Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity

Samuel Chackalamannil; Yuguang Wang; William J. Greenlee; Zhiyong Hu; Yan Xia; Ho-Sam Ahn; George Boykow; Yunsheng Hsieh; Jairam Palamanda; Jacqueline Agans-Fantuzzi; Stan Kurowski; Michael Graziano; Madhu Chintala

doi:10.1021/jm800180e

Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity

Journal of Medicinal Chemistry ◽

10.1021/jm800180e ◽

2008 ◽

Vol 51 (11) ◽

pp. 3061-3064 ◽

Cited By ~ 184

Author(s):

Samuel Chackalamannil ◽

Yuguang Wang ◽

William J. Greenlee ◽

Zhiyong Hu ◽

Yan Xia ◽

...

Keyword(s):

Receptor Antagonist ◽

Thrombin Receptor ◽

Antiplatelet Activity ◽

Sch 530348 ◽

Orally Active ◽

Thrombin Receptor Antagonist

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Convergent Synthesis of Both Enantiomers of 4-Hydroxypent-2-ynoic Acid Diphenylamide for a Thrombin Receptor Antagonist Sch 530348 and Himbacine Analogues

Advanced Synthesis & Catalysis ◽

10.1002/adsc.200900322 ◽

2009 ◽

Vol 351 (14-15) ◽

pp. 2351-2357 ◽

Cited By ~ 5

Author(s):

Alex Zaks ◽

Maria Tamarez ◽

Tao Li

Keyword(s):

Receptor Antagonist ◽

Thrombin Receptor ◽

Convergent Synthesis ◽

Sch 530348 ◽

Thrombin Receptor Antagonist

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Effect of Food, Antacid, and Age on the Pharmacokinetics of the Oral Thrombin Receptor Antagonist Vorapaxar (SCH 530348) in Healthy Volunteers

Clinical Pharmacology in Drug Development ◽

10.1002/cpdd.30 ◽

2013 ◽

Vol 2 (3) ◽

pp. 223-230 ◽

Cited By ~ 6

Author(s):

Teddy Kosoglou ◽

Larisa Reyderman ◽

Jack Tseng ◽

Bharath Kumar ◽

Fengjuan Xuan ◽

...

Keyword(s):

Healthy Volunteers ◽

Receptor Antagonist ◽

Thrombin Receptor ◽

Sch 530348 ◽

Effect Of Food ◽

Thrombin Receptor Antagonist

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Determination of a novel thrombin receptor antagonist (SCH 530348) in human plasma: Evaluation of Ultra Performance Liquid Chromatography™–tandem mass spectrometry for routine bioanalytical analysis

Journal of Pharmaceutical and Biomedical Analysis ◽

10.1016/j.jpba.2011.01.045 ◽

2011 ◽

Vol 55 (2) ◽

pp. 349-359 ◽

Cited By ~ 3

Author(s):

Cristina I. Tama ◽

Jim X. Shen ◽

James E. Schiller ◽

Roger N. Hayes ◽

Robert P. Clement

Keyword(s):

Mass Spectrometry ◽

Liquid Chromatography ◽

Tandem Mass Spectrometry ◽

Receptor Antagonist ◽

Ultra Performance Liquid Chromatography ◽

Thrombin Receptor ◽

Tandem Mass ◽

Sch 530348 ◽

Thrombin Receptor Antagonist

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1102-48 Inhibitory effect of E5555, an orally active thrombin receptor antagonist, on intimal hyperplasia following balloon injury

Journal of the American College of Cardiology ◽

10.1016/s0735-1097(04)90284-7 ◽

2004 ◽

Vol 43 (5) ◽

pp. A68 ◽

Cited By ~ 9

Author(s):

Toshiyuki Matsuoka ◽

Motoji Kogushi ◽

Tsutomu Kawata ◽

Akifumi Kimura ◽

Ken-ichi Chiba ◽

...

Keyword(s):

Receptor Antagonist ◽

Intimal Hyperplasia ◽

Inhibitory Effect ◽

Thrombin Receptor ◽

Balloon Injury ◽

Orally Active ◽

Thrombin Receptor Antagonist

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SCH 530348: a novel oral thrombin receptor antagonist

Future Cardiology ◽

10.2217/fca.09.27 ◽

2009 ◽

Vol 5 (5) ◽

pp. 435-442 ◽

Cited By ~ 8

Author(s):

Marc P Bonaca ◽

David A Morrow

Keyword(s):

Receptor Antagonist ◽

Thrombin Receptor ◽

Sch 530348 ◽

Thrombin Receptor Antagonist

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The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs

European Journal of Pharmacology ◽

10.1016/j.ejphar.2011.01.058 ◽

2011 ◽

Vol 657 (1-3) ◽

pp. 131-137 ◽

Cited By ~ 31

Author(s):

Motoji Kogushi ◽

Toshiyuki Matsuoka ◽

Tsutomu Kawata ◽

Hiroko Kuramochi ◽

Shinki Kawaguchi ◽

...

Keyword(s):

Receptor Antagonist ◽

Guinea Pigs ◽

Arterial Thrombosis ◽

Bleeding Time ◽

Thrombin Receptor ◽

The Novel ◽

Orally Active ◽

Thrombin Receptor Antagonist

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Glycoprotein IIb/IIIa Receptor Inhibitors in Combination With Vorapaxar, a Platelet Thrombin Receptor Antagonist, Among Patients With Non–ST-Segment Elevation Acute Coronary Syndromes (from the TRACER Trial)

The American Journal of Cardiology ◽

10.1016/j.amjcard.2015.02.043 ◽

2015 ◽

Vol 115 (10) ◽

pp. 1325-1332 ◽

Cited By ~ 11

Author(s):

Jan H. Cornel ◽

Pierluigi Tricoci ◽

Yuliya Lokhnygina ◽

David J. Moliterno ◽

Lars Wallentin ◽

...

Keyword(s):

Receptor Antagonist ◽

Acute Coronary Syndromes ◽

Thrombin Receptor ◽

St Segment Elevation ◽

St Segment ◽

Coronary Syndromes ◽

Thrombin Receptor Antagonist

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Effect of age on efficacy and safety of vorapaxar in patients with non–ST-segment elevation acute coronary syndrome: Insights from the Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRACER) trial

American Heart Journal ◽

10.1016/j.ahj.2016.05.012 ◽

2016 ◽

Vol 178 ◽

pp. 176-184 ◽

Cited By ~ 4

Author(s):

Luciana V. Armaganijan ◽

Karen P. Alexander ◽

Zhen Huang ◽

Pierluigi Tricoci ◽

Claes Held ◽

...

Keyword(s):

Acute Coronary Syndrome ◽

Receptor Antagonist ◽

Clinical Event ◽

Thrombin Receptor ◽

Efficacy And Safety ◽

St Segment Elevation ◽

Coronary Syndrome ◽

St Segment ◽

Thrombin Receptor Antagonist ◽

Effect Of Age

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Inhibitory effects of FR171113, a novel, thrombin receptor antagonist, on platelet aggregation and thrombosis model in guinea-pigs

The Japanese Journal of Pharmacology ◽

10.1016/s0021-5198(19)40542-8 ◽

1998 ◽

Vol 76 ◽

pp. 106

Author(s):

Yasuko Kato ◽

Yasuhiro Kita ◽

Mie Nishio ◽

Yoshimi Hirasawa ◽

Kayoko Senzaki ◽

...

Keyword(s):

Platelet Aggregation ◽

Receptor Antagonist ◽

Guinea Pigs ◽

Thrombin Receptor ◽

Inhibitory Effects ◽

Thrombosis Model ◽

Thrombin Receptor Antagonist

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The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRA•CER) trial: study design and rationale

American Heart Journal ◽

10.1016/j.ahj.2009.07.001 ◽

2009 ◽

Vol 158 (3) ◽

pp. 327-334.e4 ◽

Cited By ~ 93

Author(s):

The TRA•CER Executive and Steering Committees

Keyword(s):

Acute Coronary Syndrome ◽

Receptor Antagonist ◽

Study Design ◽

Clinical Event ◽

Thrombin Receptor ◽

Coronary Syndrome ◽

Thrombin Receptor Antagonist

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