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| Metal chelators |
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| YIGSR peptide radiopharmaceutical applications |
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| Peptide-chelator conjugates |
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5,6,7,8 Tetrahydroquinoline derivatives
| Details |
Inventors: Curran, Adrian Charles Ward;
Assignee: John Wyeth & Brother Limited (Maidenhead, EN)
Primary Examiner: Rizzo; Nicholas S.
Assistant Examiner: Wheeler; David E.
Attorney, Agent or Firm:
The invention provides a compound of formula I ##SPC1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are the same or different and represent hydrogen, or a lower alkyl radical, R.sup.5 represents hydrogen or single or multiple substitution by lower alkyl radicals, X is cyano, CONHR.sup.3, CSNHR.sup.3 or CO.sub.2 R.sup.3 wherein R.sup.3 is hydrogen or a lower alkyl radical, m is 1, 2 or 3 and R.sup.6 is hydrogen, a lower alkyl radical or a lower alkanoyl radical or an alkali-metal salt of a compound in which X is CO.sub.2 H. Compounds of formula I wherein X is CN or CSNHR.sup.3 and R.sup.6 is lower alkyl are anti-ulcer agents. The other compounds of formula I are intermediates. |
|
DETAILED DESCRIPTION I claim: 1.
A compound of the formula ##SPC15## and the non-toxic acid addition salts thereof wherein R.
sup.
1 is hydrogen or alkyl of from 1 to 6 carbon atoms, R.
sup.
2 is hydrogen, alkyl of from 1 to 6 carbon atoms or carboxylic acyl of from 1 to 6 carbon atoms, X is CN, CONHR.
sup.
3, CSNHR.
sup.
3, or CO.
sub.
2 R.
sup.
3 wherein R.
sup.
3 is hydrogen or alkyl of from 1 to 6 carbon atoms, or an alkali metal salt of a compound in which X is COOH.
2.
A compound as claimed in claim 1 wherein X is CSNH.
sub.
2 or CSNHCH.
sub.
3 3.
A compound as claimed in claim 1, which is 5-methoxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-thiocarboxamide.
4.
A compound as claimed in claim 1, which is 8-acetoxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-carboxamide.
5.
A compound as claimed in claim 1, which is 8-hydroxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-carboxamide.
6.
A compound as claimed in claim 1, which is 8-methoxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-(N-methyl)carboxamide or a pharmaceutically acceptable acid addition salt thereof.
7.
A compound as claimed in claim 1, which is 8-methoxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-(N-methyl)thiocarboxamide .
8.
A compound as claimed in claim 1, which is 8-acetoxy-8-cyano-3-methyl-5,6,7,8-tetrahydroquinoline or a pharmaceutically acceptable acid addition salt thereof.
9.
A compound as claimed in claim 1 which is 8-acetoxy-3-methyl-5,6,7,8-tetrahydroquinoline-8-thiocarboxamide.
Description:
The invention relates to novel pyridine derivatives and to process for preparing them.
The invention provides a compound of formula I ##SPC2## or an acid addition salt thereof, wherein R.
sup.
1, R.
sup.
2 and R.
sup.
4 are the same or different and represent hydrogen, or a lower alkyl radical, R.
sup.
5 represents hydrogen or single or multiple substitution by lower alkyl radicals, X is cyano, CONHR.
sup.
3, CSNHR.
sup.
3 or CO.
sub.
2 R.
sup.
3 wherein R.
sup.
3 is hydrogen or a lower alkyl radical, m is 1, 2 or 3 and R.
sup.
6 is hydrogen, a lower alkyl radical or a lower alkanoyl radical, or an alkali-metal salt of a compound in which X is CO
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