Abstract: The present invention relates to compound 7-Chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazepin-6-one (I) and to the use of the compound of formula I for the manufacture of medicaments to be used as anxiolytic and/or anticonvulsant and/or non-sedative sleep-inducing medicaments.

Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: The present invention relates to 4-hydroxy-piperidine derivatives of the general formula wherein X denotes —O—, —NH—, —CH2—, —CH═, —CHOH—, —CO—, —S—, —SO— or —SO2—; R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido; R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy; a and b may be a double bond, provided that when “a” is a double bond, “b” cannot be a double bond; n is 0-2; m is 1-3; p is 0 or 1 and to pharmaceutically acceptable addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.

Abstract: The invention relates to compounds of formula wherein R1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or is phenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is —O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is —S-lower alkyl; R2 and R4 are independently from each other hydrogen, cyano or —S(O)2-phenyl; R3 is hydrogen, halogen or is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholin

Abstract: Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention relates to a process for manufacturing a pulverous preparation of a submicron-sized biologically active compound comprising the steps of dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; and rapidly expanding the compressed solution thereby precipitating the dissolved compound. An alternative process comprises dissolving the biologically active compound in compressed dimethylether, which may optionally contain a surface modifier; and spraying the compressed solution into an antisolvent phase, optionally containing a surface modifier, under vacuum, atmospheric pressure or elevated pressure. An optional third step involves converting the antisolvent phase into a pulverous preparation using conventional powder processing.

Abstract: The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.

Abstract: The invention relates to a solid pharmaceutical form of administration containing a diphosphonic acid or a physiologically compatible salt thereof as the active substance, wherein the active substance is present in granulate form, optionally together with pharmaceutical adjuvants in the inner phase, and the outer phase contains a lubricant in the form of less than 5% by weight of stearic acid relative to the total weight of the form of administration.

Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.

Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.

Abstract: A pipet gun for drawing liquids into and dispensing liquids from a pipet which includes a variable flow valve assembly. The valve assembly includes a valve which is capable of accommodating a plurality of flow rates, and which is progressively adjustable during pipetting between a first air flow rate and a second air flow rate which is in excess of the first flow rate and which is non-progressively adjustable during pipetting to a third air flow rate which is substantially greater than the second air flow rate. The valve assembly further includes a threshold detector in the form of a spring detent, which provides an indication to the operator that the pipet gun is operating at the increased fluid rate, i.e., the “express mode” of operation.

Abstract: A syringe includes an elongate barrel having an open proximal end and a distal end that includes a fitting. It also has a plunger having a proximal end and a distal end, sized for slidable movement within the barrel thereby defining a chamber within the barrel. The plunger also has an elongate cavity therewithin that has a closed proximal end and an open distal end. The open end of the plunger is closed by a selectively releasable closure. The syringe has a hub that attaches to the barrel with a fitting conjugate to the fitting. The hub includes an elongate needle having a proximal end, a distal end and a fluid path therethrough. The needle is positioned in the passageway for slidable movement between a first position wherein the fluid path of the needle is in fluid communication with the chamber and a second position. The needle has a mount at its proximal end forming a seal with the chamber when the needle is in the first position.

Abstract: A disconnect device for placement in a medical tubing set of the present invention includes a first portion with a first passageway therethrough that has a first valve therein. While the first valve is biased in a normally closed position to close the first passageway, it is operative to an open position. The disconnect device of the invention has a second portion with a second passageway therethrough that has a second valve therein. The second valve is also biased in a normally closed position to close the second passageway and it also is operative to an open position. The second portion is releasably attached to the first portion, connecting the first and second passageways in fluid communication, to overcome the bias of the first valve and the second valve, to open the valves and to allow a fluid flow through the device.

Abstract: A circuit for causing a voltage step in a battery of a plurality of serially-connected cells is provided. The circuit causes one or more of the cells to discharge through a resistor at a higher rate than the other cells, thus producing a voltage step when the faster discharging cell dies before the other cells. A reverse-biased diode is connected in parallel to the faster discharging cell to cause the current to bypass the faster discharging cell after it has died, thus preventing it from reverse charging. This circuit may be controlled to adjust the higher rate of discharge, and thus the time of occurrence of the voltage step.

Abstract: A method for programming an electronic pipetter to provide more precise measurement and dispensing is provided, as well as an improved display for displaying clearly and in detail the programming steps and options to the user thereof. The electronic pipetter may be operated in one of five modes, including a manual mode, a quick-shot mode, a multi-dispense mode, a sequential-dispense mode and a hands-free mode.

Abstract: A corneal incision device includes a surgical blade and a frame having an inner surface with a configuration that is generally in the shape of a ring-like segment of a hollow sphere. The frame has an aperture therein to allow the surgical blade to be inserted through the frame beyond the inner surface. The aperture is sized and shaped to allow movement of the surgical blade in one axis. The device may have a protuberance affixed to the inner surface of the frame adjacent to the aperture disposed to distort a surface of a patient's eye when the device is selectively positioned on the eye by a practitioner. The device has provisions for holding, advancing and withdrawing the surgical blade through the aperture, disposed on the frame. The device is releasably retained on the patient's eye by fixation elements disposed on the inner surface of the frame. There is a handle affixed to the frame to facilitate the practitioner's manipulation of device.

Abstract: A contamination resistant connector for medical tubing includes a first portion with a first fluid passage therethrough occluded by a covered normally closed first valve and a second portion with a second fluid passage therethrough. The second portion is conjugate to and releasably attachable to the first portion with the second fluid passage also being occluded by a covered normally closed second valve. The first valve and the second valve are both only uncovered and opened so that the first fluid passage and the second fluid passage are fluidly communicatively connected, and closed and covered by the respective selective conjugate engagement and disengagement of the first portion and the second portion.

Abstract: A foam dispensing apparatus of the present invention includes a reservoir containing a foamable liquid, with a closed headspace above a surface of the liquid. The apparatus also includes a source of a gas disposed to impose a gas pressure higher than ambient atmospheric pressure into the closed headspace. There is a mixing chamber having an inside diameter, an inlet and an outlet open to the ambient atmosphere with a flow restricter having a plurality of openings therein in gaseous communication with the closed headspace.

Abstract: A surgical scalpel includes an elongate handle defining a longitudinal axis and having a proximal end and a distal end. The scalpel has a cartridge removably mounted to the handle that has a blade holder with a proximal end and a distal end. There is a blade fixedly attached to blade holder disposed so that the blade projects distally outwardly when the cartridge is mounted on the handle. The cartridge also has a shield with a proximal end, a distal end and a bottom mounted onto the blade holder. The shield is slidably movable between a distal position where the shield substantially prevents inadvertent access to the blade and a proximal position where the shield substantially surrounds a portion of the handle and the blade is exposed for use. The cartridge is releasably mountable to the handle and has elements for substantially preventing movement of the shield with respect to the blade holder unless the cartridge is mounted on the handle.