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    • 2. 发明授权
    • Bis-basic ketones of phenoxathiins and antiviral compositions thereof
    • 苯并噻唑类的双酚S基础组合物及其抗病毒组合物
    • US3808206A
    • 1974-04-30
    • US15812271
    • 1971-06-29
    • RICHARDSON MERRELL INC
    • FLEMING RDE WITT SILL A
    • A61K31/535C07D327/08A61K27/00C07D89/16
    • A61K31/535C07D327/08
    • WHEREIN X IS OXYGEN OR NR4, IS HYDROGEN OR LOWER ALKYL OF FROM 1 TO 4 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.

      BIS(Y-A-CO-)PHENOXATHIIN

      WHEREIN A IS A STRAIGHT OR BRANCHED ALKYLENE CHAIN HAVING FROM 1 TO 6 CARBON ATOMS; AND EACH Y IS SELECTED FROM (A) THE GROUP


      -N(-R1)-R2

      WHEREIN R1 AND R2 ARE INDIVIDUALLY SELECTED FROM HYDROGEN, LOWER ALKYL HAVING FROM 1 TO 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 I-POSITION OF THE ALKENYL GROUP; OR (B) THE GROUP

      -N
      WHEREIN N IS A WHOLE INTEGER OF FROM 4 TO 6 AND R3 IS SELECTED FROM HYDROGEN OR LOWER ALKYL OF FROM 1 TO 4 CARBON ATOMS AND CAN BE LINKED TO ANY ONE OF THE CARBON ATOMS OF THE HETEROCYCLIC GROUP; OR (C) THE GROUP
      -N BIS-BASIC KETONES OF PHENOXATHIINS HAVE ANTIVIRAL ACTIVITY WHEN ADMINISTERED ORALLY AND PARENTERALLY. THE COMPOUNDS ARE REPRESENTED BY THE FOLLOWING FORMULA:
    • 3. 发明授权
    • Bis-basic ketones of thioxanthene
    • BIS基础的三氯乙烯酮
    • US3856789A
    • 1974-12-24
    • US13705571
    • 1971-04-23
    • RICHARDSON MERRELL INC
    • FLEMING RSILL A
    • C07D335/12A61K27/00C07D87/34
    • C07D335/12
    • The novel bis-basic ketones of thioxanthene have antiviral activity when administered orally and parenterally. These compounds are represented by the following formula: WHEREIN A is a straight or branched alkylene chain having from 1 to about 6 carbon atoms; and each Y is A. the group WHEREIN R1 and R2 are individually hydrogen, allyl or lower alkyl having from 1 to about 4 carbon atoms; or B. the group WHEREIN N IS A WHOLE INTEGER OF 4 OR 5, AND R3 is hydrogen or lower alkyl having 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 X is oxygen or NR4, and R4 is hydrogen or lower alkyl of from 1 to about 4 carbon atoms; OR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS OF SAID BASE. These new compounds can be prepared by several different methods which are described.
    • 当口服和肠胃外给药时,噻吨酮的新型双碱性酮具有抗病毒活性。 这些化合物由下式表示:
    • 6. 发明授权
    • Bis-basic ethers and thioethers of dibenzothiophene
    • 二苯并噻吩的双酚A基和二苯醚
    • US3720680A
    • 1973-03-13
    • US3720680D
    • 1972-04-28
    • RICHARDSON MERRELL INC
    • ALBRECHT WFLEMING RHORGAN S
    • C07D333/76C07D63/24
    • C07D333/76
    • WHEREIN N IS A WHOLE INTEGER OF FROM 0 TO 2, N IS 1 OR 2, AND R2 IS HYDROGEN, (LOWER)ALKYL HAVING FROM 1 TO 6 CARBON ATOMS, OR ALKENYL OF FROM 3 TO 6 CARBON ATOMS AND HAVING THE VINYL UNSATURATION IN OTHER THAN THE 1-POSITION OF THE ALKENYL GROUP. THIS INVENTION ALSO INCLUDES PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS OF THE BASES REPRESENTED BY FORMULA 1. THESE NEW COMPOUNDS MAY BE PREPARED BY SEVERAL DIFFERENT METHODS WHICH ARE DESCRIBED.

      THE GROUP -(CH2)N-CH
      WHEREIN EACH A IS A STRAIGHT OR BRANCHED ALKYLENE CHAIN HAVING FROM 2 TO 8 CARBON ATOMS AND WHICH SEPARATES THE AMINO NITROGEN AND Y BY AT LEAST 2 CARBON ATOMS; R AND R1 ARE INDIVIDUALLY HYDROGEN, (LOWER)ALKYL HAVING FROM 1 TO 6 CARBON ATOMS, CYCLOALKY HAVING FROM 3 TO 6 CARBON ATOMS, ALKENYL HAVING FROM 3 TO 6 CARBON ATOMS AND HAVING THE VINYL UNSATURATION IN OTHER THAN THE 1-POSITION OF THE ALKENYL GROUP; OR EACH SET OF R AND R1 TAKEN TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED IS A SATURATED MONOCYCLIC HETEROCYCLIC GROUP SUCH AS PYRROLIDNO, PIPERIDINO, MORPHOLINO, OR N-(LOWER) ALKYLPIPERAZINO; OR

      THE GROUP -A-N(-R)-R1

      WHEREIN EACH Y IS OXYGEN OR DIVALENT SULFUR; AND EACH X IS

      (X-Y-)2-DIBENZOTHIOPHENE

      THE NOVEL BIS-BASIC ESTERS AND THIOETHERS OF DIBENZOTHIOPHENE OF THE PRESENT INVENTION HAVE ANTIVIRAL PROPERTIES. THESE COMPOUNDS ARE REPRESENTED BY THE FORMULA