Thomas Richard Belliotti

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Featured researches published by Thomas Richard Belliotti.

Bioorganic & Medicinal Chemistry Letters | 2009

Oxadiazolone bioisosteres of pregabalin and gabapentin.

David Juergen Wustrow; Thomas Richard Belliotti; Thomas Capiris; Clare Octavia Kneen; Justin Stephen Bryans; Mark J. Field; Dic Williams; Ayman El-Kattan; Lisa Buchholz; Jack J. Kinsora; Susan M. Lotarski; Mark G. Vartanian; Charles P. Taylor; Sean Donevan; Andrew John Thorpe; Jacob Bradley Schwarz

A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the alpha(2)-delta subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain uptake but was nevertheless active in models of osteoarthritis. The high clearance associated with compound 9 was postulated to be a consequence of efflux by OAT and/or OCT, and was attenuated on co-administration with cimetidine or probenecid.

Journal of Medicinal Chemistry | 2005

Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein

Thomas Richard Belliotti; Thomas Capiris; I. Victor Ekhato; Jack J. Kinsora; Mark J. Field; Thomas G. Heffner; Leonard T. Meltzer; Jacob Bradley Schwarz; Charles P. Taylor; Andrew John Thorpe; Mark G. Vartanian; Lawrence D. Wise; Ti Zhi-Su; Mark L. Weber; David Juergen Wustrow

Archive | 2000

Mono- and disubstituted 3-propyl gamma-aminobutyric acids

Thomas Richard Belliotti; Justin Stephen Bryans; Ihoezo Victor Ekhato; Augustine Tobi Osuma; Robert Michael Schelkun; Jacob Bradley Schwarz; Andrew John Thorpe; Lawrence D. Wise; David Juergen Wustrow; Po-Wai Yuen

Archive | 1998

Novel amines as pharmaceutical agents

Thomas Richard Belliotti; Justin Stephen Bryans; Thomas Capiris; David Christopher Horwell; Clare Octavia Kneen; David Juergen Wustrow

Archive | 1999

Improved gamma amino butyric acid analogs

Thomas Richard Belliotti; David Juergen Wustrow

Journal of Medicinal Chemistry | 1998

Aminopyrimidines with High Affinity for Both Serotonin and Dopamine Receptors

David Juergen Wustrow; Thomas Richard Belliotti; Shelly Ann Glase; Suzanne Ross Kesten; Don Johnson; Norman L. Colbry; Ronald Rubin; Anthony C. Blackburn; Hyacinth Akunne; Ann E. Corbin; M. Duff Davis; Lynn M. Georgic; Steven Z. Whetzel; Kim Zoski; Thomas G. Heffner; Thomas A. Pugsley; Lawrence D. Wise

Journal of Medicinal Chemistry | 1999

A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.

Thomas Richard Belliotti; David Juergen Wustrow; Wouter A. Brink; Kim Zoski; Yu-Hsin Shih; Steven Z. Whetzel; Lynn M. Georgic; Ann E. Corbin; Hyacinth Akunne; Thomas G. Heffner; Thomas A. Pugsley; Lawrence D. Wise

Bioorganic & Medicinal Chemistry Letters | 2007

Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.

Daniel D. Holsworth; Mehran Jalaie; Thomas Richard Belliotti; Cuiman Cai; Wendy Collard; Suzie Ferreira; Noel A. Powell; Michael Andrew Stier; Erli Zhang; Pat McConnell; Igor Mochalkin; Michael J. Ryan; John W. Bryant; Tingsheng Li; Aparna Kasani; Rajendra Subedi; Samarendra N. Maiti; Jeremy J. Edmunds

Archive | 2000