Abstract: A compound of the formula A compound of formula I has a good affinity to the A2A receptor and is useful for the treatment of diseases mediated by this receptor.

Abstract: The present invention is a compound of formula: wherein R1, R2, R2′, X, A1/A2 and B are as defined in the specification. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

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: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.

Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

Abstract: The invention relates to compounds which are represented by the formula wherein R1, R2, R3, R4, X and Y are as defined in the specification, as well as pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.

Abstract: Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms, as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.

Abstract: Conjugates of erythropoietin with poly(ethylene glycol) comprise an erythropoietin glycoprotein having at least one free amino group and having the in vivo biological activity of causing bone marrow cells to increase production of reticulocytes and red blood cells and selected from the group consisting of human erythropoietin and analogs thereof which have sequence of human erythropoietin modified by the addition of from 1 to 6 glycosylation sites or a rearrangement of at least one glycosylation site; the glycoprotein being covalently linked to “n” poly(ethylene glycol) groups of the formula —CO—(CH2)x(OCH2CH2)m—OR with the carbonyl of each poly(ethylene glycol) group forming an amide bond with one of said amino groups; wherein R is lower alkyl; x is 2 or 3; m is about 450 to about 900; n is from 1 to 3; and n and m are chosen so that the molecular weight of the conjugate minus the erythropoietin glycoprotein is from 20 kilodaltons to 100 kilodaltons.

Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

Abstract: There are described compounds of the formula in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an &agr;- or &bgr;-amino acid or a residue of the general formula Q—X—Y—  (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulfur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear “spacer” with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulfur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulfur, and Y represents one of the groups —CO—, —CS—, —CONH— and (where X contains neither sulfur nor carbonyl as a terminal component) —SO2—; and in which R1 and R2 together signify a group of the formula wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R3 represents

Abstract: The present invention is concerned with mixed anhydrides. The mixed anhydrides are prepared by adding an adjuvant base to a mixture of acid and reactive acid derivative. The mixed anhydrides play an role primarily in activating and coupling reactions.

Abstract: Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.

Abstract: Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.

Abstract: Disclosed is a method of treating a patient suffering from cancer. The method comprises administering to a patient over a period of up to about 15 days a first component and a second component. The first component consists of a pharmaceutical composition containing as an active ingredient a compound of formula I or a pharmaceutically acceptable salt or ester of said compound. The second component consists of an injection solution containing as an active ingredient paclitaxel. The amount of each component in the combination is such that the combination is therapeutically effective. The components are administered concomitantly or sequentially in a three week to four week treatment cycle for as long as the tumor remains under control and the patient tolerates the regimen.

Abstract: The present invention is concerned with the use of carbonylamino derivatives of the formula wherein R signifies lower alkyl, lower alkenyl, lower alkinyl, cycloalkyl, lower alkoxy or CF3; R1 signifies hydrogen or lower alkyl; R2 and R3 signify, independently from each other, hydrogen, halogen or nitro; Y signifies CH or N; n is 0-6; m is 0-2; as well as with their pharmaceutically acceptable salts for the treatment of diseases, which relate to metabotropic glutamate receptor antagonists and/or agonists.

Abstract: This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula wherein R1, R2, R3 and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation and a method of treatment or prevention of acute and/or chronic neurological disorders by administering an effective amount of the compound of formula I or a pharmaceuticall acceptable salt thereof.

Abstract: This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula wherein R1, R2, R3, X and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation, their use in preparation of pharmaceutical compositions and administration of an effective amount of the compounds for the treatment or prevention of acute and/or chronic neurological disorders to a patient in need of such treatment.

Abstract: The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.

Abstract: The present invention relates to the discovery of novel genes and proteins, which function in pathways involved in brain pathogenesis. In particular, the novel genes and proteins relate to inflammatory tissue responses caused by brain injuries such trauma, ischemia or autoimmune-inflammation or other diseases or processes related to neuroinflammation. The compounds disclosed in the present invention are useful as therapeutics, diagnostics and in screening assays.