Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.

Abstract: The invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I? and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.

Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.

Abstract: The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds.

Abstract: The present invention relates to compositions for oral administration. The invention preferably comprises at least one abuse-resistant drug delivery composition for delivering a drug having potential for dose dumping in alcohol, related methods of preparing these dosage forms, and methods of treating a patient in need thereof comprising administering the inventive compositions to the patient. Most preferably, the dosage form includes verapamil. These formulations have reduced potential for abuse. In another formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding.

Abstract: The present invention relates to an A?(X-38 . . . 43) oligomer having a high molecular weight, or a derivative thereof, a process for preparing the oligomer or derivative, compositions comprising the oligomer or derivative, and uses of the oligomer or derivative such as its use for treating or preventing an amyloidosis (e.g. by active immunization), for diagnosing an amyloidosis, and for providing agents that are capable of binding to the A?(X-38 . . . 43) oligomer or derivative. The subject invention also describes agents that are capable of binding to the A?(X-38 . . . 43) oligomer or derivative, e.g. antibodies, compositions comprising the agents, and uses of the agents such as their use for treating or preventing an amyloidosis (e.g. by passive immunization) and for diagnosing an amyloidosis.

Abstract: The invention provides a dispersion having an oily phase, an aqueous phase, in the form of an oil-in-water emulsion or a water-in-oil emulsion, and at least one active ingredient that is only slightly or with difficulty soluble in the oily phase and the aqueous phase. The dispersion is free from toxicologically dangerous organic solvents. The dispersion contains the active ingredient dissolved in a quantity that is greater than the quantity which results additively from its maximum solubility in the oily and the aqueous phase of the emulsion prior to forming the emulsion.

Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.

Abstract: The invention relates to a device for forming moulded bodies from a mouldable mass comprising a matrix grid (19) in which at least one receiving chamber (21) is accommodated, and at least one tool (17, 18) with which the mouldable mass can be pressed into the receiving chamber (21). Said claimed device is characterised in that the tool (17, 18) can be displaced along a guide path (3A, 3B) that comprises a moulding section (A), in which a constant pressure is exerted upon portions of the mouldable mass on the strip by the tools (17, 18), said mass being disposed in the receiving chamber (21). The invention further relates to a method for forming moulded bodies, in which a mouldable mass is formed and is guided to at least one receiving chamber of a matrix grid (1).

Abstract: A pharmaceutical dosage form comprises a solid dispersion product of at least one tyrosine kinase inhibitor, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer.

Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor.

Abstract: The present invention relates to a solid dosage form with at least one film (1), which contains an active substance at least in sections. The dosage form is characterized in that the concentration of active substance in film (1) or in the films has a gradient in a direction normal to the thickness of film (1). The invention further relates to a method of production of a solid dosage form with an active substance, in which at least one film (1) is produced, which contains an active substance at least in sections, with the concentration of active substance in film (1) or in the films having a gradient in the longitudinal direction of the film. This film is then formed to produce the dosage form.

Abstract: The invention relates to a device for forming mouldable bodies (57) from a mouldable mass by means of a matrix grid (19), in which at least one cavity (21) is formed by lateral limiting elements (20), and at least one tool (17, 18) which compresses the mouldable mass into the cavity (21). The inventive device is characterised by a compression partition (38) that can be displaced on the matrix grid (19) for portioning the mouldable mass. Said compression partition (38) comprises lateral limiting elements (39) that correspond to the lateral limiting elements (20) of the matrix grid (19). The invention also relates to a method for forming mouldable bodies (57) consisting of forming a mouldable mass and guiding it to a matrix grid (19) such that it rests on the front face (45) of the lateral limiting elements (20) of the matrix grid (19).

Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.

Abstract: Provided are cosmetic preparations for topical application containing nanocrystals of cosmetic actives leading to an increased bioactivity of the molecules in the skin and methods of making the cosmetic preparations. The nanocrystals can be added to any cosmetic topical formulation, e. g. creams, lotions and liposomal dispersions. The drug nanocrystals are produced by a combination process of low energy pearl milling followed by a high energy high-pressure homogenization leading to nanocrystal suspensions (nanosuspensions) of improved physical stability.

Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L ??(I), and acid salts thereof, wherein A, B, D, E, F, G and K are ?-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a ?-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.