- Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: Novel, highly potent and orally efficacious squalene synthase inhibitors
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We have recently reported the discovery of the new benzhydrol template, which has a highly potent inhibitory activity for squalene synthase, as typified by compound 1 (SSI IC50 = 0.85 nM). However, it was composed of a pair of easy rotatable at
- Ichikawa, Masanori,Yokomizo, Aki,Itoh, Masao,Haginoya, Noriyasu,Sugita, Kazuyuki,Usui, Hiroyuki,Terayama, Koji,Kanda, Akira
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experimental part
p. 5207 - 5224
(2011/10/08)
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- 4,4-DISUBSTITUTED-1,4-DIHYDRO-2H-3,1-BENZOXAZIN-2-ONES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS AND INTERMEDIATES AND PROCESSES FOR MAKING THE SAME
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The present invention relates to benzoxazinones of formula I, or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
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- Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz
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Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have synthesized metabolites of efavirenz to confirm their structure and to evaluate their activity as antivirals.
- Markwalder, Jay A.,Christ, David D.,Mutlib, Abdul,Cordova, Beverly C.,Klabe, Ronald M.,Seitz, Steven P.
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p. 619 - 622
(2007/10/03)
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- 4,4-disubstitued-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same
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The present invention relates to benzoxazinones of formula I: STR1 or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
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- Synthesis and evaluation of analogs of Efavirenz (SUSTIVA(TM)) as HIV-1 reverse transcriptase inhibitors
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Efavirenz (SUSTIVA(TM)) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse transcriptase enzyme during Efavirenz therapy, we sought to develop an optimized second generation series. To that end, SAR of the substituents on the aromatic ring was undertaken and the results are summarized here. The 5,6-difluoro (4f) and the 6-methoxy (4m) substituted benzoxazinones were determined to be equipotent, and as a result such substitution patterns will be incorporated in second generation scaffolds.
- Patel, Mona,Ko, Soo S.,McHugh Jr., Robert J.,Markwalder, Jay A.,Srivastava, Anurag S.,Cordova, Beverly C.,Klabe, Ronald M.,Erickson-Viitanen, Susan,Trainor, George L.,Seitz, Steven P.
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p. 2805 - 2810
(2007/10/03)
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- Use of malonic acid derivative compounds for retarding plant growth
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This invention relates to a method for retarding plant growth by applying to the plant an effective amount of a malonic acid derivative compound. This invention also relates to novel malonic acid derivative compounds and processes for the preparation thereof.
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- Synergistic plant growth regulator compositions
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This invention relates to synergistic plant growth regulator compositions containing (1) an ethylene response or ethylene-type response inducing agent and (11) a malonic acid derivative compound. This invention also relates to the use of said compositions
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