摘要:
Compounds of the formula (I), wherein X and R1 to R5 are as defined in the description, are useful for treating disorders mediated full or in part by mGluR5.
摘要:
Compounds of the formula (I), wherein X and R1 to R5 are as defined in the description, are useful for treating disorders mediated full or in part by mGluR5.
摘要:
The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)- thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)-(CH2)n 18F, O-(CH2)nF, O-(CH2)n 18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
摘要:
The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).
摘要:
The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4-4]non-7-yl)-propionam ides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
摘要:
The invention provides compounds of formula (I), wherein R, R1, R2, R3 and R4 are as defined in the description, and their preparation. The compounds of formula I are useful as biomarkers.
摘要:
The present invention provides compounds of formula (I) wherein X and Y represent CH, CH2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH2; m and o represent independently of each other 0 or 1, with the proviso that if m is 0 then the dotted line between Y and the neighboring C atom represents a bond and Y is CH or a trivalent heteroatom, if m is 1 then the dotted line between Y and the neighboring C atom is absent and Y is CH2 or a divalent heteroatom, if o is 0 then the dotted line between X and the neighboring C atom represents a bond and X is CH or a trivalent heteroatom, if o is 1 then the dotted line between X and the neighboring C atom is absent and X is CH2 or a divalent heteroatom; A represents (CH3CR4)p and Q represents (CR9R10)n; n and p represent independently of each other 0 or 1; R6, R7, R13 and R14 denote independently of each other hydrogen, halogen, (C1-4)alkyl, (C1-4)alkylSO2, SO3H, carboxy, (C1-4)alkoxy carbonyl, (C1-4)alkoxy, OH or NR15R16; R1, R2, R3, R4, R9, R10, R11 and R12 denote independently of each other hydrogen, (C1-4)alkyl, carboxy, (C1-4)alkoxy carbonyl or (C1-4)alkoxy, or, when X is CH or CH2 then R1 and R2 can also be OH or NR15R16, or when Y is CH or CH2 then R11, R12 can also be OH or NR15R16; R5, R8, R15 and R16 are independently of each other hydrogen, (C1-4)alkyl, (C1-4)alkoxy, R17O-C(O)-(C1-4)alkyl or (reactive group)-(C1-4)alkyl; and R17 represents hydrogen or (C1-4)alkyl; compositions comprising such compounds, a process for the production of such compounds of formula (I), a method of labeling target structures, especially amyloid plaques, in the brain, a method for identifying Alzheimer's disease, use of a compound of formula I as a near-infrared imaging agent and a conjugate comprising a compound of formula (I) covalently linked to a biomolecule through a reactive group.
摘要:
The invention relates to the use of an inhibitor of formula (I), or a pharmaceutically acceptable salt thereof having an activity on protein kinases PKC alpha, PKC beta, PKC gamma, PKC epsilon, PKC theta, CDK-1, KDR, PKA, Flt-1, Flt-2, Flt-3 or Flt-4, or on a combination of the above enzymes, for the treatment and/or prevention of neurological and vascular disorders related to beta-amyloid generation and/or aggregation such as neurodegenerative diseases like Down's Syndrome, memory and cognitive impairment, dementia, amyloid neuropathies, brain inflammation, nerve and brain trauma, vascular amyloidosis, or cerebral hemorrhage with amyloidosis.