JPS5535012A - Compound of epoxysuccinylamino acid - Google Patents
Compound of epoxysuccinylamino acidInfo
- Publication number
- JPS5535012A JPS5535012A JP10776678A JP10776678A JPS5535012A JP S5535012 A JPS5535012 A JP S5535012A JP 10776678 A JP10776678 A JP 10776678A JP 10776678 A JP10776678 A JP 10776678A JP S5535012 A JPS5535012 A JP S5535012A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- acid
- proteinase
- alkylene
- activities
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Landscapes
- Epoxy Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
NEW MATERIAL:The title compound (trans-form) of formula I (A is single bond, C1-4 alkylene; B is C1-5 alkylene; R is C3-10 cycloalkyl, C5-8 cycloalkenyl; R<2> is H, OH, phenyl, indolyl, etc.; R<3> is C1-4 alkyl, benzyl, etc.). EXAMPLE:N-( DL-3-cyclopentanepropyloxycarbonyloxirane-2-carbonyl )-L-leucine ethyl ester. USE:Inhibitor which strongly inhibits the activities of proteinase, e.g. papaine, ficin, bromelin, etc. The thiol group is the one exhibiting the activities of proteinase. Extremely low toxic, and no acceleration of blood vessel penetration. PROCESS:For example, an epoxysuccinic acid monoester of formula II (R<5> is H, alkali metal) is converted to the acid chloride with a halogenating agent, e.g. oxalyl chloride. The acid chloride is then treated with an amino acid ester of formula III to give the objective compound of formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10776678A JPS5535012A (en) | 1978-09-02 | 1978-09-02 | Compound of epoxysuccinylamino acid |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10776678A JPS5535012A (en) | 1978-09-02 | 1978-09-02 | Compound of epoxysuccinylamino acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5535012A true JPS5535012A (en) | 1980-03-11 |
| JPS6155508B2 JPS6155508B2 (en) | 1986-11-28 |
Family
ID=14467449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10776678A Granted JPS5535012A (en) | 1978-09-02 | 1978-09-02 | Compound of epoxysuccinylamino acid |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5535012A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5185149A (en) * | 1987-03-27 | 1993-02-09 | Merck & Co., Inc. | Methods for thrombolytic therapy |
| US5545672A (en) * | 1993-02-11 | 1996-08-13 | The University Of Texas System | Treatment of insulin resistance and type 2 diabetes mellitus with a thiol protease inhibitor |
| WO1999011640A1 (en) * | 1997-09-04 | 1999-03-11 | Nippon Chemiphar Co., Ltd. | Epoxysuccinamide derivatives |
-
1978
- 1978-09-02 JP JP10776678A patent/JPS5535012A/en active Granted
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5185149A (en) * | 1987-03-27 | 1993-02-09 | Merck & Co., Inc. | Methods for thrombolytic therapy |
| US5545672A (en) * | 1993-02-11 | 1996-08-13 | The University Of Texas System | Treatment of insulin resistance and type 2 diabetes mellitus with a thiol protease inhibitor |
| WO1999011640A1 (en) * | 1997-09-04 | 1999-03-11 | Nippon Chemiphar Co., Ltd. | Epoxysuccinamide derivatives |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6155508B2 (en) | 1986-11-28 |
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