- Imidazole derivatives as PDE10A enzyme inhibitors
-
This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr
- -
-
Page/Page column 9
(2012/06/01)
-
- SF5 DERIVATIVES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS
-
The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.
- -
-
-
- The Curtin-Hammett principle in action: 1-amino-3H-isoindole in cycloaddition reactions
-
Based on the spectral studies of 1-aminoisoindole we have observed that in solution the isoindolenine tautomer predominates. In spite of this fact but, taking into account the Curtin-Hammett principle, we undertaken the first study of the Diels-Alder reaction for 1-aminoisoindole as a typical representative of simple isoindoles in isoindoline form. We have studied the interaction of 1-aminoisoindole with maleimide derivates and demonstrated that the products are rearranged 1:2 composition adducts. We have proposed a rearrangement mechanism, detected and identified the intermediate Diels-Alder products containing both endo- and exo adducts.
- Levkov, Igor V.,Turov, Oleksandr V.,Shishkin, Oleg V.,Shishkina, Svetlana V.,Voitenko, Zoia V.
-
experimental part
p. 508 - 512
(2010/03/03)
-
- Reaction of azides with dichloroindium hydride: Very mild production of amines and pyrrolidin-2-imines through possible indium-aminyl radicals
-
Organic azides are easily reduced to the corresponding amines by reaction with dichloroindium hydride under very mild conditions and in a highly chemoselective fashion. γ-Azidonitriles give rise to outstanding five-membered cyclizations affording pyrrolidin-2-imines. A rationalization of the overall experimental data cannot exclude the occurrence of competitive radical and nonradical pathways, but certain results are, however, soundly consistent with the intermediacy of indium-bound nitrogen-centered radicals.
- Benati, Luisa,Bencivenni, Giorgio,Leardini, Rino,Nanni, Daniele,Minozzi, Matteo,Spagnolo, Piero,Scialpi, Rosanna,Zanardi, Giuseppe
-
p. 2499 - 2502
(2007/10/03)
-
- Cyclizations of N-Stannylaminyl Radicals onto Nitriles
-
(Matrix presented) Stannylaminyl radicals derived from radical reactions of Bu3SnH with azidoalkylmalononitriles exhibit highly efficient 5- and 6-exo cyclization onto either nitrile group to give aminoiminyl radicals that in turn are reduced t
- Benati, Luisa,Bencivenni, Giorgio,Leardini, Rino,Minozzi, Matteo,Nanni, Daniele,Scialpi, Rosanna,Spagnolo, Piero,Zanardi, Giuseppe,Rizzoli, Corrado
-
p. 417 - 420
(2007/10/03)
-
- SYNTHESIS AND CHARACTERIZATION OF 1H-2,4-BENZODIAZEPINES
-
Photolysis of the 4-azidoizoquinolines (1) in the presence of sodium methoxide afforded the 1H-2,4-benzodiazepines (3); this new ring system was characterized by some photochemical and thermal reactions.
- Sawanishi, Hiroyuki,Tsuchiya, Takashi
-
p. 2725 - 2728
(2007/10/02)
-
