Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.

Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

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: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.

Abstract: Pharmaceutical compositions that contain a lipase inhibitor having a melting point ?37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity.

Abstract: The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom, with the proviso that at least one of X or Y is a halogen atom. The compounds of formula I are useful as starting materials or intermediates for the preparation of pharmaceutically active compounds, especially for compounds, which are useful for the treatment of central nervous system disorders.

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.

Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.

Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.

Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.

Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract: The present invention relates to mono-sulfate and hemi-sulfate salts of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine, to crystalline and amorphous forms thereof and to their use in pharmaceutical formulations.

Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, m, A, R1 and R2 have the significance given in the description. The compounds are useful as HSL inhibitors and may be used in the treatment or prophylaxis of diabetes, dyslipidemia, atherosclerosis or obesity.

Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.

Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.