Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, 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.

Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, 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.

Abstract: 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: recrystallizing the 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, in the presence of hydrochloric acid and a recrystallization solvent; wherein the recrystallization solvent is methanol, ethanol, 2-propanol, diethyl ether, ethyl acetate, benzene, toluene, acetone, dichloromethane, chloroform, hexane, dimethylformamide, acetonitrile, or water; or mixed solvent thereof.

Abstract: Compounds having the following structure (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined herein, and wherein at least one of R1, R2 and R3 is 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.

Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, 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.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O)B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are 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; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, 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.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O)B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are 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; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, 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.

Abstract: The present invention addresses the problem of providing a novel chemically activated water-soluble prodrug. The present invention provides a compound represented by formula (1), or a pharmacologically acceptable salt thereof (in the formula, A represents A-0; X1 and X2 are the same as or different from each other and each independently represent a hydroxyl group or —O—C(?O)—Y—(C(R1A) (R1B))n-NH—R2, where X1 and X2 are not simultaneously hydroxyl groups, n is 2, 3, or 4, Y represents an oxygen atom or —NR4, R1A and R1B are the same as or different from each other and each independently represent a hydrogen atom, etc., and R2 represents a hydrogen atom, etc.; and Ra to Rd are optionally present, are the same as or different from each other, and each independently represent a hydrogen atom, etc.).

Abstract: Compounds having the following structure (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined herein, and wherein at least one of R1, R2 and R3 is 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.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O)B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are 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; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O) B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are 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; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O) B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are 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; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: Provided is a therapeutic agent for diseases associated with a cholinergic property of the central nervous system (CNS) and/or the peripheral nervous system (PNS), diseases associated with the contraction of smooth muscle, incretion disease, diseases associated with neuronal degeneration and the like, said therapeutic agent comprising a compound represented by Formula (I): [wherein X—Y—Z represents N—CO—NR4AR4B or the like; R1 represents a phenyl group or the like; R2A and R2B may be the same as or different from each other and independently represent a hydrogen atom or the like; R3A to R3D and R6 may be the same as or different from one another and independently represent a hydrogen atom or the like; R4A and R4B may be the same as or different from each other and independently represent an aryl group or the like; and n represents 1 or 2] or a pharmaceutically acceptable salt thereof and having a potent activity of regulating an ?7 nicotinic acetylcholine receptor (an ?7 nAChR).