Astellas Pharma Gmbh

Ludwig Institute for Cancer Research Limited

Yamanouchi Pharmaceutical Company Ltd.

Imperial Cancer Research Technology, Ltd.

Other

Kotobuki Pharmaceutical Co Ltd

Hiroyuki Moritomo

Minoru Okada

Masahiko Hayakawa

Mitsuaki Ohta

Hiroyuki Kaizawa

Koyo Matsuda

Mayumi Yamano

Ken-Ichi Kawaguchi

Tomonobu Koizumi

Fukushi Hirayama

Yuji Koga

Kenichi Onda

Jun Takasaki

Takao Okuda

Susumu Watanuki

Daisuke Kaga

Masaaki Hirano

Takashi Kamikubo

Eiji Kawaminami

Yasuhiro Yonetoku

Akira Toyoshima

Kazuhiko Iikubo

Shimpei Kawakami

Makoto Takeuchi

Koji Kato

Daisuke Yamashita

Hiroshi Nagata

Shigeru Yoshida

Norio Seki

Masanori Miura

Kenji Negoro

Ryota Shiraki

Takashi Sugane

Issei Tsukamoto

Ippei Sato

Sadao Kuromitsu

Shunichiro Hachiya

Norio Asai

Jiro Fujiyasu

Takahiro Nigawara

Ryutaro Wakayama

Takahiko Tobe

Shinya Nagashima

Yoshimasa Imamura

Yoh Terada

Daisuke Sasuga

Toshiyuki Kusayama

Eiichi Nakai

Naomi Hosogai

Masaki Yokota

Takahide Ohishi

Michihito Kageyama

Kazuhiro Terai

Toshio Uemura

Makoto Ohmiya

Keiko Ohga

Yumiko Moritani

Takayuki Suzuki

Atsushi Suzuki

Takashi Futami

Tomoyuki Suzuki

Atsushi Noda

Yuki Sawada

Noriyuki Kawano

Hiroshi Tomiyama

Kazuhiro Yokoyama

Tatsuya Maruyama

Keizo Sugasawa

Akira Matsuhisa

Wataru Hamaguchi

Takafumi Shimizu

Minoru Sakurai

Masakazu Imamura

Tetsuo Matsui

Kyoichi Maeno

Naoki Ishibashi

Hiroyuki Hisamichi

Isao Kinoyama

Keita Nakanishi

Nobuyuki Shiraishi

Yasuharu Urano

Yoshinori Iwai

Ikumi Kuriwaki

Nobuaki Taniguchi

Takuya Makino

Masahiro Iwata

Kenichiro Imamura

Hisashi Mihara

Daisuke Tanabe

Makoto Asaumi

Kazuhisa Tsunoyama

Ayako Moritomo

Ryuichi Sekioka

Kazuo Tokuzaki

Kozo Miyasaka

Minoru Kameda

Tetsuya Kimizuka

Yoji Miyazaki

[Problem] To provide a compound useful as an MCreceptor agonist. [Means for Solution] The present inventors studied MCreceptor agonists, and have found that a piperazine derivative has an MCreceptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MCreceptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

Piperazine derivative

To provide a compound which can be used as an MCreceptor agonist. The present inventors have investigated MCreceptor agonists, and have found that a piperazine derivative has an action related to the agonists, thereby completing the present invention. That is, the piperazine derivative of the present invention has an MCreceptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.

Heterocyclic acetamide compound

Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

Nitrogen-containing aromatic heterocyclic compound

The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: 

Tetrahydrobenzothiophene compound

To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11&#x3b2;-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11&#x3b2;-HSD1. Accordingly, the bicyclic heterocyclic compound of the present invention can be used for treating dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance, and the like.

Bicyclic heterocyclic compound

[Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.

Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.

Quinolone derivative or pharmaceutically acceptable salt thereof

As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.

Quinolone derivative

Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.

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 compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

Diaminopyrimidinecarboxamide derivative

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

A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

Quinolone derivative or salt thereof

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Tokyo, Japan

Hiroyuki Moritomo