Abstract: The present invention relates to a product of reaction between an amino functional polymer comprising at least one primary and/or secondary amine and one or more active ingredient. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.

Abstract: A rinse-off liquid personal cleansing composition comprising: (a) water; (b) from about 1% to about 60% by weight of a water soluble surfactant; (c) a water-insoluble oil selected from highly branched polyalphaolefins having formula (A) wherein R1 is H or C1-C20 alkyl, R4 is C1-C20 alkyl, R2 is H or C1-C20, and R3 is C3-C20 preferably from C5-C20, n is an integer from 0 to 3 and m is an interger of from 1 to 1000 and having a number average molecular weight of from about 1000 to about 25,000; and (d) a hydrophobic skin active component selected from antimicrobial agents, sunscreens, vitamins, perfume oils, insect repellents, anti fungal agents, and mixtures thereof, wherein the hydrophobic skin active component has a ClogP value of greater than 3. The personal cleansing compositions of the invention provide improved deposition of hydrophobic skin actives, excellent rinse feel and skin mildness.

Abstract: A low residue antimicrobial solution containing about 0.2 percent by weight of an acid selected from the group consisting of organocarboxylic acids; and about 2 percent of a volatile solvent selected from the group consisting of n-butanol, benzyl alcohol, phenylethanol, and sparingly soluble glycol ether solvents is disclosed. Preferred compositions may also contain about 0.1 percent anionic sulfated or sulfonated surfactants and about 5 percent co-solvent selected from the group consisting of completely water soluble monoprotic aliphatic alcohols and glycol ethers. The solution may be also employed as a low-residue cleaner for soiled hard surfaces.

Abstract: An economical sheetlike article for laundry whose flexibility is excellent, of which sprinkling and loss of the content are small and wherein a water-soluble substrate having a low basis weight is used. Thus, the present invention provides a sheetlike article for laundry in which a layer containing at least one composition selected from the group consisting of a detergent composition, a fiber softener composition and a bleaching agent composition, is connected with a water-soluble substrate on the both sides of the said layer, and of which the flexibility parameter calculated by a specific method is from 3 to 6.

Abstract: A provided novel colloid active component, a method for manufacturing colloid aluminum silica gel, and a surfactant containing the same are disclosed for solving water and land pollution, being safe to a human and the ecosystem, and adding economic value and applicability for the industrial use, wherein the method comprises the steps of: (a) dissolving a mixture of aluminum oxide, silicic acid, potassium, iron oxide, sulfuric acid and water into sulfuric acid; (b) adding potassium sulfate solution into the solution, and stirring at a low temperature to produce compositions with soluble aluminum double salt; (c) purifying the compositions to get very pure and dense aluminum potassium sulfate; (d) adding aluminum silicate and water to produce alkali metal polysilicate-sulfate water salt chelate; (e) polymerizing and precipitating the resultant at a low temperature to produce pectograph of aluminum silicate sieve; (f) producing chelate by adding Mgo, Fe2O3, Ca(OH)2, NaOH, KOH, and distilled water in sequence; (g

Abstract: Aqueous liquid detergent compositions containing a peracid and an effervesent system, wherein the effervescent system includes a first effervescent agent-containing component and a second acid agent-containing component, and the effervescent agent-containing component and the acid agent-containing component are chemically and/or physically separated from one another until effervescence is desired. Methods of laundering fabrics with such compositions.

Abstract: Chemical solvating, degreasing, stripping and cleaning agents. The agents are cleaning and solvating mixtures of dichloroethylene and alkoxy-substituted perfluoro compounds that contain six carbon atoms, with optionally highly fluorinated materials to retard flammability and/or other enhancement agents that improve and enhance the properties of the composition to accomplish its desired cleaning or solvating task. These other agents are one or more of the following materials: alcohols, esters, ethers, cyclic ethers, ketones, alkanes, aromatics, amines, siloxanes terpenes, dibasic esters, glycol ethers, pyrollidones, or low- or non-ozone depleting halogenated hydrocarbons. These mixtures are useful in a variety of solvating, vapor degreasing, photoresist stripping, adhesive removal, aerosol, cold cleaning, and solvent cleaning applications including defluxing, dry-cleaning, degreasing, particle removal, metal and textile cleaning.

Abstract: The invention relates to a crosslinked, carboxylic acid-based copolymer having good water absorbability and biodegradability, and a method for producing it; to an unsaturated carboxylic acid polymer having good detergency and its use; and to a biodegradable builder, a detergent composition and a dispersant. The invention includes (1) a crosslinked product of a copolymer from a monomer component that comprises an unsaturated monocarboxylic acid monomer and a specific amount of a quinone; and (2) an unsaturated carboxylic acid polymer which gives specific peaks in proton nuclear magnetic resonance spectrometry, and which has a specific number-average molecular weight and has calcium ion-sequestering ability, or an unsaturated carboxylic acid polymer having a specific structure.

Abstract: The present invention provides a liquid detergent composition being excellent in detergency and dispersion stability and a process for producing the same. The invention provides a liquid detergent composition having a degree of separation by volume of 5% or less after storage for 1 month at 25° C., comprising a liquid phase as the phase (a), a polymeric dispersant as the component (b)] and at least one selected from the group consisting of a crystalline silicate compound and an aluminosilicate compound as the component (c), wherein the component (b) has a cation exchange capacity of not less than 120 CaCO3 mg/g when the water content of the composition is 5% by weight or less and then the aluminosilicate compound only is used as the component (c) or when the water content of the composition is larger than 5% by weight.

Abstract: The present invention relates to methods of treating obesity, diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia using a neurotensin receptor ligand. The present invention also relates to pharmaceutical compositions and kits that comprise a neurotensin receptor ligand.

Abstract: Sustained delivery formulations comprising a water-insoluble complex of a peptide and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptide of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

Abstract: The present invention relates to peptides of one or more portions of the human chorionic gonadotropin &bgr;-chain as well as methods for treatment of cancer, using human chorionic gonadotropin, employing the &bgr;-chain of human chorionic gonadotropin, peptides containing a sequence of one or more portions of the &bgr;-chain of human chorionic gonadotropin and derivatives and analogues thereof. The invention further relates to fractions of sources and or preparations of human chorionic gonadotropin, such as fractions of human early pregnancy urine, which fractions have anti-cancer activity. The present invention further relates to pharmaceutical compositions for treating cancer.

Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.

Abstract: Compounds that are vancomycin analogs bearing terminal carboxyl group modifications as well as modifications to the vancosamine nitrogen and, optionally, modifications to the C6 position of the glucose residue attached to the amino acid four of the vancomycin heptapeptide chain are disclosed. Methods of making the compounds and methods of using the compounds to treat a bacterial infection in a host are also disclosed.

Abstract: The invention relates to a therapeutic agent for disorder in brain and nerve containing HGF (hepatocyte growth factor) as an active ingredient, and a method for treatment of disorder in brain and nerve comprising administration of HGF. The active ingredient HGF possesses an action to prolong survival of brain and nerve cells, and the injured brain or nerves may be regenerated and restored. Therefore, the therapeutic agent and method for treatment of the invention are useful for prevention and treatment of various disorder in brain and nerve (for example, dementia, senile dementia of Alzheimer type, cerebral stroke, and cerebral infarction).

Abstract: Mammalian kringle 5 fragments and kringle 5 fusion proteins are disclosed as a compounds for treating angiogenic diseases. Methods and compositions for inhibiting angiogenic diseases are also disclosed.

Abstract: Mutacin are bactericidal substances of proteinaceous natures produced by Streptococcus mutans. Lantibiotics are antibacterial substances containing posttranslationnally modified amino acids such as lanthionine. The present invention teaches a simple method of purifying mutacin B-Ny266 from Streptococcus mutans strain Ny266 to homogeneity. The present invention further teaches the primary amino acid sequence of mutacin B-Ny266 as well as its proposed modified structure. Further, the present invention teaches compositions comprising mutacin B-Ny266 as well as methods for the treatment and/or prophylaxy of bacterial infections comprising an administration of a suitable dose of composition comprising mutacin B-Ny266.

Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.

Abstract: A physiologically acceptable aqueous solution, and water-soluble compositions suitable for obtaining it, comprising a first physiologically acceptable compound of an acidic nature and a second physiologically acceptable compound of a basic nature that are able to give rise to a precipitate in water, characterized in that it also contains a trisubstituted salt of glycyrrhizic acid in a sufficient quantity to form a clear solution in water. A method for preparing the said solution.

Abstract: The inhibition of AP-1 activity by dominant negative deletion mutants of c-jun is disclosed. This inhibition of AP-1 activity is shown to be associated with inhibition of tumor promoter-induced neoplastic transformation. Therefore, the invention relates to the utilization of dominant negative deletion mutants of c-jun which are inhibitory to tumor promotor-induced neoplastic transformation as therapeutic agents in the prevention and treatment of cancer in mammals.

Abstract: A method is provided for treating solid tumors comprising administering a composition comprising a PDGF aptamer and a cytotoxic agent. In a preferred embodiment the PDGF aptamer is identified using the SELEX process for the Systematic Evolution of Ligands by Exponential enrichment. A method is also provided for reducing the interstitial fluid pressure (IFP) of a solid tumor comprising administering a PDGF aptamer. Finally, a method is provided for increasing the uptake of cytotoxic agents into a tumor comprising administering a composition comprising a PDGF aptamer and a cytotoxic agent.

Abstract: Methods of treating cancer by administration of FMdC followed by administration of a platinate are disclosed.

Abstract: An excipient comprising trehalose having a purity of 99.0% or more, a proportion of particles of 75 &mgr;m or more of 2 to 90 wt %, an average particle size of 10 to 250 &mgr;m, an apparent specific volume of 1.5 to 3.5 ml/g, and a whiteness of 90% or more.

Abstract: Methods for treating diseases or conditions modulated or ameliorated by nitric oxide, particularly ischemia and reperfusion injury, are provided, using glycolipids structurally related to monophosphoryl lipid A but with notable reduction in proinflammatory and pyrogenic activity.

Abstract: Long-acting antiparasitic formulations of doramectin, suitable for injection, are described herein.

Abstract: Disclosed are compounds having the formula wherein R2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula R is a lower alkylene, R′ is selected from the group consisting of moieties having the formula where X=0 or 1, Y=0 or 1, R1 is hydrogen or a pharmacologically active drug residue, R8 a pharmacologically active drug residue, R4, R5, and R6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R7 is hydroxyl or hydroxyalkyl.

Abstract: Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.

Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.

Abstract: Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized. Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphatee, N-arachidonoyl-cysteamine-S-phosphate, N-&agr;-linolenoyl-cysteamine-S-phosphate, and N-&ggr;-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-&agr;-linolenoyl-O-phospho-2-aminoethanol, N-&ggr;-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumor activity.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention relates to 4-Haloalkyl-3-heterocyclylpyridines, 4-haloalkyl-5-heterocyclyl-pyrimidines and 4-trifluoromethyl-3-oxadiazolylpyridines, Processes for Their Preparation, Compositions Comprising Them, and Their Use as Pesticides More particularly, the present invention relates to 4-trifluoromethyl-3-oxadiazolylpyridines of the formula (I′), to processes for their preparation, to compositions comprising them and to the use of these compounds for controlling animal pests, in particular insects, spider mites, ectoparasites and helminths: wherein X, Y are as defined in the description.

Abstract: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.

Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.

Abstract: The invention relates to the area of erythropoiesis, in particular to the use of tetrahydroquinolinyl-6-methyldihydrothiadiazinones of general formula (I) for treating anaemia. The invention also relates to novel tetrahydroquinolinyl-6-methyldihydrothiadiazinone derivatives and to the production thereof.

Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.

Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and a chloro at the 8-position are selective ligands for GABAZA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.

Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.

Abstract: Dihydroquinazoline derivatives of the formula where R3 is —(CH2)p—A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is —NA′A″ wherein A′ and A″ are the same or different and are each a C1-C4 alkyl group or their pharmaceutically acceptable salts possessing anti-cancer activity.

Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&m

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors.

Abstract: The present invention relates to the use of 2-amino-thiazoline derivatives of formula (I): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl or pharmaceutically acceptable salts thereof as inhibitors of inducible NO-synthase.

Abstract: Therapeutically active compounds of formula (I): in which R1 to R4 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, carboxyalkyl, hydroxyalkyl or halogenalkyl, or R2 and R3 form a ring of 5-7 carbon atoms, R5 to R9 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, acyl, hydroxy, alkoxy, alkoxycarbonyl, amino, acylamino, alkylamino, aryloxy, halogen, cyano, nitro, carboxy, alkylsufonyl, sulfonamido or trifluoromethyl, wherein each aryl residue defined above by itself or as a part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds increase the calcium sensitivity of contractile proteins of the cardiac muscle and are thus useful in the treatment of congestive heart failure.

Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, &bgr;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &bgr;-sheet mimetic is a thrombin inhibitor.

Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a

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: Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.