Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Other

Ludwig Institute for Cancer Research Limited

Imperial Cancer Research Technology, Ltd.

Masahiko Hayakawa

Minoru Okada

Hiroyuki Kaizawa

Hiroyuki Moritomo

Mitsuaki Ohta

Koyo Matsuda

Mayumi Yamano

Ken-Ichi Kawaguchi

Tomonobu Koizumi

Kenichi Onda

Takayuki Suzuki

Tatsuya Maruyama

Yasuhiro Yonetoku

Makoto Takeuchi

Ken Ikeda

Kenji Negoro

Tetsuo Matsui

Takahiro Nigawara

Shigeru Yoshida

Yasuo Isomura

Takashi Furutani

Kenichi Kawaguchi

Yoshinori Okamoto

Masakazu Imamura

Isao Kinoyama

Kazuhiko Iikubo

Ryo Naito

Nobuaki Taniguchi

Takumi Takahashi

Daisuke Sasuga

Takahide Ohishi

Takenori Kimura

Noriko Ishikawa

Satoshi Miyamoto

Akira Kanai

Hiroyuki Yokota

Shinji Soga

Mitsuaki Okumura

Kiyohiro Samizu

Hideki Endoh

Nobuaki Amino

Tetsuya Kimizuka

Ryosuke Nakano

Hiroshi Uebayashi

Keisuke Maki

Yoshiyuki Kido

Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action.

Substituted pyrazine compounds

The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

Fused heteroaryl derivatives

A method for identifying a target protein of a compound having a pharmacological action by detecting a tertiary structural change of a target protein by binding a compound having a pharmacological action to a target protein with the use of a molecular chaperone protein having a characteristic of binding to a protein by recognizing a tertiary structural change of the protein is disclosed. Further, a method for screening a therapeutic agent for diabetes using a target protein of biguanide which is a therapeutic agent for diabetes and was found by the identification method, a screening tool which can be used in the screening method and a pharmaceutical composition for treating diabetes containing a substance obtained by the screening method are disclosed.

Method for identifying target protein of drug and method for screening therapeutic agent for diabetes using the target protein

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 present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

N-phenyl-(2R,5S)dimethylpiperazine derivative

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

N-phenyl-(2R,5S) dimethylpiperazine derivative

Provided is a compound having excellent dipeptidyl peptidase IV-inhibiting activity, and a remedy based on the activity for insulin-dependent diabetes (type 1 diabetes), especially for non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, and obesity.

2-cyano-4-fluoropyrrolidine derivative or its salt

There is provided an acid addition salt of (&#x2212;)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (&#x2212;)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (&#x2212;)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity that affects the use as a drug or its drug substance, and is very useful as a drug or its drug substance.

Salts of quinuclidine derivative

The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo&lsqb;1,2-a&rsqb;pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

Imidazopyridine derivatives

Growing community of inventors

Tsukuba, Japan

Masahiko Hayakawa