摘要:
ANTIVIRAL COMPOSITIONS AND METHODS FOR INHIBITING OR INACTIVATING VIRUSES BY SUBJECTING A HOST TO AN ANTIVIRALLY EFFECTIVE QUANTITY OF A FLUORENONE OF THE FOLLOWING FORMULA I OR ACID ADDITION SALT THEREOF.
BIS(R1-N(-R2)-A-Y-CO-)-FLUOREN-9-ONE
WHEREIN EACH Y IS OXYGEN OR SULFUR; EACH A IS ALKYLENE OF 2 TO ABOUT 8 CARBON ATOMS; AND EACH R1 AND R2 IS HYDROGEN, ALKYL OF 1 TO ABOUT 6 CARBON ATOMS, CYCLOALKYL OF 3 TO 6 CARBON ATOMS, ALKENYL OF 3 TO 6 CARBON ATOMS, OR EACH SET OF R1 AND R2 TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED CAN BE A SATURATED MONOCYCLIC HETEROCYCLIC GROUP. AN ILLUSTRATIVE FLUORENONE USED IN THE INVENTION IS BIS(3-DIBTYLAMINOPROPYL)-9-OXOFLUORENE-2,7DICARBOXYLATE DIHYDROCHLORIDE.
摘要:
D R A W I N G WHEREIN X is oxygen or NR4, and R4 is hydrogen or lower alkyl of from 1 to about 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof. These compounds can be prepared by several different methods.
WHEREIN N IS A WHOLE INTEGER FROM 4 TO 6, AND R3 is hydrogen, lower alkyl of from 1 to about 4 carbon atoms and can be linked to any one of the carbon atoms of the heterocyclic group; or C. the group
WHEREIN R1 and R2 are individually hydrogen, lower alkyl having from 1 to about 6 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, alkenyl of from 3 to 6 carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group; or B. the group
Novel bis-basic ketones of xanthene and xanthen-9-one have antiviral activity when administered orally and parenterally. The compounds are represented by the following formula:
WHEREIN Z is oxygen or H2; each A is a straight or branched alkylene chain having from 1 to about 6 carbon atoms; and each Y is A. the group
摘要:
Bis-basic ketones of phenoxathiins have antiviral activity when administered orally and parenterally. The compounds are represented by the following formula:
WHEREIN A is a straight or branched alkylene chain having from one to six carbon atoms; and each Y is selected from A. the group
WHEREIN R1 and R2 are individually selected from hydrogen, lower alkyl having from one to six carbon atoms, cycloalkyl having from three to six carbon atoms, alkenyl of from three to six carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group or B. the group
WHEREIN N IS A WHOLE INTEGER OF FROM FOUR TO SIX AND R3 is selected from hydrogen or lower alkyl of from one to four carbon atoms and can be linked to any one of the carbon atoms of the heterocyclic group; or C. the group
WHEREIN X is oxygen or NR4, and R4 is hydrogen or lower alkyl of from one to four carbon atoms; OR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. These compounds can be prepared by several different methods. Antiviral compositions and methods of inhibiting or inactivating viruses by administering to hosts an antivirally effective quantity of an active ingredient are disclosed herein.
摘要:
Novel bis-basic esters and amides of xanthene and xanthone of the formula
WHEREIN: Z is oxygen or H2; each of R1 and R2 is hydrogen, (lower)alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 ring carbon atoms, alkenyl of 3 to 6 carbon atoms having the vinyl unsaturation in other than the 1-position of the alkenyl group, or each set of R1 and R2 taken together with the nitrogen atom to which they are attached is pyrrolidino, piperidino, N(lower)alkylpiperazino, or morpholino; EACH A is alkylene of 2 to about 8 carbon atoms and separates its adjacent Y and amino nitrogen by an alkylene chain of at least 2 carbon atoms; and each Y is oxygen, or
OR A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT THEREOF. These compounds can be used as pharmaceuticals for preventing or inhibiting a viral infection.
摘要:
NOVEL COMPOUNDS SELECTED FROM A BASE OF THE FORMULA
9-(X=),BIS(R3-N(-R2)-A-N(-R1)-CO-)FLUORENE
WHEREIN: X IS 0; H2; OR H,OH; EACH R1 IS HYDROGEN OR LOWER ALKYL; EACH A IS ALKYLENE OF 2 TO ABOUT 8 CARBON ATOMS AND SEPARATES ITS ADJACENT NITROGEN ATOMS BY AN ALKYLENE CHAIN OF AT LEAST 2 CARBON ATOMS; AND EACH R2 AND R3 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL HAVING 3 TO ABOUT 6 RING CARBON ATOMS, ALKENYL OF 3 TO 6 CARBON ATOMS HAVING THE VINYL UNSATURATION IN OTHER THAN THE 1POSITON OF THE ALKENYL GROUP, OR EACH SET OF R2 AND R3 TAKEN TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED IS A SATURATED MONOCYCLIC HETEROCYCLIC GROUP HAVING 4 OR 5 RING CARBON ATOMS IN SAID HETEROCYCLIC GROUP; OR AN ACID ADDITION SALT OF SAID BASE. THE COMPOUNDS CAN BE USED AS ANTI-INFECTIVE OR ANTIMICROBIAL AGENTS, SUCH AS ANTIVIRAL, ANTIBACTERIAL AND ANTIFUNGAL AGENTS.
摘要:
Novel bis basic esters of 9-substituted phenanthrene and related 9-oxa and 9-aza derivatives thereof, their preparation and use for the prevention and inhibition of viral infections are disclosed.
摘要:
NOVEL FLUORENE AND FLUORENOL BIS-BASIC ESTER COMPOUNDS, THEIR METHOD OF PREPARATION AND USE AS ANTIVIRAL AGENTS. THE COMPOUNDS ARE OF THE FORMULA
9-X,BIS(R1-N(-R2)-A-OOC-)FLUORENE
WHEREIN: (A) EACH OF R1 AND R2 IS HYDROGEN, (LOWER) ALKYL, CYCLOALKYL OF 3 TO 6 RING CARGON ATOMS, ALKENYL OF 3 TO 6 CARBON ATOMS OR EACH SET OF R1 AND R2 AKEN TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED IS PYRROLIDINO, PIPERIDINO, N - (LOWER)ALKYLPIPERAZINO OR MORPHOLINO; (B) EACH A IS ALKYLENE OF 2 TO ABOUT 8 CARBON ATOMS AND SEPARATES ITS ADJACENT OXYGEN AND NITROGEN ATOMS BY AN ALKYLENE CHAIN OF AT LEAST 2 CARBON ATOMS; AND (C) X IS H OR OH; OR A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT THEREOF.