Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.

Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present and when x=0, W is not phenyl.

Abstract: Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.

Abstract: A process for the preparation of a cyclopropane derivative of Formula (I), by reacting an olefin of Formula (II), with a carbene of the formula:CR1R2, in a reaction vessel, optionally in the presence of a solvent, wherein, R1 and R2 are each independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R7 or —NR82; R3, R4, R5 and R6 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R9, —NR102, —SR11, —S(O)R11, or —SO2R11, or R3 and R6 are as defined above and R4 and R5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R7 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy, heteroaryl or —NR102; R8 is hydrogen, C1-C6 alkyl, C1-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R9 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy or heteroaryl; R10 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, a

Abstract: A process for the preparation of a cyclopropane derivative of Formula (I), by reacting an olefin of Formula (II), with a carbene of the formula: CR1R2, in a reaction vessel, optionally in the presence of a solvent, wherein, R1 and R2 are each independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R7 or —NR82; R3, R4, R5 and R6 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R9, —NR102, —SR11, —S(O)R11, or —SO2R11, or R3 and R6 are as defined above and R4 and R5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R7 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy, heteroaryl or —NR102; R8 is hydrogen, C1-C6 alkyl, C1-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R9 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy or heteroaryl; R10 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl,

Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present.

Abstract: Compounds of the Formula (I), wherein L1, L?1, L?1, L2, L?2, L?2, L3, L?3, L?3, L4, L?4 and L?4 for example are hydrogen or COT; R, R? and R? for example are hydrogen, C6-C12aryl or C3-C20heteroaryl; X, X? and X? for example are O, S, single bond, NRa or NCORa, T is for example hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C2-C20alkenyl, C5-C12cycloalkenyl, C7-C18cycloalkylenaryl, C5-C18cycloalkylenheteroaryl, C6-C14aryl, providedthat at least one of R, R? or R? is unsubstituted or substituted C3-C20heteroaryl; and Y is an inorganic or organic anion; are suitable as photolatent acid generators.

Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.

Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.

Abstract: The invention is related to novel azulene-oxindole compounds having formula (I) shown below, wherein one of R1, R2 and R3 represents a moiety of formula (II), each of A1 and A2 independently is nitrogen, oxygen or sulfur, each of the others of R1, R2, R3, R1, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 is as recited in the specification. The novel compound potentially inhibits multiple kinases and thus can be used to treat some disease like cancer or inflammatory.

Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.

Abstract: The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I) pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.

Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.

Abstract: A fluorescent dye-doped crystalline assay is employed for selection and detection of thiophilic heavy metal ions. While comparable in analytical performance to known solution based methodologies, the formation of crystalline analytes provides for signal amplification, and consequently, a powerful platform whose analysis is directly amenable to high-throughput video capture systems. In a microcapillary format, this assay is capable of screening hundreds of samples per day for the presence of subnanomolar concentrations of Hg2+ using a conventional fluorescence microscope.

Abstract: A dispersion, and a film and optoelectronic devices formed from the dispersion are provided. The dispersion comprising conducting polymer containing particles having a particle size of less than 450 nm, wherein the conducting polymer comprises substituted or unsubstituted, uncharged or charged polymerized units of thieno[3,4-b]thiophene, and wherein a film drop cast from the dispersion has a conductivity from 10?1 to 10?6 S/cm measured using the four point probe method.

Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.

Abstract: Thienothiophene monomers having an SF5 group and conducting oligomers and polymers formed by the polymerization of such monomers and their use as hole injection materials, charge transport materials, or as semiconductors. The compound may be of the formula: where X and X? are independently H, halogen atoms (e.g., F, Cl, Br, and I), MgCl, MgBr, MgI, Sn(R?)3, where R? is C1-6 alkyl or —OC1-6 alkyl, boronic acid, boronic ester, —CH?CHR? (where R? is H or C1-6 alkyl), —OC1-6 alkyl, —COOC1-6 alkyl, —S—COR?? and —COR?? (where R?? is H or C1-6 alkyl), —C?CH, or polymerizable aromatic rings (such as phenyl, naphthalene, pyrrole, dithiophene, thienothiophene, thiophene and so forth.

Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: Compounds of general formula (I): wherein R1, Y, (X)0, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therpeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description

Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1

Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

Abstract: Novel pyrimidin-4-one and pyrimidin-4-thione derivatives of formula (I) wherein A is phenyl, thienyl (including all 3 isomers), thiazolyl or pyridyl; X is oxygen or sulfur; R1 is hydrogen, halogen or trimethylsilyl; R2 is hydrogen, halogen or trimethysilyl; and at least one of R1 and R2 is not hydrogen; R3 is C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6haloalkenyl, C2-C6alkynyl, C2-C6haloalkynyl, —(CH2)n—C3-C8cycloalkyl which are unsubstitituted or substituted by halogen, C1-C6alkyl or C1-C6haloalkyl, C1-C4alkoxy-C1-C6alkyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkythio-C1-C6alkyl; C1-C4alkylthio-C2-C6alkenyl; C1-C4alkythio-C2-C6alkynyl; mono-C1-C4alkylamin-C1-C6alkyl; mono-C1-C4alkylamin-C1-C6alkenyl; mono-C1-C4alkylamin-C2-C6alkynyl; —(CH2)n—C1-C4alkoxy-C3-C6cycloalkyl; —(CH2)n—C1-C4alkylthio-C3-C6cycloalkyl; —(CH2)2-mono-C1-C4alkylamin-C3-C6cycloalkyl; or N═CR9R10; n is 1, 2, 3, or 4; R4, R5, R6, R7, and R8 are each independently of the

Abstract: The invention provides novel benzothiophenes of the formula: wherein R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R2 is —H, —OH, —Cl, —Br, —O(C1-C4 alkyl), —OCO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R3 is —H, —F, —Cl, —(C1-C4 alkyl), —CN, or —O(C1-C3 alkyl); R4 is —H, —F, —Cl, —(C1-C4 alkyl), —CN or —O(C1-C3 alkyl); R5 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); and R6 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is —CO—, —CHOH—, or &mda

Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: 1

Abstract: Benzothiophene derivatives of the formula (I) are used as components of liquid-crystal mixtures where the symbols and indices have the following meanings: X1 and X2, independently of one another, are —CH—, —CF—, the —(R1)C— group or the —(R1—A1—M1)C— group, with the provisos that x1) X1 and X2 are not simultaneously the —(R1)C— or —(R1—A1—M1)C— group, and x2) X1 and X2 are only simultaneously —CH— or —CF— if Z is fluorine Y1 and Y2, independently of one another, are hydrogen or fluorine, but both are not simultaneously fluorine z is hydrogen or fluorine R1 and R2, independently of one another, are, for example, a straight-chain or branched alkyl radical (with or without asymmetrical carbon atoms) having 1 to 20 carbon atoms, A1 and A2 are, for example, phenylene-1,4-diyl, M1 is undirected and is —OC(═O)—, —OC(═O)O—, —OCH2&mdas

Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B  (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

Abstract: A method for treating a fungal infection is disclosed.

Abstract: This invention provides novel benzothiophene compounds of the formula I: which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.

Abstract: The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg.

Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.

Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.

Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.

Abstract: The present invention provides novel compounds of Formula 1 or Formula 2 and compositions thereof, methods of their use, and methods of their manufacture, wherein X, Y, Z, W, R1, R2 and R3 are defined more fully in the description. These compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and a number of other diseases.

Abstract: This invention provides novel benzothiophene compounds of the formula I: ##STR1## which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.

Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and other cardiovascular pathologies.

Abstract: An aromatic carboxylic acid bicyclic sulfur compound of the following formula: ##STR1## wherein X.sup.1 is selected from the group consisting of C.sub.1 to C.sub.4 alkyl, halogen, C.sub.1 to C.sub.4 haloalkyl, C.sub.2 to C.sub.4 alkoxyalkyl, C.sub.1 to C.sub.4 alkoxy and C.sub.1 to C.sub.4 haloalkoxy; each of X.sup.2 and X.sup.3 is independently selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl and C.sub.1 to C.sub.4 haloalkyl; X.sup.4 is selected from the group consisting of hydrogen, halogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 haloalkyl and C.sub.1 to C.sub.4 alkoxy; each of X.sup.5, X.sup.6, X.sup.7 and X.sup.8 is independently hydrogen or C.sub.1 to C.sub.4 alkyl; the bond between X.sup.2 and X.sup.5 is saturated or unsaturated; the bond between X.sup.5 and X.sup.7 is saturated or unsaturated; p is an integer of 0 or 1; and n is an integer of 0, 1 or 2; or a salt thereof.

Abstract: Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.

Abstract: The present invention provides a compound of formula ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is a hydroxy protecting group;R.sup.6 is --H or a hydroxy protecting group which can be selectively removed;R.sup.11 is non-existent or .dbd.O; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.

Abstract: The instant invention provides novel benzo[b]thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.

Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations containing a compound of formula I, and methods of using a compound of formula I for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: A method of controlling Take-All disease of plants by applying a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is .[.benzothiophene.]..Iadd.thiophene.Iaddend.; andA is .[.selected from.]. --C(X)-amine .[.wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical.]..Iadd.wherein the amine is a monosubstituted or a disubstituted amine, wherein one of the substituents has a cyclic moiety, said cyclic moiety which is chosen from the group consisting of thienyl, furanyl, and a non-heterocyclic substituent, wherein when the amine is disubstituted, the second substituent is a non-cyclic substituent.Iaddend., --C(O)--SR.sub.3, --NH--C(X)R.sub.4, .[.and.]. .Iadd.or .Iaddend.--C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from .[.O-tolyl.]..Iadd.o-tolyl.Iaddend., 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.