Sumitomo Pharma Co., Ltd.

Sumitomo Dainippon Pharma Co., Ltd.

Boston Biomedical, Inc.

Sumitomo Pharma Oncology, Inc.

Sumitomo Dainippon Pharma Oncology, Inc.

Seiji Kamioka

Hitoshi Ban

Naoaki Shimada

Wataru Hirose

Yusuke Sawayama

Chiang Jia Li

Akihiko Arakawa

Kazuto Yamazaki

Kenjiro Hira

Miki Hashizume

Hiroki Umehara

Kento Hayashi

Makoto Matsuoka

Hiroyuki Kitano

Tomoyuki Furuta

Akihiko Yokoyama

Shoukou Ri

The present disclosure provides a compound that exerts an anticancer action based on CHK1 inhibition. The present disclosure was completed by finding that a compound represented by formula (1) or a pharmaceutically acceptable salt thereof exhibits an excellent antitumor action by having a potent inhibitory action against CHK1: wherein R, R, L, V, W, and Q are as defined herein, X, Y, and Z each independently represent CRor a nitrogen atom, wherein X, Y, and Z are not simultaneously CR, and Ris as defined herein.

5-heteroaryl-1H-pyrazol-3-amine derivative

The present invention relates to the compound of formula (I) wherein R, R, R, and Rare hydrogen atom, etc., Rand Rare hydrogen atom, etc., R, R, R, and Rare hydrogen atom, etc., L is bond, etc., V is Calkylene, Q is optionally-substituted imidazole, or a pharmaceutically acceptable salt thereof, as a novel anti-tumor agent that targets CSCs which are thought to be closely involved in the persistent proliferation of malignant tumor, metastasis or recurrence of cancer, and resistance to anti-tumor agents.

Dihydrochromene derivatives

The compound of formula (1a) wherein p is 1 or 2, R-Rare hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

Optically active azabicyclo ring derivative

The present invention relates to the compound of formula (I) wherein R, R, R, and Rare hydrogen atom, etc., Rand Rare hydrogen atom, etc., R, R, R, and Rare hydrogen atom, etc., L is bond, etc., V is Calkylene, Q is optionally-substituted imidazole, or a pharmaceutically acceptable salt thereof, as a novel anti-tumor agent that targets CSCs which are thought to be closely involved in the persistent proliferation of malignant tumor, metastasis or recurrence of cancer, and resistance to anti-tumor agents. 

A process for producing a hydrate of a hydrochloride salt of 2,2'-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid of the formula: wherein the process comprises the following step:

Process for producing a hydrate of a hydrochloride salt of 2,2'-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid

The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R-Rare hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin. 

The present invention relates to the compound of formula (I) wherein p is 1 or 2, Ris &#x2014;CFor the like, R, R, R, and Rare hydrogen atom or the like, X is &#x2014;C(&#x2550;O)&#x2014;or the like, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin. 

Optically active crosslinked cyclic secondary amine derivative

This invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. Specifically, the present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof [Therein, A is O, S, or N&#x2014;R; ring G is a 5-membered or 6-membered aromatic ring, etc., including 1-3 heteroatoms selected from O, S and N as constituent atoms; Rand Rare each independently a hydrogen atom, a halogen atom, or an optionally-substituted Calkyl carbonyl group, etc.; R, Rand Rare each independently a hydrogen atom, a halogen atom, or an optionally-substituted Calkyl carbonyl group, etc.; and Ris a hydrogen atom or an optionally-substituted Calkyl group, etc.]. 

Tricyclic quinone derivative

The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein Aand Aare identical or different, and each independently &#x2014;C(&#x2550;O)B, &#x2014;C(&#x2550;O)CRRB, &#x2014;COB, &#x2014;C(&#x2550;S)OB, &#x2014;CONRB, &#x2014;C(&#x2550;S)NRB, a hydrogen atom, or the like, wherein Aand Aare not both hydrogen atoms, wherein B is an optionally substituted 3- to 12-membered monocyclic or polycyclic heterocyclic group, an optionally substituted 3- to 12-membered cyclic amino group, or a group represented by the following formula (B), wherein the 3- to 12-membered monocyclic or polycyclic heterocyclic group and the 3- to 12-membered cyclic amino group have at least one or more secondary nitrogen atoms in the ring; Ris a hydrogen atom or the like; R, R, R, and Rare identical or different, and each independently a hydrogen atom or the like; and Ris alkyl. wherein * denotes a bonding position.

Substituted naphtho[2,3-b]furans as water-soluble prodrugs for preventing and/or treating cancer

The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein Aand Aare identical or different, and each independently &#x2014;C(&#x2550;O) B, &#x2014;C(&#x2550;O)CRRB, &#x2014;COB, &#x2014;C(&#x2550;S)OB, &#x2014;CONRB, &#x2014;C(&#x2550;S)NRB, a hydrogen atom, or the like, wherein Aand Aare not both hydrogen atoms, wherein B is an optionally substituted 3- to 12-membered monocyclic or polycyclic heterocyclic group, an optionally substituted 3- to 12-membered cyclic amino group, or a group represented by the following formula (B), wherein the 3- to 12-membered monocyclic or polycyclic heterocyclic group and the 3- to 12-membered cyclic amino group have at least one or more secondary nitrogen atoms in the ring; Ris a hydrogen atom or the like; R, R, R, and Rare identical or different, and each independently a hydrogen atom or the like; and Ris alkyl. wherein * denotes a bonding position.

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Osaka, Japan

Seiji Kamioka