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Dive into the research topics where Raymond F. Horvath is active.

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Featured researches published by Raymond F. Horvath.


Bioorganic & Medicinal Chemistry Letters | 2008

The design, synthesis and structure–activity relationships of 1-aryl-4-aminoalkylisoquinolines: A novel series of CRF-1 receptor antagonists

Taeyoung Yoon; Stéphane De Lombaert; Robbin Brodbeck; Michael Gulianello; Jayaraman Chandrasekhar; Raymond F. Horvath; Ping Ge; Mark T. Kershaw; James E. Krause; John H. Kehne; Diane Hoffman; Dario Doller; Kevin J. Hodgetts

The design, synthesis and structure-activity relationships of a novel series of CRF-1 receptor antagonist, the 1-aryl-4-alkylaminoisoquinolines, is described. The effects of substitution on the aromatic ring, the amino group and the isoquinoline core on CRF-1 receptor binding were investigated.


Journal of Medicinal Chemistry | 2011

Discovery of N-(1-Ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98−2): An Orally Active Corticotropin Releasing Factor-1 (CRF-1) Receptor Antagonist

Kevin J. Hodgetts; Ping Ge; Taeyoung Yoon; Stéphane De Lombaert; Robbin Brodbeck; Michael Gulianello; Andrzej Kieltyka; Raymond F. Horvath; John H. Kehne; James E. Krause; George D. Maynard; Diane Hoffman; Younglim Lee; Laurence Fung; Dario Doller

The design, synthesis, and structure-activity relationships of a novel series of pyrazines, acting as corticotropin releasing factor-1 (CRF-1) receptor antagonists, are described. Synthetic methodologies were developed to prepare a number of substituted pyrazine cores utilizing regioselective halogenation and chemoselective derivatization. Noteworthy, an efficient 5-step synthesis was developed for the lead compound 59 (NGD 98-2), which required no chromatography. Compound 59 was characterized as an orally bioavailable, brain penetrant, and highly selective CRF-1 receptor antagonist. Occupancy of rat brain CRF-1 receptors was quantified using ex vivo receptor occupancy assays, using both brain tissue homogenates as well as brain slices receptor autoradiography. Behaviorally, oral administration of 59 significantly antagonized CRF-induced locomotor activity at doses as low as 10 mg/kg and dose-dependently reduced the restraint stress-induced ACTH increases.


Bioorganic & Medicinal Chemistry Letters | 2008

2-Arylpyrimidines : Novel CRF-1 receptor antagonists

Taeyoung Yoon; Stéphane De Lombaert; Robbin Brodbeck; Michael Gulianello; James E. Krause; Alan Hutchison; Raymond F. Horvath; Ping Ge; John H. Kehne; Diane Hoffman; Jayaraman Chandrasekhar; Dario Doller; Kevin J. Hodgetts

The design, synthesis and structure-activity relationship studies of a novel series of CRF-1 receptor antagonists, the 2-arylpyrimidines, are described. The effects of substitution on the aromatic ring and the pyrimidine core on CRF-1 receptor binding were investigated. A number of compounds with K(i) values below 10 nM and lipophilicity in a minimally acceptable range for a CNS drug (cLogP<5) were discovered.


Bioorganic & Medicinal Chemistry Letters | 2016

1-Sulfonyl-6-Piperazinyl-7-Azaindoles as potent and pseudo-selective 5-HT6 receptor antagonists.

Charles-Henry Fabritius; Ullamari Pesonen; Josef Messinger; Raymond F. Horvath; Harri Salo; Michal Galezowski; Mariusz Galek; Klaudia Stefańska; Joanna Szeremeta-Spisak; Marta Olszak-Płachta; Anna Małgorzata Buda; Justyna Adamczyk; Marcin Król; Peteris Prusis; Magdalena Sieprawska-Lupa; Maciej Mikulski; Katja Kuokkanen; Hugh Chapman; Radosław Obuchowicz; Timo Korjamo; Niina Jalava; Mateusz Nowak

A series of 1-Sulfonyl-6-Piperazinyl-7-Azaindoles, showing strong antagonistic activity to 5-HT6 receptor (5-HT6R) was synthesized and characterized. The series was optimized to reduce activity on D2 receptor. Based on the selectivity against this off-target and the analysis of the ADME-tox profile, compound 1c was selected for in vivo efficacy assessment, which demonstrated procognitive effects as shown in reversal of scopolamine induced amnesia in an elevated plus maze test in mice. Compound 3, the demethylated version of compound 1c, was profiled against a panel of 106 receptors, channels and transporters, indicating only D3 receptor as a major off-target. Compound 3 has been selected for this study over compound 1c because of the higher 5-HT6R/D2R binding ratio. These results have defined a new direction for the design of our pseudo-selective 5-HT6R antagonists.


Archive | 1999

AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES

Raymond F. Horvath; James W. Darrow; George D. Maynard


Archive | 2004

Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands

Ping Ge; Raymond F. Horvath; Lu Yan Zhang; Yasuchika Yamaguchi; Bernd Kaiser; Xuechun Zhang; Suoming Zhang; He Zhao; Stanly John; Neil Moorcroft; Greg Shutske


Archive | 2004

5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds

Kevin J. Hodgetts; Stanly John; Neil Moorcroft; Greg Shutske; Bernd Kaiser; Yasuchika Yamaguchi; Ping Ge; Raymond F. Horvath


Archive | 2002

Certain pyrrolopyridine derivatives; novel crf1 specific ligands

Raymond F. Horvath; Alan Hutchison


Archive | 2001

Benzimidazole and indole derivatives as crf receptor modulators

Lombaert Stephane De; Ping Ge; Raymond F. Horvath; Taeyoung Yoon


Archive | 1999

Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors

Ping Ge; Raymond F. Horvath; Stéphane De Lombaert

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Tomasz Rzymski

University of California

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Yasuchika Yamaguchi

Nagasaki International University

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