- Fluorescent hydrophobic probes based on intramolecular charge transfer state for sensitive protein detection in solution
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New hydrophobic intramolecular charge transfer probes, comprising an aminostyryl and a cyanopyranyl moieties, were developed for sensitive protein quantification in solution. The probes exhibited dramatic increase of fluorescence quantum yields with accompanying blue-shift of the emission when bound to protein-sodium dodecyl sulfate (SDS) complexes. Using this emission enhancement, the synthesized probes were successfully applied for determining protein concentrations in solution.
- Jun, Hyunsook,Soo, Yeon Hong,Seung, Soo Yoon,Kang, Chulhun,Suh, Myungkoo
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- SELECTIVE DETECTION OF BED BUGS
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A device, system, and method of controlling pests are disclosed. A pest control device includes a sensor having a sensor cell and a controller. A surface of the sensor cell is coated with an agent that reacts with a targeted biochemical analyte secreted b
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- 2-OXOIMIDAZOLIDINE-4-CARBOXAMIDES AS NAV1.8 INHIBITORS
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Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
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- ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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A compound comprising a first ligand LA of Formula I, is disclosed. In the structure of Formula I, ring A is a 5-membered or 6-membered carbocyclic or heterocyclic ring; Z1-Z4 are each independently C or N; at least two co
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- Semiconducting Material Comprising a Phosphine Oxide Matrix and Metal Salt
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The present invention is directed to a semiconducting material comprising: i) a compound according to formula (I) wherein R1, R2 and R3 are independently selected from C1-C30-alkyl, C3-C30 cycloalkyl, C2-C30-heteroalkyl, C6-C30-aryl, C2-C30-heteroaryl, C1-C30-alkoxy, C3-C30-cycloalkyloxy, C6-C30 aryloxy, and from structural unit having general formula E-A-, wherein—A is a C6-C30 phenylene spacer unit, and—E is an electron transporting unit that is selected from C10-C60 aryl and C6-C60 heteroaryl comprising up to 6 heteroatoms independently selected from O, S, P, Si and B and that comprises a conjugated system of at least 10 delocalized electrons, and—at least one group selected from R1, R2 and R3 has the general formula E-A-; and ii) at least one complex of a monovalent metal having formula (II) wherein—M+ is a positive metal ion bearing a single elementary charge, and each of A1, A2, A3 and A4 is independently selected from H, substituted or unsubstituted C6-C20 aryl and substituted or unsubstituted C2-C20 heteroaryl, wherein a heteroaryl ring of at least 5 ring-forming atoms of the substituted or unsubstituted C2-C20 heteroaryl comprises at least one hetero atom selected from O, S and N.
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- Subcutaneous Delivery of Poly(oxazoline) Polymer Conjugates
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The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.
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- Semiconducting Material Comprising Aza-Substituted Phosphine Oxide Matrix and Metal Salt
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The present invention relates to a semiconducting material including at least one salt or complex of a metal cation and an aza-substituted phosphine oxide compound with improved electrical properties, and to a compound suitable for this organic semiconducting material and an electronic device utilizing the improved electrical properties of the semiconducting material.
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- SENESCENCE TRACERS
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The instant invention relates to novel compounds useful for visualizing cell senescence, their preparation and use. In particular, this invention relates to novel fucose and aminoquinoline derivatives useful as senescence traces and their preparation.
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(2015/06/24)
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- ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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Compounds having the structure of Formula M(LA)x(LB)y and Formula III, are disclosed. In Formula M(LA)x(LB)y, Ligand LA is and ligand LB is a mono anionic bidentate ligand. In these compounds, metal M has an atomic number greater than 40; x is 1, 2, or 3; y is 0, 1, or 2; x+y is the oxidation state of metal M; L11 represents a linking group selected from alkyl, cycloalkyl, aryl, and heteroaryl; L12 represents a linking group selected from NR15 and PR15; each R1, R2, R3, R4, R5, R6, R11, R12, R13, R14, and R15 is independently selected from a group of substituents, wherein any adjacent substituents are optionally joined to form a fused or unfused ring; and LA and LB are optionally joined to form a ligand that is at least tetradentate. Formulations and devices, such as OLEDs, that include the compound of Formula M(LA)x(LB)y are also described.
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- POLYNUCLEOTIDES HAVING BIOREVERSIBLE GROUPS
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The disclosure provides methods and compositions for delivering polynucleotides into cells. The disclosure provides transiently protected polynucleotides comprising an anionic charge-neutralizing moiety/group, which may also confer additional functionalit
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- Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
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PI3Kβ selective compounds having the structure
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- Polymer and organic electronic device
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A polymer comprising repeat units of formula (I) and one or more co-repeat units: Ar1 in each occurrence independently represent an aryl or heteroaryl group; R1 and R2 in each occurrence independently represent a substitue
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(2014/06/24)
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- CYCLIC ETHER PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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(2014/04/03)
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- Branched Linker for Protein Drug Conjugates
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The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.
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(2014/01/07)
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- HOST MATERIALS FOR PHOSPHORESCENT OLEDS
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Novel aryl silicon and aryl germanium host materials are described. These compounds improve OLED device performance when used as hosts in the emissive layer of the OLED.
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(2013/03/26)
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- Process for making bivalirudin
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The present invention relates to the efficient commercial synthesis of Bivalirudin.
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- Host materials for oled
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Novel aryl silicon and aryl germanium host materials are described. These compounds improve OLED device performance when used as hosts in the emissive layer of the OLED.
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- Use of PI3K inibitors for the treatment of obesity
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The first aspect of the invention relates to a phosphoinositide 3-kinase inhibitor for use in the treatment or prevention of a disease or condition associated with the expression of peroxisome proliferator-activated receptor gamma coactivator 1-α (Pgc1α)
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- PEPTIDE ANALOGUES
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The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists
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- HIGHLY ACTIVE METATHESIS CATALYSTS SELECTIVE FOR ROMP AND RCM REACTIONS
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The present invention relates to a kind of novel carbene ligands and ruthenium catalysts, which is highly active and selective for ROMP and RCM reactions, respectively. It discloses the significant electronic and steric effect of different substituted carbene ligands on the catalytic activity and stability of corresponding carbene ruthenium complexes; some of novel ruthenium complexes in the invention can be broadly used as catalysts highly effectively and selective for ROMP and RCM reactions. The invention also relates to preparation of new ruthenium catalysts and the uses in metathesis. Moreover, the invention also provides effective methods of making various functional polymers by ROMP reaction in the presence of new ruthenium catalysts.
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- METHODS OF NEUROPROTECTION USING NEUROPROTECTIVE STEROIDS AND A VITAMIN D
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Described herein are compositions and methods for treating or preventing nervous system injury. In particular, the methods and compositions relate to the use of at least one neuroprotective steroid, such as progesterone, and vitamin D.
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- COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PRODRUGS OF ACTIVE AGENTS AND INHIBITORS THEREOF
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The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.
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- Process for Making Bivalirudin
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The present invention relates to the efficient commercial synthesis of Bivalirudin.
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- POLYPEPTIDE COMPOUND
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[Problems] To provide an antibacterial agent, particularly a novel polypeptide compound having an antifungal action. [Means for Solution] As a result of an extensive study on a novel antifungal agent, the inventors have found that an excellent anti-deep-f
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- NUCLEIC ACID TERMINATORS INCORPORATING A CATIONIC MOIETY AND METHODS FOR THEIR USE
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Disclosed are methods and kits applicable to sequencing methods, such as Sanger dideoxy sequencing methods. The methods and kits disclosed utilize a cationically charged nucleic acid terminator in combination with a discriminatory polymerase.
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- Methods for the detection, identification, and/or enumeration of yeast, particularly in wine
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This invention is related to novel probes, probe sets, methods and kits pertaining to the detection, identification and/or quantitation of yeasts and particularly Dekkera bruxellensis (a.k.a. Brettanomyces) an organism that spoils wine. Preferred probes for the detection of one or more species of the Dekkera/Brettanomyces genus comprise a probing nucleobase sequence, at least a portion of which is selected from the group consisting of: AGC-GGG-TCT-ATT-AGA (Seq. ID No. 1); CCA-GGT-GAG-GGT-CGC (Seq. ID No. 2); CGG-TTG-CCC-GAT-TTC (Seq. ID No. 3); TCG-CCT-TCC-TCC-TCT (Seq. ID No. 4); CGG-TCT-CCA-GCG-ATT (Seq. ID No. 5); CAC-AAG-ATG-TCC-GCG (Seq. ID No. 6); GCG-GGC-ACT-AAT-TGA (Seq. ID No. 7); CAT-CCA-CGA-GGA-ACG (Seq. ID No. 8); GTG-TAA-ACC-AGG-TGC (Seq. ID No. 9); ATG-GCT-CCC-AGA-ACC (Seq. ID No. 10) and GAC-AGA-ATC-GAA-GGG (Seq. ID No. 11). The probes, probe sets, methods and kits of this invention are particularly well suited for use in the analysis of yeast in wine, beer and liquor and in the monitoring of contamination of in-process product as well as the equipment and facilities used to manufacture product in wineries and breweries.
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- 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives
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This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as δ-opioid or μ-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
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- Compound
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The present invention provides a process for preparing a modified lipid of the formula comprising reacting (I) a compound of the formula; and (ii) a compound of the formula wherein component (ii) is formulated as a liposome; wherein B is a lipid; wherein
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- N-heterocyclic inhibitors of TNF-α expression
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N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
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- Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
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The invention concerns Use of a compound of formula (I) or a physiologically acceptable salt, solvate or derivative thereof, in the manufacture of a medicament for the treatment of diseases ameliorated by LDL-r upregulation, to novel compounds and pharmac
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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- Modulators of LXR
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Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.
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- New phenylalanine derivatives
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Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
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- Novel guanidinobenzamides
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Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical form
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- N-heterocyclic inhibitors of TNF-alpha expression
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N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
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- N- heterocyclic inhibitors of TNF-alpha expression
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N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
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- Azabicyclooctane derivatives useful in the treatment of cardiac arrhythmias
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There is provided compounds of formula (I), wherein R1, R2, R3 and Ra to Rh have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias, a process for the preparation of compounds of formula (I), and intermediate compounds.
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- Phenylindole derivatives as 5-HT2A receptor ligands
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A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2Areceptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or preve
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- 2,5-substituted benzolsulfonylureas and thioureas methods for the production thereof use thereof and pharmaceutical preparations containing the same
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Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are
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- Cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives, processes for their preparation, their use, and pharmaceutical preparations comprising them
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The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.
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- Synthetic polymers and methods, kits or compositions for modulating the solubility of same
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This invention pertains to solubility enhanced polymers and methods, kits and compositions which enhance the aqueous solubility of said polymers. One set of preferred methods, kits and compositions embody or utilize phosphorous containing synthons and are most useful for modulating the solubility of synthetic nucleic acids and synthetic nucleic acid analogs. A second set of preferred methods, kits and compositions are most useful for modulating the aqueous solubility of peptides, other polyamides and most preferably peptide nucleic add (PNA) polymers.
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- N-cinnamoyl derivatives of beta-carboline
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Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3′,5′-monophoshate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be benef
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- Bicyclic inhibitors of protein farnesyl transferase
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PCT No. PCT/US98/03025 Sec. 371 Date Aug. 2, 1999 Sec. 102(e) Date Aug. 2, 1999 PCT Filed Feb. 11, 1998 PCT Pub. No. WO98/34921 PCT Pub. Date Aug. 13, 1998The present invention provides compounds of Formula (I). The present invention also provides a metho
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- L-N6 -(1-iminoethyl)lysine derivatives useful as nitric oxide synthase inhibitors
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There is disclosed a novel amino glycol derivatives of L-N6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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- Carboline derivatives
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Carboline derivatives of formula (I) are potent and selective inhibitors of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP-specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.
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- Indole derivatives and pharmaceutical use thereof
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The invention relates to the compound of formula (I) STR1 wherein A represents an unsubstituted ethenyl group in the trans (E) configuration or a physiologically acceptable salt or metabilically labile ester thereof which are antagonists of excitatory ami
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- Memory enhancing and analgesic 1,2,3a,8,8a-hexahydro-3a,8(and 1,3a,8)-di(and tri)methylpyrrolo[2,3-b]indoles
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There are disclosed various derivatives of eseroline and related compounds of the formula below STR1 where R,R1, X,Z and m are as defined in the specification, which compounds being useful for enhancing cholinergic function, as antidepressant agents and as analgesic agents.
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