Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor

Abstract: This invention provides O-?-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimehtylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): wherein the variables R1 and R2 are defined herein, and where the configuration at the steriogenic center (*) may be R, S, or RS (the racemate).

Abstract: This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula: wherein: A is C or N; B is O, S, N, or CH?CH; X is CO, CH(OH), CH2, or —CH—S-2-benzothiazole; Y is H, alkyl, or halo; Z is O, S, or N; R is H, nitro, alkyl, alkoxy, halo, or CF3; R1 is alkyl, aryl, aralkyl, halo, Het-alkyl, or optionally substituted aryl; Het is G is O, S, or N; R2 is H, halo, alkyl, or —OR5; R3 and R4 are H, halo, alkyl, aryl, nitro, amino, alkylsulfoamide, arylsulfoamide, cycloalkyl, heterocycle, or optionally substituted aryl; R5 is H, alkyl, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, CH(R7)(CH2)nCO2R9, or —CH(R7)C6H4CO2R9; R6 is alkylene; R7 is H, alkyl, aryl, aralkyl, cycloalkyl, phthalic acid, or Q-alkyl; Q is R8 is —CO2R11, —CONHR11, tetrazole, or —PO3R11; R9 is H, alkyl, aryl, or aralkyl; W is O, N, or S; R11 is H, alkyl, aryl, or aralkyl; n=1-6; or a pharmaceutically acceptable salt or ester form thereof.

Abstract: The present invention relates to processes for preventing particulate formation (e.g., aggregation, precipitation) of polysaccharide-protein conjugates comprised in a container means. In certain embodiments, the invention relates to processes for preventing particulate formation of polysaccharide-protein conjugates which are processed, developed, formulated, manufactured and/or stored in container means such as fermentors, bioreactors, vials, flasks, bags, syringes, rubber stoppers, tubing and the like.

Abstract: The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors.

Abstract: A method for treating a disease or disorder characterized by amyloid deposit of A-beta comprising administering to the subject a therapeutically effective amount of an antibody that binds specifically to RAGE and inhibits the binding of a RAGE binding partner.

Abstract: The present invention addresses an ongoing need in the art to improve the stability of immunogenic compositions such as polysaccharide-protein conjugates and protein immunogens. The invention broadly relates to novel formulations which stabilize and inhibit precipitation of immunogenic compositions. More particularly, the invention described hereinafter, addresses a need in the art for formulations which stabilize and inhibit particulate formation (e.g., aggregation, precipitation) of immunogenic compositions which are processed, developed, formulated, manufactured and/or stored in container means such as fermentors, bioreactors, vials, flasks, bags, syringes, rubber stoppers, tubing and the like.

Abstract: This invention relates to a method for recombinantly producing, via rescue of mumps virus, a nonsegmented, negative-sense, single-stranded RNA virus, and immunogenic compositions formed therefrom. Additional embodiments relate to methods of producing the mumps virus as an attenuated and/or infectious virus. The recombinant viruses are prepared from cDNA clones, and, accordingly, viruses having defined changes, including nucleotide/polynucleotide deletions, insertions, substitutions and re-arrangements, in the place of the genome are obtained.

Abstract: The present invention provides a salt form, and compositions thereof, useful as a modulator of one or more GPCRs and which exhibits desirable characteristics for the same. The present invention also provides methods for preparing said salt form.

Abstract: The construction of recombinant respiratory syncytial virus (RSV) strains deleted of the region of G protein most likely to induce unwanted type 2 T cell responses in susceptible recipients is disclosed. Using reverse genetics, recombinant RSV strains were engineered with deletions of amino acids 151-221 and 178-219. Both RSV strains replicated in the respiratory tract of BALB/c mice and elicited serum neutralization and anti-F protein IgG titers that were equivalent to cp-RSV and contributed to a 3.9 log 10 reduction in RSV A2 four days after challenge. Importantly, pulmonary eosinophilia was significantly diminished in BALB/c mice primed with native G protein and challenged with either recombinant RSV strain. These findings are important for the development of immunogenic compositions against RSV.

Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y?C, or substituted diene fused to Y when Y?C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, 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: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor

Abstract: The invention provides a process for recovering CCI-779 from mother liquors.

Abstract: The present invention is directed to crystal forms of the 5-HT2C agonist (S)-(8-(2,6-dichlorophenyl)-6-fluoro-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanamine hydrochloride, as well as compositions, processes of preparation, and uses thereof.

Abstract: The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making said hemifumarate.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Methods for preparing substituted phenylsulfonamide compounds of the following structure are provided: or a pharmaceutically acceptable salt thereof, wherein, R1-R7 are defined herein. Also provided are methods for preparing compounds of the following structure: wherein, R9, m, n, p, r, and s are defined herein.

Abstract: Novel purification processes for obtaining vesicular stomatitis virus (VSV) of improved purity from mammalian cell culture are described herein. More particularly, in certain embodiments, a process is described for purifying VSV from cell culture fluid of a mammalian cell culture infected with VSV, the process comprising: clarifying the cell culture fluid by low-speed centrifugation and recovering the VSV in the supernatant; filtering the supernatant through a 0.2 to 0.

Abstract: A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated with alkyl, substituted aryl or substituted heteroaryl is described. The method involves reacting a di-tert-butyl diazene-1,2-dicarboxylate with a (4S)-4-benzyl-3-[(S)-trifluoromethyl-alkyl substituted alkanoyl]-1,3-oxazolidin-2-one to afford a di-tert-butyl 1-(1S,2S)-([(4S)-4-benzyl-2-oxo-1,3-oxazolidine-3-yl]-carbonyl}-trifluoromethyl-alkyl substituted alkyl)hydrazine-1,2-dicarboxylate. This dicarboxylate is then reduced to yield di-tert-butyl 1-(1S,2S)-[trifluoromethyl-alkyl substituted alkyl]hydrazine-1-(hydroxymethyl)-1,2-dicarboxylate. The resulting product is deblocked with an acid to yield the acid addition salt of (2S,3S)-trifluoro-hydrazino-methyl alkan-1-ol. The acid addition salt of (2S,3S)-trifluor-2-hydrazino-methyl alkan-1-ol is hydrogenated in the presence of a suitable metal catalyst to yield the amino alcohol (2S,3S)-2-amino-trifluoro-methyl alkan-1-ol HCl.