Abstract: This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.

Abstract: A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide.

Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

Abstract: The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Ar5 form a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

Abstract: Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I wherein A represents a multi-substituted alkyl group or aromatic ring.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: It has been found that inhibitors of the renin-angiotensin system are useful for the treatment or prevention of conditions associated with hypoxia or impaired metabolic function or efficiency. In particular, they may be used in connection with therapy of stroke or its recurrence, the acute treatment of myocardial infarction, and the treatment or prevention of wasting or cachexia, and are thus useful in treatment of the symptoms and signs of aging. These inhibitors may also be used to enhance function in healthy subjects.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: This invention relates to biocidal compositions and methods of using same. Also provided is a process for the manufacturing of a biocidal composition in the form of a tablet and a method of using the biocidal compositions for the disinfection of water that may contain microorganisms and biofilms.

Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2,R4a, R4b, and R4c are as defined in the specification.

Abstract: The present invention relates to antimicrobial compositions including a critical, near critical, or supercritical (densified) fluid and an antimicrobial agent, to methods of forming these compositions, and to methods employing these compositions. An antimicrobial agent can be generated in the presence of a densified fluid, for example, by reacting an oxidizing agent with a precursor to the antimicrobial agent.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Fecal bacterial contamination in an animal is reduced by providing it with drinking water containing a microbiocidally-effective amount of halogen-based microbiocide resulting from mixing with water (A) a product formed in water from (i) bromine, chlorine, or bromine chloride, or any two or more thereof, (ii) a water-soluble source of sulfamate anion, and (iii) a water-soluble base; (B) at least one 1,3-dihalo-5,5-dialkylhydantoin in which one of the halogen atoms is a chlorine atom and the other is a chlorine or bromine atom, and in which each alkyl group, independently, contains in the range of 1 to about 4 carbon atoms; (C) at least one 1,3-dibromo-5,5-dialkylhydantoin in which one of the alkyl groups is a methyl group and the other alkyl group contains in the range of 1 to about 4 carbon atoms; or (D) any two or more of (A), (B), and (C).

Abstract: The present invention is to provide an imidazolidinedione derivative and oxazolidinedione derivative represented by the following general Formula (I) having the chymase and/or tryptase inhibition activity [wherein R1 and R2 are the same or different, and denote a lower alkyl group or a phenyl group, or R1 and R2 are taken together to form a ring, R3 denotes an optionally substituted naphthyl group or heterocyclic group, A denotes oxygen or NR4 (R4 is hydrogen or optionally substituted lower alkyl group), or NB2R5 (R5 is aryl group, and B2 is carbonyl group or sulfonyl group), and B1 denotes a carbonyl group or a sulfonyl group], or a pharmaceutically acceptable salt thereof.

Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The object of the present invention is to provide a microbicidal deodorant in a tractable liquid form that has excellent long-term storage stability. The microbicidal deodorant of the present invention comprises: at least one substance selected from the group consisting of halogenated dialkyl hydantoins represented by the general formula (1) and halogenated succinimides represented by general formula (2); and at least one substance selected from the group consisting of tetrahydrothiophene 1,1-dioxide, 3-methyltetrahydrothiophene 1,1-dioxide, and 2,5-dihydrothiophene 1,1-dioxide.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.

Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, 1

Abstract: Low volume safe for injection formulations of dantrolene yield significant advantages over the currently approved and marketed dantrolene for MH threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. Additionally, a safe for injection low volume formulation of dantrolene can be made widely available to non-anesthesiologist practitioners who have occasion to use dantrolene intravenously in the treatment of other potentially life threatening conditions, including in the field.

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

Abstract: The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of a sodium ion channel blocker in combination with a cyclooxygenase-2 selective inhibitor.

Abstract: The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.

Abstract: Compounds of the formula I 1

Abstract: It is found out that compounds represented by the formula (I): wherein R1 is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; and R2 and R3 taken together with the adjacent carbon atom form an optionally substituted heterocyclic group having one or more of oxo and/or thioxo; have an HCV RNA-dependent RNA synthase inhibitory effect.

Abstract: Compounds of formula (I) 1

Abstract: The present application describes novel hydantoin derivatives of formula (I): 1

Abstract: This invention was created with a unique and specific Formulation and a specific Method for the treatment of fever blister/cold sores, and minor lip irritations. The specific Formulation consists of a topical gel solution. The specific Method of treatment is to apply the gel directly on the lesion every four hours. The formulations significant ingredients are: lidocaine hcl 1.00%, tocopheryl acetate 0.2%, and allantoin 0.1%. The formulation and the method were clinically tested. The study demonstrated a marked reduction of pain and a reduction in healing time as compared to existing formulations and methods.

Abstract: Compounds, compositions and methods are provided for the treatment and prophylaxis of infections and associated diseases caused by viruses of the Flaviviridae family by administering certain rhodanine derivatives, and analogs thereof, tri- and tetracyclic rhodanine alkanoic acids and rhodanine benzoic acids being particularly effective.

Abstract: An office product which has at least one exposed surface that is subject to infectious microorganisms, and an antimicrobial agent associated with the exposed surface to render ineffective or destroy infectious microorganisms. The antimicrobial agent may be present on the exposed surfaces of the office product as a coating, or as an integral part of a material used to form the exposed surface(s) of the office product. The antimicrobial agent is ineffective until activated using. Preferably, the antimicrobial agent is an amine which can be activated by a halogen. The present invention also relates to a process of making an infectious microorganism resistant office product which comprises providing the office product with an antimicrobial agent.

Abstract: Methods and compositions for treating skin ailments are described herein. Embodiments of the invention include a therapeutic composition. The thereapeutic composition is adapted for cleansing and treating skin and further includes an emu oil based composition. The emu oil based composition includes from about 20 wt. % to about 75 wt. % of refined sterilized emu oil, from about 0.01 wt. % to about 33 wt. % of one or more aromatic alcohols, from about 10 wt. % to about 25 wt. % of one or more benzoic acids, from about 0.2 wt. % to about 2.0 wt. % of allantoin, from about 0.025 wt. % to about 1.25 wt. % of methylparaben, from about 1.0 wt. % to about 13.0 wt. % of one or more alkyl esters and from about 0.01 wt. % to about 0.30 wt. % of propylparaben. Embodiments of the invention further include a composition including an aqeous emu oil based composition, wherein the aqueous emu oil based composition is adapted for cleansing and treating skin. Embodiments of the invention further include an absorbent article.

Abstract: An allantoin-containing skin cream composition can comprise allantoin and at least one anionic or nonionic emulsifier that is substantially hydrophilic and is soluble in water. The pH of the composition is in a range of from about 3.0 to about 6.0; preferably, the pH of the composition is from about 5.0 to about 6.0. The composition can further comprise an acidic anionic polymer. A preferred acidic anionic polymer is a carboxypolymethylene polymer. The composition can further comprise a carbohydrate polymer such as galactoarabinan, polygalactose or polyarabinose. The composition can additionally comprise other ingredients such as herbal extracts, an antioxidant component, an emollient component, a chelator, a solvent component, or a preservative component. The composition is useful as a skin protectant.

Abstract: The invention relates to a combination which comprises a P-glycoprotein (P-gp) inhibitor and an antiepileptic drug selected from phenyloin (5,5-diphenyl-2,4-imidazolidinedione), carbamazepine, lamotrigine, gabapentin, oxcarbazepin, valproic acid, and topiramate, and its use for the prevention, delay of progression or treatment of diseases, in particular epilepsy, especially epilepsy which is resistant to antiepileptic drugs.

Abstract: The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HIV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.

Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.

Abstract: A pesticidal composition comprising an oxadiazine compound given by formula (A): 1

Abstract: Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: The present invention relates to acne and rosacea compositions by a six-prong synergistic combination treatment strategy that includes (1) control of excess sebum production, (2) control of undesirable bacteria or mites, (3) control of inflammation, (4) enhanced desquamation of follicular infundibulum cells, (5) reduction of irritation from anti-acne or rosacea compositions themselves, and (6) enhancement of the topical bioavailability of anti-acne and rosacea compositions. This is achieved by a synergistic combination of commonly utilized topical anti-acne and rosacea ingredients with a topical bioavailability enhancement composition, which results in enhanced anti-acne and rosacea action from such ingredients. Moreover, additional inclusion of an anti-inflammatory composition, and also a vascular micro-circulation enhancement composition, further results in synergistic superior anti-acne and rosacea benefits from such compositions.

Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.

Abstract: The invention provides a metalloproteinsae inhibitor compound comprising a metal binding group having formula (I), for use in the treatment of a disease or condition mediated by one or more metalloproteinase enzymes wherein X is selected from NR1, O, S; B is C or CH, Y1 and Y2 are idenpendently selected from O, S; R1 is selected from H, alkyl, haloalkyl.

Abstract: Compounds of formula I: t,0010

Abstract: Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.

Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: This invention discloses and claims diary heterocycles of formula (I) 1

Abstract: The present invention relates to novel imidazolidine derivatives of the formula I, in which B, E, W, Z, R, R0, R2, R3, e and h have the meanings indicated in the application. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.

Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

Abstract: The invention features methods for decreasing necrosis. The invention also features methods for treating a subject with a condition in which necrosis occurs. The invention further features chemical compounds used to decrease necrosis.

Abstract: A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity.