Carbocyclic Amino Ketones by Bredt's Rule-Arrested Kulinkovich-de Meijere Reaction
The TiII-mediated formation of cyclopropylamines from alkenes and amides, the Kulinkovich-de Meijere reaction, involves two carbon-carbon bond-forming steps. Strategic use of a tricyclic intermediate can arrest the process if the second step requires formation of a bridgehead double bond. Use of this Bredt's rule constraint results in the production of carbocyclic amino ketones, key alkaloid building blocks. Frustrated by Bredt's rule: An inability to consummate a Kulinkovich-de Meijere cyclopropanation that would involve a bridgehead double bond transforms the reaction into a transannular cyclization of an unsaturated lactam yielding an amino ketone product with potential for alkaloid synthesis.
Finn, Paul B.,Derstine, Brenden P.,Sieburth, Scott McN.
supporting information
p. 2536 - 2539
(2016/02/18)
COMBINATION THERAPY WITH INHIBITORS OF INDUCIBLE NITRIC OXIDE SYNTHASE AND ALKYLATING AGENTS
A combination therapy comprising administration of a carbamoylating chemotherapeutic agent in conjunction with administration of a selective iNOS inhibitor compound is disclosed. Optionally, resection and radiation therapy are provided with the therapeutic combination. A medicament comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound together with a pharmaceutically acceptable carrier is further disclosed. A kit comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound is further disclosed.
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Page/Page column 114-115
(2010/02/11)
METHODS FOR TREATMENT AND PREVENTION OF GASTROINTESTINAL CONDITIONS
Therapeutic methods for the prevention ad treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOs in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
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Page/Page column 114-115
(2010/02/06)
Synthesis and evaluation of radiolabeled inhibitors of inducible nitric oxide synthase
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Khan, A. R.,McCarthy, T J.,Welch, M. J.
p. S298 - S300
(2007/10/03)
Amidino derivatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
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(2008/06/13)
2-Iminohomopiperidinium salts as selective inhibitors of inducible nitric oxide synthase (iNOS)
An attractive approach to the treatment of inflammatory conditions such as osteo- and rheumatoid arthritis, inflammatory bowel disease, and sepsis is through the selective inhibition of human inducible nitric oxide synthase (hiNOS) since localized excess
Hansen Jr., Donald W.,Peterson, Karen B.,Trivedi, Mahima,Kramer, Steven W.,Webber, Ronald K.,Tjoeng, Foe S.,Moore, William M.,Jerome, Gina M.,Kornmeier, Christine M.,Manning, Pamela T.,Connor, Jane R.,Misko, Thomas P.,Currie, Mark G.,Pitzele, Barnett S.
p. 1361 - 1366
(2007/10/03)
Amidino dervatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.
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(2008/06/13)
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