211489-99-5Relevant articles and documents
3-Amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors
Sanderson, Philip E. J.,Cutrona, Kellie J.,Savage, Kelly L.,Naylor-Olsen, Adel M.,Bickel, Denise J.,Bohn, Dennis L.,Clayton, Franklin C.,Krueger, Julie A.,Lewis, S. Dale,Lucas, Bobby J.,Lyle, Elizabeth A.,Wallace, Audrey A.,Welsh, Denice C.,Yan, Youwei
, p. 1441 - 1444 (2007/10/03)
We describe a series of highly potent and efficacious thrombin inhibitors based on a 3-amino-4-sulfonylpyridinone acetamide template. The functionally dense sulfonyl group stabilizes the aminopyridinone, conformationally constrains the 4-substituent, and
Pyridone derivatives, their preparation and their use as synthesis intermediates
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, (2008/06/13)
The invention concerns compounds of formula (I) in which: R is —NO2or —NHR3, R3being hydrogen, —COR4(R4selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, —COOR5(R5selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), —CONHR6or SO2R6(R6selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), —SO2NR7R8(R7and R8independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a —CH2—, —SO2or —NR1— group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.
