Sertindole prodrugs, compositions and use

Details Sertindole prodrugs, compositions and use Sertindole prodrugs, compositions and use

1993-03-30

1995-06-27

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514323, 544130, 546201, A61K 31445, A61K 31535, C07D40114, C07D41314

Patent

active

054280362

ABSTRACT:
Reaction products of sertindole with an acid or an activated acid, with formaldehyde alone, formaldehyde in the presence of an alcohol or an amine, or with an acyloxymethylene halide, and having general formula (1) wherein X is CO, CS, or CH.sub.2, and if X is CO or CS, R is (i) hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl or cycloalk(en)ylalk(en)yl optionally substituted with hydroxy, or optionally substituted phenyl; or (ii) YR.sup.1, wherein Y is O or S and R.sup.1 is one of the substituents defined for R under (i) above; or (iii) NR.sup.2 R.sup.3, wherein R.sup.2 and R.sup.3 independently are selected from the substituents defined for R under (i) above or R.sup.2 and R.sup.3 are combined to form a heterocyclic ring; or if X is CH.sub.2, R is: (iv) a group YR.sup.1 as defined in (ii); (v) a group NR.sup.2 R.sup.3 as defined in (iii); or (vi) a group OC(O)R.sup.4, wherein R.sup.4 is as defined for R.sup.1 ; are prodrugs of sertindole and show sustained release of sertindole when injected as formulated in a suitable oil. The compounds are useful in the treatment of mental disorders such as schizophrenia including both negative and positive symptoms, non-schizophrenic psychoses, depression and anxiety.

REFERENCES:
patent: 3408356 (1968-10-01), Horovitz
patent: 3996211 (1976-12-01), Lassen
patent: 4038305 (1977-07-01), Eliasson et al.
patent: 4710500 (1987-12-01), Perregaard
H. Bundgaard, "Design of Prodrugs", Elsevier (1985), Chapter 4, pp. 157-176.
J. Hyttel et al. Pharmacology and Toxicology, 61:126-129, 1987.

Affiliated with

Also associated with

Rating

Sertindole prodrugs, compositions and use does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Sertindole prodrugs, compositions and use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Sertindole prodrugs, compositions and use will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-287727