Taiho Pharmaceutical Company Limited

Yoshimitsu Suda

Tetsuji Asao

Yukio Tada

Tomohiro Yamashita

Kenji Yamamoto

Shozo Yamada

Hidenori Fujita

Shigeo Okajima

Hiromi Oshiumi

Kazuhiko Shigeno

Nobuhiko Katunuma

Nobuhiko Katsunuma

Kosuke Egami

Koji Murakami

Atsuhiko Uemura

Provided is a c-Met inhibitory antitumor agent which mitigates side effects by selectively affecting tumor cells in which c-Met is specifically expressed, having a formula (I) or its salt: wherein each of Rand Rare independently a hydrogen atom, an optionally substituted Calkyl, Ccycloalkyl, Caromatic hydrocarbon, or saturated or unsaturated heterocyclic group, or Rand Rmay form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; Ris a Calkyl group; and R, R, and R, are independently a hydrogen atom, a halogen atom, an optionally substituted Calkyl group, a Calkoxy group, a Calkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or Rand Rmay form a ring together with the phenyl ring to which they are attached.

Acylthiourea compound or salt thereof, and use thereof

The present invention provides a compound that exhibits an excellent antitumor effect and reduces side effects, such as skin disorders, of the existing retinoid by selectively activating on the nuclear receptor RAR&#x3b1;, thereby possibly producing significant improvement of clinical profits. Specifically, the present invention provides a bis(trimethylsilyl)phenyl compound represented by Formula (I): wherein X is N or CH; Y is O or S; R1, R2, and R3 are the same or different and are hydrogen or lower alkyl; R4 and R5 are the same or different and are hydrogen, lower alkyl, or halogen; and a bond between a carbon atom to which R1 is attached and a carbon atom to which R2 is attached is a single bond or a double bond;or a salt thereof.

Bis(trimethylsilyl)phenyl compound or salt thereof, and use thereof

The present invention provides a peptide derivative of formula (I) or a pharmaceutically acceptable salt thereof wherein X is &#x2014;CH(OH)&#x2014; or &#x2014;CO&#x2014;; Ris hydrogen or an amino protecting group; Ris hydroxyl or lower alkoxy; one of Rand Ris the side chain (R group) of lysine the amino group of which may be protected with a protecting group and the other of Rand Ris the side chain (R group) of arginine the guanidino group of which may be protected with a protecting group; and Rand Rmay be the same or different and are hydrogen, lower alkyl or aralkyl. The present invention further provides a production process and use thereof.

Peptide derivative, and pharmaceutically acceptable salt thereof, process for producing the same, and use thereof

The present invention provides a peptide derivative of formula (I)wherein X is &#x2014;CHOH&#x2014; or &#x2014;CO&#x2014;; Rand Rare hydrogen or substituted oxycarbonyl; Ris substituted oxycarbonyl; Ris hydroxyl, lower alkoxy, optionally substituted piperazinyl or the like; Ris a R-group side chain of an &#x3b1;-amino acid optionally protected by a protective group, Ris hydroxyl, lower alkoxy or the like; m is 0 or 1; and n is an integer of 2 to 6; ora pharmaceutically acceptable salt thereof. The present invention further provides a production process and use thereof.

Peptide derivatives and their pharmaceutically acceptable salts, thereof, processes for preparation of both and use thereof

Epoxysuccinamide derivative or salt thereof

Epoxysuccinamide derivative or salt thereof, and medicine comprising the

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Hanno, Japan

Yoshimitsu Suda