Astellas Pharma Gmbh

Takahide Ohishi

Shigeru Yoshida

Hiroyuki Moritomo

Masahiko Hayakawa

Kenji Negoro

Jun Takasaki

Kenichi Onda

Masazumi Kamohara

Takatoshi Soga

Yasuhiro Yonetoku

Takahiro Nigawara

Mitsuyuki Matsumoto

Tetsu Saito

Kazuhiko Iikubo

Daisuke Sasuga

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

The invention relates to a convenient screening tool for identifying an agent for treating diabetes. The screening tool is a G protein-coupled receptor, a variant of the G protein-coupled receptor, or a homolog of the G protein-coupled receptor, which promotes insulin secretion under a high glucose concentration by activation. The invention also relates to cells transformed with an expression vector comprising a polynucleotide encoding and expressing the screening tool. The invention provides a convenient screening method for identifying an agent for treating diabetes, pharmaceutical compositions comprising the agent, and a process for manufacturing the pharmaceutical composition.

Method for screening agents for the treatment of diabetes

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

A screening tool for an antiplatelet agent wherein the tool is a human ADP receptor P2Tprotein, a variation functionally equivalent thereto, or a homologous protein thereof, and a screening tool for an antiplatelet agent wherein the tool is a transformant which is transformed with an expression vector comprising a DNA encoding the protein and is expressing the polypeptide are disclosed. Further, a method for detecting an ADP receptor P2Tligand, antagonist, or agonist by using the screening tool for an antiplatelet agent, and a method for screening an antiplatelet agent by the detecting method are disclosed.

Method of screening antiplatelet agents

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Tokyo, Japan

Takahide Ohishi