Daiichi Sankyo Company, Limited

Btg International Limited

Amgen Inc.

Narihiro Toda

Shinji Ashida

Mitsuhiro Iwamoto

Takeshi Masuda

Kensuke Nakamura

Hiroaki Uchida

Takashi Nakada

Ichiro Hayakawa

Daisuke Okajima

Kazuo Koyama

Keiko Suzuki

Koji Matsumoto

Masahiro Inoue

Yusuke Ota

Hirofumi Hamada

Tomoko Terauchi

Masaki Meguro

Fuminao Doi

Naoya Harada

Shinji Marumoto

Rieko Takano

Takahiro Katagiri

Takeshi Shida

Mami Yamazaki

Hiroshi Kogen

Takeshi Honda

Yasuyuki Ogawa

Masao Yoshida

Ming Yu

Zice Fu

Xiaolin Hao

Leping Li

Hui Tian

Sarah Lively

Zhaodan Cao

Mike Elias Lizarzaburu

Satoshi Shibuya

Yong-Jae Kim

Ryutaro Nakashima

Ryo Okuyama

Sarah E Lively

Mike Lizarzaburu

The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.

Methods of treating a tumor by administering a claudin-6 (CLDN6) or CLDN9 antibody-pyrrolobenzodiazepine derivative conjugate

Provided are novel antibody-pyrrolodiazepine derivative and novel antibody-pyrrolodiazepine derivative conjugates, as well as methods of using the same, and a novel CLDN6 and/or CLDN9 antibody. The disclosed compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics, and include substituted benzo[e]pyrrolo[1,2-α][1,4]diazepine.

Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines

A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].

Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-&#x3b1;][1,4]diazepines

Antibody-pyrrolobenzodiazepine derivative conjugate and method of use thereof for treating a tumor

To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; Rrepresents a hydrogen atom or a C1-C3 alkyl group; Rrepresents a hydrogen atom or a C1-C3 alkyl group; Rrepresents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; Rrepresents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, &#x2014;O&#x2014;, &#x2014;NH&#x2014;, &#x2014;N(C1-C3 alkyl)-, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;S(O)&#x2014;, or a single bond. 

Piperazinyl cyclohexane compounds as GPR38 agonists

Piperazinyl methyl phenyl cyclohexane compound

To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents &#x2550;C(R5)- or &#x2550;N&#x2014;; Y represents &#x2014;O&#x2014; or &#x2014;NH&#x2014;; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; Rrepresents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R, R, R, and Rmay be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group. In this connection, the alkyl group moieties of Rand Rmay be bonded to each other to form a 5- to 6-membered heterocyclic ring containing one oxygen atom. 

Carboxylic acid compound

Compounds having formula I: where A, A, L, V, W, R, R, R, Rand Rare as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.

N-aryl pyrazole compounds, compositions, and methods for their use

A compound of the formula (I): wherein Ris a C-Calkyl, an amino, a (C-Calkyl)amino, a di(C-Calkyl)amino or a nitrogen-containing saturated heterocyclic; Rand Rare the same or different and are a hydrogen or a C-Calkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C-Calkyl, halogeno C-Calkyl, C-Calkoxy, C-Calkylthio, C-Calkylenedioxy, C-Calkanoyl, C-Calkyloxycarbonyl, amino, C-Calkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propylene; Ris a hydrogen, a C-Calkyl or a C-Calkenyl; E is a single bond, an oxygen, a sulfur or &#x2014;NR&#x2014;, wherein Ris a hydrogen or a C-Calkanoyl; Xand Xare the same or different and are an oxygen or a sulfur, or a pharmacologically acceptable salt or ester thereof.

Benzylamine analogues

A compound of the formula (I): wherein Ris a C-Calkyl group, an amino group, a (C-Calkyl)amino group, a di(C-Calkyl)amino group or a nitrogen-containing saturated heterocyclic group; Ris a hydrogen atom or a C-Calkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, C-Calkyl, halogeno C-Calkyl, C-Calkoxy, C-Calkylthio, C-Calkylenedioxy, C-Calkanoyl, C-Calkyloxycarbonyl, amino, C-Calkanoylamino, hydroxyl, mercapto, cyano, nitro and carboxyl; A is a C-Calkylene group; Rtogether with Ris a C-Calkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: &#x2014;NR&#x2014;, wherein Ris a hydrogen atom or a C-Calkanoyl group; Xand Xare the same or different and are an oxygen atom or a sulfur atom, or a pharmacologically acceptable salt or ester thereof.

A compound of the formula (I): wherein Rrepresents C&#x2013;Calkyl, amino(C&#x2013;Calkyl)amino, di(C&#x2013;Calkyl)amino or a nitrogen-containing saturated heterocyclic; Rand Rare the same or different and represent hydrogen or C&#x2013;Calkyl; Rrepresents C&#x2013;Calkyl or C&#x2013;Calkenyl or together with Rrepresents a C&#x2013;Calkylene; Arom represents aryl or heteroaryl; A represents a C&#x2013;Calkylene; E represents a single bond, oxygen, sulfur or RNR&#x2014;, wherein Ris hydrogen or C&#x2013;Calkenoyl; Xand Xare the same or different and represent oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating or preventing Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.

Growing community of inventors

Tokyo, Japan

Narihiro Toda