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US5010087A Expired / Lapsed US ⏱️ 0.0 years remaining

Tricyclic compounds and TXA2 antagonistic compositions thereof

Assignee: KH Neochem Co Ltd
•
Filing: 1989-07-18
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Granted: 1991-04-23
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Expires: 2009-07-18
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Abstract

Abstract Novel tricyclic compounds having a TXA 2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A 2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.

Inventors

  • 👤 Etsuo Oshima
  • 👤 Hiroyuki Obase
  • 👤 Akira Karasawa
  • 👤 Kazuhiro Kubo
  • 👤 Ichiro Miki
  • 👤 Akio Ishii

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 06:03
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/12; C07C; C07C311/00; C07C311/15; C07C311/16; C07C323/00; C07C323/23; C07C323/39; C07C323/43; C07C323/44; C07C323/46; C07C323/48; C07C323/49; C07D313/00; C07D313/02; C07D313/06; C07D313/10; C07D313/12; C07D337/00; C07D337/02; C07D337/06; C07D337/10; C07D337/12; C07D407/00; C07D407/02; C07D407/12; C07D409/00; C07D409/02; C07D409/12; C07D495/00; C07D495/02; C07D495/04; C07C2603/00; C07C2603/02; C07C2603/04; C07C2603/30; C07C2603/32

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 357 words
A tricyclic compound of the formula: ##STR144## wherein: X 1 --X 2 is selected from the group consisting of --CH 2 --O-- or ##STR145## (wherein l represents 0, 1, or 2); L is selected from the group consisting of --CH═CH-- or --S--; is a single or double bond; W is selected from the group consisting of --S--, --O--, --NH--, --CH 2 --, --NHCO-- or ═CH--, and the left side of each formula is bound to the tricyclic nucleus; n is 0,1,2, or 3; Z is selected from the group consisting of --NR 1 CO--, --NR 1 SO 2 --, --NR 1 CONH--, --NR 1 CSNH--, --NR 1 NHCONH--, --NR 1 NHCSNH--, --NR 1 COO-- or --NR 1 COS--, wherein R 1 is hydrogen or lower alkyl, and the right side of each formula is bound to Q; Q is selected from the group consisting of optionally substituted, N-substituted or unsubstituted pyrrolyl, (wherein the N-substituent is lower alkyl, phenyl or benzyl), pyridyl, quinolyl or isoquinolyl wherein substitution means 1 to 3 substituents on the aromatic ring, independently selected from lower alkyl, phenyl, benzyl, halogen, triflouromethyl, nitro, OR 2 or SR 2 , (wherein R 2 represents hydrogen, lower alkyl, phenyl or benzyl); one of R A and R B is hydrogen and the other is --Y--M-- wherein Y is selected from the group consisting of a single bond, --CR 3 R 4 --(CH 2 ) m -- and --CR 3 ═CR 4 --(CH 2 ) m )-- and each of R 3 and R 4 are independently hydrogen or lower alkyl and m is 0, 1, 2, 3, or 4, wherein the left side of each formula is bound to the tricyclic nucleus; M is --COOR 5 and R 5 is hydrogen, lower alkyl or --CONR 5a R 5b and each of R 5a and R 5b independently are hydrogen or lower alkyl; each of G A and G B are independently lower alkyl, halogen or OR 6 and R 6 represents hydrogen, lower alkyl, phenyl or benzyl; each of g A and g B are independently 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 357 words
A tricyclic compound of the formula: ##STR144## wherein: X 1 --X 2 is selected from the group consisting of --CH 2 --O-- or ##STR145## (wherein l represents 0, 1, or 2); L is selected from the group consisting of --CH═CH-- or --S--; is a single or double bond; W is selected from the group consisting of --S--, --O--, --NH--, --CH 2 --, --NHCO-- or ═CH--, and the left side of each formula is bound to the tricyclic nucleus; n is 0,1,2, or 3; Z is selected from the group consisting of --NR 1 CO--, --NR 1 SO 2 --, --NR 1 CONH--, --NR 1 CSNH--, --NR 1 NHCONH--, --NR 1 NHCSNH--, --NR 1 COO-- or --NR 1 COS--, wherein R 1 is hydrogen or lower alkyl, and the right side of each formula is bound to Q; Q is selected from the group consisting of optionally substituted, N-substituted or unsubstituted pyrrolyl, (wherein the N-substituent is lower alkyl, phenyl or benzyl), pyridyl, quinolyl or isoquinolyl wherein substitution means 1 to 3 substituents on the aromatic ring, independently selected from lower alkyl, phenyl, benzyl, halogen, triflouromethyl, nitro, OR 2 or SR 2 , (wherein R 2 represents hydrogen, lower alkyl, phenyl or benzyl); one of R A and R B is hydrogen and the other is --Y--M-- wherein Y is selected from the group consisting of a single bond, --CR 3 R 4 --(CH 2 ) m -- and --CR 3 ═CR 4 --(CH 2 ) m )-- and each of R 3 and R 4 are independently hydrogen or lower alkyl and m is 0, 1, 2, 3, or 4, wherein the left side of each formula is bound to the tricyclic nucleus; M is --COOR 5 and R 5 is hydrogen, lower alkyl or --CONR 5a R 5b and each of R 5a and R 5b independently are hydrogen or lower alkyl; each of G A and G B are independently lower alkyl, halogen or OR 6 and R 6 represents hydrogen, lower alkyl, phenyl or benzyl; each of g A and g B are independently 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 10 words
A compound according to claim 1, wherein L is --CH═CH--.
Claim 4
Dependent Claim 21 words
A compound according to claim 1, wherein one of R A and R B represents hydrogen and the other represents --Y--COOH.
Claim 5
Dependent Claim 20 words
A compound according to claim 3, wherein Y is a member selected from the group consisting of single bond, ##STR146##
Claim 6
Dependent Claim 12 words
A compound according to claim 1, wherein W is --S-- or ═CH--.
Claim 7
Dependent Claim 14 words
A compound according to claim 1, wherein Z is --NR 1 SO 2 --.
Claim 8
Dependent Claim 11 words
A compound according to claim 6, wherein R 1 is hydrogen.
Claim 9
Dependent Claim 21 words
A compound according to claim 1, wherein M is --COOH; W is --S or ═CH--; and Z is --NHSO 2 --.
Claim 10
Dependent Claim 16 words
A compound according to claim 8, wherein n is 1 or 2; and L is --CH═CH--.
Claim 11
Dependent Claim 24 words
A pharmaceutical composition comprising a pharmaceutical carrier and, as an active ingredient, a therapeutically effective amount of a tricyclic compound defined in claim 1.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1994-04-22 1994-10-22 1995-04-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1998-04-22 1998-10-22 1999-04-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2002-04-22 2002-10-22 2003-04-23 $7700.00 Window Closed / Lapsed

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