Abstract: Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality. The functionalities can be carboxylate, amine, or sulfate groups and/or polyethylene glycol and can optionally include crosslinking groups.

Abstract: This invention provides a method for treating an eye disease in a patient comprising: providing a photosensitive prodrug that releases upon exposure to light an active ingredient to treat the eye disease; administering the prodrug in a pharmaceutically accepted vehicle to the subject, and exposing the eye of the subject to an external light source to cause the prodrug to release the active ingredient. This invention also provides a composition for the treatment of glaucoma, comprising a compound containing a lithium ion-chelated in a crown ether- or aza-crown ether-containing chromene or diazene derivative and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

Abstract: The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention is directed to bioconjugates of complexes represented by the formula: wherein R, R?, R1, R?1, R2, R?2, R3, R?3, R4, R?4, R5, R?5, R6, R?6, R7, R?7, R8, R?8, R9, R?9, M, X, Y, Z and n are defined herein for use as contrast agents in diagnostic imaging.

Abstract: Chiral synthesis from an achiral starting material by chiral diamine-mediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.

Abstract: The metal complexes of general formula I in which Hal stands for bromine or iodine, and A1 and A2 have different meanings, are suitable as contrast media.

Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.

Abstract: Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duoden

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:

Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality.

Abstract: This invention features a compound of the following formula: wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative or crown ether derivative.

Abstract: The invention concerns novel cdc25 phosphatase inhibitors, and in particular cdc25-C, which correspond to the general formula (I) wherein: A represents a carbocyclic aryl radical optionally substituted 1 to 3 times by one or more radicals independently selected among a halogen atom and an alkyl, hydroxy, alkoxy, alkylthio or NR1R2 radical wherein R1 and R2 represent a hydrogen atom or an alkyl radical or R1 and R2 form together with the nitrogen atom a heterocycle of 4 to 7 members comprising 1 to 2 heteroatoms, the members required to complete the heterocycle being selected independently among the CR3R4—, —O—, —S and NR5-radicals, R3 and R4 representing independently each time they are involved a hydrogen atom or an alkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino radical, and R5 representing independently each time it is involved a hydrogen atom or an alkyl radical, or A represents a phenyl radical substituted by a phenyl radical optionally substituted 1 to 3 times by one or more radicals selected

Abstract: Compounds of general formula (I): in which: R1 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C2–C10 alkylene group or an ortho disubstituted arylene; R2 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R3, R4 and R5 are hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb 67Ga 68Ga 72As 111In 113In 90Y 97Ru 62Cu 64Cu 52Fe 52mMn 140La 175Yb 153Sm 166Ho 149Pm 177Lu 142Pr 159Gd 212Bi 47Sc 149Pm 67Cu, 111Ag, 199Au, 161Tb and 51Cr as well as the salts thereof with physiologically compatible bases or acids

Abstract: Provided is a method for producing a phenol condensate by oxidative condensation of a phenol compound not having a substituted group on at least one ortho-position, in the presence of a specific complex (II) and oxygen, wherein a condensate coupled at para-position of the phenol can be produced in an excellent yield, L-M (X)n??(II) wherein L represents a ligand having 2 to 4 nitrogen atoms as donor atoms, M represents copper ion, nickel ion, cobalt ion, iron ion, manganese ion, chromium ion or vanadyl ion, X represents a counter ion, n is a number of Xs.

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

Abstract: Agents and methods to alter rAAV transduction, including agents and methods to enhance rAAV transduction, are provided. For instance, the invention provides methods to identify agents that enhance AAV transduction after viral binding to the cell membrane and before second strand synthesis.

Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.

Abstract: An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate.

Abstract: Fluorescent chelates of lanthanide, terbium, europium and dysprosium with tetraazamacrocyclic compounds are discussed which can be used as fluorescent in vitro or in vivo diagnostic agents. These chelates are tissue specific imaging agents for soft tissue cancers.

Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.

Abstract: A cyclic tertiary amine compound represented by a formula (1) and an organic luminescent device are disclosed. Use of the cyclic tertiary amine compound as a hole transport material, a hole injection material or an organic electroluminescent material can provide organic EL devices having high luminous efficiency and a long service life.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.

Abstract: The invention concerns a novel dyeing composition for dyeing keratinous fibers, in particular human hair, comprising a cationic azo-dye of formula (I): W1-N?N-W2-W3, as well as the dyeing method using said composition and the novel compounds of formula (I).

Abstract: The present invention provides a bleaching composition comprising a [3.3.1] bicyclo compound carrying at least one tertiary amine group the bleaching composition substantially devoid of a peroxygen source.

Abstract: The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic chiral diphosphine ligand, an amino-thioether ligand, and a base.

Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the

Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Compounds having the formula: are disclosed. M1 and M2 are the same or different and are transition metal atoms or ions; Z2 and Z3, independently, are the atoms necessary to complete a 3-12 membered heterocyclic ring; Z1 is an alkylene or arylene group; Q1 and Q2 are the same or different and are electron withdrawing groups; L1 and L3, taken together, represent —O—CR13—O—; L2 and L4, taken together, represent —O—CR14—O—; and R13 and R14 are the same or different and are selected from the group consisting of alkyl groups and aryl groups or R13 and R14 represent alkylene or arylene groups that are directly or indirectly bonded to one another. Methods for making such compounds are also disclosed, as are intermediates which can be used in their preparation. Also disclosed are methods for carrying out C—H insertion reactions using bis-transition metal catalysts, such as the above compounds.

Abstract: This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consisting of 1

Abstract: This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consisting of wherein R and R′ can be the same or different and represent allyl, alkoxyl or alkyl groups containing from 1 to about 10 carbon atoms, and wherein X represents a halogen atom, and wherein m represents an integer from 4 to about 10, and wherein X represents a halogen atom; and (2) reacting the vinyl halide containing secondary amine with a vinyl magnesium halide to produce the monomer having a structural formula wherein R and R′ can be the same or different and represent alkyl, allyl or alkoxyl groups containing from 1 to about 10 carbon atoms, and wherein m represents an integer from about 4 to about 10.

Abstract: An ammonium selective ionophore for use in ion selective electrodes.

Abstract: The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts.

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Compounds represented by the following general formula: 1

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group, consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the

Abstract: The present invention provides novel sigma-2 ligands (labeled and unlabeled) and the use of the compounds in medical therapy or diagnosis.

Abstract: The present invention provides certain N-substituted sulfonamide 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 relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclodimerization, depending on the particular reaction conditions. Any alkyne metathesis catalyst can be used as the catalyst, regardless of whether said catalysts are heterogeneously or homogeneously present in the reaction medium. The preferred catalysts or pre-catalysts are transition metal alkylidyne complexes, transition metal compounds which form alkylidyne complexes under the reaction conditions, and transition metal compounds with metal-metal triple bonds. The method can be carried out with numerous functional groups, solvents, and additives.

Abstract: The present application describes novel amides and derivatives thereof of formula 1

Abstract: Fuel additives comprise a compound having a group represented by the formula >C═=N—  (1). Also disclosed are fuel compositions containing such additives. The additives have a superior detergent effect to conventional gasoline detergents and an excellent detergency of the injection nozzles of a diesel engine and is free from being sludge.

Abstract: This invention provides the use of macrocyclic amines for inhibition of cellular invasion or angiogenesis. Compounds and pharmaceutical compositions of this invention are useful in the treatment of conditions characterized by cellular invasion or angiogenesis, including cancer. Compounds that may be used in this invention include the motuporamines.