194995-47-6Relevant articles and documents
PRODRUGS OF KALLIKREIN INHIBITORS
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Page/Page column 127; 138, (2018/05/24)
Disclosed are compounds of formula I, II, and III, and pharmaceutically acceptable salts thereof, which are inhibitors of kallikrein. Also provided are pharmaceutical compositions comprising such a compound, and methods involving use of the compounds and compositions in the treatment and prevention of acquired or hereditary angioedema, or other diseases and conditions characterized by aberrant kallikrein activity. (I) (II) (III)
PROCESSES FOR THE PREPARATION AND PURIFICATION OF GABAPENTIN ENACARBIL
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Page/Page column 26-27, (2010/06/17)
Gabapentin enacarbil was prepared and purified from intermediates such as 1- haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C 10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C 10 ether, C2 to C7 ester, C5 to C 10 hydrocarbon and a combination thereof; a 1-haloalkyl halo formate of the following formula:(I) wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.
Mono and bis double ester prodrugs of novel aminomethyl-THF 1β-methylcarbapenems
Lin, Yang-I.,Bitha, Panayota,Li, Zhong,Sakya, Subas M.,Strohmeyer, Timothy W.,Lang Jr., Stanley A.,Yang, Youjun,Bhachech, Niraja,Weiss, William J.,Petersen, Peter J.,Jacobus, Nilda V.,Bush, Karen,Testa, Raymond T.
, p. 1811 - 1816 (2007/10/03)
Mono and bis double ester prodrugs of aminomethyl THF 1β-methylcarbapenems 1 were Mono double ester derivatives (2, 4 and 7) did not demonstrate significantly improved oral activity due to the presence of the charged species. However, bis double ester derivatives (3 and 5) demonstrated enhanced oral activity.