Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.

Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

Abstract: A method including resolution of a diastereomeric mixture represented by the formula 1

Abstract: The present invention relates to novel scyphostatin analogues, which distinguish themselves by acting as SMase inhibitors so that they are of therapeutic use for a number of diseases such as a HIV infection, neurodegenerative diseases, inflammatory diseases, apoplexy, ischemia, myocardial infarction or in the case of atherosclerosis.

Abstract: The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: A magnetic recording medium and method for forming the magnetic recording medium are described. The magnetic recording medium includes a magnetic layer formed on a non-magnetic support, and a lubricant layer over the magnetic layer. The lubricant layer includes a compound selected from the group consisting of hydrocarbyl-substituted cyclopentanes, hydrocarbyl-substituted cyclopentenes, hydrocarbyl-substituted cyclopentadienes, and mixtures or derivatives thereof. The lubricant layer also may be used on a magnetic head for reading and writing information on a magnetic recording medium. The magnetic recording medium and the magnetic head may be used to manufacture computer disk drives, compact disk drives, audio equipment, and video equipment.

Abstract: The compounds of formula 1, 1

Abstract: The present invention provides a process for preparing optically active &agr;-hydroxy acids and derivatives thereof by subjecting the alkylated 1,3-dioxolanones of formula (IV) wherein R1 and R2 are the same or different and are each independently H or C1-6 alkyl; R5 is H, C1-16 alkyl, or unsubstituted or substituted phenyl; and R6 is C1-8 alkyl, C2-7 alkenyl or unsubstituted or substituted benzyl, to either alcoholysis or hydrolysis, in which the alkylated 1,3-dioxolanones are obtained by using 10-camphorsulfonamide as a chiral auxiliary.

Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example are valuable ligands for metal complexes of the d-8 metals of the periodic table of elements. The metal complexes in question are catalysts or catalyst precursors for the asymmetric hydrogenation or asymmetric transfer hydrogenation with hydrogen donors of prochiral organic compounds with carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.

Abstract: The present invention relates to compounds useful as catalysts in asymmetric synthesis of chiral compounds, methods for the synthesis of said catalysts, and methods for synthesizing chiral compounds with high enantioselectivity.

Abstract: Disclosed are thermally-stable, colored, photopolymerizable compounds containing a vinyl group which are capable of being copolymerized with reactive vinyl monomers to produce colored compositions such as polyacrylates, polymethacrylates, polystyrene, etc. The compounds exhibit good thermal stability, fastness (stability) to UV-light, good solubility in the reactive monomers and good color strength.

Abstract: This invention relates to compounds of the general formula 1

Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.

Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.

Abstract: This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.

Abstract: A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Abstract: This invention provides a method for treating or preventing arrhythmias in a human subject comprising the administration of an effective amount of a calcium/calmodulin-dependent protein kinase inhibitor. Also provided are pharmaceutical compositions comprising a calcium/calmodulin-dependent protein kinase inhibitor and a pharmaceutically acceptable carrier and methods for identifying agents useful for the treatment of arrhythmias.

Abstract: D- and L- &agr;-amino acids and D- and L-&agr;-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant &bgr;-hydoxycarbamate is deprotected to yield the corresponding &bgr;-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant &bgr;-hydroxysulfonamide is deprotected to yield the corresponding &bgr;-hydroxyamine.

Abstract: This invention provides a method for the determination of bicarbonate ion existing in liquid using phosphenolpyruvate carboxylase and malate dehydrogenase as conjugate enzyme wherein thioNAD(P)H is used as substrate of malate dehydrogenase. The use of the thioNAD(P)H enables the measurement with visible light, and enables the simple and accurate determination of bicarbonate ion concentration of biological liquid sample in the clinical test.

Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are ea

Abstract: The present invention relates to compounds that are inhibitors of interleukin-1&bgr; converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1&bgr; converting enzyme.

Abstract: Propargylether derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7, and R8 are each independently hydrogen or alkyl and R9 is a group R10 is optionally substituted aryl or optionally substituted heteroaryl, R11 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl, Z is hydrogen —CO—R16, —COOR16, —CO—COOR16 or —CONR16R17, R12 is hydrogen, or optionally substituted alkyl, alkenyl or alkynyl, R13 is hydrogen or alkyl, R14 is hydrogen, alkyl, cycloalkyl or cycloalkyl-alkyl, R15 is alkyl, alkenyl, alkynyl, optionally substituted aryl or optionally substituted aryl-alkyl, and R16 and R17 are independently of each other hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: A process for producing sulfonylimide compound is represented by the formula (I) MN(SO2Rf1) (SO2Rf2) industrially easily at a low cost in an efficient manner comprising reactions of at least one sulfonyl halogenides represented by the formula (II) RfSO2X with anhydrous ammonia or an ammonium salt in the presence of a fluorine compound represented by the formula (III) MF, in which X represents either F or Cl among halogen elements of VIIb group in the periodic table, and M represents any one of Li, Na, K and Cs among alkali metals of group Ia in the periodic table, Rf1 and Rf2, which may be the same or different, respectively represent any one of a straight chain or branched compound of a fluoroalkyl, perfluoroalkyl, fluoroallyl or fluoroalkenyl group having 1 to 12 carbon atoms, and Rf in the formula (II) represents the same group as Rf1 or Rf2 in the formula (I).

Abstract: The invention relates to methods for forming combinatorial libraries. The invention provides methods suitable for the rapid and convenient synthesis of very large combinatorial libraries of small organic molecules. In particular, the invention provides a method for forming combinatorial libraries combining amide, sulfonamide, or urea bond formation with reductive amination.

Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.

Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Abstract: The present invention relates to acetylenic aryl sulfonamide thiols which act as inhibitors of TNF-&agr; converting enzyme (TACE). The compounds of the present invention are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: The invention relates to methods for forming combinatorial libraries. The invention provides methods suitable for the rapid and convenient synthesis of very large combinatorial libraries of small organic molecules. In particular, the invention provides a method for forming combinatorial libraries combining amide bond formation with epoxide opening.

Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.

Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: The present invention provides a monomer having the formula A-B, wherein A is represented by Formula I: wherein B is selected from —OCF═CF2 and —A; wherein, when B is—OCF═CF2, the orientation of B is meta or para to the trifluorovinyloxy group of A; wherein, when B is A, the bond joining the A groups is para to the trifluorovinyloxy group of each A; and wherein each Z is independently selected from —SO2F, —SO2Cl, —SO3H, —SO2—N(M)—SO2CF3, and —SO2—N(M)—SO2Rf; wherein M is any suitable cation and Rf is a C1 to C10 fluorocarbon or fluorinated ether group. The present invention also provides a monomer according to Formula II: wherein X is F, Cl, or N(M)SO2Rf, wherein M is any suitable cation and Rf is a C1 to C10 fluorocarbon or fluorinated ether group.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: 2-Sulfamoylbenzoic acid derivatives of general formula (I): which have both an antagonistic effect on the leukotriene D4 receptor and an antagonistic effect on the thromboxane A2 receptor and salts thereof, pharmaceuticals, anti-allergic agents and leukotriene-thromboxane A2 antagonistic agents containing them as an active ingredient.

Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.

Abstract: A process for producing sulfonylimide compound is represented by the formula (I) MN(SO2Rf1) (SO2Rf2) industrially easily at a low cost in an efficient manner comprising reactions of at least one sulfonyl halogenides represented by the formula (II) RfSO2X with anhydrous ammonia or an ammonium salt in the presence of a fluorine compound represented by the formula (III) MF, in which X represents either F or Cl among halogen elements of VIIb group in the periodic table, and M represents any one of Li, Na, K and Cs among alkali metals of group Ia in the periodic table, Rf1 and Rf2, which may be the same or different, respectively represent any one of a straight chain or branched compound of a fluoroalkyl, perfluoroalkyl, fluoroallyl or fluoroalkenyl group having 1 to 12 carbon atoms, and Rf in the formula (II) represents the same group as Rf1 or Rf2 in the formula (I).

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac

Abstract: A compound of formula (I) useful as metalloproteinase inhibitors.

Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.

Abstract: The present invention discloses new efficient processes for various bond forming reactions, including Suzuki reactions and aryl aminations. Organic compounds (e.g., ligands), their metal complexes and compositions using those compounds, provide useful catalysts. The invention also relates to performing Suzuki cross coupling reactions with unreactive aryl-chlorides.

Abstract: The present invention discloses new efficient processes for various bond forming reactions, including Suzuki reactions. Organic compounds (e.g., ligands), their metal complexes and compositions using those compounds, provide useful catalysts. The invention also relates to performing Suzuki cross coupling reactions with unreactive aryl-chlorides.

Abstract: Acylsulfamoylbenzamides of the formula I and crop protection compositions comprising them are described. In this formula I, R1, R2, R3, R4 and R5 are various organic radicals and X is CH or N.

Abstract: Provided are methods of purification of an organic lithium salt comprising the steps of: (a) dissolving an impure organic lithium salt in a solution comprising an organic complexing solvent; (b) crystallizing from said solution a solid solvate complex comprising said lithium salt and said organic complexing solvent; (c) separating said solid solvate complex from said solution; (d) dissociating said solid solvate complex to yield: (i) said lithium salt in a solid form, and, (ii) a volatile composition comprising said organic complexing solvent; and, (e) removing said volatile composition to yield said lithium salt in a solid form of purity greater than the purity of said impure lithium salt. The present invention also pertains to electrolytes for electric current producing cells comprising such purified lithium salts.

Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q  II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.