Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-04-19
1998-01-13
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514330, 514331, 514535, 514538, 514539, 514540, 514542, 514562, 544393, 544400, 546226, 546233, 548537, 560 13, 562430, C07D21122, C07C31106, A61K 3124, A61K 31445
Patent
active
057079943
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel 2,3-diaminopropionic acid derivative being useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.
BACKGROUND ART
Proteins, which participate in adhesion between a cell and an interstitial connective tissue and show various biological activities concerning the cell functions of animal cells, are called cell adhesive proteins. For example, there are known fibronectin, vitronectin, laminin, etc. It is known that the core sequence of the cell adhesion site of these proteins Suzuki, S., et al., J. Biol. Chem., 259, 15307 (1984), Plow, E., et al., Proc. Natl. Acad. Sci. U.S.A., 82, 8057 (1985)!. The RGD interacts with a receptor of a cell adhesive protein, and as a result, it shows various pharmacological activities.
For example, fibrinogen being present in plasma interacts with a platelet membrane glycoprotein complex IIb/IIIa via RGD to cause a platelet aggregation, and it is considered that a synthetic peptide having RGD inhibits the interaction between fibrinogen and a platelet membrane glycoprotein complex IIb/IIIa and hence, it is useful as a platelet is also known that a peptide having a RGD derived from snake venom Cell Biol., 111, 1713 (1990)!.
Besides, fibronectin is considered to participate in differentiation and (1983)!, but since it stimulates migration of fibroblast and macrophage, it is expected to be applied to the treatment of wound or the regulation of immune mechanism. Particularly, fibronectin has been tried in the local treatment of corneal disorders by utilizing the promotion effect thereof
Moreover, cell adhesive proteins have been drawing attention as a substance participating in cancer metastasis. A cancer cell forms a multicellular mass in the presence of fibronectin or laminin so that it can more easily grow or survive. In fact, it has been confirmed that an RGD sequence, which is an adhesive core of fibronectin, inhibits the metastasis of
Thus, since cell adhesive proteins show various biological activities, a medicament which can selectively interact with a receptor of these proteins can be expected to be useful in the prophylaxis or treatment of various diseases.
On the other hand, a lot of screening on non-peptide compounds interacting with a receptor of these proteins has been as reported, for example, in EP 512831, EP 540334, WO 94/8962, WO 94/12181, EP 445796, etc. However, there is no compound which can clinically be used.
Under these circumstances, it has been desired to develop a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor, which selectively interacts with a receptor of a cell adhesive protein such as fibrinogen, fibronectin, etc., and shows excellent absorbability and excellent stability in living body.
DISCLOSURE OF INVENTION
The present inventors have intensively studied and have found a novel 2,3-diaminopropionic acid derivative which can selectively interact with a receptor of a cell adhesive protein, such as fibrinogen, fibronectin, etc.
That is, the gist of the present invention is as follows. ##STR2## 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; 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; .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); --NR.sup.6 -- (wherein R.sup.6 is a hydrogen atom or a lower alkyl group), an oxygen at
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Ikeda Yoshihara
Kamikawa Yumiko
Kishimoto Hisakazu
Nishihara Toshio
Ueki Yasuyuki
Rao Deepak R.
Shah Mukund J.
Sumitomo Pharmaceuticals Company Limited
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