Claims
- 1. A compound of the formula (1): ##STR202## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclic group, a substituted lower alkyl group, a substituted cycloalkyl group, a substituted lower alkenyl group, a substituted lower alkynyl group, a substituted aryl group or a substituted heterocyclic group;
- R.sup.2 is a lower alkyl group, a cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclic group, a substituted lower alkyl group, a substituted cycloalkyl group, a substituted lower alkenyl group, a substituted lower alkynyl group, a substituted aryl group or a substituted heterocyclic group;
- A.sup.1 is --CO-- or --CO--A.sup.4 -- (wherein A.sup.4 is a residue of an .alpha.-amino acid, an .alpha.-amino acid derivative, a .beta.-amino acid or a .beta.-amino acid derivative, or a residue of a peptide consisting of 2 or 3 residues thereof);
- A.sup.2 and A.sup.3 are the same or different and each a single bond, --NR.sup.6 -- (wherein R.sup.6 is a hydrogen atom or a lower alkyl group), an oxygen atom, S(O).sub.n (wherein n is 0, 1 or 2), --CO--NR.sup.7 -- (wherein R.sup.7 is a hydrogen atom or a lower alkyl group), --NR.sup.7 --CO-- (wherein R.sup.7 is the same as defined above), --CO--A.sup.5 --NR.sup.8 -- (wherein R.sup.8 is a hydrogen atom or a lower alkyl group, A.sup.5 is a residue of an .beta.-amino acid, an .alpha.-amino acid derivative, a .beta.-amino acid or a .beta.-amino acid derivative, or a reside of a dipeptide consisting of 2 residues thereof), --NR.sup.8 --A.sup.5 --CO-- (wherein R.sup.8 and A.sup.5 are the same as defined above), a divalent group of a monocyclic hydrocarbons or a divalent group of a monocyclic heterocyclic group;
- R.sup.3, R.sup.4 and R.sup.5 are the same or different and each a single bond, or an alkylene, alkenylene or alkynylene group, which may optionally be substituted by 1 to 4 groups selected from the hydroxy group, an oxo group, a halogen atom, an aryl group and a cycloalkyl group, provided that when A.sup.2 and A.sup.3 are the same or different and each --NR.sup.6 -- (wherein R.sup.6 is the same as defined above), an oxygen atom or S(O).sub.n (wherein n is the same as defined above), R.sup.4 should not be a single bond;
- the definition for X and the number of atoms comprising a divalent main chain represented by --R.sup.5 --A.sup.3 --R.sup.4 --A.sup.2 --R.sup.3 --A.sup.1 -- are shown in the following (a):
- (a) X is a group of the formula (4): ##STR203## wherein Y.sup.2 and Y.sup.3 are the same or different and each a methine group or a nitrogen atom, V.sup.3 is a hydrogen atom, an alkyl group, a substituted lower alkyl group, a cycloalkyl group, an amino group, an acylamino group, a lower alkyloxycarbonyl group or a lower alkyloxycarbonyl group substituted by an aryl group, m is 2 or 3, and the number of atoms comprising a divalent main chain represented by --R.sup.5 --A.sup.3 --R.sup.4 --A.sup.2 --R.sup.3 --A.sup.1 -- is 4 to 9,
- or a pharmaceutically acceptable salt thereof.
- 2. The compound according to claim 1, wherein R.sup.2 is an aryl group, a substituted aryl group, an aromatic heterocyclic group or a substituted aromatic heterocyclic group, or a pharmaceutically acceptable salt thereof.
- 3. The compound according to claim 1, wherein R.sup.2 is an aryl group, an aromatic heterocyclic group, or an aryl group substituted by 1 or more groups selected from a lower alkyl group, a lower alkyl group substituted by a halogen atom, a lower alkyloxy group, a lower alkyloxy group substituted by a halogen atom, an amino group, a dialkylamino group, an acylamino group, a halogen atom, a nitro group and a carboxyl group, or a pharmaceutically acceptable salt thereof.
- 4. The compound according to any one of claims 1 to 3, wherein A.sup.1 is --CO--, and R.sup.3 is --CH.sub.2 --CHR.sup.9 -- (wherein R.sup.9 is a hydrogen atom or a lower alkyl group), or a pharmaceutically acceptable salt thereof.
- 5. The compound according to claim 4, wherein the definition for X and the number of atoms comprising a divalent main chain represented by --R.sup.5 --A.sup.3 --R.sup.4 --A.sup.2 --R.sup.3 --A.sup.1 -- are defined by the following (a), or a pharmaceutically acceptable salt thereof:
- (a) X is a group of the formula (4): ##STR204## wherein Y.sup.2, Y.sup.3, V.sup.3 and m are the same as defined above, and the number of atoms comprising a divalent main chain represented by --R.sup.5 --A.sup.3 --R.sup.4 --A.sup.2 --R.sup.3 --A.sup.1 -- is 5 or 6.
- 6. The compound according to claim 5, which is a compound of the formula (5): ##STR205## wherein R.sup.1 and R.sup.2 are the same as defined above, X and A.sup.6 are defined by the following (a), or a pharmaceutically acceptable salt thereof:
- (a) X is a group of the formula (4): ##STR206## wherein Y.sup.2, Y.sup.3, V.sup.3 and m are the same as defined above, A.sup.6 is a divalent group selected from the following groups:
- --(CH.sub.2).sub.f --CONR.sup.10 --CH.sub.2 --CHR.sup.9 -- (R.sup.9 and R.sup.10 are the same as defined above, and f is 0 or 1);
- --Y.sup.4 --(CH.sub.2).sub.d -- (Y.sup.4 is a methylene group or an oxygen atom and d is 3 or 4);
- --(CH.sub.2).sub.f --CO--(CH.sub.2).sub.d -- (f and d are the same as defined above);
- --(CH.sub.2).sub.f --CH(OH)--(CH.sub.2).sub.d -- (f and d are the same as defined above);
- --NR.sup.10 CO--(CH.sub.2).sub.d -- (R.sup.10 is a hydrogen atom or a lower alkyl group and d is the same as defined above);
- --Y.sup.4 --(CH.sub.2).sub.g --Y.sup.5 -- (Y.sup.4 is the same as defined above, Y.sup.5 is an oxygen atom or --NR.sup.11 -- (R.sup.11 is a hydrogen atom or a lower alkyl group), and g is 2 to 4);
- a group of the formula: ##STR207## wherein a is 1 or 2 and f is the same as defined above; a group of the formula: ##STR208## wherein f is the same as defined above, Y.sup.6 is a methine group or a nitrogen atom;
- a group of the formula: ##STR209## wherein Y.sup.5 and f are the same as defined above, and h is 0 or 1; a group of the formula: ##STR210## wherein Y.sup.4, Y.sup.5 and h are the same as defined above.
- 7. The compound according to claim 6, wherein X and A.sup.6 are defined by the following (a), or a pharmaceutically acceptable salt thereof:
- (a) X is a group of the formula (4): ##STR211## wherein Y.sup.2, Y.sup.3, V.sup.3 and m are the same as defined above, A.sup.6 is a divalent group selected form the following groups:
- --(CH.sub.2).sub.f --CONR.sup.10 --CH.sub.2 --CHR.sup.9 -- (R.sup.9, R.sup.10 and f are the same as defined above);
- --Y.sup.4 --(CH.sub.2).sub.d -- (Y.sup.4 and d are the same as defined above);
- --(CH.sub.2).sub.f --CO--(CH.sub.2).sub.d -- (f and d are the same as defined above);
- a group of the formula: ##STR212## wherein a and f are the same as defined above; a group of the formula: ##STR213## wherein f and Y.sup.6 are the same as defined above.
- 8. The compound according to claim 7, wherein X is a group of the formula (4): ##STR214## wherein Y.sup.2, Y.sup.3, V.sup.3 and m are the same as defined above, A.sup.2 and A.sup.3 are the same or different and each a single bond, --NR.sup.6 -- (R.sup.6 is the same as defined above), an oxygen atom, S(O).sub.n (n is the same as defined above), --CO--NR.sup.7 -- (R.sup.7 is the same as defined above), NR.sup.7 --CO-- (R.sup.7 is the same as defined above), --CO--A.sup.5 --NR.sup.8 -- (A.sup.5 and R.sup.8 are the same as defined above), --NR.sup.8 --A.sup.5 --CO-- (R.sup.8 and A.sup.5 are the same as defined above), a divalent group of aliphatic monocyclic hydrocarbons or a divalent group of aliphatic monocyclic heterocyclic group, or a pharmaceutically acceptable salt thereof.
- 9. The compound according to claim 1, wherein the stereoconfiguration of the 2-position thereof is S-configuration, or a pharmaceutically acceptable salt thereof.
- 10. A pharmaceutical composition comprising an effective amount of a compound of claim 1; and a pharmaceutically acceptable carrier.
- 11. A method of inhibiting platelets which comprises administering an effective amount of a compound according to claim 1 to a patient in need thereof.
- 12. A method of inhibiting cancer metastasis which comprises administering an effective amount of a compound according to claim 1 to a patient in need thereof.
- 13. A method of healing a wound which comprises administering an effective amount of a compound according to claim 1 or 9 to a patient suffering from a wound.
- 14. A method of inhibiting bone resorption which comprises administering an effective amount of a compound according to claim 1 or 9 to a patient in need thereof.
Priority Claims (2)
Number |
Date |
Country |
Kind |
6-286091 |
Oct 1993 |
JPX |
|
6-350177 |
Dec 1993 |
JPX |
|
Parent Case Info
This application is a divisional of application Ser. No. 08/633,800 filed on Apr. 19, 1996 now U.S. Pat. No. 5,707,994 the entire contents of which are hereby incorporated by reference which is a 371 of PCT/JP94/01700 filed Oct. 11, 1994.
US Referenced Citations (9)
Foreign Referenced Citations (6)
Number |
Date |
Country |
0478363 |
Apr 1992 |
EPX |
0512829 |
Nov 1992 |
EPX |
0512831 |
Nov 1992 |
EPX |
52-31061 |
Mar 1977 |
JPX |
4288051 |
Oct 1992 |
JPX |
9412181 |
Jun 1994 |
WOX |
Divisions (1)
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Number |
Date |
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Parent |
633800 |
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