Physiologically active substance P-23924, its production and use

Abstract

The compound of the formula: ##STR1## wherein R 1 is hydrogen, methyl or hydroxymethyl, R 2 is hydrogen or methoxy, R 3 is hydroxy or methoxy, and R 4 is hydrogen or a group ##STR2## is novel, and the compound is of use as inhibitors of animal tissue fibrosis, or biochemical reagents.

What we claim is: .[.1. A compound represented by the formula: ##STR16## wherein R 1  is hydrogen, methyl or hydroxymethyl, R 2  is hydrogen or methoxy, R 3  is hydroxy or methoxy and R 4  is hydrogen or a group ##STR17## 
     
        .]. .[.2.  A compound as claimed in claim 1, wherein R 4  is a group ##STR18## 
     
     
        .]. .[.3.  A compound as claimed in claim 1, wherein R 4  is hydrogen..]. .[.4. A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is hydrogen, R 3  is methoxy and R 4  is a group ##STR19## 
     
     
        .]. .[.5.  A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is methoxy, R 3  is methoxy and R 4  is a group ##STR20## 
     
     
        .]. .[.6.  A compound as claimed in claim 1, wherein R 1  is hydrogen, R 2  is methoxy, R 3  is methoxy and R 4  is a group ##STR21## 
     
     
        .]. .[.7.  A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is methoxy, R 3  is hydroxy and R 4  is a group ##STR22## 
     
     
        .]. .[.8.  A compound as claimed in claim 1, wherein R 1  is hydroxymethyl, R 2  is hydrogen R 3  is methoxy and R 4  is a group ##STR23## 
     
     
        .]. .[.9.  A compound as claimed in claim 1, wherein R 1  is hydroxymethyl, R 2  is methoxy, R 3  is methoxy and R 4  is a group ##STR24## 
     
     
        .]. .[.10.  A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is hydrogen, R 3  is methoxy and R 4  is hydrogen..]. .[.11. A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is methoxy, R 3  is methoxy and R 4  is hydrogen..]. .[.12. A compound as claimed in claim 1, wherein R 1  is hydrogen, R 2  is methoxy, R 3  is methoxy and R 4  is hydrogen..]. .[.13. A compound as claimed in claim 1, wherein R 1  is methyl, R 2  is methoxy, R 3  is hydroxy and R 4  is hydrogen..]. .[.14. An antifibrotic preparation comprising an effective amount of at least one compound of claim 1 and a 
     
     
        pharmaceutically acceptable carrier, excipient or diluent..]. .Iadd.15.  A compound represented by the formula: ##STR25## wherein R 1  is hydrogen, methyl or hydroxymethyl, R 2  is hydrogen or methoxy, R 3  is hydroxy or methoxy and R 4  is a group ##STR26## 
     
     
        .Iaddend. .Iadd.16.  A compound as claimed in claim 15, wherein R 1  is methyl, R 2  is hydrogen and R 3  is methoxy. .Iaddend. .Iadd.17. A compound as claimed in claim 15, wherein R 1   is methyl, R 2  is methoxy and R 3  is methoxy. .Iaddend. .Iadd.18. A compound as claimed in claim 15, wherein R 1  is hydrogen, R 2  is methoxy and R 3  is methoxy. .Iaddend. .Iadd.19. A compound as claimed in claim 15, wherein R 1  is methyl, R 2  is methoxy and R 3  is hydroxy. .Iaddend. .Iadd.20. A compound as claimed in claim 15, wherein R 1  is hydroxymethyl, R 2  is hydrogen and R 3  is methoxy. .Iaddend. .Iadd.21. A compound as claimed in claim 15, wherein R 1  is hydroxymethyl, R 2  is methoxy and R 3  is methoxy. .Iaddend. .Iadd.22. A compound represented by the formula: ##STR27## 
     
     
        .Iaddend. .Iadd.23.  A compound represented by the formula: ##STR28## 
     
     
        .Iaddend. .Iadd.24.  A compound represented by the formula: ##STR29## 
     
     
        .Iaddend. .Iadd.25.  A compound represented by the formula: ##STR30## 
     
     
        .Iaddend. .Iadd.26.  An antifibrotic preparation comprising an effective amount of at least one compound of any one of claims 15 or 22-25, and a pharmaceutically acceptable carrier, excipient or diluent. .Iaddend.