Abstract: The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt and to pharmaceutically acceptable salts and hydrates thereof, wherein X, Y, R1, R2 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.

Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.

Abstract: A pharmaceutical composition comprising a LH antagonist or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier is useful for deferring the onset of menopause.

Abstract: The present invention relates to a new method of shuffling especially heterologous polynucleotide sequences, screening and/or selection of new recombinant proteins resulting therefrom having a desired biological activity, and especially to production and identification of novel proteases exhibiting desired properties.

Abstract: The present invention relates to GLP-1 derivatives having a lipophilic substituent, pharmaceutical compositions comprising same, and methods of making an using same. The GLP-1 derivatives of the present invention have a protracted profile of action.

Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

Abstract: A syringe having a dose setting mechanism, a button which can be operated to inject a set dose, a switch operated at a time between the start and completion of injection, and an electronic presentation of parameters such as the size of a set dose and the size of the last dose administered. The syringe also has a stop watch which is reset and started responsive to operation of the switch. The electronic presentation includes an indication of the number of hours elapsed from the activation of the switch, and may also include, for a predetermined period initially following the activation of the switch, a presentation of the number of seconds elapsed. The latter presentation can provide a visual indication to the patient of the length of time, after the injection button has been actuated to inject the dose, that the needle should remain inserted in the skin.

Abstract: The present invention relates to animal feed additives, which additives comprise a monocomponent xylanase derived from a strain of Byssochlamus, Chaetomium, Humicola, Malbranchea, Mucor, Myceliophthora, Paecilomyces, Talaromyces, Thermoascus, or Thielavia. In other aspects, the invention relates to monocomponent xylanase preparations, DNA constructs, recombinant expression vectors, host cells, and methods of producing monocomponent xylanase preparations.

Abstract: 1,2,4-Benzothiadiazine derivatives represented by formula wherein D, R1, R2, R3, R4, R5, R12, R13, R14, R15 are defined in the description, composition thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.

Abstract: A new salt of (2R,3R,4R)-3,4-dihydroxy-2-hyroxymethylpyrrolidine is disclosed. Specifically, (2R,3R,4R-3,4-dihydroxy-2-hydroxymethylpyrrolidine, 2-naphthalenesulfonate is disclosed, as well as its preparation and use for treating and preventing diabetes and obesity and for regulating appetite. This salt is characterized as having a high melting point and low hygroscopicity.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The invention relates to compounds inhibiting the activation of FX to FXa by TF/FVIIa. The compounds are anticoagulants. The invention also relates to a method of identifying a drug candidate.

Abstract: The present invention provides an injection syringe comprises a housing including a holder for containing a cartridge of medicine, a piston rod with a non-circular cross-section having an outer thread, a piston rod drive, a one way coupling having an annular ring of internal ratchet notches, which annular ring can be integral with the housing, and a pawl having at least a pair of resilient arms each having a free end.

Abstract: The present invention relates to fused 1,4-thiazine-2-carbonitrile derivatives, compositions thereof and methods for preparing the compounds. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.

Abstract: An injection member for a jet spray injection device through which device a dose of medicine is administered for subcutaneous or intramuscular injection has a jet nozzle designed as a skin-penetrating member having a length of 0.05-0.3 mm enabling it just to penetrate the stratum corneum.

Abstract: 1,2,4-Thiadiazine and 1,4-thiazine derivates represented by formula (I): wherein A, B, D, R1, R2, R3 and R4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.

Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.

Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt th

Abstract: An enzyme from Aspergillus aculeatus exhibiting endoglucanase activity encoded by the DNA sequence of SEQ ID NO:17 or 18, and useful for degrading plant cell walls.