Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.

Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus.

Abstract: Adenosine analogue-type A3 receptor agonists having the formula wherein D is N or CH; E is O; X1 is a group of the formula —CR20R2 1-CYCLE, where R20 and R21 are the same or different and are H, F or CH3; CYCLE is where G is N, CH, CF, CCH3 or CCF3, M is H, Y is —O— or N?, and Z is —N? when Y is O, or is O when Y is —N?; R5 is H, CH3, I, Br, Cl, CF3, OH or NH2; and R8 is —NR9R10, —CHR9R10 or —N?CR9R10, where R9 and R10 are the same and are C1-C4 alkyl, C1-C4 alkenyl or C1-C4 alkoxyalkyl X2 is mono-N— or di-N,N—(C1-C4)alkylaminocarbonyl, mono-N—or di-N,N—(C3-C5)cycloalkyl-aminocarbonyl or N-(C1-C4)alkyl-N-(C3-C5)cycloalkylamino-carbonyl; X3 is OH or NH2; X4 is OH; X5 is H , halogen, (C1-C10)alkyl , (C2-C10)alkenyl , (C2-C10)alkynyl , or either of the latter two groups where terminally substituted by an aryl or heteroaryl group and, when having a terminal methyl group, optionally further terminally substituted by hydroxyl.

Abstract: Acetyl-L-carnitine (ALCAR) and L-carntine (LCAR) are nutraceuticals with indications in treating a variety of mental health disorders. A metabolomics-guided bioprocess method is presented to enhance ALCAR and LCAR formation in germinating plant seeds. Metabolic fluxes are manipulated by germination in bioreactors to increase oxygen availability as well as provide an aseptic environment to alter carbohydrate consumption and feedback repress gluconeogenesis. Large shifts in sunflower seed fatty acid, phospholipid and high-energy metabolism change the germination environment and these metabolic changes lead to an approximate 1000-fold increase in natural LCAR and ALCAR production by the seeds. The resulting LCAR and ALCAR products from the seeds are used for treating mental health disorders including Alzheimer's disease, geriatric depression, non-geriatric depression and schizophrenia.

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: Functionalized supports for polynucleotide synthesis are disclosed. The supports have linker moieties that are stable to conditions used in polynucleotide synthesis, but may be cleaved to release synthesized polynucleotides from the support. Methods of making the functionalized supports and methods of using are also disclosed.

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: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: This invention provides a method for treating a cancer subject comprising administering to the subject a combination of ATP-depleting agents at concentrations which deplete the ATP level to at least 15% of normal in cancer cells, a pyrimidine antagonist, and an anticancer agent to which the treated cancer is sensitive. This invention also provides a composition comprising a combination of ATP-depleting agents at concentrations which deplete the ATP level to at least 15% of normal in cancer cells, a pyrimidine antagonist, and an anticancer agent to which the treated cancer is sensitive. Finally this invention provides a pharmaceutical composition comprising the above composition or a combination thereof and a pharmaceutically acceptable carrier.

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: The present invention provides a therapeutic method for treating an inflammatory response caused by autoimmune stimulation, comprising the administration to a patient in need thereof of an antiinflammatory amount amount of an A2A adenosine receptor agonist. The autoimmune stimulation can be caused by arthritis, particularly rheumatoid arthritis. Optionally, the method includes administration of a type IV PDE inhibitor.

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: This invention relates to methods of inducing dephosphorylation of a hyperphosphorylated cell cycle regulatory protein in a tumor cell in which hyperphosphorylation of said protein contributed to cell transformation, the method comprising contacting the tumor cell with a procyanidin oligomer of five monomeric units connected via a C-4?C-8 linkage. Examples of such compounds are [EC-(4??8)]4-EC, and [EC-(4??8)]3-EC-(4??8)-C, wherein EC is epicatcchin and C is catechin.

Abstract: Alkyl-linked nucleotide non-homogeneous solid supports and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.

Abstract: The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1?7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e.

Abstract: The present invention provides methods of administering amifostine, WR-1065, or a combination thereof, to patients receiving radiation therapy or chemotherapy in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compounds as compared with conventional intravenous administration.

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: The present invention provides dinucleoside boranophosphate derivatives of the general formula I: wherein X and X? each independently is an unsubstituted or substituted purine or pyrimidine residue; Y and Y? each independently is H or OH; Z1 to Z5 each independently is O? or BH3?, but excluding the compounds wherein Z1 to Z5 are each O?; W1 to W4 each independently is O, CH2, NH or C(Halogen)2; n and n? each independently is 0 or 1; m is 3, 4 or 5; and M+ represents a pharmaceutically acceptable cation, and to pharmaceutical compositions thereof. These dinucleoside boranophosphates are useful for prevention or treatment of diseases or disorders modulated by P2Y receptors such as type 2 diabetes, cystic fibrosis and cancer.