144686-65-7Relevant academic research and scientific papers
DRUG DERIVATIVES
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, (2013/09/12)
The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
DRUG DERIVATIVES
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, (2012/05/31)
The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
Asymmetric synthesis of (R)-nilvadipine and (S)-NB 818 via regioselective bromination of chiral 1,4-dihydropyridines as a key step and enzymatic resolution of racemic 2-hydroxymethyl-1,4-dihydropyridine derivatives
Ebiike, Hirosato,Maruyama, Kaori,Ozawa, Yumi,Yamazaki, Yukiyoshi,Achiwa, Kazuo
, p. 869 - 876 (2007/10/03)
Optically active 2-hydroxymethyl-1,4,dihydropyridines were obtained by lipase-catalyzed hydrolysis or transesterification of racemic materials. Chiral NB 818 and nilvadipine have been synthesized from chiral 2- hydroxymethyl-1,4-dihydropyridine. On the ot
Enzymatic Synthesis of Optically Active 2-Carbamoyloxymethyl-1,4-dihydropyridines, (R)-(+)- and (S)-(-)-NB 818
Ebiike, Hirosato,Maruyama, Kaori,Achiwa, Kazuo
, p. 1153 - 1156 (2007/10/02)
Racemic dihydropyridines were resolved by enzyme-catalyzed hydrolysis in an organic solvent saturated with water.The chiral derivatives obtained were converted to (S)- and (R)-NB 818.
