Chugai Seiyaku Kabushiki Kaisha

Nissan Chemical Industries Limited

Chugai Seikayu Kabushiki Kaisha

Takuya Shiraishi

Hitoshi Yoshino

Atsushi Matsuo

Tsutomu Sato

Satoshi Tsuchiya

Masahiro Nishimoto

Haruhiko Sato

Hirotaka Kashiwagi

Yoshikazu Nishimura

Nobuyuki Hori

Masahide Aoki

Yoshiyuki Furuta

Satoshi Tanida

Hiroko Ogawa

Takuma Kamon

Shoshin Yoshida

Kyoko Oguri

Takahiro Kawai

Masateru Ohta

Takashi Emura

Kazutaka Tachibana

Mitsuaki Nakamura

Hiromitsu Kawata

Tatsuya Kato

Kaori Kimura

Atsushi Ohta

Shojiro Kadono

Tetsuo Kojima

Hitoshi Iikura

Koji Takano

Yusuke Yamagishi

Mikimasa Tanada

Naoaki Murao

Ryuichi Takeyama

Kazuhiko Nakano

Kousuke Asou

Takuya Torizawa

Ryusuke Takano

Nozomi Hisada

Shiori Kariyuki

Takeo Iida

Miki Kojima

Ikuhiro Imaoka

Masahiro Nagamuta

Yoshiaki Watanabe

Kazuhiko Ohrai

Masahiro Sakaitani

Yoshiyuki Suzuki

Takanori Shimizu

Keishi Hayashi

Nobuya Ishii

Masataka Minami

Masami Hasegawa

Michiaki Adachi

Etsuro Onuma

Koji Toyama

Kenji Taniguchi

Masayuki Haramura

Toshiro Kozono

Akihisa Sakamoto

Akie Honma

Takaki Koga

Masakazu Sugiyama

The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

Pyrazolopyridine derivative having GLP-1 receptor agonist effect

An object of the present invention is to provide methods of discovering drugs effective for tough targets, which have conventionally been discovered only with difficulty. The present invention relates to novel methods for cyclizing peptide compounds, and novel peptide compounds and libraries comprising the same, to achieve the above object.

Peptide-compound cyclization method

The present invention provides the compound, 3-[(1S,2S)-1-[5-[(4S)-2,2-Dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one, or a pharmaceutically acceptable salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound.

An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted Calkyl group; E is independently selected from a Calkyl group; Rand Rare independently selected from Calkyls; Xand Xare independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is &#x2014;CON(&#x2014;Ra)&#x2014;, &#x2014;CO&#x2014;, &#x2014;OOO&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;NH)NRb&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;N&#x2014;CN)NRb&#x2014;, &#x2014;N(&#x2014;Ra)COO&#x2014;, &#x2014;C(&#x2550;NH)&#x2014;, &#x2014;SO&#x2014;, &#x2014;SON(&#x2014;Ra)&#x2014;, &#x2014;SONR&#x2014;, &#x2014;N(&#x2014;Ra)CO&#x2014;, &#x2014;N(&#x2014;Ra)CON(&#x2014;Rb)&#x2014;, &#x2014;N(COR)CO&#x2014;, &#x2014;N(&#x2014;Ra)SO&#x2014;, &#x2014;N(SOR)SO&#x2014;, &#x2014;N(&#x2014;Ra)&#x2014; or &#x2014;N(&#x2014;Ra)SON(&#x2014;Rb)&#x2014;; Ris independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from Calkyl group, heterocyclic group, aryl group, Ccycloalkyl group and Ccycloalkenyl group; or salt or prodrug thereof.

Imidazolidine derivative and use thereof

The present invention provides novel &#x3b1;-amino acid derivatives of formula (1): (wherein, R, R, R, R, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have &#x3b2;ARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.

&#x3b1;-amino acid derivatives and medicaments containing the same as an active ingredient

The present invention provides a compound represented by formula (I):  A is cyano or the like; B is hydrogen, halogen, or the like; Xand Xare each independently selected from O and S; E is a Calkyl group; and R, R, Rand Rare each independently selected from a hydrogen atom and a C-Calkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.

Imidazolidine derivatives

The present invention provides a compound represented by formula (I): [Formula 1] wherein n is an integer selected from 1 to 20, and Rand R, which may be the same or different, each represent a hydrogen atom, or a linear or branched C-Calkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical composition containing the compound, and the like.

A compound of Formula (1):&#x2003;wherein A crystal of a complex between factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor. A medium carrying a part or all of structure coordinate data of a complex between human factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor, obtainable by X-ray crystal structure analysis of the crystal. A method for computationally designing a low-molecular weight reversible factor VIIa inhibitor using the coordinate data.

Peptide derivatives

Growing community of inventors

Gotenba, Japan

Takuya Shiraishi