US4235885A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Inhibitors of mammalian collagenase
Assignee: ER Squibb and Sons LLC
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Filing: 1979-06-25
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Granted: 1980-11-25
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Expires: 1999-06-25
Abstract
Abstract Mammalian collagenase is inhibited by compounds having the formula ##STR1## and salts thereof, wherein R 1 is hydrogen or alkanoyl of 2 to 10 carbon atoms; R 2 is hydroxy, amino, or ##STR2## R 3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR3## R 4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; and m is 0 or an integer of 1 to 9.
Inventors
- 👤 Joseph E. Sundeen
- 👤 Tamara Dejneka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 00:13
CPC Classifications
C; C07; C07C; C07C51/00; C07C51/347; C07C51/377; A; A61; A61P; A61P43/00; C07C323/00; C07C327/00; C07C51/08; C07C51/367; C07C51/58; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; A61K; A61K38/00
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
91 words
A method for reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR29## or a salt thereof wherein R 1 is hydrogen or alkanoyl of 2 to 10 carbon atoms; R 2 is hydroxy, amino or ##STR30## R 3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR31## R 4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; and m is 0 or an integer of 1 to 9.
Claim 2
Independent Claim
91 words
A method for reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR29## or a salt thereof wherein R 1 is hydrogen or alkanoyl of 2 to 10 carbon atoms; R 2 is hydroxy, amino or ##STR30## R 3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR31## R 4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; and m is 0 or an integer of 1 to 9.
Claim 3
Dependent Claim
14 words
A method in accordance with claim 1 wherein the mammalian host has rheumatoid arthritis.
Claim 4
Dependent Claim
12 words
A method in accordance with claim 1 wherein R 1 is hydrogen.
Claim 5
Dependent Claim
18 words
A method in accordance with claim 1 wherein R 1 is alkanoyl of 2 to 10 carbon atoms.
Claim 6
Dependent Claim
12 words
A method in accordance with claim 3 wherein R 2 is hydroxy.
Claim 7
Dependent Claim
12 words
A method in accordance with claim 3 wherein R 2 is amino.
Claim 8
Dependent Claim
12 words
A method in accordance with claim 3 wherein R 2 is ##STR32##
Claim 9
Dependent Claim
11 words
A method in accordance with claim 7 wherein m is 0.
Claim 10
Dependent Claim
16 words
A method in accordance with claim 7 wherein m is an integer of 1 to 9.
Claim 11
Dependent Claim
12 words
A method in accordance with claim 7 wherein R 3 is hydrogen.
Claim 12
Dependent Claim
18 words
A method in accordance with claim 7 wherein R 3 is alkyl of 1 to 4 carbon atoms.
Claim 13
Dependent Claim
12 words
A method in accordance with claim 7 wherein R 3 is ##STR33##
Claim 14
Dependent Claim
12 words
A method in accordance with claim 7 wherein R 3 is ##STR34##
Claim 15
Dependent Claim
12 words
A method in accordance with claim 3 wherein R 4 is hydroxy.
Claim 16
Dependent Claim
12 words
A method in accordance with claim 3 wherein R 4 is amino.
Claim 17
Dependent Claim
17 words
A method in accordance with claim 3 wherein R 4 is arginine, leucine, glutamine, alanine or glycine.
Claim 18
Dependent Claim
16 words
A method in accordance with claim 3 wherein the compound administered is 2-(mercaptomethyl)-4-methylpentanoic acid, ammonium salt.
Claim 19
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is 2-(mercaptomethyl)-4-methylpentanamide.
Claim 20
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[2-(mercaptomethyl)-4-methyl-1-oxopentyl]glycine.
Claim 21
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[6-[2-[(acetylthio)methyl]-4-methyl-1-oxopentyl]-1-oxohexyl]-L-arginine.
Claim 22
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[6-[[2-(mercaptomethyl)]-4-methyl-1-oxopentyl]amino-1-oxohexyl]-L-arginine.
Claim 23
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is 6-[[2-[(acetylthio)methyl]-4-methyl-1-oxopentyl]amino]hexanamide.
Claim 24
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[N-[2-(mercaptomethyl)-4-methyl-1-oxopentyl]glycyl]-L-arginine.
Claim 25
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[5-[[2-(mercaptomethyl)-4-methyl-1-oxopentyl]amino]-1-oxopentyl]-L-arginine.
Claim 26
Dependent Claim
13 words
A method in accordance with claim 3 wherein the compound administered is N-[8-[[2-(mercaptomethyl)-4-methyl-1-oxopentyl]amino]-1-oxooctyl]-L-arginine.
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) | 1983-11-25 | 1984-05-26 | 1984-11-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-11-25 | 1988-05-26 | 1988-11-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-11-25 | 1992-05-26 | 1992-11-25 | $7700.00 | Window Closed / Lapsed |