| pubmed-article:19046881 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19046881 | lifeskim:mentions | umls-concept:C2267054 | lld:lifeskim |
| pubmed-article:19046881 | lifeskim:mentions | umls-concept:C0332256 | lld:lifeskim |
| pubmed-article:19046881 | lifeskim:mentions | umls-concept:C0205250 | lld:lifeskim |
| pubmed-article:19046881 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:19046881 | pubmed:dateCreated | 2008-12-26 | lld:pubmed |
| pubmed-article:19046881 | pubmed:abstractText | We previously disclosed a series of highly potent FXa inhibitors bearing alpha-substituted (CH(2)NR(1)R(2)) phenylcyclopropyl P4 moieties in the pyrazolodihydropyridone core system. Herein, we describe our continuous SAR efforts in this series. Effects of the C-3 substitution of the pyrazolodihydropyridone core and the alpha-substitution (R group) of the cyclopropyl ring on FXa binding affinity (FXa K(i)), human plasma anticoagulant activity (PT EC(2x)) and permeability are discussed. A set of compounds obtained from optimization of the R group and the C-3 substituent were orally bioavailable in dogs. Furthermore, representative compounds were highly efficacious in the rabbit arterio-venous shunt thrombosis model (EC(50)s=29-81nM). | lld:pubmed |
| pubmed-article:19046881 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19046881 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19046881 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19046881 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19046881 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19046881 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19046881 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19046881 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:19046881 | pubmed:issn | 1464-3405 | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:NAOYY | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:WexlerRuth... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:LamPatrick... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:WongPancras... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:KnabbRobert... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:LuettgenJosep... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:QiaoJennifer... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:RendinaAlan... | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:XinBaominB | lld:pubmed |
| pubmed-article:19046881 | pubmed:author | pubmed-author:KingSarah RSR | lld:pubmed |
| pubmed-article:19046881 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19046881 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:19046881 | pubmed:volume | 19 | lld:pubmed |
| pubmed-article:19046881 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19046881 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19046881 | pubmed:pagination | 462-8 | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:meshHeading | pubmed-meshheading:19046881... | lld:pubmed |
| pubmed-article:19046881 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19046881 | pubmed:articleTitle | Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties. | lld:pubmed |
| pubmed-article:19046881 | pubmed:affiliation | Research and Discovery, Bristol-Myers Squibb Company, P.O. Box 5400, Princeton, NJ 08543-5400, USA. jennifer.qiao@bms.com | lld:pubmed |
| pubmed-article:19046881 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19046881 | lld:chembl |
