Patent EP0578083A2 successfully refreshed from Google Patents.
EP0578083A2
Expired / Lapsed
EP
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Cyclic adhesion inhibitors
Assignee: Merck Patent GmbH
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Filing: 1993-06-26
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Granted: —
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Expires: 2013-06-26
Abstract
Abstract Pharmaceutical compositions comprising at least one cyclopeptide of formulae I (a)-(r) (a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala); (b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); (c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); (d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); (e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); (f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); (g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala); (h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly; (i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); (j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); (k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); (l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); (m) cyclo(-D-Arg-Gly-Asp-Phe-Val); (n) cyclo(-Arg-D-Ala-Asp-Phe-Val); (o) cyclo(-Arg-Gly-Asp-D-Phe-Val); (p) cyclo(-Arg-Ala-Asp-D-Phe-Val); (q) cyclo(-Arg-Gly-Asp-Phe-D-Val; (r) cyclo(-Arg-Gly-D-Asp-Phe-Val); or a salt thereof are useful as cell adhesion inhibitors.
Inventors
- 👤 Alfred Dr. Jonczyk
- 👤 Günter Dr. Hölzemann
- 👤 Brunhilde Dr. Felding-Habermann
- 👤 Guido Dr. Melzer
- 👤 Beate Diefenbach
- 👤 David A. Dr. Cheresh
- 👤 Horst Prof. Dr. Kessler
- 👤 Marion Dr. Gurrath
- 👤 Gerhard Dr. Glaxo SpA Centro Ricerche Müller
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 19:33
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/04; A61K38/12; C; C07; C07K; C07K14/00; C07K14/435; C07K14/745; C07K14/75; A61P; A61P17/00; A61P17/02; A61P19/00; A61P19/08; A61P19/10; A61P29/00; A61P35/00; A61P43/00; A61P7/00; A61P7/02; A61P9/00; A61P9/10; C07K14/78; C07K7/00; C07K7/04; C07K7/06
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
69 words
A pharmaceutical composition comprising: at least one cyclopeptide of formulae I (a)-(r) in an amount effective for inhibiting adhesion of animal cells: (a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala); (b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); (c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); (d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); (e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); (f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); (g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala); (h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly; (i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); (j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); (k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); (l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); (m) cyclo(-D-Arg-Gly-Asp-Phe-Val); (n) cyclo(-Arg-D-Ala-Asp-Phe-Val); (o) cyclo(-Arg-Gly-Asp-D-Phe-Val); (p) cyclo(-Arg-Ala-Asp-D-Phe-Val); (q) cyclo(-Arg-Gly-Asp-Phe-D-Val; (r) cyclo(-Arg-Gly-D-Asp-Phe-Val), or a physiologically acceptable salt thereof; and a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim
16 words
A pharmaceutical composition according to claim 1, wherein said animal cells are somatic cells of mammals.
Claim 3
Dependent Claim
14 words
A pharmaceutical composition according to claim 1, wherein said animal cells are cancer cells.
Claim 4
Dependent Claim
16 words
A pharmaceutical composition according to claim 1, wherein said composition contains 0.05-500 mg of said cyclopeptide.
Claim 5
Dependent Claim
16 words
A pharmaceutical composition according to claim 1, wherein said composition contains 0.5-100 mg of said cyclopeptide.
Claim 6
Dependent Claim
26 words
A method for the treatment and prophylaxis of thrombosis, myocardial infarct, apoplexy, arteriosclerosis, inflammations, angina pectoris and/or tumors, comprising administering a composition according to claim 1.
Claim 7
Dependent Claim
20 words
A method according to claim 6, wherein the amount of said cyclopeptide administered daily is 0.01-2 mg/kg of body weight.
Claim 8
Dependent Claim
21 words
A method of inducing an adhesion-receptor-antagonistic effect in a subject, comprising administering to said subject a composition according to claim 1.
Claim 9
Dependent Claim
20 words
A method according to claim 8, wherein the amount of said cyclopeptide administered daily is 0.01-2 mg/kg of body weight.
Claim 10
Dependent Claim
23 words
A method according to claim 8, wherein said cyclopeptide is cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala; cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); cyclo(-Arg-Gly-Asp-D-Phe-Val); or cyclo(-Arg-Gly-Asp-Phe-D-Val).
Claim 11
Dependent Claim
23 words
A method according to claim 6, wherein said cyclopeptide is cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala; cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); cyclo(-Arg-Gly-Asp-D-Phe-Val); or cyclo(-Arg-Gly-Asp-Phe-D-Val).
Claim 12
Independent Claim
56 words
A method of blocking β₃ integrin fibrogen binding comprising administering an effective amount of a cyclopeptide of formula I (a)-(r): (a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala); (b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); (c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); (d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); (e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); (f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); (g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala); (h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly; (i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); (j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); (k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); (l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); (m) cyclo(-D-Arg-Gly-Asp-Phe-Val); (n) cyclo(-Arg-D-Ala-Asp-Phe-Val); (o) cyclo(-Arg-Gly-Asp-D-Phe-Val); (p) cyclo(-Arg-Ala-Asp-D-Phe-Val); (q) cyclo(-Arg-Gly-Asp-Phe-D-Val); (r) cyclo(-Arg-Gly-D-Asp-Phe-Val).
Claim 13
Dependent Claim
17 words
A method for the treatment or prophylaxis of osteoporosis comprising administering a composition according to claim 1.
Claim 14
Dependent Claim
19 words
A method of inhibiting cell adhesion in the formation of osteoclasts comprising administering a composition according to claim 1.
Claim 15
Dependent Claim
61 words
In a wound healing composition, the improvement comprising said composition containing at least one cyclopeptide of formula I(a)-(r): I (a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala); (b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala); (c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala); (d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala); (e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly); (f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly); (g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala); (h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly); (i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly); (j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly); (k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala); (l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala); (m) cyclo(-D-Arg-Gly-Asp-Phe-Val); (n) cyclo(-Arg-D-Ala-Asp-Phe-Val); (o) cyclo(-Arg-Gly-Asp-D-Phe-Val); (p) cyclo(-Arg-Ala-Asp-D-Phe-Val); (q) cyclo(-Arg-Gly-Asp-Phe-D-Val); (r) cyclo(-Arg-Gly-D-Asp-Phe-Val), or a physiologically acceptable salt thereof.
References Cited (Backward Citations)
No citation records indexed.
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