77778-15-5Relevant academic research and scientific papers
ETHYNYL COMPOUNDS
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Page/Page column 24, (2012/11/08)
The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
ETHYNYL DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE MGLUR5
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Page/Page column 31-32, (2012/11/13)
The present invention relates to ethynyl derivatives of formula I wherein X is N or C-R, wherein R is hydrogen or halogen; G is N or CH; with the proviso that maximum one of G or X can be nitrogen; R1 is phenyl or pyridinyl, which are optionally substituted by halogen; R2 is hydrogen, lower alkyl, hydroxy, lower alkoxy or C(O)O-benzyl; R3,R3', R4, R4, R6, R6' are independently from each other hydrogen or lower alkyl; or R6 and R4 may form together with the carbon atom to which they are attached a C4-6-cycloalkyl ring, if m is 0 and n is 1 or 2; R5 is hydrogen or lower alkyl; n is 0, 1 or 2; m is 0 or 1; with the proviso that n and m are not simultaneously 0; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They may be used for the treatment of schizophrenia or cognitive disorders.
Highly selective mono-substitution in Pd-catalyzed cross-coupling reactions of 3,6-dichloropyridazine with organozinc compounds
Chekmarev, Dmitriy S.,Stepanov, Alexander E.,Kasatkin, Alexander N.
, p. 1303 - 1305 (2007/10/03)
Pd-catalyzed cross-coupling reactions of 3,6-dichloropyridazine (1) with benzyl, aryl, and alkyl organozinc compounds led to selective mono-substitution of one of the chlorine atoms. The subsequent cross-coupling of the resulting monochlorides with RZnCl afforded unsymmetrical 3,6-carbon-disubstituted pyridazines.
Pyrazolopyridine adenosine antagonists
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Page column 30, (2008/06/13)
The present invention relates to a novel pyrazolopyridine compound of the following formula: whereinR1 is aryl, andR2 is cyclo(lower)alkyl which may have one or more suitable substituent(s), etc;and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; etc.
Desymmetrization of dichloroazaheterocycles
Goodman, Allan J.,Stanforth, Stephen P.,Tarbit, Brian
, p. 15067 - 15070 (2007/10/03)
3,6-Dichloropyridizine 1a was converted in good yield into its mono-iodo derivative 1b when treated with a mixture of hydriodic acid and sodium iodide. Pure samples of the mono-iodo derivatives 2b, 3b and 4b could not be obtained from their corresponding dichlorinated precursors with these reagents. Compounds 1b and 4b underwent palladium catalysed Suzuki, Sonogashira and other coupling reactions.
