- Pyran-2-ones and 5,6-dihydropyran-2-ones useful for treating hyperplasia and other diseases
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Certain 2H-pyran-2-ones are useful for treating benign prostatic hypertrophy or hyperplasia, prostatic cancer, alopecia, hirsutism, acne vulgaris and seborrhea.
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- Aryne intermediates and a process for the preparation thereof
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There are provided aryne intermediates of formula I, useful in the manufacture of herbicidal compounds. STR1 Also provided is a method to prepare the formula I intermediates via the palladium catalyzed coupling of an o-halonitrobenzene or o-haloaniline wi
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- Aryne intermediates towards the preparation of herbicidal sulfamoyl urea and a process for their preparation
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There are provided aryne intermediates of formula I, useful in the manufacture of herbicidal compounds. Also provided is a method to prepare the formula I intermediates via the palladium catalyzed coupling of an o-halonitrobenzene or o-haloaniline with 3-
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- Structure-based design of nonpeptidic HIV protease inhibitors: The sulfonamide-substituted cyelooctylpyranones
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Recently, cyclooctylpyranone derivatives with m-carboxamide substituents (e.g. 2c) were identified as potent, nonpeptidic HIV protease inhibitors, but these compounds lacked significant antiviral activity in cell culture. Substitution of a sulfonamide group at the meta position, however, produces compounds with excellent HIV protease binding affinity and antiviral activity. Guided by an iterative structure-based drug design process, we have prepared and evaluated a number of these derivatives, which are readily available via a seven-step synthesis. A few of the most potent compounds were further evaluated for such characteristics as pharmacokinetics and toxicity in rats and dogs. From this work, the p-cyanophenyl sulfonamide derivative 35k emerged as a promising inhibitor, was selected for further development, and entered phase I clinical trials.
- Skulnick, Harvey I.,Johnson, Paul D.,Aristoff, Paul A.,Morris, Jeanette K.,Lovasz, Kristine D.,Howe, W. Jeffrey,Watenpaugh, Keith D.,Janakiraman, Musiri N.,Anderson, David J.,Reischer, Robert J.,Schwartz, Theresa M.,Banitt, Lee S.,Tomich, Paul K.,Lynn, Janet C.,Horng, Miao-Miao,Chong, Kong-Teck,Hinshaw, Roger R.,Dolak, Lester A.,Seest, Eric P.,Schwende, Francis J.,Rush, Bob D.,Howard, Gina M.,Toth, Lisa N.,Wilkinson, Karen R.,Kakuk, Thomas J.,Johnson, Carol W.,Cole, Serena L.,Zaya, Renee M.,Zipp, Gail L.,Possert, Peggy L.,Dalga, Robert J.,Zhong, Wei-Zhu,Williams, Marta G.,Romines, Karen R.
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p. 1149 - 1164
(2007/10/03)
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- Herbicide intermediate o-nitrophenyl cyclopropyl ketone and a method for the preparation thereof
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There is provided o-nitrophenyl cyclopropyl ketone, a key intermediate in the manufacture of the crop-selective, herbicidal agent 1-{[o-(cyclopropylcarbonyl)phenyl]sulfamoyl}-3-(4,6-dimethoxy-2-pyrimidinyl)urea and a method for the preparation of said ket
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