Abstract: An N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of the formula (I): wherein X, Y, W and R are as defined herein.

Abstract: The invention relates to novel fluorescence-based assays for protein kinases and phosphatases which can be used in high throughput screening. The methods of the invention utilize a competitive immunoassay to determine the amount of substrate that is phosphorylated or dephosphorylated during the course of a kinase or phosphatase reaction to yield a product, as well as the phosphorylating or dephosphorylating activity of a kinase or phosphatase.

Abstract: The invention provides methods to identify specific inhibitors of HPV E7 binding to CDK2 and methods to identify specific inhibitors of E7-induced CDK2 kinase activity. Specific inhibitors identified by the methods, compositions comprising the specific inhibitors, and methods of treatment using the compounds are also provided.

Abstract: The sustained release tablet of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) which is disclosed permits twice daily administration of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) to treat humans with Parkinson's disease.

Abstract: A soluble antibody conjugate comprising an antibody linked to a structure which is recognized by T-cells and has the ability to direct T-cells to lyse the target cell, which is recognized by the antibody. The conjugate is characterized by the structure being a superantigen. One important mode is a method for the lysis of target cells, wherein the target cells are contacted with a target cell lysis effective amount of the conjugate. The method of lysis is part of a potent treatment regime for cancer, autoimmunity, parasitic infestations and fungal, viral and bacterial infections. The specification also describes modes such as the synthesis of the conjugate and pharmaceutical compositions and their manufacture.

Abstract: The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.

Abstract: The present invention provides the use of pramipexole in the treatment of restless legs syndrome.

Abstract: A compound of formula (I), wherein W is —NHOH or —OH, R1 is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R2 is free or protected hydroxy, R3 and R4 is an organic group, R5 is hydrogen or methyl, or R4 and R5, together with the nitrogen atom to which they are attached, constitute an azaheterocyclyl group, and the solvates, hydrates and pharmaceutically acceptable salts thereof, can inhibit matrix metalloproteinases and the release of tumour necrosis factor (TNF). Processes for producing the compound, intermediates involved in the processes, and pharmaceutical compositions containing the compound are also described.

Abstract: The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is —H or —CH3; wherein R2 is —H or —CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).

Abstract: The present invention provides a method of topically administering antimicrobial agents such as premafloxacin, premafloxacin-like compound, premafloxacin ester, ciprofloxacin, enrofloxacin, cefquinome, cefpodoxime, gentamicin or erythromycin for the treatment of systemic bacterial diseases in mammals.

Abstract: The invention provides a method of identifying a therapeutic useful for treating or preventing asthma, which method includes the steps of contacting a identify compounds that inhibit the binding of human JAK2 protein to the &bgr;c first molecule comprising at least the N terminal 294 residues of JAK2 protein as shown in SEQ ID NO: 5 with a second molecule comprising at least 13 membrane proximal cytoplasmic amino acid residues of the &bgr;c subunit of the IL-3, IL-5, and GM-CSF receptors as shown in SEQ ID NO: 3 in the presence of a candidate compound to subunit of the IL-3, IL-5 and GM-CSF receptors. Compounds that block the signalling pathways of the IL-3, IL-5 and GM-CSF receptors may be of use in the treatment of asthma.

Abstract: An anthracycline glycoside of formula I wherein R is one of the two following residues: or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.

Abstract: This invention comprises new formulations and methods of preparing a new formulations of prostaglandins and in particular dinoprost tromethamine, where the pH of the formulation is adjusted to between about 5.5-7.5 and where the the concentration of benzyl alcohol is between about 1.2 to 2.0 mg/ml.

Abstract: Compounds selected from the group consisting of formulae III, IV, VI and VIII wherein R is H is NH2, or a pharmacologically acceptable salt thereof, are suitable for use in methods for treating non-insulin-dependent diabetes mellitus (NIDDM) or obesity in a patient susceptible to or experiencing NIDDM or obesity by the systemic administration of such a compound in an amount effective to treat the NIDDM or obesity.

Abstract: Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegrant in an amount from about 6 to about 40% where the rapidly precipitating drug, “binder” and superdisintegrant are mixed and compressed into a tablet without heating, solvent or grinding.

Abstract: The present invention provides for the treatment of non-insulin dependent diabetes mellitus or obesity comprising the systemic administration of a compound having the formula or a pharmacologically acceptable salt thereof, wherein each R is H or NH2, and with the proviso that at least one R group must be NH2.

Abstract: A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.

Abstract: The invention is an oxazolidine ester of silylated baccatin III of formula (VII) which is a useful intermediate to produce pharmaceutically useful anti-cancer compounds.

Abstract: A delivery device including a) a housing, b) a container for a fluid arranged in the housing, the container having an opening, c) a delivery conduit connected in fluid communication with the opening, the conduit having a front end in flow respect distal from the container and a rear end in flow respect proximal to the container, the front end and the rear end defining an axis therebetween and a forward direction and a rearward direction, and d) a pump arranged to deliver fluid at least in a direction from the container through the conduit, the device comprising, a sensor able to change state in at least one respect in response to a predetermined proximity of an object to the sensor in a sensing direction, a converter, separate from or integral with the sensor, converting at least one of the sensor states into an electromagnetic signal, and a processor, receiving the electromagnetic signal and delivering a control signal to an operational component of the device.