US5268384A
Expired / Lapsed
US
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Inhibition of angiogenesis by synthetic matrix metalloprotease inhibitors
Assignee: Glycomed Inc
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Filing: 1992-01-07
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Granted: 1993-12-07
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Expires: 2012-01-07
Abstract
Abstract Synthetic mammalian matrix metalloprotease inhibitors are useful in controlling angiogenesis. These compounds are thus useful in controlling the growth of tumors and in controlling neovascular glaucomas.
Inventors
- 👤 Richard E. Galardy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 23:12
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/55; A61K31/00; A61K31/16; A61K31/165; A61K31/17; A61K31/185; A61K31/19; A61K31/195; A61K31/33; A61K31/395; A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/435; A61K31/44; A61K31/445; A61K31/4523; A61K31/454; A61K38/04; A61P; A61P9/00; C; C07; C07C; C07C259/00; C07C259/04; C07C259/06; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06139; C07K5/06156
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
63 words
A method to inhibit angiogenesis which method comprises contacting a tissue in which unwanted angiogenesis is occurring with an effective amount of a synthetic mammalian matrix metalloprotease inhibitor, wherein said inhibitor is selected from the group consisting of inhibitors of the formulae: ##STR14## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 2
Independent Claim
63 words
A method to inhibit angiogenesis which method comprises contacting a tissue in which unwanted angiogenesis is occurring with an effective amount of a synthetic mammalian matrix metalloprotease inhibitor, wherein said inhibitor is selected from the group consisting of inhibitors of the formulae: ##STR14## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 3
Dependent Claim
12 words
The method of claim 1 wherein the inhibitor is NHOHCOCH 2 CH(i-Bu)CO-L-Trp-NHMe.
Claim 4
Dependent Claim
61 words
A composition for inhibition of angiogenesis which composition comprises at least one synthetic mammalian matrix metalloprotease inhibitor in admixture with at least one pharmaceutically acceptable excipient, wherein said inhibitor is selected from the group consisting of inhibitors of the formulae: ##STR15## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 5
Dependent Claim
61 words
A composition for inhibition of angiogenesis which composition comprises at least one synthetic mammalian matrix metalloprotease inhibitor in admixture with at least one pharmaceutically acceptable excipient, wherein said inhibitor is selected from the group consisting of inhibitors of the formulae: ##STR15## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 6
Dependent Claim
12 words
The composition of claim 3 wherein the inhibitor is NHOHCOCH 2 CH(i-Bu)CO-L-Trp-NHMe.
Claim 7
Dependent Claim
33 words
The method of claim 1 wherein said inhibitor is of the formula: ##STR16## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 8
Dependent Claim
25 words
The method of claim 1 wherein said inhibitor is of the formula: ##STR17## and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 9
Dependent Claim
33 words
The composition of claim 3 wherein said inhibitor is of the formula: ##STR18## wherein R is H or lower alkyl (1-6C); and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 10
Dependent Claim
25 words
The composition of claim 3 wherein said inhibitor is of the formula: ##STR19## and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 11
Independent Claim
49 words
A method to inhibit angiogenesis which method comprises contacting a tissue in which unwanted angiogenesis is occurring with an effective amount of a synthetic mammalian matrix metalloprotease inhibitor, wherein the inhibitor is of the formula: ROCCH.sub.2 CH(i-Bu)CO-L-Trp-NHCHMePh and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 12
Independent Claim
49 words
A method to inhibit angiogenesis which method comprises contacting a tissue in which unwanted angiogenesis is occurring with an effective amount of a synthetic mammalian matrix metalloprotease inhibitor, wherein the inhibitor is of the formula: ROCCH.sub.2 CH(i-Bu)CO-L-Trp-NHCHMePh and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 13
Dependent Claim
12 words
The method of claim 9 wherein the inhibitor is NHOHCOCH 2 CH(i-Bu)CO-L-Trp-NHCHMePh.
Claim 14
Dependent Claim
12 words
The method of claim 9 wherein the inhibitor is HOOCCH 2 CH(i-Bu)CO-L-Trp-NHCHMePh.
Claim 15
Dependent Claim
47 words
A composition for inhibition of angiogenesis which composition comprises at least one synthetic mammalian matrix metalloprotease inhibitor in admixture with at least one pharmaceutically acceptable excipient, wherein said inhibitor is of the formula: ROCCH.sub.2 CH(i-Bu)CO-L-Trp-NHCHMePh and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 16
Dependent Claim
47 words
A composition for inhibition of angiogenesis which composition comprises at least one synthetic mammalian matrix metalloprotease inhibitor in admixture with at least one pharmaceutically acceptable excipient, wherein said inhibitor is of the formula: ROCCH.sub.2 CH(i-Bu)CO-L-Trp-NHCHMePh and wherein R 4 is (3-indolyl)methylene, and the pharmaceutically acceptable amides thereof.
Claim 17
Dependent Claim
12 words
The composition of claim 12 wherein the inhibitor is NHOHCOCH 2 CH(i-Bu)CO-L-Trp-NHCHMePh.
Claim 18
Dependent Claim
12 words
The method of claim 12 wherein the inhibitor is HOOCCH 2 CH(i-Bu)CO-L-Trp-NHCHMePh.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-12-06 | 1997-06-07 | 1997-12-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-12-06 | 2001-06-07 | 2001-12-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-12-06 | 2005-06-07 | 2005-12-07 | $7700.00 | Window Closed / Lapsed |