Astellas Pharma Gmbh

Kotobuki Pharmaceutical Co Ltd

Daisuke Sasuga

Kenji Negoro

Kenichi Onda

Shigeru Yoshida

Hiroyuki Moritomo

Masahiko Hayakawa

Yasuhiro Yonetoku

Kazuhiko Iikubo

Takahiro Nigawara

Takahide Ohishi

Seiji Yoshimura

Noriyuki Kawano

Norio Seki

Takanori Koike

Hideyuki Watanabe

Fukushi Hirayama

Ryota Shiraki

Masakazu Imamura

Ken-Ichi Suzuki

Daisuke Kaga

Jiro Fujiyasu

Keita Nakanishi

Nobuyuki Shiraishi

Ryosuke Munakata

Hiroaki Hoshii

Kayoko Mihara

Hiroki Fukudome

Tomoaki Kawano

Masamichi Yuda

[Problem] A compound, which can be used for preventing or treating diseases, in which 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with &#x2014;O&#x2014; (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11&#x3b2;-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Triazole derivative or salt thereof

A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

Cocrystal of C-glycoside derivative and L-proline

Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.

Benzene derivative or salt thereof

The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, &#x2014;O-(lower alkyl), halogen atom, carboxyl, &#x2014;CO-(lower alkyl), and carbamoyl, Rrepresents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and Rrepresents a group represented by formula (II) or an optionally substituted cyclic amino: wherein Rand Rmay be identical or different and each represents &#x2014;H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or &#x2014;O-(lower alkyl), each of which is optionally substituted.

Pyrimidine derivative condensed with a non-aromatic ring

There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.

Aromatic-ring-fused pyrimidine derivative

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Tokyo, Japan

Daisuke Sasuga