Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, A, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

Abstract: The present invention relates to the use of compounds of general formula I wherein R?, R1, R2 and R3 are as defined herein, or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, and for methods to treat a variety of neurodegenerative and neuropsychiatric diseases.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ?O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, A, B, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, A, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, A, B, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, A, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ?O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture

Abstract: A method for determining a biological response of a target (41, 42) to a soluble candidate substance comprises the steps: introducing a soluble candidate substance into a laminar flow of a buffer liquid (2) to form a candidate substance solute (3) having an initial concentration profile (31); dispersing the initial concentration profile (31) to form a dispersed concentration profile (32); directing the dispersed concentration profile (32) into a detection channel (12) to form a final symmetrical concentration profile (33) therein; introducing a target into the detection channel (12) to obtain a combined concentration profile comprising a constant target concentration profile overlying the final symmetrical concentration profile (33); holding in the detection channel (12) at least one half of the combined concentration profile; and optically scanning the combined concentration profile to detect an optical signal representative of the biological response of the target to the soluble candidate substance.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.

Abstract: The present invention relates to the use of compounds of general formula wherein R? is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)—NH-lower alkyl, CH2—C(O)—NH-lower alkyl, CH2—NH—C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy,

Abstract: This invention relates to 1-pyridazinyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

Abstract: This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.