Abstract: The invention relates to a process for deblocking substantially a blocked, detectably labeled oligonucleotide by contacting the blocked detectably labeled oligonucleotide with an effective amount of a nucleophilic amino compound under conditions that result in substantial deblocking of the oligonucleotide, thereby giving the substantially deblocked oligonucleotide.

Abstract: The invention relates to conjugates including at least one linker, a biomolecule coupled to the linker, and cyclohexane derivatives of the following formula: and oligomers thereof.

Abstract: Methods of inhibiting angiogenesis in humans and animals by administering a effective amount of a secondary plant metabolite from jojoba, having the general formula I shown below, are disclosed. Preferred compounds having general formula I include 4-desmethylsimmondsin, 5-desmethylsimmondsin, 4,5-didesmethylsimmondsin, 4,5-dimethylsimmondsin, 4-desmethylsimmondsin-2?-ferulate, 5-desmethylsimmondsin-2?-ferulate, 4,5-didesmethylsimmondsin-2?-ferulate and 4,5-dimethylsimmondsin-2?-ferulate. Such compounds can be synthesized chemically according to well known techniques or can be isolated from refined and de-oiled jojoba flour by conventional extraction techniques using polar solvents such as a ketone or a low boiling point alcohol.

Abstract: 1-?-D-Arabinofuranosyluracil in 3?,5?-hydroxyl-protected form is reacted with a trifluoromethanesulfonylating agent in the presence of an organic base to convert it into a 2?-triflate form, and then it is reacted with a fluorinating agent containing “a salt or complex formed by an organic base and hydrofluoric acid” to produce 2?-deoxy-2?-fluorouridine in 3?,5?-hydroxyl-protected form. A deprotecting agent is further caused to act thereon to obtain 2?-deoxy-2?-fluorouridine. The 2?-deoxy-2?-fluorouridine obtained can efficiently be purified by temporarily converting it into a 3?,5?-diacetyl form, recrystallizing the 3?,5?-diacetyl form, and then deacetylating it. Thus, high-purity 2?-deoxy-2?-fluorouridine can be produced.

Abstract: Embodiments of the present invention include compositions and pharmaceutical compositions comprising citrulline and Hmg-CoA reductase inhibitors. Further embodiments relate to the use of such composition treat subjects and stimulating nitric oxide synthase.

Abstract: A method for treating an adenocarcinoma excluding colon cancer, lung cancer and gastric cancer, comprising administering to a subject in need thereof and suffering from adenocarcinoma cancer, a pharmaceutically effective amount of at least one sulfoquinovosylacylglycerol compound represented by formula (1): wherein R101 represents an acyl residue of an unsaturated higher fatty acid, and R102 represents a hydrogen atom, and/or at least one pharmaceutically acceptable salt thereof.

Abstract: Processes for isolation and purification of enantiomerically enriched compositions comprising tramadol and topiramate, and also for the subsequent isolation of 1S,2S-tramadol hydrochloride, are disclosed herein.

Abstract: Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.

Abstract: Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or pharmacology as, for example, active compounds for crop protection or pharmaceuticals for humans or animals.

Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2, and L are defined in the description.

Abstract: An improved process for preparing N6 -substituted aminopurine ribofuranose nucleosides. Compounds of this type are known to be usefull in the prepartation of compounds having activitity at adenosine receptors, e.g. Adenosine A1 receptor. The process comprises the step of reacting a 6-halopurine ribofuranose nucleoside with an amine in the presence of CaCO3 , wherein acid is added to the reaction mixture.

Abstract: The present invention is directed to the process for the preparation of 2?-deoxy-2?-halo-?-L-arabinofuranosyl nucleosides, and in particular, 2?-deoxy-2?-fluoro-?-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.

Abstract: The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with ?-effect nucleophiles. The ?-effect nucleophile irreversibly cleave the carbonate protecting groups while simultaneously oxidizing the internucleotide phosphite triester linkage to a phosphodiester linkage. The procedure may be carried out in aqueous solution at neutral to mildly basic pH. The method eliminates the need for separate deprotection and oxidation steps, and, since the use of acid to remove protecting groups is unnecessary, acid-induced depurination is avoided. Fluorescent or other readily detectable carbonate protecting groups can be used, enabling monitoring of individual reaction steps during oligonucleotide synthesis. The invention is particularly useful in the highly parallel, microscale synthesis of oligonucleotides.

Abstract: Surfaces containing high purity silica (silicon dioxide) exhibit high loading potential for nucleic acids. Formulations containing nucleic acids and materials which mask the electrostatic interactions between the nucleic acids and surfaces are disclosed. By masking the phosphate charges of the nucleic acids, undesired interactions may be minimized or eliminated, thereby allowing the covalent bonding of the nucleic acids to the surface to proceed. The use of such formulations additionally minimizes nonspecific binding of the nucleic acids to the surface. Examples of materials to be included in such formulations include cations, xanthines, hexoses, purines, arginine, lysine, polyarginine, polylysine, and quaternary ammonium salts.

Abstract: A process for the synthesis of phosphorothioate oligonucleotides is provided which comprises assembling an oligonucleotide bound to a solid support in the presence of acetonitrile; prior to cleaving the oligonucleotide from the solid support removing the acetonitrile; and cleaving the oligonucleotide from the solid support. The process is particularly suited to the large scale synthesis of nucleotides. The acetonitrile may be removed from the solid support by one or both of drying and by washing with solvents. Preferred washing solvents comprise trialkylamines.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.

Abstract: Provided are methods of producing phosphitylated compounds, including 3?-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula II wherein R3, R4, R5, R6, and R7 are independently hydrogen, C1–C10 alkyl, C3–C10 cycloalkyl, C6–C10 aryl, C7–C10 aralkyl, C1–C10 heteroalkyl, or C1–C10 heteroaryl, and at least one of R3, R4, R5, R6, and R7 is not hydrogen; (2) zwitterionic amine complexes; and (3) combinations of two or more thereof, to produce a phosphitylated compound. Further provided are methods for purifying phosphitylated compounds comprising the steps of providing a phosphitylated compound in a solution solvent, contacting said phosphitylated compound with a precipitation solvent, and precipitating said phosphitylated compound.

Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

Abstract: The present invention concerns novel C2,5?-disubstituted and N6,C2,5?-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.

Abstract: Antimicrobial compounds having the formula as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.