953048-71-0Relevant articles and documents
SUBSTITUTED URACILS AS CHYMASE INHIBITORS
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, (2016/09/26)
Substituted uracil derivatives of formula (I), processes for their preparation, their use alone or in combinations for the treatment and/or prophylaxis of diseases, and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF
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, (2015/06/03)
The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
Sequential one-pot access to molecular diversity through aniline aqueous borylation
Erb, William,Albini, Mathieu,Rouden, Jacques,Blanchet, Jrme
, p. 10568 - 10580 (2015/01/08)
On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.
Nonsteroidal Cardiotonics. 2. The Inotropic Activity of Linear, Tricyclic 5-6-5 Fused Heterocycles
Saal, Wolfgang von der,Hoelck, Jens-Peter,Kampe, Wolfgang,Mertens, Alfred,Mueller-Beckmann, Bernd
, p. 1481 - 1491 (2007/10/02)
We previously reported the structure-activity relationships (SAR) of adibendan (1), a potent and long-acting cardiotonic.This paper describes the synthesis of a novel series of linear, tricyclic fused heterocycles of the 5-6-5 type.The compounds were evaluated for positive inotropic activity in anesthetized rats, cats, and dogs.Changes in left ventricular dP/dt were measured as an index of cardiac contractility.The increase in contractility was not mediated via stimulation of β-adrenergic receptors.The data revealed the intrinsic positive inotropic activity of the parent compound of this series, 5,7-dihydro-7,7-dimethylpyrrolobenzimidazol-6(1H)-one (2).The structural features that impart optimal inotropic activity are presented and compared with those of the 4,5-dihydro-3(2H)-pyridazinone series.The most potent compounds were evaluated orally in conscious dogs with implanted Konigsberg pressure transducers to measure ventricular pressures, and their effect on left ventricular dP/dt was compared with that of 1, pimobendan, and indolidan.After administration of 1 mg/kg, 1, 3, 7, 19, 22, 24, 31, 54, pimobendan, and indolidan were equipotent, but only with 1, 31, pimobendan, and indolidan, durations of action exceeded 6 h.