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US4512990A Expired / Lapsed US ⏱️ 0.0 years remaining

Benzthiazine analogs as antiinflammatory agents

Assignee: Syntex USA LLC
•
Filing: 1982-02-18
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Granted: 1985-04-23
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Expires: 2002-02-18
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Abstract

Abstract Compounds of the formula: <IMAGE> and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S; Y is halo, alkoxy, alkyl, or dialkylamino; a is 0, 1 or 2; b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is -NH2, b cannot be 2-5; and X is selected from the group consisting of: -OH, OR1, -NH2, -NHR1, NR1/2, <IMAGE> and -NHCONHR2 in which each R1 is independently alkyl or cycloalkyl or, in -NR1/2, both R1s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or -CH2CH2OH; and R2 is alkyl, cycloalkyl, or optionally substituted phenyl; have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.

Inventors

  • 👤 Peter H. Nelson
  • 👤 Howard J. Ringold
  • 👤 Stefan H. Unger
  • 👤 Thomas R. Thieme

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 13:25
CPC Classifications
C; C07; C07D; C07D279/00; C07D279/10; C07D279/14; C07D279/16; C07D215/00; C07D215/02; C07D215/04; C07D215/06; C07D215/08

Claims Analysis

Total Claims: 2
Claim 1
Independent Claim 198 words
A method for inhibiting, preventing, or reducing inflammation which method comprises administering to a subject in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR11## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S; Y is halo, alkoxy, alkyl, or dialkylamino; a is 0, 1 or 2; b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH or NH 2 , b cannot be 2-5; and X is selected from the group consisting of: --OH, OR 1 , --NH 2 , --NHR 1 , NR 2 1 , ##STR12## and --NHCONHR 2 in which each R 1 is independently alkyl or cycloalkyl or, in --NR 2 1 , both R 1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH 2 CH 2 OH; and R 2 is alkyl, cycloalkyl, or phenyl optionally substituted with 1-3 substituents selected from the group consisting of halo, lower alkyl of 1-4 carbon atoms, lower alkoxy of 1-4 carbon atoms, hydroxy, and trifluoromethyl.
Claim 2
Independent Claim 198 words
A method for inhibiting, preventing, or reducing inflammation which method comprises administering to a subject in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR11## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S; Y is halo, alkoxy, alkyl, or dialkylamino; a is 0, 1 or 2; b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH or NH 2 , b cannot be 2-5; and X is selected from the group consisting of: --OH, OR 1 , --NH 2 , --NHR 1 , NR 2 1 , ##STR12## and --NHCONHR 2 in which each R 1 is independently alkyl or cycloalkyl or, in --NR 2 1 , both R 1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH 2 CH 2 OH; and R 2 is alkyl, cycloalkyl, or phenyl optionally substituted with 1-3 substituents selected from the group consisting of halo, lower alkyl of 1-4 carbon atoms, lower alkoxy of 1-4 carbon atoms, hydroxy, and trifluoromethyl.

References Cited (Backward Citations)

US2374181A Cited
US3117124A Cited
US3817995A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-04-22 1988-10-22 1989-04-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-04-22 1992-10-22 1993-04-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-04-22 1996-10-22 1997-04-23 $7700.00 Window Closed / Lapsed

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