Isoindoline derivatives

This application is a Continuation of application Ser. No. 10/534,414, which is the US National Stage application of PCT/JP2003/014986, filed Nov. 25, 2003, which claims priority from Japanese patent application 2002-342399, filed Nov. 26, 2002. The entire contents of each of the aforementioned applications are incorporated herein by reference.

The present invention relates to novel isoindoline derivatives. The derivatives of the invention are useful for manufacturing pharmaceutical compositions, especially anesthetics.

Many compounds having isoindoline structure have been reported to have effects on central nerves system. Most of those reports aimed for developing tranquilizers, antispasmodics or anxiolytics (Japanese Patent Application Laid Open Nos. 47-12322 and 58-189163). Heretofore, no isoindoline derivative having anesthetic property has been reported.

As for agents affecting on the CNS, especially intravenous anesthetics, rapid induction and recovery from anesthesia are desired. In order to prepare an injectable dosage form, the anesthetic compounds are also desired to be water-soluble. However, clinically used anesthetic compounds, for example propofol (2,6-diisopropylphenol), are slightly water-soluble and thus, the clinically used intravenous anesthetics are provided in the form of emulsion with soy-oil, glycerin and purified egg phospholipid. Due to the formulation, the clinical intravenous products have side effects such as venous pain during injection and lipid deposition as well as high susceptibility to microbial infection.

Heretofore, no CNS active agent that is enough soluble or miscible in water as well as induces no or little side effect has been reported.

One object of the present invention is to provide a water-soluble or water-miscible novel compound useful for manufacturing an anesthetic, especially intravenous anesthetic.

The present invention provides a compound represented by formula (I):

wherein R₁s are the same or different 1-3 groups, each of them is selected from the group consisting of C1-3 alkyl and C1-3 alkoxy, or when R₁s are two adjacent groups, the two R₁s taken together may form a saturated or unsaturated 5- or 6-membered cyclic group which may have 1 or 2 hetero atoms selected from the group consisting of sulfur, nitrogen and oxygen:

X is oxygen or sulfur:

R₂ is selected from the group consisting of phenyl, benzyl, pyridyl, pyridylmethyl, pyrimidinyl, cyclohexyl, methylpiperazinyl, indanyl and naphthyl, all of which may optionally be substituted; provided that when R₂ is phenyl, the 3- and 4-positions of the phenyl moiety are not substituted by alkoxy groups at the same time:

represents a single bond or double bond: and

L is

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Drug, bio-affecting and body treating compositions

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