409359-13-3Relevant academic research and scientific papers
Orally active factor Xa inhibitors: Investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy
Uchida, Masahiko,Okazaki, Kosuke,Mukaiyama, Harunobu,Isawa, Hidetoshi,Kobayashi, Hiroaki,Shiohara, Hiroaki,Muranaka, Hideyuki,Kai, Yuichiro,Kikuchi, Norihiko,Takeuchi, Hideki,Yokoyama, Kenji,Tsuji, Eiichi,Ozawa, Tomonaga,Hoyano, Yuji,Koizumi, Takashi,Misawa, Keiko,Hara, Kiyoto,Nakano, Shigeru,Murakami, Yasuoki,Okuno, Hiroaki
scheme or table, p. 4682 - 4687 (2009/04/08)
A series of novel and potent 3-amidinophenylsulfonamide derivatives of factor Xa inhibitors were designed and synthesized using an amidoxime prodrug strategy. We focused on systemic clearance of parent compounds in rats, and performed in vivo pharmacokinetic screening. Incorporation of a carboxymethoxy group markedly improved systemic clearance (compound 43), and the related amidoxime 44 showed sufficient prodrug conversion. Compound 45, the double prodrug of 43, exhibited practicable bioavailability after oral administration in rats. Among the various compounds under investigation, KFA-1982 was selected for clinical development.
PREVENTIVE OR THERAPEUTIC AGENT FOR KIDNEY DISEASE
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Page 22-23, (2008/06/13)
The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.
5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES FOR THEIR PREPARATION
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, (2008/06/13)
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group,
