Abstract: The present invention provides an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.

Abstract: The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.

Abstract: Compounds of the present invention are 4-phenyl-pyridine derivatives with activity as NK-1 receptor antagonists.

Abstract: The invention relates to use of diphosphonic acids or physiologically compatible salts or esters thereof for preventive treatment of disturbances to ossary mineralization which may occur after operative extension of the urine bladder by augmentation plasties or replacement of the urine bladder by replacement plasties but often do not appear until years after the operation.

Abstract: The present invention provides a method of preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.

Abstract: The present invention provides a method for preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.

Abstract: The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula  wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas

Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;

Abstract: The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q, X, A, Y B are as defined in the specification.

Abstract: Phenyl substituted quinolin 4-yl derivatives and pharmaceutical compositions with activity as NMDA-receptor subtype selective blockers. The compounds of the invention modulate neuronal activity and plasticity.

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.

Abstract: The present invention provides a pharmaceutical combination preparation comprising an erythropoietin preparation that provides active erythropoietin and at least one modified haemoglobin wherein the erythropoietin preparation and modified haemoglobin can be present in separate forms of administration or in a single form of administration. The pharmaceutical combination preparations of the present invention can be used to treat manifest anemias with or without iron utilization disorders.

Abstract: The invention relates to a compound of the formula its R,R-, S,S-enantiomers and racemic mixtures thereof and to their pharmaceutically acceptable acid addition salts. The compound of formula I and its R,R- and S,S-enantiomers may be used as medicaments for the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

Abstract: The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.

Abstract: The present invention provides a process for the preparation of D-asparagine derivatives of formula I wherein R1 is an amino protecting group and R2 is an alkyl, a substituted alkyl or a group of formula A R3(OCH2CH2)n—  A wherein R3 is hydrogen or an lower alkyl group and n is 1, 2 or 3, which process comprises reacting a compound of formula II wherein R1 and R2 are as defined above, with a protease in an aqueous solution at a pH of 6.0-7.5 and an organic solvent, and subsequently extracting the enantiomeric pure product of formula I. Compounds of formula I can be used as intermediates in the production of antibacterial substances.

Abstract: The invention is a compound of the formula wherein R is a) —C(O)(CH2)nC(O)OH, b)  wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl, c) —P(O)(OH)2, or is d) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); and R2/R3 are hydrogen or lower alkyl; n is 1, 2, 3 or 4; or a pharmaceutically acceptable acid addition salt thereof

Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.

Abstract: This invention relates to new retinoic acid receptor selective retinoid agonists, to pharmaceutical compositions containing such compounds, and to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, for the treatment of emphysema and related pulmonary diseases.

Abstract: The present invention is a series of 2H-tetrazole-5-yl-amide derivatives showing activity as ligands of metabotropic glutamate receptors.

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.