Abstract: The present invention relates to compounds of Formula I: Formula I which are agonists of the M-1 muscarinic receptor.

Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and t

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The present invention includes a number of structural analogues of UK-1. A comparision of the anticancer activity of the UK-1 analogues with their ability to inhibit the growth of methicillin-sensitive and methicillin-resistant Staphylococcus aureus demonstrates that a structurally simplified analogue of UK-1 retains the natural product's selective activity against cancer cells. Structurally conservative changes to UK-1 that diminish Mg2+-binding ability may result in a dramatic decrease in cancer cell cytotoxicity. The results may establish a minimum structural pharmacophore as well as a functional role for Mg2+-binding in the selective cytotoxicity of UK-1.

Abstract: Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R? groups, —CO—NHR? groups, NH—COR? groups and —S—COR? groups, wherein R?, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least on

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.

Abstract: Cosmetic compositions for topical use for protecting the skin and the hair, containing, in a cosmetically acceptable support, at least one compound of formula (1) or (2) in which X1 represents R3—(C?O)—, R3—SO2— or R3—O—(C?O)—, X2 represents —(C?O)—R?3—(C?O), —SO2—R?3—SO2— or —(C?O)—O—R?3—O—(C?O)—, Y represents —(C?O)—R4 or —SO2R5, R2 represents a C1-8 alkyl group, n is 0, 1 or 2, R3 represents C1-30 alkyl or C3-30 alkenyl, R?3 represents a single bond or a divalent C1-30 alkylene or C3-30 alkenylene radical, R4 represents —OR6 or —NHR6, R5 represents C1-30 alkyl or a phenyl nucleus, R6 represents C1-30 alkyl or C3-30 alkenyl, and novel compounds of formula (2).

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: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g.

Abstract: Substituted cyclohexylcarboxylic acid amide compounds, processes for their production, pharmaceutical compositions containing these compounds and the use of substituted cyclohexylcarboxylic acid compounds for producing pharmaceutical compositions for treating conditions or disease states associated with the opioid receptor system and/or with noradrenalin and/or serotonin re-uptake.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.

Abstract: This invention relates to novel compounds useful as potassium channel modulators. More specifically the invention provides chemical compounds useful as modulators of SKCa and/or IKCa channels.

Abstract: Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ? 4 integrin, such as inflammatory diseases in which ? 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.

Abstract: Bicyclic amide derivatives of formula (I) or tautomers or pharmaceutically acceptable salts thereof or both are provided: Also provided are processes for preparing the bicyclic amide derivatives as well as pharmaceutical compositions containing the same and therapeutic uses. The bicyclic amide derivatives are useful for treating a variety of conditions associated with the abnormal modulation of one or more Kv1.1 voltage-gated potassium channels.

Abstract: The invention relates to a bait matrix which includes a gelling agent and a pesticide. The bait matrix is useful for controlling pests by attracting and poisoning them. The gel matrix is substantially weatherproof and hence can be used when exposed to the weather.

Abstract: Methods for the treatment of a proliferative disorder are provided in which a subject in need of such treatment is administered an effective amount of a compound selected from: compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1 and X2 are independently H, Cl, F, Br, I, CN, CF3 or NO2, and Ar1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and compounds of formula (II) wherein X3 and X4 are each independently H, Cl, F, Br, I, CN, CF3 or NO2; Y is (C2–C6)alkylene or (C2–C6)heteroalkylene; and Z is Cl, F, Br, I, CN, CF3 or NO2.

Abstract: The present invention provides crystalline biphenyl-4-carboxylic acid (R)-(6-(1-((4-fluorobenzyl)methylamino)ethylideneamino)-2(R)-hydroxyindan-1-yl)amide hemihydrate, compositions thereof, methods of using the same, processes for making the same, and processes for making intermediates thereof.

Abstract: The present application is directed to the use of X-ray contrast media that act as universal antigens that are labeled herein as “pseudoantigens.” X-ray contrast media have the potential to exist in an aggregated state that is greater in increased concentrations. In this aggregated state, contrast media assume the role of multivalent antigens and can successfully compete with any other antigens involved in antibody-antigen reactions that lead to anaphylaxis. In this competition, the large quantity of contrast media serves to inhibit the adverse effects of antibody-antigen reactions without the contrast media itself creating antibodies or creating toxicity problems.

Abstract: Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

Abstract: Cellular transcription is modulated by increasing or decreasing the amount of active HEXIM1 in the cell. The methods are applied to the treatment of HIV infection and cardiac hypertrophy. Assays using reconstituted 7SK:P-TEFb snRNP screen for agents that modulate HEXIM1-P-TEFb binding.

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1–C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function.

Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-?v?3 are inhibited by an inhibitor compound of formula (I): wherein G1 and G2 are each independently NH—C(O)—O—R1, —NH—C(O)—O—(CH2)v—(C6H4)—X3, —NH—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—O—(CH2)v—(C6H4)—X3, or NH—C(O)—CH2—(C6H4)—X3; Y1 and Y2 are each independently OH, C1–C4 alkyl, C1–C4 hydroxyalkyl, C1–C4 alkoxy, phenyl, benzyl, or NH2; R1 is C1–C4 alkyl; X1 and X2 are each independently halo or C1–C4 alkoxy; X3 is halo, nitro, C1–C4 alkyl, C1–C4 alkoxy, or C1–C4 perfluoroalkyl; Z is —C?C—, —C6H4—, cis-CH?CH—, trans CH?CH—, cis-CH2—CH?CH—CH2—, trans —CH2—CH?CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r, and v are each independently an integer having a value of 1 or 2; with provisos that when A

Abstract: A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.

Abstract: Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ?CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1 or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.

Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.

Abstract: A method for treating or preventing a disorder or a condition by double inhibition of serotonin (5-HT) and noradrenaline (NA) reuptake in a subject in need thereof, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity, comprising the step of administering to said subject a mixture of enantiomers of milnacipran enriched in the (1S,2R) enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts.

Abstract: A method of forming polymers in the presence of nucleic acid using template polymerization. Also, a method of having the polymerization occur in heterophase systems. These methods can be used for the delivery of nucleic acids, for condensing the nucleic acid, for forming nucleic acid binding polymers, for forming supramolecular complexes containing nucleic acid and polymer, and for forming an interpolyelectrolyte complex.

Abstract: Polyacetals comprising a recurring units represented by a formula selected from the group consisting of formula (I) and (II): wherein A comprises at least one acetal group; B is selected from the group consisting of —CH—, —CH(CH3)—, CH2CH—, —CH2C(CH3)—, —CH(CH3)CH—, and —CHCH(CH3)CH(CH3)—; Z is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VU; V is a linker group; U is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, hexadecaamine dendrimer, enhancer, and targeting receptor; R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl; D is a linkage selected from the group consisting of carboxylic amide, carboxylic ester, urea, and urethane; and G is selected from the group consisting of C4 to C20 alkyl, C6-C10 aryl, and —(OCH2CH2)n—, where n is in the range of 1 to about 250, are useful in nucleic acid delivery applications.

Abstract: The invention provides compounds of Formula (I): wherein R1–R4 have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.

Abstract: The present invention provides a microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, wherein component I is the compound 2-[.alpha.-{[(.alpha.

Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: A cosmetic composition is provided which includes an alpha- or beta-hydroxycarboxylic acid at least partially neutralized and a taurate copolymer in a low pH system. The taurate copolymer improves skinfeel and provides viscosity to the system.

Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.

Abstract: The present invention relates to a novel class of polymeric compounds having specific quaternized amine based upon a dimer acid amido amine quaternary compound. 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 cationic 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: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), X= R3= Y= Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl. Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R?=H or O(?) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addition and obesity based thereon.

Abstract: The present invention ralates to compounds of formula (I): wherein R is hydrogen (H) or C1-6 alkyl; and X is defined such that —NH—(X)—COOH is the residue of an amino acid, which amino acid may itself optionally be substituted at any pendant amino group thereof by a residue of a carboxylic acid or a derivative thereof; or a salt thereof.

Abstract: The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.

Abstract: Pharmaceutical compositions for oral administration comprising a cyclosporin or macrolide as active ingredient, and a polyethoxylated saturated hydroxy-fatty acid.

Abstract: Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of C2-substituted indan-1-one systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in methods of embodiments of the invention may include compounds of the formula in which the radicals are as defined, and their physiologically acceptable salts.

Abstract: Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.

Abstract: A method for reducing the production of malodor in sulfur containing dermatological compositions by adjusting the pH of the composition to between about 6.5 to about 8.1. Also, sulfur containing dermatological compositions having a pH between about 6.5 and about 8.1.

Abstract: A polymer comprising recurring units represented by formula (I): wherein X is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VZ, where R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl, where V is a labile linker group, and where Z is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, and hexadecaamine dendrimer; and wherein Y is selected from the group consisting of —(CH2)2—, —(CH2)2—O—(CH2)2—, —(CH2)2—O—(CH2)2—, and —(CH2)3—NHC(O)—(CH2)6—C(O)NH—(CH2)3— is useful in nucleic acid delivery applications. Polyacetals of the formula (I) are preferably made by reacting appropriate diols and divinyl ethers. In preferred embodiments, complexes formed between polyacetals of the formula (I) and polynucleotides are useful as transfection reagents.

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.

Abstract: Methods and products for inhibiting growth of fungus and fungal disease on a plant. Methods comprise contacting at least a portion of a plant or plant seed together with a fungicidal composition comprising a fungicidal carboxamide. Products comprise any of leaves, crowns, roots, stolons, seed, seedlings, sod, and any combination thereof, treated with a fungicidal carboxamide. Preferred pathogens are of the genus Colletotrichum, preferred disease is anthracnose, preferred fungicides are carboxamides, and preferred plants are turfgrass.