Claims
- 1. A compound of the formula I ##STR55## wherein R.sub.1 is lower alkoxycarbonyl,
- R.sub.2 is phenyl substituted by 1 or more hydroxy, lower alkoxy, lower alkoxy-lower alkoxy or phenyl-lower alkoxy, and optionally further substituted by 1 or more lower alkyl,
- R.sub.3 is cyclohexyl, cyclohexenyl or phenyl or phenyl substituted by 1 or more lower alkyl, hydroxy, lower alkoxy, lower alkoxy-lower alkoxy, phenyl or cyanophenyl,
- R.sub.4 is lower alkyl,
- R.sub.5 is lower alkyl, and
- n is 1 or 2,
- or a salt thereof, provided at least one salt-forming group is present.
- 2. A compound of the formula I according to claim 1, in which
- R.sub.1 is lower-alkoxycarbonyl,
- R.sub.2 and R.sub.3 are, independently of each other, phenyl which is substituted by one or more radicals which are selected, independently of each other, from hydroxyl, lower alkoxy, phenyl-lower-alkoxy and loweralkoxy-lower alkoxy,
- R.sub.4 is lower alkyl,
- R.sub.5 is lower alkyl, and
- n is 1 or 2,
- or a salt thereof, provided at least one salt-forming group is present.
- 3. A compound of the formula I according to claim 1, wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5, R.sub.6 and n have the meanings specified in claim 1 and R.sub.3 is 2,3,4-lower-alkoxyphenyl, or a salt thereof, provided at least one salt-forming group is present.
- 4. A compound of the formula I according to claim 1, wherein
- R.sub.1 is lower-alkoxycarbonyl,
- R.sub.2 and R.sub.3 are present in the following combinations;
- R.sub.2 is 4-(lower alkoxy-lower alkoxy)phenyl and R.sub.3 is 4-(phenyl-lower alkoxy),
- R.sub.4 is lower alkyl,
- R.sub.5 is lower alkyl; and
- n is 1 or 2,
- or a salt thereof, provided at least one salt-forming group is present.
- 5. A compound of the formula I according to claim 1, in which
- R.sub.1 is selected from the group consisting of ethoxycarbonyl and tert-butoxycarbonyl,
- R.sub.2 and R.sub.3 are selected from 4-(benzyloxy)-phenyl, 2-, 3- or 4-methoxyphenyl, 4-isobutyloxyphenyl, trimethoxyphenyl, 4-(2-methoxyethoxy)phenyl, 4-methoxy-2-hydroxyphenyl, 4-methoxy-2,3-dimethylphenyl, 4-hydroxyphenyl and dimethoxyphenyl,
- R.sub.4 is isopropyl,
- R.sub.5 is methyl, ethyl or n-propyl, and
- n is 1 or 2,
- or a salt thereof, provided at least one salt-forming group is present.
- 6. A compound of the formula I according to claim 1, in which
- R.sub.1 is tert-butoxycarbonyl,
- R.sub.2 and R.sub.3 are selected from 4-(benzyloxy)-phenyl, 2-, 3- or 4-methoxyphenyl, 4-isobutyloxyphenyl, trimethoxyphenyl, 4-(2-methoxyethoxy)phenyl, 4-methoxy-2-hydroxyphenyl, 4-methoxy-2,3-dimethylphenyl, 4-hydroxyphenyl and dimethoxyphenyl,
- R.sub.4 is isopropyl,
- R.sub.5 is methyl or ethyl, and
- n is 1 or 2,
- or a salt thereof, provided at least one salt-forming group is present.
- 7. A compound of the formula I according to claim 1, in which
- R.sub.1 is lower-alkoxycarbonyl,
- R.sub.2 is 4-(lower alkoxy-lower alkoxy)phenyl and R.sub.3 is 4-phenyl-lower-alkoxyphenyl,
- R.sub.4 is isopropyl,
- R.sub.5 is methyl, and
- n is 1.
- 8. A compound according to claim 1, which is of the formula I', which comes under formula I, ##STR56## in which the radicals have the meanings specified in each case for compounds of the formula I.
- 9. A compound of the formula I according to claim 8 which is 5(S)-(Boc-amino)-4(S)-hydroxy-6-�p-(2-methoxyethoxy)phenyl!-2(R)-�(p-benzyloxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide.
- 10. A compound of the formula I according to claim 8 which is selected from the group consisting of
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-benzyloxyphenyl)-2(R)-�(p-benzyloxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-benzyloxyphenyl)-2(R)-�(p-methoxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-hydroxyphenyl)-2(R)-�(p-methoxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-methoxyphenyl)-2(R)-�(p-methoxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-(isobutoxy)phenyl)-2(R)-�(p-methoxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-methoxyphenyl)-2(R)-(phenylmethyl)hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-methoxyphenyl)-2(R)-(cyclohexylmethyl)hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(4-methoxyphenyl)-2(R)-�cyclohexen-1-ylmethyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-�p-(2-methoxyethoxy)phenyl!-2(R)-�(p-hydroxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-�p-(2-methoxyethoxy)phenyl!-2(R)-�(p-methoxyphenyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide, and
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-�p-(2-methoxyethoxy)phenyl!-2(R)-{�(p-(2-methoxyethoxy)phenyl!methyl}hexanoyl-(L)-Val-N-(2-methoxyethyl)amide, or a salt thereof, provided at least one salt-forming group is present.
- 11. A compound of the formula I according to claim 1, which is selected from the group consisting of
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-benzyloxyphenyl)-2(R)-�(4-biphenylyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-hydroxyphenyl)-2(R)-�(4-biphenylyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-methoxyphenyl)-2(R)-�(4-biphenylyl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-benzyloxyphenyl)-2(R)-�({2'-cyanobiphenyl}-4-yl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-hydroxyphenyl)-2(R)-�({2'-cyanobiphenyl}-4-yl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- 5(S)-(Boc-amino)-4(S)-hydroxy-6-(p-methoxyphenyl)-2(R)-�({2'-cyano-biphenyl}-4-yl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide, and
- 5(S)-(3-hydroxy-2-methylphenylcarboxyamino)-4(S)-hydroxy-6-(p-methoxy-phenyl)-2(R)-�({2'-cyanobiphenyl}-4-yl)methyl!hexanoyl-(L)-Val-N-(2-methoxyethyl)amide,
- or a salt thereof, provided at least one salt-forming group is present.
- 12. A pharmaceutical preparation which is appropriate for the treatment of a disease that is caused by a retrovirus, said preparation comprising an amount of a compound of formula I according to claim 1 that is active against a retroviral disease, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier material.
- 13. A method for treating diseases caused by retroviruses, where a combination, which is therapeutically effective against retroviral diseases, of a) a novel compound of the formula I according to claim 1 and b) a further compound, or two or more thereof, which is effective against retroviruses is administered to a mammal in a quantity which is therapeutically effective against retroviral diseases in order to treat a retroviral disease.
Priority Claims (2)
Number |
Date |
Country |
Kind |
3140/94 |
Oct 1994 |
CHX |
|
2382/95 |
Aug 1995 |
CHX |
|
Parent Case Info
This is a divisional of Ser. No. 08/545,170, filed Oct. 19, 1995 now U.S. Pat. No. 5,663,200.
US Referenced Citations (3)
Foreign Referenced Citations (12)
Number |
Date |
Country |
0278158 |
Aug 1988 |
EPX |
0311012 |
Apr 1989 |
EPX |
0329609 |
Aug 1989 |
EPX |
0337714 |
Oct 1989 |
EPX |
0356223 |
Feb 1990 |
EPX |
0374097 |
Jun 1990 |
EPX |
0434365 |
Jun 1991 |
EPX |
0487270 |
May 1992 |
EPX |
0528661 |
Feb 1993 |
EPX |
8802374 |
Apr 1988 |
WOX |
9106561 |
May 1991 |
WOX |
9110442 |
Jul 1991 |
WOX |
Non-Patent Literature Citations (2)
Entry |
Rich, et al., J. Med Chem. 34, 1225-1228 (1991). |
de Solms, et al., J. Med. Chem., 34, 2852-2857, (1991). |
Divisions (1)
|
Number |
Date |
Country |
Parent |
545170 |
Oct 1995 |
|