Tetracyclic compound

Details Tetracyclic compound Tetracyclic compound

1995-05-22

1997-07-08

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D22118

Patent

active

056462832

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP94/01591 filed Sep. 28, 1994.


TECHNICAL FIELD

This invention relates to a novel tetracyclic compound which is useful as an immunosuppressive agent and as an agent for treating autoimmune disease.
1. Background Art
Japanese Laid-Open Patent Application No. Heisei 2-233661 discloses that a compound represented by formula (A) ##STR2## (wherein R.sup.1 represents CO.sub.2 H, or the like, each of R.sup.2 and R.sup.3 independently represents H, F, or the like, and each of R.sup.4 and R.sup.5 independently represents H or the like) is effective as a cancer chemotherapeutant. Furthermore, an usage of the compound as an immunosuppressive agent is disclosed in WO92/00739.
A compound represented by the formula ##STR3## (wherein p is an integer of 5 to 8) is disclosed, but its pharmacological activity is unknown [Liebigs Ann. Chem., 610, 57 (1957)].
2. Disclosure of the Invention
An object of this invention is to provide a novel tetracyclic compound which is useful as an immunosuppressive agent and as an agent for treating autoimmune disease.
This invention provides a novel tetracyclic compound represented by formula (I) [hereinafter referred to as "compound (I)", ##STR4## or its pharmacologically acceptable salt, (wherein X.sup.1 and X.sup.2 are the same or different and each represents hydrogen, a lower alkyl, halogen, nitro, hydroxy or a lower alkoxy, X.sup.3 and X.sup.4 are the same or different and each represents hydrogen or a lower alkyl, X.sup.5 and X.sup.7 are the same or different and each represents hydrogen, a lower alkyl, halogen, hydroxy or a lower alkoxy, X.sup.6 represents a substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, cycloakyl, bicycloalkyl or tricycloalkyl, and n is an integer of 1 to 4; substituted or unsubstituted aromatic heterocyclic group, cycloalkyl, bicycloalkyl or tricycloalkyl, or X.sup.6 represents an unsubstituted aryl, and at least one of X.sup.5 and X.sup.7 represents a substituent mentioned above other than hydrogen; formula (II), ##STR5## X.sup.5a represents a lower alkyl, halogen or a lower alkoxy, and X.sup.3, X.sup.4, X.sup.7 and n are the same as defined above.)
In the definition of each group of formula (I), a lower alkyl and an alkyl moiety of a lower alkoxy include straight or branched alkyl group having 1 to 6 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, neopentyl and hexyl. Examples of the halogen atom include fluorine, chlorine, bromine and iodine. Examples of cycloalkyl include cycloalkyl groups having from 3 to 8 carbon atoms such as cyclopropyl, cyclopentyl, cyclohexyl and cyclooctyl. Examples of bicycloalkyl include bicycloalkyl group having 6 to 12 carbon atoms such as bicyclohexyl, bicyclooctyl and bicylododecyl. Examples of tricycloalkyl include tricycloalkyl groups having from 8 to 12 carbon atoms such as tricyclooctyl, tricyclononyl, tricyclodecyl and tricyclododecyl. Examples of aryl include phenyl and naphthyl. Examples of the aromatic heterocyclic group include pyridyl, thienyl, furyl, pyrazolyl, oxazolyl and imidazolyl. Substituted aryl and the substituted aromatic heterocyclic ring have 1 to 3 of the same or different substituents such as lower alkyl, trifluoromethyl, halogen, nitro, hydroxy and a lower alkoxy. Lower alkyl, halogen and lower alkoxy are the same as defined above.
The pharmacologically-acceptable salt of compound (I) includes an acid-addition salt, a metal salt, an ammonium salt, an organic-amine-addition salt and an amino-acid addition salt.
Examples of the pharmacologically acceptable acid addition salt of compound (I) include salts of inorganic acids such as hydrochloric acid, sulfuric acid and phosphoric acid; salts of organic acids such as acetic acid, maleic acid, fumaric acid, tartaric acid and citric acid. Examples of the pharmacologically acceptable metal salts include alkali metal salts such as sodium salt and potassium salt, alkaline-earth metal salts such as magnesium salt and calcium salt,

REFERENCES:
patent: 4918077 (1990-04-01), Behrens
Huisgen et al., Liebigs Ann. Chem., No. 610 (Jun. 1957) 57-66.

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