Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-06-12
2000-08-01
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540593, A61K 3155, C07D22316
Patent
active
060967366
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel benzazepine derivatives which have vasopressin antagonistic, vasopressin agonistic and oxytocin antagonistic activities and are useful as medicines.
BACKGROUND ART
Various benzazepine derivatives analogous to the compounds of the present invention have been known to have vasopressin antagonistic or oxytocin antagonistic activities. For example, it is described in U.S. Pat. No. 5,258,510 (=WO 91/05549), and WO 94/01113 that the benzazepine compounds of the following formula have vasopressin antagonistic and oxytocin antagonistic activities and further are useful as a medicament for the treatment of cataract. ##STR2## wherein R.sup.1 is H, halogen, lower alkyl, amino, alkylamino, etc., R.sup.2 is H, halogen, lower alkoxy, OH, etc., R.sup.3 is --NR.sup.4 R.sup.5 (R.sup.4 is H, alkyl, etc., R.sup.5 is substituted or unsubstituted benzoyl, phenylalkoxycarbonyl, alkanoyl, pyridyl-carbonyl, etc.) or --CONR.sup.11 R.sup.12, and W is --(CH.sub.2).sub.p -- (p is 3-5) or --CH.dbd.CH--(CH.sub.2).sub.q -- (q is 1-3) which may have 1-3 substituents selected from alkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyloxy, aminocarbonylalkoxy, sulfoxyimino, --O--A--CO--NR.sup.82 R.sup.83 (A being alkylene, R.sup.82, R.sup.83 being H, alkyl, hydroxyalkyl, pyridylalkyl, etc., or combine together with nitrogen atom to form heterocyclic groups), --(CO).sub.n --NR.sup.14 R.sup.15, etc. However, these known compounds are different from the compounds of the present invention in the kinds of the substituents at 1- and 5-positions, and further in that the compounds of the present invention have further vasopressin agonistic activity.
It is also described in U.S. Pat. No. 5,244,898 (=European Patent 0514667) that the benzazepine compounds of the following formula have vasopressin antagonistic activity. ##STR3## wherein R.sup.1 is H, halogen, OH, alkanoyloxy, amino-alkoxy, etc., R.sup.2 is H, alkyl, halogen, alkoxy, R.sup.3 is substituted benzoylamino, R.sup.4 is H, --NR.sup.6 R.sup.7 (R.sup.6, R.sup.7 being H, alkyl, etc.), alkenyloxy, --O--A--CO--NR.sup.8 R.sup.9 (A being alkylene, R.sup.8, R.sup.9 being H, alkyl, or combine together with nitrogen atom to form heterocyclic groups), --A--CONR.sup.11 R.sup.12 (A being alkylene, and R.sup.11, R.sup.12 being H, alkyl, piperidinyl having optionally phenylalkyl substituent, etc., or combine together with nitrogen atom to form heterocyclic groups), --O--A--CO--NR.sup.23 R.sup.24, etc., and R.sup.5 is H or OH. However, these known compounds are different from the compounds of the present invention in the kinds of the substituents at 1-position, and further in that the compounds of the present invention have further vasopressin agonistic activity.
WO 94/08582 discloses also that benzazepine compounds the same as or very close to those of the above U.S. Pat. No. 5,244,898 have vasopressin antagonistic and oxytocin antagonistic activities, but these known compounds are different from the compounds of the present invention in the kinds of the substituents at 1-position, and further in that the compounds of the present invention have further vasopressin agonistic activity.
It is further disclosed in JP-A-5-320135 that the benzazepine compounds of the following formula have vasopressin antagonistic activities. ##STR4## wherein R is formyl or .dbd.CR.sup.1 R.sup.2 (R.sup.1, R.sup.2 : one being H, another being alkoxy, alkoxycarbonyl, phenyl), and R.sup.3 is H or alkyl. However, these known compounds are different from the compounds of the present invention in the kinds of the substituents at 1- and 5-positions, and further in that the compounds of the present invention have further vasopressin agonistic activity.
It is further disclosed in WO 94/20473 that the benzazepine compounds of the following formula have vasopressin antagonistic activity. ##STR5## wherein L.sub.1 is alkylene, R.sup.1 is --COOH, --CONR.sup.6 R.sup.7 (R.sup.6, R.sup.7 being H, alkyl, pyridyl-substituted alkyl), or --CO--heterocyclic group. However, these known compounds
REFERENCES:
patent: 5244898 (1993-09-01), Ogawa et al.
patent: 5258510 (1993-11-01), Ogawa et al.
patent: 5622947 (1997-04-01), Ogawa et al.
CAS structure search results of WO 94/08582 and WO 95/34540, 1999.
Kan Keizo
Kondo Kazumi
Kurimura Muneaki
Mori Toyoki
Morita Seiji
Kifle Bruck
Otsuka Pharmaceutical Company Limited
Shah Mukund J.
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