; the film having a porosity of 20 to 80%, a Gurley air permeability of 5,000 sec/100 cc or lower as measured according to JIS P-8117, a water vapor permeability of 2,000 g/m2·24 h or higher as measured according to JIS Z-0208 and a water pressure resistance of 75 kPa or higher as measured according to JIS L-1092 using an aqueous surfactant solution; a process for producing the same; and an absorbent article employing the porous film as a backsheet.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.

Abstract: The object of the invention is to provide a diphenylsquarylium compound which has a sharp minimum value within the wavelength range of from 550 to 610 nm in the light transmittance curve and from which a filter causing no reduction of brightness of the visual field can be obtained when used by containing in a filter for display, and a filter for display which contains this diphenylsquarylium compound. Constructions of the invention are a diphenylsquarylium compound represented by the following general formula (I) and a filter for display which contains this diphenylsquarylium compound.

Abstract: The invention relates to compounds of formula (1) 1

Abstract: Compounds having the formula (I), 1

Abstract: A 4-membered compound is represented by the following formula (I) is disclosed (in the formula, X1 and X2 each independently represent an oxygen atom, a sulfur atom or a substituted or unsubstituted imino group, Y1 and Y2 each independently represent a single bond, an oxygen atom or a substituted or unsubstituted imino group, B1 and B2 each independently represent an optionally substituted aliphatic, aliphatic carbonyl, aromatic or aromatic carbonyl group having 1-20 carbon atoms, and A1 and A2 each independently represent a group represented by the following formula (II) (Ar1, Ar2 and Ar3 each independently represent a cyclic group having 5-14 carbon atoms, L1 and L2 each independently represent a single bond or a divalent linking group, and p represents an integer of 0-2)). There is also disclosed a birefringence medium containing a 4-membered compound represented by the formula (I) and an optical element comprising the birefringence medium.

Abstract: Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.

Abstract: A process comprising the steps of a) reacting in an esterification reaction (i) a plurality of different plyols with; (ii) a plurality of different polycarboxylic acids and/or precursors therefor; in a manner to retain a plurality of free hydroxy groups in the resultant polyester(s) and retain substantial amounts of un-crosslinked polyesters in the resultant product; followed by b) reacting substantially all of the free hydroxy groups present in the resultant mixture of polyesters with an acrylating agent; to form a mixture having a hydroxy (OH) number (measured using ASTM E222-73) of no more than about 100 mg KOH/g. Use of the mixture as a composition for lithographic or flexographic inks.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I 1

Abstract: The present invention is directed to polymeric prodrug transport forms and methods of making and using the same. In one preferred aspect, the prodrugs are of the formula: wherein G is a polymeric residue; Z is one of: and B is a residue of a biologically active amine-containing moiety or a hydroxyl-containing moiety.

Abstract: Universal supports for oligonucleotide synthesis include a support material represented by the following formula: In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl, or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.

Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: The present invention describes compounds of the general formula I 1

Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.

Abstract: Diaminodicarboxylic acid:peptide gemini surfactant compounds are disclosed. Uses of the diaminodicarboxylic acid: peptide-based gemini surfactant compounds and methods for their production are also disclosed.

Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.

Abstract: The present invention provides a series of compounds having structural formulas 1

Abstract: Compounds of the formula I, 1

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: A compound of the formula (I):

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: A magnetic circuit component having a plurality of claws arranged in a plurality of rows, with the base of each claw connected to a common yoke. A plurality of non-interlaced coils constituting a multi-phase winding are included, with the coils being wound around the bases of corresponding claws, and being distributed uniformly in the direction of motion.

Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.

Abstract: The present invention is directed to a process for the synthesis of monoalkylated C—H acidic methylene group-containing compounds, such as malonic esters, and malonic ester nitriles.

Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.

Abstract: Biphenyl derivatives represented by the following formula (1): 1

Abstract: The present invention relates to compounds of formula (I): 1

Abstract: A composition is provided comprising a novel cationic lipid compound having hydrophobic tails and two quaternary ammonium headgroups bridged by a linker. The composition is useful as a cytofectin for facilitating delivery and transfection of biologically active agents, particularly anionic bioactive agents such as DNA, into cells. The composition is useful also as an adjuvant for enhancing the humoral immune response of a vertebrate to an immunogen, especially an immunogen encoded by a polynucleotide-based vaccine. In certain preferred embodiments, the cationic lipid compound is a dimer containing quaternary ammonium headgroups bridged by a linker having DNA and/or cell receptor binding affinity, such as a polypeptide or polyamine. Also disclosed is an immunogenic composition comprising an immunogen and the composition of the present invention.

Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.

Abstract: In accordance with the present invention, there are provided thermosetting resin compositions with a reduced propensity to shrink in volume upon cure and methods of use therefor. The compositions of the present invention include compounds having aromatic, rigid-rod like spacer groups between the crosslinkable moieties. As such, these compounds impart a degree of liquid crystal-like character to the thermosetting resin composition which results in lower shrinkage upon cure. This effect follows from the well-known expansion that occurs when liquid crystal-like materials pass from a nematic liquid crystal-like state to an isotropic state. Further provided by the present invention are low shrinkage die attach pastes and methods of use therefor.

Abstract: Aminobutylic acid derivatives of the formula (I): 1

Abstract: A method of synthesis of dinitro-diaza-alkanes and intermediate products thereto from alkylamines and esters, whereby a dialkyl ester of a dicarboxylic acid is reacted with an alkylamine in an aqueous medium to form the corresponding dialkyldiamide of the dicarboxylic acid; the resulting dialkyldiamide is nitrated by means of conventional nitration agents to form the corresponding dialkyldinitroamide of the dicarboxylic acid and; the resulting dialkyldinitroamide is reacted with methylamine and/or ethylamine in an aquous medium to yield a corresponding alkylnitroamine and the dimethyldiamide and/or diethyldiamide of the dicarboxylic acid, and the alkylnitroamine is isolated from that, and the isolated alkylnitroamine is condensed in a known manner to form the dinitro-diaza-alkanes.

Abstract: The invention relates to novel Acyl coenzyme-A mimics, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The Acyl coenzyme-A mimics, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, bacterial infection and impotence. In certain embodiments, the Acyl coenzyme-A mimics, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: Antipathogenic benzamide compounds having the formula 1

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI) The paramagnetic complexes of the polycarboxylic ligands possess advantageous tensioactive properties and are useful as MRI contrast media in formulations for investigating the blood pool.

Abstract: A method of making HIV protease inhibitors of general formula (1): 1

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: One aspect of the present invention relates to base-labile crosslinkers. A second aspect of the present invention relates to degradable crosslinked polymers and hydrogels comprising a base-labile crosslinker. The present invention also relates to a method of influencing the degradation rate of a crosslinked polymer or hydrogel, comprising the step of incorporating uncharged acrylamides into the crosslinked polymer or hydrogel.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.

Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.