Abstract: A catalyst composition, method of formation and process of use in the polymerization of olefin monomers, said composition comprising a catalyst compound, an activator capable of converting said catalyst compound into an active catalyst for addition polymerization, optionally a carrier, further optionally a liquid diluent, and a hydroxycarboxylate metal salt additive.

Abstract: A 1-butene/ethylene copolymer having a content of ethylene derived units from 0.1% to 5% by weight in which an ethylene content in the polymer (C2) and a melting point of the polymer (Tm) meet the following relation: Tm<?0.3283C23+4.7184C22?22.454C2+114.

Abstract: A polymerization initiator composition which does not burn or ignite even when it contacts paper or the like in air and can provide high polymerization activity to a polymerizable composition to cure it in a short period of time, and an adhesive composition comprising the same. The above polymerization initiator composition comprises 100 parts by weight of (A) an organic boron compound such as a trialkyl boron, alkoxyalkyl boron, dialkylborane, monocyclo or bicyclo compound having a boron atom as a hetero atom or partially oxidated trialkyl boron, 5 to 40 parts by weight of (B) an aprotic solvent having a boiling point of 50 to 120° C., and 0.2 to 5 parts by weight of (C) an alcohol having a boiling point of 60 to 180° C.

Abstract: A method of modifying a polyethylene is disclosed. In the method ethylene or a mixture of ethylene and a C3-C10 ?-olefin is polymerized in an organic solvent with a Ziegler or single-site catalyst to form an initial polyethylene solution. The initial polyethylene solution is then reacted with a free radical initiator to produce a modified polyethylene. The modified polymer has an enhanced melt elasticity and increased long chain branching index, and is essentially free of gel.

Abstract: The present invention relates to a process for the removal of solvent from a polymer emulsion or suspension, by use of a decanter centrifuge (10). The decanter centrifuge (10) provides an efficient thickening method. The process is especially useful for emulsion or suspension polymer compositions having high levels of solvent (low polymer solids) that could benefit from a thickening or dewatering step prior to drying in a dryer (14).

Abstract: A polyvinylidene difluoride copolymer with a fluoroolefin selected from 2,3,3,3-tetrafluoropropene, 1,1,3,3,3-pentafluoropropene, 2-chloro-pentafluoropropene, hexafluoropropylene, trifluoroethylene, chlorotrifluoroethylene, 3,3,3-trifluoro-2-trifluoromethylpropene and a mixture thereof, wherein the stoichiometry of the co-monomers defines the barrier properties of the copolymer. Such polymers include moisture barrier copolymers and oxygen barrier copolymer. Processes for preparing such moisture barrier copolymers and oxygen barrier copolymers are also provided.

Abstract: In a process for producing crosslinkable organopolysiloxane compositions, in particular organopolysiloxane compositions which can be crosslinked at room temperature, the organopolysiloxane compositions are stored in a storage unit before being packed in moisture-proof containers, the storage having a storage capacity of at least 15 minutes of production capacity of the mixture, the essentially dead-space-free storage unit continually having an internal pressure of more than 1200 hPa during filling.

Abstract: A polysiloxane represented by the formula (1) or (2): where R, R1, R2, m and n are defined in the specification.

Abstract: In a method for crystallising plastic granules with a tendency to conglutinate, in particular PET and PU granules, the granules are subjected to vibratory excitation in a vibrating trough (1) transversely to the direction of longitudinal extension of the vibrating trough (1), at around their reaction temperature. The flow of granules follows a spiral path through the trough, achieving a narrow dwell time spectrum and a homogenous temperature gradient for the granules. Conglutination is also reliably prevented.

Abstract: The present invention is directed to a method for reducing the onset or incidence of gelation/fibrillation/aggregation during the up- and down-stream processing and purification of peptides, polypeptides and proteins analogs and/or derivatives thereof, including Glucagon-Like Peptides (GLPs). More particularly, the present invention relates to methods of processing and purifying such peptides, polypeptides and proteins in the presence of tris(hydroxymethyl)aminomethane.

Abstract: A novel method for side chain cyclisation of peptides by means of lactamization is provided.

Abstract: The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

Abstract: The invention relates to modified proteins of the superfamily of “ubiquitin-like proteins”, proteins that have a ubiquitin-like fold and fragments or fusion proteins thereof. As a result of said modification, the proteins have a binding affinity with respect to a predetermined binding partner that did not exist previously. The invention also relates to a method for the production and utilization of said proteins.

Abstract: The present invention relates to compositions and methods for fusion protein separation utilizing a peptide linker comprising a novel thrombin cleavage site.

Abstract: The present invention is directed to a method for synthesizing a peptide using solid-state chemistry in which at least one amide bond is N-methylated, wherein said method of synthesis utilizes N-Boc protected amino acids. For example, the a peptide is first synthesized using N-BOC protected amino acids and 4-methylbenzylhydrylamine functionalized 1% cross linked polystyrene resin until reaching the amide bond to be N-methylated. Then, the amino group at the desired methylation site is methylated. If desired, the synthesis of additional peptide using N-BOC protected amino acids may continued until the desired peptide is complete.

Abstract: The invention provides isolated nucleic acid and amino acid sequences of novel human tumor suppressors, antibodies to such tumor suppressors, methods of detecting such nucleic acids and proteins, methods of screening for modulators of tumor suppressors, and methods of diagnosing and treating tumors with such nucleic acids and proteins.

Abstract: The invention provides for a polyvalent protein complex (PPC) comprising two polypeptide chains generally arranged laterally to one another. Each polypeptide chain typically comprises 3 or 4 “v-regions”, which comprise amino acid sequences capable of forming an antigen binding site when matched with a corresponding v-region on the opposite polypeptide chain. Up to about 6 “v-regions” can be used on each polypeptide chain. The v-regions of each polypeptide chain are connected linearly to one another and may be connected by interspersed linking regions. When arranged in the form of the PPC, the v-regions on each polypeptide chain form individual antigen binding sites.

Abstract: The present invention discloses a method for targeting maytansinoids to a selected cell population, the method comprising contacting a cell population or tissue suspected of containing the selected cell population with a cell-binding agent maytansinoid conjugate, wherein one or more maytansinoids is covalently linked to the cell-binding agent via a non-cleavable linker and the cell-binding agent binds to cells of the selected cell population.

Abstract: The present invention describes a novel process for large scale purification of therapeutic grade quality of recombinant human G-CSF from microbial cells, wherein the protein is expressed as inclusion bodies. The process involves the novel use of Hydrophobic Interaction Chromatography (HIC) step to purify G-CSF eluted from a cation exchange column. A combination of these two chromatography steps provides good purity and yields which are essential for a production scale process. The host cell related contaminants like proteins, DNA and endotoxins are estimated to be within the specifications outlined by the drug regulatory authorities.

Abstract: The present invention relates to a new optically active rare earth complex (1) represented by a general formula (1); (in the formula, X1 and X2 each independently represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxyl group having 1 to 4 carbon atoms; Y1, Y2, Y3, and Y4, each independently represents a hydrogen atom, a halogen atom, or an alkyl group having 1 to 4 carbon atoms; R1 represents an alkyl group having 1 to 8 carbon atoms, a fluorine-substituted alkyl group having 1 to 8 carbon atoms, or a phenyl group: R2 is a group selected from the group consisting of (a) cyclopentadienyl groups, (b) phenyl groups, and (c) naphthyl groups).

Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2?-arabino-fluoronucleoside and an internucleoside 3?-NH—P(?O)(OR)—O-5? linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2?-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

Abstract: The preparation and use of nucleic acid fragments encoding plant fatty acid modifying enzymes associated with conjugated double bond formation or functionally equivalent subfragments thereof are disclosed. Chimeric genes incorporating such nucleic acid fragments or functionally equivalent subfragments thereof or complement thereof and suitable regulatory sequences can be used to create transgenic plants having altered lipid profiles.

Abstract: The invention relates to an isolated RNA that mediates RNA interference of an mRNA to which it corresponds and a method of mediating RNA interference of mRNA of a gene in a cell or organism using the isolated RNA.

Abstract: The invention relates to an isolated RNA that mediates RNA interference of an mRNA to which it corresponds and a method of mediating RNA interference of mRNA of a gene in a cell or organism using the isolated RNA.

Abstract: The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with alkyl halide or alkyl sulfonate in the presence of alcohol of Chemistry (FIG. 1) as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

Abstract: An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

Abstract: The present invention discloses a method for targeting maytansinoids to a selected cell population, the method comprising contacting a cell population or tissue suspected of containing the selected cell population with a cell-binding agent maytansinoid conjugate, wherein one or more maytansinoids is covalently linked to the cell-binding agent via a non-cleavable linker and the cell-binding agent binds to cells of the selected cell population.

Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(methanolate) and ways to make it are disclosed.

Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(tetrahydrofuranate) and ways to make it are disclosed.

Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(carboxylate)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one methanolate pentahydrate and ways to make it are disclosed.

Abstract: A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a —(CH2)2—OH group or a —(CH2)2-0-(CH2)2—OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR)4, where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is —CH2)2-0-(CH2)2—OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate.

Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.

Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Abstract: A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric amine with a halogen-substituted heterocyclic compound, or a stereoisomeric ketone or aldehyde with an amino-substituted heterocyclic compound. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.

Abstract: This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

Abstract: The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one.

Abstract: The present invention provides pure paliperidone as well as purification processes to obtain thereof.

Abstract: Compounds of the formula wherein, provided that at least one of R1, R2, and R3 is not hydrogen, R1, R2, and R3 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R1 and R2 can also be alkoxy, aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or wherein X is a direct bond, oxygen, sulfur, —NR40— wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or —CR50R60— wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl.

Abstract: This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity. Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.

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

Abstract: A novel solventless process is described for the preparation of imidazole-2-thiones. The new solventless process tolerates a variety of bases as co-reactants which introduces feedstock flexibility into the process while the solventless feature renders the process more environmentally friendly by eliminating volatile organic solvents from the process, reducing energy consumption (associated with solvent recovery and/or recycling), and allows shorter reaction time and workup. Furthermore, the elimination of solvents enhances workplace safety by obviating the need for flammable and/or toxic solvents.

Abstract: A Polymorph Form G of Fluvastatin sodium having X-ray diffraction peak at 2? value of 3.48 is provided. A process for the preparation of the novel polymorph Form G comprising spray drying a 3 to 10% w/v solution of Fluvastatin sodium in a solvent using a spray gun at inlet temperature of 120 to 200° C. and outlet temperature of 60 to 110° C. of the spray gun is also provided.

Abstract: The present invention provides an improved process for preparation of highly pure trandolapril. The process comprises of the following steps: (i) crystallization of mixture of racemic benzyl trans-(2S, 3aR, 7aS)-octahydro-1H-indole carboxylate p-toluene sulphonic acid salt (IIa.p-TsOH) and benzyl trans-(2R, 3aS, 7aR)-octahydro-1H-indole carboxylate p-toluene sulphonic acid salt (IIb.p-TsOH) through appropriate selection of solvents to enrich the purity to >99% from a mixture containing the other diastereomers (IIc-h.

Abstract: A plug-in Wi-Fi access point device and system is provided that is configured for Wi-Fi or other wireless network and to be directly plugged into a face plate/workstation. The plug-in Wi-Fi access point device and system advantageously provides ease of integration into an existing wired network without the use of a patch cord, security from removal by unauthorized personnel, non obtrusiveness in relation to other face plate/workstation jacks, and the ability to be powered through an Ethernet connection to avoid the need for a separate power source. Furthermore, the plug-in Wi-Fi access point device and system may beneficially permit the integration of complementary connections within the access point including, for example, data, voice, and video connection types.

Abstract: A compound of formula 10 is useful in making duloxetine.

Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.