Claims
- 1. A compound of the formula ##STR196## or salts thereof wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;
- R.sub.1 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl;
- R.sub.2 is hydrogen;
- R.sub.3 is ##STR197## R.sub.4 is hydrogen, lower alkyl or arylalkyl; R.sub.7 and R.sub.8 are each independently selected as hydrogen, lower alkyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --;
- m is an integer from 0 to 7; p is an integer from 1 to 3;
- AA.sub.n is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3;
- when p is 1, AA.sub.n is AA.sub.1 ;
- when p is 2, AA.sub.n is AA.sub.1 -AA.sub.2 ;
- when p is 3, AA.sub.n is AA.sub.1 -AA.sub.2 -AA.sub.3 ;
- AA.sub.1 is glycine or alanine;
- AA.sub.2 is glycine or alanine;
- AA.sub.3 is leucine, glutamine or isoleucine, and physiologically acceptable salts thereof.
- 2. A compound of claim 1 wherein R is hydrogen, R.sub.3 is ##STR198## and m is 0 to 3.
- 3. A compound of claim 2 wherein n is 3.
- 4. The compound having the name (.+-.)-N-�2-(dimethylamino)ethyl!-N.sup.2 -�2-(mercaptomethyl)-4-methyl-1-oxopentyl!glycinamide, barbituric acid (1:1) salt.
- 5. The compound of claim 1 having the name (.+-.)-N-�4-�(aminoiminomethyl)amino!butyl!-N.sup.2 -�2-(mercaptomethyl)-4-methyl-1-oxopentyl!glycinamide, acetate (1:1) salt.
- 6. The compound having the name (.+-.)-4-����-2-(mercaptomethyl)-4-methyl-1-oxopentyl!amino!acetyl!amino!butanoic acid.
- 7. A pharmaceutical composition for reducing the adverse effects of mammalian collagenase which comprises a compound as defined in claim 1 and a pharmaceutically acceptable carrier therefor.
- 8. 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 as defined in claim 1.
- 9. A method for treating rheumatoid arthritis in a mammalian host, which comprises administering an effective amount of a compound as defined in claim 1.
Parent Case Info
This is a division of application Ser. No. 273,142, filed June 12, 1981, now U.S. Pat. No. 4,382,081.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4235885 |
Sundeen et al. |
Nov 1980 |
|
4382081 |
Sundeen et al. |
May 1983 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
1989 |
Jun 1979 |
EPX |
Non-Patent Literature Citations (1)
Entry |
"Structure-Inhibition Relationships Among Metal-Binding Collagen Peptide Analogues" Hussain Saneii and Arno F. Spatola (Spon: John W. Brown) University of Louisville, Ky., 40292, May 1, 1981, vol. 40, No. 6. |
Divisions (1)
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Number |
Date |
Country |
Parent |
273142 |
Jun 1981 |
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