Ono Pharmaceutical Co., Ltd.

Taihei Nishiyama

Takashi Kondo

Motoyuki Tanaka

Sho Kouyama

Atsushi Hiramatsu

Tomoyuki Koda

Yasuo Hirooka

Steve Courtney

Chris Yarnold

Stuart Flanagan

Osamu Ichihara

Akira Imagawa

Tohru Kambe

Yusuke Tanaka

Tatsunori Ino

Hideki Moriguchi

Shinichiro Tsujiyama

Yohei Ueda

A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

Dihydroindolizinone derivative

A method for producing a compound, such as 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate, and a novel intermediate suitable for the method, whereby the compound can be stably supplied with a high total reaction yield, by changing the starting material and improving the metathesis reaction, asymmetric reduction reaction and the like.

Method for producing bicyclic compound

The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases. 

Substituted pyrrolidines as factor XIa inhibitors for the treatment thromboembolic diseases

Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases

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Osaka, Japan

Taihei Nishiyama