Claims
- 1. An N-acylamino acid derivative of the following formula or its pharmaceutically acceptable salt: ##STR146## where m is an integer of 0 to 2;
- n is an integer of 0 to 3;
- R.sup.1 represents a hydroxy-substituted or unsubstituted C.sub.1-5 alkyl group, C.sub.3-6 cycloalkyl group, C.sub.4-8 cycloalkylalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group,
- R.sup.2 represents a C.sub.1-15 alkyl group, tetrahydronaphthylmethyl group, naphthylmethyl group, quinolylmethyl group, or a benzyl group which may be substituted with a C.sub.1-5 alkyl group;
- R.sup.3 and R.sup.5 represent hydrogen,
- R.sup.4 represents a C.sub.1-5 alkyl group which may be substituted with an imidazolyl group or a C.sub.4-8 cycloalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group;
- R.sup.6 represents a C.sub.1-5 alkyl group, C.sub.4-8 cycloalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group;
- A is a group represented by the formula --CH(OH--)--(CH.sub.2).sub.q --R.sup.7 wherein q is 0, 1 or 2; and R.sup.7 represents a morpholino group which is unsubstituted or substituted with a C.sub.1-5 alkyl substituent.
- 2. An N-acylamino acid derivative of the following formula or its pharmaceutically acceptable salt: ##STR147## wherein m is an integer of 0 to 2;
- n is an integer of 0 to 3;
- R.sup.1 represents a hydroxy-substituted or unsubstituted C.sub.1-5 alkyl group, C.sub.3-6 cycloalkyl group, C.sub.4-8 cycloalkylalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group,
- R.sup.2 represents a quinolylmethyl group;
- R.sup.3 and R.sup.5 represent hydrogen,
- R.sup.4 represents a C.sub.1-5 alkyl group which may be substituted with a hydroxy group, carboxy group, amino group, C.sub.2-5 alkylcarbonyloxy group, C.sub.1-5 alkylthio group or imidazolyl group or a C.sub.4-8 cycloalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group;
- R.sup.6 represents a C.sub.1-5 alkyl group, C.sub.4-8 cycloalkylalkyl group, C.sub.6-10 aryl group or C.sub.7-15 aralkyl group;
- A is a group represented by the formula --CH(OH--)--(CH.sub.2).sub.q --R.sup.7 wherein q is 0, 1 or 2; and R.sup.7 represents a morpholino group which is unsubstituted or substituted with a C.sub.1-5 alkyl substituent.
- 3. A compound selected from the group consisting of: (2S,3R,4S)-4-{L-N.sup..alpha. -[(2S)-3-ethylsulfonyl-2-(1-naphthylmethyl)propionyl]histidyl}amino-5-cyclohexyl-1-morpholino-2,3-pentanediol and (2S,3R,4S)-4-{L-N-[(2S)-3-tert-butylsulfonyl-2-(1-naphthylmethyl)propionyl]norleucyl}amino-5-cyclohexyl-1-morpholino-2,3-pentanediol.
Priority Claims (1)
Number |
Date |
Country |
Kind |
62-244934 |
Sep 1987 |
JPX |
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Parent Case Info
This is a Continuation, of application Ser. No. 08/179,195 filed on Jan. 10, 1994, which is a Division of Ser. No. 07/868,140 filed on Apr. 14, 1992, now U.S. Pat. No. 5,319,082 issued on Jun. 7, 1994, which is a Division of Ser. No. 07/240,725, filed on Sep. 6, 1988, now U.S. Pat. No. 5,122,523 issued on Jun. 16, 1992.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4304771 |
Suh et al. |
Dec 1981 |
|
4619944 |
Youssefyeh et al. |
Oct 1986 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
2054586 |
Feb 1981 |
GBX |
Non-Patent Literature Citations (1)
Entry |
Bolis et al J. Med. Chem. 1987, 30, 1729-1737. |
Divisions (2)
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Number |
Date |
Country |
Parent |
868140 |
Apr 1992 |
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Parent |
240725 |
Sep 1988 |
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Continuations (1)
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Number |
Date |
Country |
Parent |
179195 |
Jan 1994 |
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