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US 8,026,232 B2Granted
Benzothiophene oxide derivative and salt thereof
AssigneeToyama Chemical Co., Ltd.
InventorsTetsuro Nakamura, Hiroshi Kato
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AssigneeToyama Chemical Co., Ltd.
InventorsTetsuro Nakamura, Hiroshi Kato
Estimating the term…
Disclosed is a benzothiophene oxide derivative represented by the general formula (wherein R1 and R2 are the same or different and each represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n are the same or different and each represents an integer of 1-6) or a salt thereof, which is useful as a prodrug of a benzothiophene derivative or a salt thereof.
A benzothiophene oxide derivative represented by the following general formula or a salt thereof:
1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol S-oxide or a salt thereof.
Dependencies are inferred from the claim text.
From the US filing history. Foreign family members aren’t listed.
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
Drugs for disorders of the nervous system
Drugs for disorders of the nervous system: for peripheral neuropathies
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00
About 2 years 7 months of term left · ends 26 May 2029 (estimated)
This application is a 371 of PCT/JP09/59576 filed May 26, 2009 and claims the benefit of JP 2008-139007 filed May 28, 2008.
The present invention relates to a benzothiophene oxide derivative or a salt thereof which is useful as a prodrug of a therapeutic agent for central and peripheral nerve diseases.
In the study of a therapeutic agent, many drugs have been found by a method using an in vitro model. However, some drugs have a low bioavailability and have limited therapeutic usefulness. In order to avoid these problems, there have been known means of chemically modifying a compound to form a prodrug.
FIG. 1 is a graph showing the concentration of a compound A in the plasma after administering a compound A maleate and a compound A oxide maleate; and
FIG. 2 is a graph showing the concentration of a compound A in the brain after administering a compound A maleate and a compound A oxide maleate.
The present invention will be described in detail below.
In this description, unless otherwise specified, each term has the following meaning.
The term “a compound A” means “1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol”.
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