Daiichi Sankyo Company, Limited

Shoko Yoshida

Yuuichi Sugimoto

Makoto Ono

Toru Taniguchi

Keisuke Yoshida

Kouichi Uoto

Hidenori Namiki

Tsuyoshi Soneda

Shigeo Yamanoi

Yuichi Ochiai

Masaki Miyazaki

Fuminao Doi

Masaki Setoguchi

Katsuji Kagechika

Madoka Hoshino

Akitake Yamaguchi

Takanori Wakabayashi

Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3'R,4&#x2032;S,5&#x2032;R)&#x2014;N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6&#x2033;-chloro-4&#x2032;-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2&#x2033;-oxo-1&#x2033;,2&#x2033;-dihydrodispiro[cyclohexane-1,2&#x2032;-pyrrolidine-3&#x2032;,3&#x2033;-indole]-5&#x2032;-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.

Crystals of dispiropyrrolidine derivatives

Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3'R,4'S,5&#x2032;R)&#x2014;N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6&#x2033;-chloro-4&#x2032;-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2&#x2033;-oxo-1&#x2033;,2&#x2033;-dihydrodispiro[cyclohexane-1,2&#x2032;-pyrrolidine-3&#x2032;,3&#x2033;-indole]-5&#x2032;-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.

Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3'R,4&#x2032;S,5&#x2032;R)-N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6&#x2033;-chloro-4&#x2032;-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2&#x2033;-oxo-1&#x2033;,2&#x2033;-dihydrodispiro[cyclohexane-1,2&#x2032;-pyrrolidine-3&#x2032;,3&#x2033;-indole]-5&#x2032;-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.

Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3'R,4&#x2032;S,5&#x2032;R)&#x2014;N&#x2014;[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6&#x2033;-chloro-4&#x2032;-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2&#x2033;-oxo-1&#x2033;,2&#x2033;-dihydrodispiro [cyclohexane-1,2&#x2032;-pyrrolidine-3&#x2032;,3&#x2033;-indole]-5&#x2032;-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.

The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein Rrepresents a C1-C3 alkyl group, each substituent Rmay be the same or different and may each represent a C1-C3 alkyl group, Rrepresents an optionally substituted pyridyl group or the like, Rand R, which are the same or different, each represent a C1-C3 alkyl group, Rand R, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.

Phenylxanthene derivatives

A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R, R, R, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification. 

Dispiropyrrolidine derivatives

The present invention relates to [7-[(7S)-7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hemihydrate. This hemihydrate is stable and easy to prepare, and has excellent properties for a pharmaceutical bulk powder.

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Tokyo, Japan

Shoko Yoshida