Author: Kosuke Okazaki ; Kiyoto Hara ; Shigeru Nakano ; Harunobu Mukaiyama ; Hiroaki Okuno ; Norihiko Kikuchi ; Hiroaki Kobayashi ; Keiko Misawa ; Hidetoshi Isawa ; Hideyuki Muranaka ; Tomonaga Ozawa ; Takashi Koizumi ; Yuichiro Kai ; Hiroaki Shiohara ; Kenji Yokoyama ; Hideki Takeuchi ; Masahiko Uchida ; Eiichi Tsuji ; Yasuoki Murakami ; Yuji Hoyano

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.

01 Dec 2005·Current Topics in Medicinal ChemistryQ4 · MEDICINE

Small Molecule Coagulation Cascade Inhibitors in the Clinic

Q4 · MEDICINE

Review

Author: Soares, Chris ; Saiah, Eddine

Venous thromboembolic disease, including deep vein thrombosis and pulmonary embolism, is a cause of significant mortality and morbidity. For several decades, anticoagulant options for the treatment and prevention of thrombosis have been limited mainly to agents such as unfractionated heparin and oral vitamin K antagonists such as warfarin. Although these therapies have proven benefits, they also have important limitations that result in their underuse in routine clinical practice. A variety of novel anticoagulants with improved pharmacologic and clinical profiles are in development, offering benefits over traditional therapies. Specifically, progress has been made in the development of small molecule Factor Xa inhibitors and thrombin inhibitors. The most advanced drugs reviewed include DPC-423, DPC-602, razaxaban, GSK's 813893, Portola's Xa inhibitors (formerly Millennium), otamixaban, DU-176b, KFA-1982, BAY-59-7939, DX-9065a, YM-150, LY-517717, Exanta, 3DP's thrombin inhibitors, SSR-182289, LB-30057, LB-30870, BIBR-1048 and Merck's thrombin inhibitors. With their potentially consistent and predictable pharmacological profile, oral formulation, and decreased need for coagulation monitoring, these new agents will likely increase the use and duration of anticoagulation treatment in thromboembolic disorders and reduce the burden associated with long-term management.

100 Deals associated with KFA-1982

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Indication	Highest Phase	Country/Location	Organization	Date
Thrombosis	Phase 1	JP	Kissei Pharmaceutical Co., Ltd.	-
Venous Thrombosis	Phase 1	-	-	-
Venous Thrombosis	Phase 1	-	Kissei Pharmaceutical Co., Ltd.	-

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