Sumitomo Dainippon Pharma Co., Ltd.

Sumitomo Pharma Co., Ltd.

Boston Biomedical, Inc.

Sumitomo Pharma Oncology, Inc.

Sumitomo Dainippon Pharma Oncology, Inc.

Yusuke Sawayama

Hitoshi Ban

Seiji Kamioka

Chiang Jia Li

Miki Hashizume

Adam Siddiqui-Jain

Wataru Hirose

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 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

Compounds having the following structure (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R, Rand Rare as defined herein, and wherein at least one of R, Rand Ris not H, are provided. Pharmaceutical compositions comprising the compounds and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided. 

Alvocidib prodrugs and their use as protein kinase inhibitors

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

Yusuke Sawayama