Abstract: A process for manufacturing multiparticulate pharmaceutical compositions using a roller compactor. The process is particularly useful for producing minitablets without the need of the use of a tablet press. The roller compactor features rolls having depressions or molds in the surface. Upon compaction of pharmaceutical blend, the minitablets are formed by the depressions in the roller surfaces.

Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:

Abstract: The invention relates to a pouch for containing a product. The pouch comprises a first wall and a second wall which are sealed together in sealed regions. The sealed regions substantially surround a compartment portion within which a product can be located. The pouch includes a tear initiating weakness located away from an edge of the pouch, the tear initiating weakness comprising an elongate weakness which extends along a first axis such that a user can fold the pouch across the tear initiating weakness and initiate a tear from the folded edge substantially along the first axis, the pouch further comprises at least one tear guiding weakness, said tear guiding weakness extending along a second axis transverse to the first axis such that a tear extending substantially along the first axis will meet the at least one tear guiding weakness and be guided along the second axis.

Abstract: Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32-hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and ?,??-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.

Abstract: Microparticles consisting of (a) a matrix with a mixture of (a1) at least one hydrophobic, biologically degradable polymer and (a2) optionally at least one water-soluble polymer, (b) a pharmaceutical active ingredient distributed in the matrix, and (c) in addition at least one water-insoluble, surface-active substance from the group of lecithins and phospholipids, distributed in the matrix, and a three-phase emulsion process for their preparation.

Abstract: Novel chemical compounds of the general formula K+A?, in which K+ is a 5- or 6-membered heterocyclic ring having 1-3 hetereo atoms, which can be independently N, S, or O; with the proviso that at least one of the hetereo atoms must be a quaternized nitrogen atom having a —R?CN substituent, wherein R? is alkyl (C1 to C12); the heterocyclic ring having up to 4 or 5 substituents independently chosen from the moieties: (i) H; (ii) halogen or (iii) alkyl (C1 to C12), which is unsubstituted or partially or fully substituted by further groups, preferably F, Cl, N(CnF(2n+1?x)Hx)2, O(CnF(2n+1?x)Hx), SO2(CnF(2n+1?x)Hx)2 or CnF(2n+1?x)Hx where 1<n<6 and 0<x<13; and (iv) a phenyl ring which is unsubstituted or partially or fully substituted by further groups, preferably F, Cl, N(CnF(2n+1?x)Hx)2, O(CnF(2n+1?x)Hx), SO2(CnF(2n+1?x)Hx)2 or CnF(2n+1?x)Hx where 1<n<6 and 0<x?13; and A? is any anion that provides a salt with a low melting point, below about 100° C.

Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceutical excipient, to the formulation. The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceutical excipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.

Abstract: The invention provides methods of protecting solid-state proteins from the effects of ionizing radiation which comprise combining the protein with a radiation-protecting amount of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde; radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde, and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid; or radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde and isopropanol, prior to exposing the protein to ionizing radiation.

Abstract: Pharmaceutical kits are provided that reduce or prevent oxidative degradation of oxygen-sensitive pharmaceutically active ingredients in solid unit dosage forms that are supplied in oxygen permeable containers. Stabilization of the active ingredient is accomplished by incorporating an oxygen absorber into a sealed oxygen permeable container.

Abstract: This invention relates to methods for preparing certain cholesteryl ester transfer protein (CETP) inhibitors and intermediates useful in the preparation of said CETP inhibitors.

Abstract: Sustained release dosage forms of sertraline which release sertraline at a rate between 1 mgA/hr and 40 mgA/hr. The dosage forms may exhibit an initial delay period during which sertraline is released at a rate less than 1 mgA/hr.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula at least one coupler comprising a compound of the formula (1): wherein R is selected from of C1 to C2 alkyl and hydroxyethyl, R1 and R2 are each independently selected from the group consisting of C1 to C5 alkyl, C3 to C6 cycloalkyl, C1 to C5 alkoxy, C1 to C5 hydroxyalkyl, C1 to C5 hydroxyalkoxy, or R1 and R2 together with the carbon atom to which they are attached form a C3 to C6 cycloalkyl group.

Abstract: 1-(2,5-Diaminophenyl)ethanol useful as a primary intermediate for the oxidative dyeing of hair.

Abstract: Inorganic peroxymonosulfate salts used as oxidizing agents for the oxidative dyeing of hair.

Abstract: The invention provides compositions for mending split ends of keratinous fibers, particularly human hair. The compositions of the present invention contain guar, a betaine based polyurethane surfactant and a silicone polyurethane.

Abstract: An immunological method to determine protein activity wherein a variety of proteins may be assayed with a single antibody on standard equipment is provided.

Abstract: There is provided a method or system that utilizes fluorescence in a sample that would otherwise yield inaccurate results due to spectrally interfering components. The system quantifies spectral interference of a fluorescent label.

Abstract: Described herein is the use of a substantially pure form of an oxidized polyamine, and especially spermine dialdehyde, in the treatment of tissue grafts or other organs for transplantation. The compounds and treatment are especially useful in treating grafts for bone marrow transplants, whether they be allogeneic or autograft transplants.

Abstract: 5-Heterocyclic 2-(2-imidazolin-2-yl)pyridine compounds which are effective for the control of undesirable plant species are described. Also described are a method for the herbicidal use of said compounds and a method for their preparation.

Abstract: There are provided certain 13-halo-23-imino-LL-F28249 compounds which are useful for controlling endo- and ectoparasites, insects, acarids and nematodes.