4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel.

Caroff, Eva; Hubler, Francis; Meyer, Emmanuel; Renneberg, Dorte; Gnerre, Carmela; Treiber, Alexander; Rey, Markus; Hess, Patrick; Steiner, Beat; Hilpert, Kurt; Riederer, Markus A

Caroff, Eva; Hubler, Francis; Meyer, Emmanuel; Renneberg, Dorte; Gnerre, Carmela; Treiber, Alexander; Rey, Markus; Hess, Patrick; Steiner, Beat; Hilpert, Kurt; Riederer, Markus A.

Afiliación

Caroff E; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Hubler F; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Meyer E; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Renneberg D; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Gnerre C; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Treiber A; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Rey M; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Hess P; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Steiner B; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Hilpert K; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Riederer MA; Drug Discovery and Preclinical Research and Development, Actelion Pharmaceuticals Ltd. , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.

J Med Chem ; 58(23): 9133-53, 2015 Dec 10.

Article en En | MEDLINE | ID: mdl-26550844

Asunto(s)

Piperazinas/química; Piperazinas/uso terapéutico; Profármacos/química; Profármacos/uso terapéutico; Antagonistas del Receptor Purinérgico P2Y/química; Antagonistas del Receptor Purinérgico P2Y/uso terapéutico; Trombosis/tratamiento farmacológico; Animales; Ácidos Carboxílicos/química; Ácidos Carboxílicos/farmacocinética; Ácidos Carboxílicos/uso terapéutico; Clopidogrel; Perros; Descubrimiento de Drogas; Esterificación; Humanos; Masculino; Piperazinas/farmacocinética; Agregación Plaquetaria/efectos de los fármacos; Inhibidores de Agregación Plaquetaria/química; Inhibidores de Agregación Plaquetaria/farmacocinética; Inhibidores de Agregación Plaquetaria/uso terapéutico; Profármacos/farmacocinética; Antagonistas del Receptor Purinérgico P2Y/farmacocinética; Pirrolidinas/química; Pirrolidinas/farmacocinética; Pirrolidinas/uso terapéutico; Ratas; Ratas Wistar; Ticlopidina/análogos & derivados; Ticlopidina/uso terapéutico

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Piperazinas / Trombosis / Profármacos / Antagonistas del Receptor Purinérgico P2Y Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Suiza

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