Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limitjed

Tsuneo Yasuma

Nobuyuki Negoro

Takashi Sohda

Tsuneo Oda

Yukio Fujisawa

Shigehisa Taketomi

Haruhiko Makino

Toshiaki Nagata

Osamu Ujikawa

Masatoshi Hazama

Nobuyuki Takakura

Zenichi Ikeda

Shinobu Sasaki

Tohru Yamashita

Kazuhiro Maeda

Isao Aoki

Albert Charles Gyorkos

Masato Yoshida

Hiroyuki Kimura

Lei Zhu

Atsuo Baba

Christopher Peter Corrette

Yasufumi Miyamoto

Shuji Kitamura

Ikuo Fujimori

Hideki Hirose

Nozomu Sakai

Hiroshi Yamaguchi

Shuji Hinuma

Makoto Kamata

Masahiro Ito

Nobuhiro Suzuki

Yuya Oguro

Masataka Murakami

Atsuko Ochida

Yoshihide Tomata

Masakuni Kori

Masayuki Takizawa

Junji Mizoguchi

Ryo Mizojiri

Nobuyuki Matsunaga

Misaki Homma

Asato Kina

Akira Mori

Masahiro Itou

Masahiro Kawase

Takuya Fujimoto

Hideki Saito

Scott Alan Pratt

Masahiro Mizuno

Mitsuru Nonogawa

John Daniel Bailey

Yoshihiro Banno

Marianne Langston

Tomoya Yukawa

Masataka Harada

Naohiro Taya

Yoshito Terao

Masayuki Yamashita

Koichiro Fukuoka

Kazuko Yonemori

Yasuaki Ito

Minoru Ikoma

Sachie Morimoto

Masahiro Itoh

Kentaro Iwata

Kohji Fukatsu

Landon J Durak

Kyoko Toyofuku

Kei Masuda

Joshua David Waetzig

Hidehisa Iwata

Kentaro Hashimoto

Kazuko Aoki

Kazuyuki Akiyama

Shruti Gour

Siddhesh Dinanath Patil

Lilly Roy

The present disclosure relates to crystalline forms of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one hemihydrate (Compound 1) and/or tautomers thereof, wherein Compound 1 has the structure: (I)&#xb7;0.5HO; processes for preparing crystalline forms of Compound 1 and/or tautomers thereof; pharmaceutical compositions comprising the crystalline forms; methods of inhibiting a cell division cycle 7 in a mammal comprising administering the crystalline forms; and methods of treating a cell division cycle 7 mediated cancer in a mammal comprising administering the crystalline forms or a pharmaceutical composition comprising the crystalline forms.

Crystalline forms of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one hemihydrate

The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.

Process for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one

In this method, an oligonucleotide represented by formula (II) [wherein Y, Q, Base, r and r' are each as defined in claim] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R, Y, Base, Z, Ar, R, Rand n are each as defined in claim]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3&#x2032;-direction but also in the 5&#x2032;-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide. 

Method for liquid-phase synthesis of nucleic acid

In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R, Y, Base, Z, Ar, R, Rand n are each as defined in Claim]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method cars dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3'-direction but also in the 5&#x2032;-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide. 

There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; Xis CR, CRR, N or NR; Xis N or NR; Y is C, CRor N, Z is CR, CRR, N or NR; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; andis a single bond or a double bond; R, R, R, R, R, R, Rand Rare independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CRor N; R, R, R, Rand Rare independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X, R, R, Y and Xin formula (II) and (III) as before.

Substituted pyrazolo[1,5-A] pyrimidines as calcium receptor modulating agents

The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. 

Aromatic ring compound

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Bicyclic compound

The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.

Glucokinase activator compounds, methods of activating glucokinase and methods of treating diabetes and obesity

The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.

The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof. 

Fused ring compounds and use thereof

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Fused cyclic compounds

The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.

Fused ring compound and use thereof

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description,or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Glucokinase-activating fused heterocyclic compounds and methods of treating diabetes and obesity

Growing community of inventors

Osaka, Japan

Tsuneo Yasuma