Tricyclic benzodiazepine derivates, their preparation, and pharm

Details Tricyclic benzodiazepine derivates, their preparation, and pharm Tricyclic benzodiazepine derivates, their preparation, and pharm

1993-02-19

1994-06-21

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540497, A61K 3155, C07D48704

Patent

active

053228421

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to new tricyclic compounds and pharmaceutically acceptable salts thereof which are useful as a medicament.


BACKGROUND ART

Some tricyclic compounds have been known as described, for example, in EP 0360079Al.


DISCLOSURE OF INVENTION

This invention relates to new tricyclic compounds and pharmaceutically acceptable salts thereof.
More particularly, it relates to new tricyclic compounds and pharmaceutically acceptable salts thereof which are cholecystokinin (CCK) antagonists and therefore useful as therapeutical and/or preventive agents for emesis, pancreatitis, disorders of appetite regulatory systems, pain, insulinoma, gastroparesis, carcinoma of pancreas, gallbladder disease (e.g. acute cholecystitis, calculus, etc.), disorders associated with intestinal smooth muscle hyperactivity (e.g. irritable bowel syndrome, sphincter spasm, etc.), hyperinsulinemia, dyspepsia, nausea, etc.
The tricyclic compounds of this invention can be represented by the following formula (I): ##STR2## wherein R.sup.1 is hydrogen or an organic group,
According to the present invention, the new tricyclic compounds (I) can be prepared by the processes which are illustrated in the following scheme. ##STR3## wherein R.sup.1, R.sup.2 and A are each as defined above,
The starting compound (II) is novel and can be prepared by the following processes. ##STR4## wherein R.sup.1, R.sup.2, R.sup.4 and A are each as defined above,
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and include a metal salt such as an alkali metal salt (e.g. sodium salt, potassium salt, etc.) and an alkaline earth metal salt (e.g. calcium salt, magnesium salt, etc.), an ammonium salt, an organic base salt (e.g. trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.), an organic acid salt (e.g. acetate, maleate, tartrate, methanesulfonate, benzenesulfoante, formate, toluenesulfonate, trifluoroacetate, etc.), an inorganic acid salt (e.g. hydrochloride, hydrobromide, sulfate, phosphate, etc.), a salt with an amino acid (e.g. arginine, aspartic acid, glutamic acid, etc.), and the like.
In the above and subsequent descriptions of the present specification, suitable examples and illustrations of the various definitions which the present invention include within the scope thereof are explained in detail as follows.
The term "lower" is intended to mean 1 to 6 carbon atom(s), unless otherwise indicated.
The term "higher" is intended to mean 7 to 20 carbon atoms, unless otherwise indicated.
Suitable "organic group" may include lower alkyl (e.g., methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, neopentyl, tert-pentyl, hexyl, etc.),
lower alkenyl (e.g., vinyl, 1-propenyl, allyl, 1-methylallyl, 1 or 2 or 3-butenyl, 1 or 2 or 3 or 4-pentenyl, 1 or 2 or 3 or 4 or 5-hexenyl, etc.),
lower alkynyl (e.g., ethynyl, 1-propynyl, propargyl, 1-methylpropargyl, 1 or 2 or 3 butynyl, 1 or 2 or 3 or 4-pentynyl, 1 or 2 or 3 or 4 or 5-hexynyl, etc.),
aryl (e.g., phenyl, naphthyl, etc.),
ar(lower)alkyl such as phenyl(lower)alkyl (e.g., benzyl, phenethyl, phenylpropyl, etc.) and the like.
Suitable "aryl" may include phenyl, naphthyl and the like.
Suitable "substituent" in the term "aryl which may have suitable substituent(s)" may include halogen, amino, lower alkoxy, mono(or di or tri)halo(lower)alkyl and the like.
Suitable "halogen" and "halogen moiety" in the term "mono(or di or tri)halo(lower)alkyl" may include chlorine, bromine, fluorine and iodine.
Suitable "lower alkoxy" may include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, t-butoxy, pentyloxy, t-pentyloxy, hexyloxy and the like.
Suitable "lower alkyl" and "lower alkyl moiety" in the term "mono(or di or tri)halo(lower)alkyl" may include straight or branched one having 1 to 6 carbon atom(s), such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, t-pentyl, hexyl or the like, preferably one having 1 to

REFERENCES:
patent: 4929614 (1990-05-01), Calvet et al.
patent: 4981847 (1991-01-01), Sato et al.
patent: 5155101 (1992-10-01), Sato et al.

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