102878-14-8Relevant articles and documents
SUBSTITUTED SULFONAMIDES USEFUL AS ANTIAPOPTOTIC BCL INHIBITORS
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Page/Page column 99-100, (2012/12/13)
Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites
Komoriya, Satoshi,Haginoya, Noriyasu,Kobayashi, Shozo,Nagata, Tsutomu,Mochizuki, Akiyoshi,Suzuki, Masanori,Yoshino, Toshiharu,Horino, Haruhiko,Nagahara, Takayasu,Suzuki, Makoto,Isobe, Yumiko,Furugoori, Taketoshi
, p. 3927 - 3954 (2007/10/03)
Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine derivatives
Haginoya, Noriyasu,Kobayashi, Syozo,Komoriya, Satoshi,Hirokawa, Yumiko,Furugori, Taketoshi,Nagahara, Takayasu
, p. 2935 - 2939 (2007/10/03)
In our investigation of factor Xa inhibitors, a series of 1-(6-chloronaphthalen-2-yl)sulfonyl-4-(4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine-2-carbonyl)piperazines 3a-i were synthesized. In vitro inhibitory activities of the compounds against factor Xa and coagulation are summarized. Among the compounds, 3c and 3d, possessing a carbamoyl or N-methylcarbamoyl moiety, showed potent inhibitory activities when administered orally to rats.