US5354861A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-(benzyl)-3-arylbenzofurans as antitumour and hypocholesterolemic agents
Assignee: National University of Singapore
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Filing: 1992-11-04
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Granted: 1994-10-11
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Expires: 2012-11-04
Abstract
Abstract The synthesis and the biological evaluation of a series of basic ethers of 2-benzyl-3-arylbenzofurans as antitumor agents is described. These compounds bind significantly to the antiestrogen-binding sites but only poorly to the estrogen receptor sites and are cytotoxic to tumor cells. Some of these compounds also significantly inhibited de novo cholesterol biosynthesis in an estrogen receptor negative lymphoma cell line rich in antiestrogen-binding sites.
Inventors
- 👤 Keng-Yeow Sim
- 👤 Oi-Lian Kon
- 👤 Chin-Chin Teo
- 👤 Siu-Choon Ng
- 👤 Srikanth Natarajan
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 01:15
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/78; C07D307/79; C07D307/80
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
72 words
2-(Benzyl)-3-arylbenzo[b]furan in free base form and pharmaceutically acceptable acid-addition salts thereof, of formula (1 ##STR10## where R represents H, or methyl group, R 1 , R 2 are identical or different and represent C 1-2 alkyl or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group, and their pharmaceutically acceptable acid addition salts and X represents bromo, chloro, fluoro or hydrogen.
Claim 2
Dependent Claim
72 words
2-(Benzyl)-3-arylbenzo[b]furan in free base form and pharmaceutically acceptable acid-addition salts thereof, of formula (1 ##STR10## where R represents H, or methyl group, R 1 , R 2 are identical or different and represent C 1-2 alkyl or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group, and their pharmaceutically acceptable acid addition salts and X represents bromo, chloro, fluoro or hydrogen.
Claim 3
Dependent Claim
37 words
2-(Benzyl)-3-arylbenzo[b]furan according to claim 1, wherein said C 1-2 alkyl is independently methyl or ethyl, or R 1 and R 2 together with the nitrogen to which they are attached represent a pyrrolidino, piperidino or morpholino group.
Claim 4
Dependent Claim
1 words
2-(P-Chlorobenzyl)-3-[p-(2-dimethylaminoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 5
Dependent Claim
1 words
2-(P-Chlorobenzyl)-3-[p-(2-dimethylaminoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 6
Dependent Claim
4 words
2-(p-Chlorobenzyl )-3-[p-(2-pyrrolidinoethoxy)phenyl ]-6-methoxy-benzo [b]furan.
Claim 7
Dependent Claim
4 words
2-(p-Chlorobenzyl )-3-[p-(2-pyrrolidinoethoxy)phenyl ]-6-methoxy-benzo [b]furan.
Claim 8
Dependent Claim
1 words
2-(P-Chlorobenzyl)-3-[p-(2-piperidinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 9
Dependent Claim
1 words
2-(P-Chlorobenzyl)-3-[p-(2-piperidinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 10
Dependent Claim
1 words
2-(p-Chlorobenzyl)-3-[p-(2-morpholinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 11
Dependent Claim
1 words
2-(p-Chlorobenzyl)-3-[p-(2-morpholinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 12
Dependent Claim
3 words
2-(p-Fluorobenzyl )-3-[p-( 2-dimethylaminoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 13
Dependent Claim
3 words
2-(p-Fluorobenzyl )-3-[p-( 2-dimethylaminoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 14
Dependent Claim
13 words
2 - ( p-Fluorobenzyl ) - 3 - [p- ( 2 -pyrrolidinoethoxy)phenyl]-6-methoxy-benzo [b]furan.
Claim 15
Dependent Claim
13 words
2 - ( p-Fluorobenzyl ) - 3 - [p- ( 2 -pyrrolidinoethoxy)phenyl]-6-methoxy-benzo [b]furan.
Claim 16
Dependent Claim
1 words
2-(p-Fluorobenzyl)-3-[p-(2-piperidinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 17
Dependent Claim
1 words
2-(p-Fluorobenzyl)-3-[p-(2-piperidinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 18
Dependent Claim
1 words
2-(p-Fluorobenzyl)-3-[p-(2-morpholinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
Claim 19
Dependent Claim
1 words
2-(p-Fluorobenzyl)-3-[p-(2-morpholinoethoxy)phenyl]-6-methoxy-benzo[b]furan.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-10-10 | 1998-04-11 | 1998-10-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-10-10 | 2002-04-11 | 2002-10-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-10-10 | 2006-04-11 | 2006-10-11 | $7700.00 | Window Closed / Lapsed |