178242-64-3Relevant articles and documents
CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
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Page/Page column 172; 176, (2021/11/26)
This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Synthesis and structure-activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors
Gilmore, John L.,King, Bryan W.,Harris, Cathy,Maduskuie, Thomas,Mercer, Stephen E.,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Ribadeneria, Maria D.,Vaddi, Krishna,Trzaskos, James M.,Newton, Robert C.,Decicco, Carl P.,Duan, James J.-W.
, p. 2699 - 2704 (2007/10/03)
A novel series of achiral TNF-α converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-α production in an LPS-stimulated whole blood assay with an IC5
Novel 5-hydroxytryptamine 4 (5-HT4) receptor agonists. Synthesis and gastroprokinetic activity of 4-amino-N-[2-(1-aminocycloalkan-1-yl)ethyl]-5- chloro-2-methoxybenzamides
Suzuki, Takeshi,Imanishi, Naoki,Itahana, Hirotsune,Watanuki, Susumu,Miyata, Keiji,Ohta, Mitsuaki,Nakahara, Hideaki,Yamagiwa, Yoko,Mase, Toshiyasu
, p. 1116 - 1124 (2007/10/03)
A novel series of 4-amino-N-[2-(1-aminocycloalkan-1-yl)ethyl]-5-chloro- 2-methoxybenzamide derivatives (1), which had amines conformationally restricted due to the effect of repulsion by neighboring substituents, were prepared and evaluated for 5-hydroxytryptamine 4 (5-HT4) agonistic activities by using the contraction of longitudinal muscle myenteric plexus (LMMP) of guinea pig ileum. One of the most potent compounds in this series was 4-amino-5-chloro-N-[2-(1-dimethylamino-1-cyclohexyl)ethyl]-2- methoxybenzamide (1c, YM-47813) with an EC50 value of 1.0 μM on LMMP. This compound effectively enhanced gastric motility and gastric emptying in conscious dogs by oral administration (1-3 mg/kg).
Synthesis of novel restricted diamines; 2-(1-aminocycloalkan-1- yl)ethylamines
Suzuki, Takeshi,Imanishi, Naoki,Itahana, Hirotsune,Watanuki, Susumu,Ohta, Mitsuaki,Mase, Toshiyasu
, p. 701 - 712 (2007/10/03)
Novel restricted diamines, 2-(1-aminocycloalkan-1-yl)ethylamines 1,were prepared by using Michael addition of ethyl cyclohexylideneacetate 2 and cycloalkylideneacetonitriles 7 with amines. In Michael addition, ester 2 needed high reaction temperature and gave several products, whereas 7 reacted smoothly and gave 2-(1-amino-1-cyclohexyl)acetonitriles 8 in good yield (NH3 85%, MeNH2 89%, EtNH2 80%) and were easily convened to diamines 1.