Structural modification of the P2′ position of 2,7-dialkyl- substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets

Journal of Medicinal Chemistry

Volumn 50, Issue 20, 2007, Pages 4832-4844

  Maibaum, Jürgen ^a   Stutz, Stefan ^a,b   Göschke, Richard ^a   Rigollier, Pascal ^a   Yamaguchi, Yasuchika ^a,c   Cumin, Frédéric ^a   Rahuel, Joseph ^a   Baum, Hans Peter ^a   Cohen, Nissim Claude ^a,d   Schnell, Christian R ^a   Fuhrer, Walter ^a   Gruetter, Markus G ^a,e   Schilling, Walter ^a,f   Wood, Jeanette M ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b Speedel Experimenta AG   (Switzerland)

^c NAGASAKI INTERNATIONAL UNIVERSITY   (Japan)

^d Synergix Ltd   (Israel)

^e Biochemisches Institut   (Switzerland)

^f F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINO 4 HYDROXY 2 ISOPROPYL 7 [4 METHOXY 3 (3 METHOXYPROPOXY)BENZYL] 8 METHYLNONANOIC ACID BUTYLAMIDE; ALDOSTERONE; ALISKIREN; AMIDE; ANGIOTENSIN; ANTIHYPERTENSIVE AGENT; OCTANE; RENIN; RENIN INHIBITOR; SODIUM; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CHEMICAL MODIFICATION; CHEMICAL STRUCTURE; CONTROLLED STUDY; DOSE RESPONSE; DRUG INDICATION; DRUG POTENCY; DRUG SYNTHESIS; DRUG TARGETING; HYPERTENSION; MARMOSET; MEAN ARTERIAL PRESSURE; NONHUMAN; RENIN ANGIOTENSIN ALDOSTERONE SYSTEM; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; ANTIHYPERTENSIVE AGENTS; BLOOD PRESSURE; CALLITHRIX; CRYSTALLOGRAPHY, X-RAY; FUMARATES; HEART RATE; HUMANS; KINETICS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; OCTANOIC ACIDS; PROTEIN BINDING; RENIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34848869297     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm070316i     Document Type: Article

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