Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N?X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.

Abstract: This invention relates to novel compounds of the class of succinoyl lactams, such as diazepinee of Formula (Id), or a pharmaceutically acceptable salt thereof, as described above, having drug and bio-affecting properties. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of Alzheimer's disease.

Abstract: The present invention relates to new 1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one compounds of formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, useful for treatment of impotence diseases: wherein R1 and R2 may be the same or different and independently be C1-6 alkyl. The present invention also provides a method of preparing the compounds of formula (I).

Abstract: The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: and pharmaceutical compositions thereof, and methods for controlling the level of one or more inflammation inducing cytokines selected from the group consisting of, interleukin-1 (IL-1), Tumor Necrosis Factor-?(TNF-?), interleukin-6 (IL-6), and interleukin-8 (IL-8), thereby controlling, mediating, or abating disease states affected by the level of extracellular inflammatory cytokines in humans.

Abstract: [7-(3-chloro-4-methoxybenzylamino)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-ylmethoxy]acetic acid, is disclosed, as well as a process for its preperation and intermediates in the process of preparing the same.

Abstract: Compounds of formula (I): are described herein. The compounds can be used, for example, in the treatment of chemokine mediated diseases, including inflammatory diseases such as psoriasis and COPD.

Abstract: The present invention relates to pyrazolopyrimidines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.

Abstract: A method for isolating nucleic acid which comprises: (a) applying a sample comprising cells containing nucleic acid to a filter, whereby the cells are retained as a retentate and contaminants are removed; (b) lysing the retentate from step (a) while the retentate is retained by the filter to form a cell lysate containing the nucleic acid; (c) filtering the cell lysate with the filter to retain the nucleic acid and remove remaining cell lysate; (d) optionally washing the nucleic acid retained by the filter; and (e) eluting the nucleic acid, wherein the filter composition and dimensions are selected so that the filter is capable of retaining the cells and the nucleic acid. Additionally, there is provided a substrate for lysing cells and purifying nucleic acid having a matrix and a coating and an integrity maintainer for maintaining the purified nucleic acid.

Abstract: The present invention relates to certain substituted phenyl piperazinyl oxazolidinones, for example, to those having the structure of Formula I with the variables as defined within, and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight or branched alkyl, Ar-substituted- (C1-C10)-straight or branched alkyl, (C2-C10)-straight or branched alkenyl or alkynyl, or Ar-substituted-(C2-C10)-straight or branched alkenyl or alkynyl; wherein one to two CH2 groups of said alkyl, alkenyl, or alkynyl chains in each of R1, R2, R3 and R4 are optionally and independently replaced with O, S, S(O), S(O), S(O)2, C(O) or N(R5) in a chemically stable arrangement, wherein the CH2 group of R1 and R2 bound directly to said nitrogen cannot be replaced with C(O); or R1 and R2 taken together form a 4 to 7 membered ring; or R3 and R4 taken together form a 3 to 7 membered ring; wherein a CH2 in either the R1 and R2 ring system or the R3 and R4 ring system is independently and optionally replaced with O, C(O), N(R5), S, S(O), S(O)2 in a chemically stable arrangement; or wherein either or both of the R1 and R2 ring system and the R3 and R4 ring sy

Abstract: A method of treating psychosis in a patient which comprises administering a pharmaceutical composition useful in treating psychosis containing a therapeutically effective amount of 1-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one as an active ingredient.

Abstract: Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, being represented by the general formula (I). are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

Abstract: Two new crystalline forms of 1S-[1alpha(2S*, 3R*), 9alpha]6, 10-dioxo-N-(2-ethoxy-5-oxo-tetrahydro-3-furany1)-9 [[(1-isoquinolyl) carbony1]amino]octahydro-6H-pyridazino [1,2-a][1,2]diazepin-1-carboxamide (anhydrous or hydrated), their preparation process and the pharmaceutical compositions containing them.

Abstract: Compounds of the formula which are useful in disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: A process for the manufacture of: wherein R is (1-4C)alkyl, carboxyl(1-4C)alkyl or 1,3,4-oxadiazol-2-yl comprises: (a) reaction of the diazonium salt of 3-amino-2-chloropyridine with thionyl chloride in water and an electron transfer catalyst; (b) reaction with isobutyl-(3-methoxy-5-methylpyrazin-2-yl)carbamate and an alkali metal hydride in inert solvent; and (I) where R is (1-4C)alkyl, carboxy(1-4C)alkyl: (c) reaction with a boronic acid: (or an anhydride or ester therof) in the presence of a base and a palladium or nickel catalyst in solvent; and removal of the isobutoxy carbonyl group; or (ii) where R is 1,3,4-oxadiazol-2-yl (c) reaction with 4-methoxycarbonylphenylboronic acid (or an anhydride or ester thereof) with a source fluoride ion under aqueous conditions; (d) removal of the isobutoxycarbonyl protecting group; (e) conversion of the methyl ester group to the hydrazide; and (f) conversion to a 1,3,4-oxadiazol-2-yl moiety.

Abstract: In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of rotamers of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance.

Abstract: The invention relates to new 6-phenylpyrrolopyrimidine derivatives of formula (I): wherein: —X—C—Y— represents or —X—C—Y— represents and to their use as selective cyclic GMP specific phosphodiesterase (PDE 5)inhibitors, processes for producing them, intermediates used in their production, compositions containing them and their applicability in medical treatment of the human or animal body.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.