Patent US5010087A successfully refreshed from Google Patents.
US5010087A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Tricyclic compounds and TXA2 antagonistic compositions thereof
Assignee: KH Neochem Co Ltd
•
Filing: 1989-07-18
•
Granted: 1991-04-23
•
Expires: 2009-07-18
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 14:14
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.
References Cited (Backward Citations)
US3420851A
Cited
US3354155A
Cited
GB1167263A
Cited
US3905972A
Cited
US4585788A
Cited
US4282365A
Cited
US4465835A
Cited
US4396550A
Cited
JPS57139073A
Cited
EP0085870A1
Cited
JPS59227879A
Cited
US4596804A
Cited
US4749703A
Cited
JPS61152673A
Cited
JPS61152675A
Cited
JPS61152674A
Cited
EP0188802A2
Cited
JPS61152676A
Cited
JPS61257981A
Cited
EP0214779A1
Cited
JPS62153280A
Cited
WO1987005014A1
Cited
EP0235796A2
Cited
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 |