70622-91-2Relevant articles and documents
Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure
Manickam, Manoj,Jalani, Hitesh B.,Pillaiyar, Thanigaimalai,Sharma, Niti,Boggu, Pulla Reddy,Venkateswararao, Eeda,Lee, You-Jung,Jeon, Eun-Seok,Jung, Sang-Hun
, p. 379 - 391 (2017/04/24)
A series of flexible urea derivatives have been synthesized and demonstrated as selective cardiac myosin ATPase activator. Among them 1-phenethyl-3-(3-phenylpropyl)urea (1, cardiac myosin ATPase activation at 10?μM?=?51.1%; FS?=?18.90; EF?=?12.15) and 1-benzyl-3-(3-phenylpropyl)urea (9, cardiac myosin ATPase activation?=?53.3%; FS?=?30.04; EF?=?18.27) showed significant activity in?vitro and in?vivo. The change of phenyl ring with tetrahydropyran-4-yl moiety viz., 1-(3-phenylpropyl)-3-((tetrahydro-2H-pyran-4-yl)methyl)urea (14, cardiac myosin ATPase activation?=?81.4%; FS?=?20.50; EF?=?13.10), and morpholine moiety viz., 1-(2-morpholinoethyl)-3-(3-phenylpropyl)urea (21, cardiac myosin ATPase activation?=?44.0%; FS?=?24.79; EF?=?15.65), proved to be efficient to activate the cardiac myosin. The potent compounds 1, 9, 14 and 21 were found to be selective for cardiac myosin over skeletal and smooth myosins. Thus, these urea derivatives are potent scaffold to develop as a newer cardiac myosin activator for the treatment of systolic heart failure.
Preparation method for alkyl/benzyl/aryl urea compounds through heterogeneous-phase catalysis
-
Paragraph 0063-0071; 0072; 0073; 0074; 0075; 0078; 0079, (2016/10/09)
The invention discloses a preparation method for formula (I) compounds, and the compounds are obtained by reacting a formula (II) compound with a formula (III) compound in a solvent in carbon monoxide atmosphere under catalysis of a heterogeneous-phase pa
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
-
Paragraph 0413-0416; 0683-0686, (2016/10/07)
Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016