US4327111A
Expired / Lapsed
US
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N-Substituted mercaptoacyl pripionamides
Assignee: ER Squibb and Sons LLC
•
Filing: 1980-07-14
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Granted: 1982-04-27
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Expires: 2000-07-14
Abstract
Abstract Mammalian collagenase is inhibited by compounds having the formula ##STR1## or a salt thereof, wherein R 1 is hydrogen, alkanoyl of 2 to 10 carbon atoms, or arylcarbonyl; ##STR2## wherein R 4 is hydrogen, alkyl or aryl; R 3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; and n is an integer of 1 to 20.
Inventors
- 👤 Joseph E. Sundeen
- 👤 Tamara Dejneka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 05:04
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/12; C07D295/125; C07D295/13; C07C; C07C51/00; C07C51/08; C07C51/09; C07C51/347; C07C51/367; C07C51/377
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
106 words
A compound having the formula ##STR40## or a salt thereof, wherein R 1 is hydrogen, alkanoyl, or arylcarbonyl; ##STR41## wherein R 4 is hydrogen, alkyl or aryl; R 3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; and n is an integer of 1 to 20; wherein the term "aryl" refers to phenyl or phenyl substituted; with 1, 2 or 3 alkyl, alkoxy, halogen, amino, hydroxy or alkanoyloxy groups; the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 10 carbon atoms.
Claim 2
Dependent Claim
106 words
A compound having the formula ##STR40## or a salt thereof, wherein R 1 is hydrogen, alkanoyl, or arylcarbonyl; ##STR41## wherein R 4 is hydrogen, alkyl or aryl; R 3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; and n is an integer of 1 to 20; wherein the term "aryl" refers to phenyl or phenyl substituted; with 1, 2 or 3 alkyl, alkoxy, halogen, amino, hydroxy or alkanoyloxy groups; the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 10 carbon atoms.
Claim 3
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is hydrogen.
Claim 4
Dependent Claim
18 words
A compound in accordance with claim 1 wherein R 1 is alkanoyl of 2 to 10 carbon atoms.
Claim 5
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is arylcarbonyl.
Claim 6
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is ##STR42##
Claim 7
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is ##STR43##
Claim 8
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is ##STR44##
Claim 9
Dependent Claim
12 words
A compound in accordance with claim 6 wherein R 4 is hydrogen.
Claim 10
Dependent Claim
12 words
A compound in accordance with claim 7 wherein R 4 is hydrogen.
Claim 11
Dependent Claim
14 words
A compound in accordance with claim 1 wherein n is 2, 3 or 4.
Claim 12
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 3 is 2-methylpropyl.
Claim 13
Dependent Claim
8 words
The compound in accordance with claim 1 N-(2,2-dimethoxyethyl)-2-[(acetylthio)methyl]-4-methylpentanamide.
Claim 14
Dependent Claim
8 words
The compound in accordance with claim 1 N-(2,2-dimethoxyethyl)-2-(mercaptomethyl)-4-methylpentanamide.
Claim 15
Dependent Claim
10 words
The compound in accordance with claim 1 2-[(acetylthio)methyl]-4-methyl-N-[4-[(aminoiminomethyl)amino]butyl]pentanamide, acetate (1:1).
Claim 16
Dependent Claim
10 words
The compound in accordance with claim 1 2-(mercaptomethyl)-4-methyl-N-[4-[(aminoiminomethyl)amino]butyl]pentanamide, acetate (1:1).
Claim 17
Independent Claim
133 words
A method for reducing the adverse effects of mammalian collagenase in a host mammal in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR45## or a salt thereof, wherein R 1 is hydrogen, alkanoyl, or arylcarbonyl; ##STR46## wherein R 4 is hydrogen, alkyl or aryl; R 3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; and n is an integer of 1 to 20; wherein the term "aryl" refers to phenyl or phenyl substituted; with 1, 2 or 3 alkyl, alkoxy, halogen, amino, hydroxy or alkanoyloxy groups; the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 10 carbon atoms.
Claim 18
Independent Claim
133 words
A method for reducing the adverse effects of mammalian collagenase in a host mammal in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR45## or a salt thereof, wherein R 1 is hydrogen, alkanoyl, or arylcarbonyl; ##STR46## wherein R 4 is hydrogen, alkyl or aryl; R 3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; and n is an integer of 1 to 20; wherein the term "aryl" refers to phenyl or phenyl substituted; with 1, 2 or 3 alkyl, alkoxy, halogen, amino, hydroxy or alkanoyloxy groups; the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 10 carbon atoms.
References Cited (Backward Citations)
US4105776A
Cited
EP0001989A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-04-26 | 1985-10-26 | 1986-04-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-04-26 | 1989-10-26 | 1990-04-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-04-26 | 1993-10-26 | 1994-04-27 | $7700.00 | Window Closed / Lapsed |