Claims
- 1. A compound of the structural formula ##STR58## in which R.sup.1 and R.sup.2, independently of one another, denote hydrogen or pharmaceutically acceptable groups which are bonded to the remaining part of the molecule via carbon-carbon single bonds and are selected from the group consisting of substituted or unsubstituted alkyl, alkenyl, alkinyl, cycloalkyl, alkylcycloalkyl, alkylcycloalkenyl, cycloalkylalkyl, alkenylcycloalkyl, cycloalkenylalkyl, aryl, aralkyl, aralkenyl, aralkinyl, carboxyl or cyano, where the foregoing alkyl, alkenyl or alkinyl molecule parts contain 1 to 6 carbon atoms, and the cycloalkyl or cycloalkenyl molecule parts contain 3 to 6 carbon atoms and the aryl molecule parts contain 6 to 10 carbon atoms, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkinyl or alkylheterocyclyl, where the foregoing alkyl, alkenyl or alkinyl molecule parts contain 1 to 6 carbon atoms and the heterocyclic molecule part is monocyclic or bicyclic and contains 3 to 10 ring atoms, of which one or more are selected from the group consisting of oxygen, sulphur and nitrogen, and where the substituents of the abovementioned groups may be protected or unprotected hydroxyl, hydroxyalkoxy, aminoalkoxy, amidinoalkoxy, alkoxy, acyloxy, aryloxy, heterocyclyloxy, carbamoyl, carbamoyloxy, thiocarbamoyl, thiocarbamoyloxy, alkylcarbamoyloxy, alkylthiocarbamoyloxy, mercapto, alkylthio, hydroxyalkylthio, aminoalkylthio, amidinoalkylthio, acylthio, arylthio, alkylheterocyclylthio, hydroxyalkylheterocyclylthio, heterocyclylthio, carbamoylthio, alkylcarbamoylthio, thiocarbamoylthio or alkylthiocarbamoylthio, protected or unprotected amino or monoalkylamino, dialkylamino, oxo, protected or unprotected oximino or alkylamino, cycloalkylamino, arylamino, heterocyclylamino, alkanoylamino, amidino, alkylamidino, guanidino, alkylguanidino, carbamoylamino, alkylcarbamoylamino, thiocarbamoylamino, alkylthiocarbamoylamino, nitro, chlorine, bromine, fluorine, iodine, azido, cyano, alkylsulphinyl, alkylsulphonyl, sulphonamido, sulphamoyloxy, alkylsulphonyloxy or protected or unprotected sulpho, sulphoxy or carboxyl, where the substituents, independently of one another, occur once or several times and their alkyl molecule part contains 1 to 6 carbon atoms and their aryl molecule part contains 6 to 10 carbon atoms, and where the heterocylic molecule part is monocyclic or bicyclic and contains 3 to 10 ring atoms, of which one or more are selected from the group consisting of oxygen, sulphur and nitrogen, and R.sup.3, R.sup.4 and R.sup.5, independently of one another, are selected from the abovementioned, pharmaceutically acceptable groups which are bonded to the remaining part of the molecule via carbon-carbon single bonds.
- 2. A compound according to claim 1, in which R.sup.1 and R.sup.2, independently of one another, denote hydrogen, alkyl, protected or unprotected hydroxyalkyl or protected or unprotected dihydroxyalkyl, each having 1 to 6 carbon atoms.
- 3. A compound according to claim 1, in which R.sup.3 and R.sup.4 denote methyl, and R.sup.5 is selected from the group consisting of CH.sub.3, ##STR59##
- 4. An antibacterial composition comprising an antibacterially effective amount of a compound according to claim 1 and a pharmaceutical excipient therefor.
- 5. An antibacterial composition according to claim 4 in unit dose form.
- 6. A compound according to claim 1, in which R.sup.2 is hydrogen, CR.sup.3 R.sup.4 R.sup.5 denotes a pharmaceutically acceptable optionally substituted t-butyl group, and R.sup.6 denotes hydrogen or a pharmaceutically acceptable ester or protecting group.
- 7. A compound according to claim 1, in which
- R.sup.1 and R.sup.2 each independently is hydrogen, or optionally hydroxy-substituted or optionally protected-hydroxy-substituted alkyl, alkenyl, alkinyl, cycloalkyl, alkylcycloalkyl, alkylcycloalkenyl, cycloalkylalkyl, alkenylcycloalkyl, cycloalkenylalkyl, aryl, aralkyl, aralkenyl, aralkinyl, carboxyl and cyano, the alkyl, alkenyl or alkinyl radicals having 1 to 6 carbon atoms, the cycloalkyl or cycloalkenyl radicals having 3 to 6 carbon atoms and the aryl radicals having 6 to 10 carbon atoms, and
- R.sup.3, R.sup.4 and R.sup.5 each, independently is a hydrocarbyl radical containing 1 to 10 carbon atoms or
- R.sup.5 additionally may be a radical selected from the group consisting of ##STR60## or a pharmaceutically acceptable salt, ester or amide thereof.
- 8. A compound according to claim 7, in which
- R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, or optionally protected monohydroxyalkyl or dihydroxyalkyl, the alkyl radicals having 1 to 6 carbon atoms.
- 9. A compound according to claim 7, in which --CR.sup.3 R.sup.4 R.sup.5 is t-butyl.
- 10. A compound according to claim 7, in which
- R.sup.3 and R.sup.4 are methyl, and
- R.sup.5 is selected from the group consisting of ##STR61##
- 11. A method of combating an infection in a patient in need thereof which comprises administering to such patient an antibacterially effective amount of a compound according to claim 1.
- 12. A compound according to claim 7, in which
- R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, or optionally protected monohydroxyalkyl or dihydroxyalkyl, the alkyl radicals having 1 to 6 carbon atoms, and
- --CR.sup.3 R.sup.4 R.sup.5 is t-butyl.
Priority Claims (1)
Number |
Date |
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Kind |
3725375 |
Jul 1987 |
DEX |
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Parent Case Info
This application is a continuation, of application Ser. No. 382,596, filed July 19, 1989, now abandoned. Which is a continuation of application Ser. No. 226,255, filed July 29, 1988 now abandoned.
Foreign Referenced Citations (4)
Number |
Date |
Country |
0018305 |
Oct 1980 |
EPX |
2747350 |
Apr 1978 |
DEX |
2808116 |
Sep 1978 |
DEX |
1591438 |
Dec 1978 |
GBX |
Non-Patent Literature Citations (5)
Entry |
Bentley JCS Chem. Comm. |
Cherry, JCS Chem. Comm. 1978, 469-470. |
Bentley J.C.S. Chem. Comm. 1977, 905. |
Cherry, J.C.S. Chem. Comm. 1978, 469-470. |
Current Antibicrobial Patents 1989, pp. 1067-1068. |
Continuations (2)
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Number |
Date |
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Parent |
382596 |
Jul 1989 |
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Parent |
226255 |
Jul 1988 |
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