25899-96-1Relevant academic research and scientific papers
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Yoshikawa, Kenji,Yoshino, Toshiharu,Yokomizo, Yoshihiro,Uoto, Kouichi,Naito, Hiroyuki,Kawakami, Katsuhiro,Mochizuki, Akiyoshi,Nagata, Tsutomu,Suzuki, Makoto,Kanno, Hideyuki,Takemura, Makoto,Ohta, Toshiharu
, p. 2133 - 2140 (2011/04/24)
We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the identification of compound 30h which showed both good in vitro activity (fXa IC50 = 2.2 nM, PTCT2 = 3.9 μM) and in vivo antithrombotic efficacy.
Benzene derivatives having NGF production-promoting activity
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, (2008/06/13)
A compound of the formula (I): STR1 wherein R1 is an unsubstituted or substituted amino group, a protected amino group, or a nitro group; R2 is an unsubstituted or substituted amino group, a protected amino group, an unsubstituted or substituted hydroxy group or a protected hydroxy group; R3 is an unsubstituted or substituted amino group, m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n is an integer from 2 to 6, and pharmaceutically acceptable salts thereof. Compounds of formula (I) except those wherein R1 is a nitro group have activity in promoting the production of nerve growth factor.
Immunomodulating agent
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, (2008/06/13)
Phenylacetic acid derivatives of the formula: STR1 wherein R1 is hydrogen or STR2 wherein R5 is an alkyl group of 1-6 carbon atoms or an aryl group; R2 and R3 are independently hydrogen or an alkyl group of 1-4 carbon atoms; R4 is hydrogen or an alkyl group of 1-4 carbon atoms, have been found to possess immunomodulating activity.
Tertiary aminoacids
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, (2008/06/13)
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula STR1 and functional derivatives thereof, are anti-inflammatory agents.
Tertiary aminoacids
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, (2008/06/13)
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula STR1 AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
