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AssigneeKyowa Hakko Kirin Co., Ltd.
InventorsTakayuki Furuta, Takashi Sawada, Tomohiro Danjo, Takahiro Nakajima, Noriaki Uesaka
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The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. [wherein, R1 represents optionally substituted lower alkyl and the like, R2 represents optionally substituted lower alkyl and the like, R3 represents the formula (II): (wherein, n represents 0 or 1, R3a represents a hydrogen atom and the like, R3b represents a hydrogen atom and the like, and R3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W1 represents a nitrogen atom and the like, W2 represents a nitrogen atom and the like].
A ring-fused heterocyclic compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof:
A method for treating pruritus, which comprises a step of administering an effective amount of the ring-fused heterocyclic compound selected from the group consisting of:
Dependencies are inferred from the claim text.
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In which the condensed system contains two hetero rings: ortho-condensed systems
Ortho- or peri-condensed with heterocyclic ring systems: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring…
Containing further heterocyclic ring systems: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
Containing further heterocyclic ring systems: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
About 6 years 9 months of term left · ends 31 Jul 2033 (estimated)
The present application claims priority to International Patent Application No. PCT/JP2013/070755 filed Jul. 31, 2013, which also claims priority to Japanese Patent Application No 2012-169480, filed Jul. 31, 2012, the entire contents of both applications are incorporated herein for all purposes by this reference.
The present invention relates to a novel ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory activity and useful as a therapeutic and/or preventive agent for pruritus, and the like, and a T-type calcium channel inhibitor and the like which comprise, as an active ingredient, the ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof.
Voltage-dependent calcium channels are ion channels that cause influx of calcium ions into cells under the potential difference between the interior and the exterior of a cell, and are known to have important biological functions, including neuronal excitation, synaptic transmission, muscle contraction, cardiac automaticity, secretion of neurotransmitters and hormones, cell proliferation and differentiation, and the like. Voltage-dependent calcium channels have been classified into any of the five categories T, L, P/Q, N, and R by their electrophysiological and pharmacological properties [Physiological Review, Vol. 83, p. 117 (2003)]. Among these five channels, only the T-type channels are activated by high membrane potentials, and are called low-voltage-activated channels. The other four channels are called high-voltage-activated (hereinafter, “HVA”) channels, because of their activation at low membrane potentials. As the name suggests, the T (transient)-type calcium channels are characterized by transient activation and quick inactivation. On the other hand, the HVA channels require a long time for inactivation.
Hereinafter, a compound represented by the general formula (I) is referred to as Compound (I). Compounds having the other formula numbers are referred to in the same manner.
In a definition of each group in the general formula (I),
examples of the lower alkyl and the lower alkyl moiety of the lower alkanoyl, the lower alkoxy, the lower alkylsulfonyl, and the mono-lower alkylamino include linear or branched alkyl having 1 to 10 carbon atoms, more specifically, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, heptyl, octyl, nonyl, decyl, and the like.