The discovery of N -[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy] ethoxy]-4-pyrimidinyl]- N ′-propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist

Journal of Medicinal Chemistry

Volumn 55, Issue 17, 2012, Pages 7849-7861

  Bolli, Martin H ^a   Boss, Christoph ^a   Binkert, Christoph ^a   Buchmann, Stephan ^a   Bur, Daniel ^a   Hess, Patrick ^a   Iglarz, Marc ^a   Meyer, Solange ^a   Rein, Josiane ^a   Rey, Markus ^a   Treiber, Alexander ^a   Clozel, Martine ^a   Fischli, Walter ^a   Weller, Thomas ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ENDOTHELIN B RECEPTOR; MACITENTAN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; FEMALE; IC 50; IN VIVO STUDY; MALE; NONHUMAN; PULMONARY HYPERTENSION; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTIHYPERTENSIVE AGENTS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG DISCOVERY; PYRIMIDINES; RATS; RATS, INBRED DAHL; RECEPTOR, ENDOTHELIN A; RECEPTOR, ENDOTHELIN B; SULFONAMIDES;

EID: 84866307803     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3009103     Document Type: Article

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