Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR11, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.

Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.

Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.

Abstract: This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor.

Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.

Abstract: Novel phosphotetrahydropyran compounds that mimic mannose-6-phosphate but that are more resistant to phosphatases and mannosidases, and pharmaceutical compositions thereof, are disclosed. These compounds and compositions inhibit T lymphocyte migration from blood to tissues or to other extravascular sites. By inhibiting such migration, these compounds are useful for treating diseases or disorders that are mediated at least in part by such T lymphocyte migration. Such diseases and disorders include rheumatoid arthritis, multiple sclerosis, acute disseminated encephalomyelitis, psoriasis, inflammatory bowel disease, T cell-mediated dermatitis, stromal keratitis, uveitis, thyroiditis, sialitis and type I diabetes.

Abstract: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins

Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.

Abstract: An attachment for cooperation with an associated electric switch mounting box and an associated faceplate which includes an elongated bolt; a plurality of beads, each having an internal bore dimensioned for allowing passage of an axial portion of the elongated bolt, and first and second finish washers, the beads being disposed on the elongated bolt when each of the beads being disposed in adjacent relationship to at least one other of the beads, the plurality of beads comprising an elongated stack, the first and second finish washers being disposed respectively at the axial extremities of the stack. In some forms of the invention the finish washers have cupped peripheral edges which may be disposed in facing relationship whereby the axial extremities of the stack have smooth surfaces. The beads may have respective colors associated with a country. The colors may be red, white and blue.

Abstract: An apparatus, system, and method are disclosed for generating a reproducible virtual environment in a computer software program. This invention describes a method of generating a realistic virtual environment dependent on a sequence of pseudo-random numbers generated by a pseudo-random number generator initialized by a seed value that may be created by the user. If a user starts with the same initial seed, the same virtual environment is created each time the program is run. However, if a new seed is used, a new virtual environment will be created.

Abstract: This invention relates to compounds of formula (1) wherein B is optionally substituted aryl; R1 and R2 are the same or different and are independently selected from hydrogen or C1-3 alkyl; n is 1 or 2, preferably n is 1; m is 0 or 1; R3 is hydrogen or acyl; R4 and R5 are the same or different and are independently selected from amino, alkylamino, dialkylamino, arylamino and C2-C8 cycloalkylamino; X and Y are independently selected from C, H or N provided at least one of X and Y is N; and salts thereof, solvates thereof, pharmaceutically acceptable derivatives thereof, prodrugs thereof, tautomers thereof and/or isomers thereof; and processes for their preparation and methods of treatment, pharmaceutical formulations and uses involving them.

Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.

Abstract: This invention relates to a purification method, particularly for purifying tyrosine kinase receptor related polypeptides, and to products made by the method. The method comprises a method of producing tyrosine kinase receptor-related polypeptides, the method comprising expressing a tyrosine kinase receptor-related polypeptide in a recombinant expression system and separating expressed monomeric tyrosine kinase receptor-related polypeptide from multimeric form(s) of the expressed polypeptide in a separation step, the separation step allowing refolding of the expressed tyrosine kinase receptor-related polypeptide into a biologically active form.

Abstract: An optical mount has a frame and a barrel moveably positioned within the frame, the barrel including an optical connector housing optical wave-guide. The optical connector is mounted within the barrel at a mount angle, the optical connector having an end face polished at a polish angle relative to the axis of the optical connector. The frame has two angled contact surfaces symmetric relative to each other across a plane of symmetry, a leaf spring having an end adapted to maintain contact with the barrel along a plane of symmetry. The barrel is axially and rotationally moveable within the frame allowing for precise positioning of the optical wave-guide relative to the frame thereby minimizing polarization dependent loss (PDL). A focus tool having an offset eccentric pin can be used with a circumferential groove of the barrel to allow for precise axial movements of the barrel within the frame.

Abstract: A method is provided for removing carbon dioxide, ethane and heavier components from high pressure natural gas (10) comprises: partly condensing and expanding the high pressure natural gas (10) to obtain a gaseous stream (30) enriched in methane and carbon dioxide and two liquid streams (37 and 40) enriched in ethane and heavier components which are introduced into fractionation column (35); removing from fractionation column (35) fluid stream (45), heating (46) the fluid stream to obtain a reboiling stream (47) which is introduced into the fractionation column (35); removing from fractionation column (35) liquid stream (50) enriched in carbon dioxide, ethane and heavier components; removing from the top of fractionation column (35) a gaseous overhead stream (55) enriched in methane; cooling (56) the gaseous overhead stream (55) to obtain a two-phase fluid, separating (58) the two-phase fluid into cooled gaseous overhead stream (60) and first reflux stream (62) which is introduced into the fractionation colum

Abstract: An automated HPLC system separates, identifies, purifies, and quantitates complex mixtures of reaction products or natural products on a semi-preparative or preparative scale, thus enabling rapid compilation of combinatorial libraries with minimal operator involvement.