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- Nachgewiesen in: USPTO Patent Applications
- Sprachen: English
- Document Number: 20200164114
- Publication Date: May 28, 2020
- Appl. No: 16/636908
- Application Filed: August 09, 2017
- Assignees: National Taiwan University (Taipei, TW), NATIONAL CHENG KUNG UNIVERSITY (Tainan City, TW), DCB-USA LLC (Wilmington, DE, US)
- Claim: 1. A disintegrin variant comprising: (a) a linker having the amino acid sequence selected from the group consisting of SEQ ID Nos. 1, 4, 7, 8, and 9; (b) a RGD loop having the amino acid sequence selected from the group consisting of SEQ ID Nos. 10, 11, 12 13, 14, 15, 16, 17, 18, 19, 20, 24, and 25; and (c) a C-terminus having the amino acid sequence selected from the group consisting of SEQ ID Nos. 3, 6, 21, 22, and 23.
- Claim: 2. The disintegrin variant of claim 1, wherein the disintegrin is albolabrin, applagin, basilicin, batroxostatin, bitistatin, cereberin, cerastin, crotatroxin, durissin, elegantin, eristicophin, flavoridin, flavostatin, halysin, halystatin, jararacin, jarastatin, kistrin, lachesin, lutosin, molossin, rhodostomin, salmosin, saxatilin, tergeminin, trimestatin, trimucrin, trimutase, ussuristatin, or viridian.
- Claim: 3. The disintegrin variant of claim 1, wherein the disintegrin variant comprises, (a) the linker of SEQ ID No: 1; (b) the RGD loop of any of SEQ ID Nos: 10-20; and (c) the C-terminus of any of SEQ ID Nos: 3, 21, 22, or 23.
- Claim: 4. The disintegrin variant of claim 3, wherein the disintegrin variant comprises the linker of SEQ ID No: 1, the RGD loop of SEQ ID No: 14, and the C-terminus of SEQ ID No. 21.
- Claim: 5. The disintegrin variant of claim 1, wherein the disintegrin variant comprises, (a) the linker of SEQ ID No: 7; (b) the RGD loop of SEQ ID Nos: 13 or 18; and (c) the C-terminus of any of SEQ ID Nos: 3, 21, or 22.
- Claim: 6. The disintegrin variant of claim 1, wherein the disintegrin variant comprises, the linker of SEQ ID Nos: 8; the RGD loop of SEQ ID No: 14; and the C-terminus of any of SEQ ID No: 21.
- Claim: 7. The disintegrin variant of claim 1, wherein the disintegrin variant comprises, (a) the linker of SEQ ID No: 9; (b) the RGD loop of SEQ ID Nos: 14 or 20; and (c) the C-terminus of any of SEQ ID No: 3, 21, or 23.
- Claim: 8. The disintegrin variant of claim 1, wherein the disintegrin variant comprises the linker of SEQ ID No: 4; the RGD loop of SEQ ID No: 24 or 25; and the C-terminus of SEQ ID No: 6.
- Claim: 9. The disintegrin variant of claim 1, further comprising a polyethylene glycol (PEG) chain having 2-20 repeats of ethylene glycol (EG) units linked to the N-terminus of the disintegrin variant.
- Claim: 10. A pharmaceutical composition comprising an effective amount of the disintegrin variant of claim 1, and a pharmaceutically acceptable carrier.
- Claim: 11. The pharmaceutical composition of claim 10, wherein the disintegrin variant comprises the linker of SEQ ID No: 1, the RGD loop of SEQ ID No: 14, and the C-terminus of SEQ ID No. 21.
- Claim: 12. The pharmaceutical composition of claim 10, wherein the N-terminus of the disintegrin variant further comprises a polyethylene glycol (PEG) chain having 2-20 repeats of ethylene glycol (EG) units linked thereto.
- Claim: 13. A method of treating a subject having or suspected of having a disease resulting from platelet aggregation comprising administering to the subject the pharmaceutical composition of claim 10, for alleviating or ameliorating the symptoms associated with the disease.
- Claim: 14. The method of claim 13, wherein the disease is a thrombotic disorder.
- Claim: 15. The method of claim 14, wherein the thrombotic disorder is selected from the group consisting of, abrupt vessel closure following angioplasty or stent placement, atherothrombosis, acute thrombotic stroke, myocardial infarction, thrombosis resulted from periphery vascular surgery, unstable angina, and venous thrombosis.
- Claim: 16. The method of claim 13, further comprising administering an anti-coagulant to the subject.
- Claim: 17. The method of claim 16, wherein the anti-coagulant is selected from the group consisting of, abciximab, apixaban, aspirin, clopidogrel, dipyridamole, edoxaban, eptifibatide, rivaroxaban, tirofiban, ticlopidine, warfarin, and vitamin K.
- Claim: 18. The method of claim 13, wherein the disintegrin variant comprises the linker of SEQ ID No: 1, the RGD loop of SEQ ID No: 14, and the C-terminus of SEQ ID No. 21.
- Claim: 19. The method of claim 18, wherein the N-terminus of the disintegrin variant further comprises a polyethylene glycol (PEG) chain having 2-20 repeats of ethylene glycol (EG) units linked thereto.
- Claim: 20. The method of claim 18, wherein the disintegrin variant is applied as a coating on an implantable device.
- Claim: 21. The method of claim 20, wherein the implantable device is a stent or a catheter.
- Claim: 22-39. (canceled)
- Current International Class: 61; 07; 61
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