Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.

Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

Abstract: A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.

Abstract: The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.

Abstract: Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound and pharmaceutically acceptable salts thereof, and methods of using said compounds. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract: Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, pharmaceutical compositions containing them, as well as the use of the above-mentioned compounds in the treatment, control or prevention of illnesses such as cancer.

Abstract: The invention relates to carboxamide derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as mGluR1 enhancers in the treatment and prevention of neurological disorders and diseases, such as Alzheimer's disease and dementia.

Abstract: The (R) and (S) enantiomers of a compound of formula I are novel antiproliferative therapeutic agents. These compounds have HDAC inhibitor activity and are useful in the treatment of cancer. Also disclosed are methods of making and using compounds of formula (I), as well as pharmaceutical compositions containing compounds of formula (I).

Abstract: The present invention provides a method for testing an agent for its potential to inhibit heparanase catalytic activity, comprising the steps of: interacting immobilized heparanase substrate binding protein on a solid support with labeled heparanase substrate to provide immobilized labeled heparanase substrate, interacting a heparanase enzyme solution with the immobilized labeled heparanase substrate in the presence of the agent, and detecting the presence or absence of label in the solution remote from the solid support. The labeled heparanase substrate may be bound to an immobilization bridge which binds to immobilized molecules on a solid support, to provide bridge-immobilized labeled heparanase substrate.

Abstract: The present application relates to compounds of the formula wherein R1 is hydrogen, halogen or lower alkoxy; R2 is hydrogen or is —C(O)-lower alkyl or —C(O)-phenyl, wherein the phenyl ring is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl, or is —C(O)-furanyl or —C(O)-thiophenyl, wherein the rings are unsubstituted or substituted by halogen; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases associated with the adenosine A2 receptor.

Abstract: The compounds of formula (I) wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.

Abstract: The present invention relates to the compound of formulae ##STR1## and to a process for the manufacture of compounds of the general formula ##STR2## which are ligands for the metabotropic glutamate receptors of group II, whereinT is tritium;R.sup.1 is hydroxy, lower alkoxy, lower alkenyloxy, benzyloxy, hydrogen, deuterium or tritium;R.sup.11 is hydrogen, deuterium or tritium, hydroxy or amino, andR.sup.2 is hydrogen or tritium, orR.sup.1 and R.sup.2 form a bond.

Abstract: The present invention is concerned with a novel process for the carbamoylation of substituted pyridines, especially with a process for the preparation of compounds of formula I ##STR1## wherein R.sup.4 to R.sup.8 represent hydrogen, lower-alkoxy or halogen; or optionally salts thereof.

Abstract: The present invention provides orally administrable pharmaceutical compositions containing an inhibitor of gastrointestinal lipase, and at least one compound selected from the group consisting of chitosan, its derivatives and salts thereof. Methods are provided for preventing and treating anal leakage of oil in a patient to whom a composition containing an inhibitor of gastrointestinal lipase is orally administered.

Abstract: Polyethylene and polypropylene protein conjugates which modulate body weight of ani is and humans for the treatment, prevention and control obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.

Abstract: The present invention provides a combination of IL-12 and IFN.alpha. together with a pharmaceutically acceptable carrier useful for treatment and prophylaxis of infectious diseases, preferably chronic infectious diseases and more preferably viral infections, e.g. HSV, HIV, Hepatitis B, Hepatitis C, papilloma etc., bacterial infections, e.g. tuberculosis, salmonellosis, listeriosis, etc., and parasite infections, e.g. malaria, leishmaniasis, and schistosomiasis. These compositions are characterized by the synergistic interaction of IL-12 and IFN.alpha.. The present invention also provides the use of the above combination for the treatment and prophylaxis of infectious diseases.

Abstract: A compound of the formula ##STR1## useful for treating vitamin D dependent disorders.