50921-41-0Relevant academic research and scientific papers
New oxybenzamide derivatives useful for inhibiting factor Xa or VIIa
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, (2008/06/13)
The present invention relates to compounds comprising the following formula: R0—Q—X—Q′—W—U—V—G—M??(I) These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.
A polar substituent effect on the ring-cleavage rearrangement of 1-arylcyclobutylmethyl Grignard reagents
Hill, E. Alexander,Li, Baoju
, p. 9 - 14 (2007/10/02)
The kinetics of the ring-cleavage rearrangements of 1-phenylcyclobutylmethylmagnesium chloride and its p-methyl and p-chloro analogs have been determined.The first-order rate constants are correlated by the Hammett equation, with ρ=-0.47.The results are consistent with a concerted mechanism with a cyclic transition state having significant polar character, although polar effects on the stabilities of reactant and product may also contribute.The phenyl group itself slows the reaction by a factor of 0.031, which is interpreted principally in terms of steric destabilization of the transition state.
Therapeutic agents
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, (2008/06/13)
Compounds of formula I STR1 in which R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R2 is H or C1-3 alkyl; R3 and/or R4 are H, formyl, C1-3 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-7 cycloalkyl or R3 and R4 together with the nitrogen atom form a heterocyclic ring system; R5 and/or R6 are H, halo, CF3, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylthio or R5 and R6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
Arylcyclobutylalkylamines and anti-depression composition and methods using same
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, (2008/06/13)
Compounds of formula I STR1 in which R1 is H or C1-3 alkyl; R2 is H or C1-3 alkyl; R3 and/or R4 are H, C1-3 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-7 cycloalkyl or R3 and R4 together with the nitrogen atom form a heterocyclic ring system; R5 and/or R6 are H, halo, CF3, or C1-3 alkyl (with the proviso that R5 and R6 cannot both be H or methyl) or R5 and R6 together with the carbon atoms to which they are attached form a second benzene ring and R7 and/or R8 are H or C1-3 alkyl show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
