You are 3 steps away
from making better decisions

Serving leading biopharmaceutical companies globally:

McKesson
Merck
Mallinckrodt
McKinsey
Harvard Business School
Dow

Last Updated: August 12, 2020

DrugPatentWatch Database Preview

Claims for Patent: 6,541,450

➤ Get the DrugPatentWatch Daily Briefing
» See Plans and Pricing

« Back to Dashboard

Summary for Patent: 6,541,450
Title: Parathyroid hormone analogues for the treatment of osteoporosis
Abstract:This invention describes analogues of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailability. The peptides described are derivatives of hPTH-(1-31) which are cyclized for example, by formation of lactams between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogues have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogues also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat. An assay which correlates hypotensive activity with osteogenic activity is also described.
Inventor(s): Barbier; Jean-Rene (Gatineau, CA), Morley; Paul (Ottawa, CA), Neugebauer; Witold (Ottawa, CA), Whitfield; James F. (Ottawa, CA), Willick; Gordon E. (Orleans, CA)
Assignee: National Research Council of Canada (Ontario, CA)
Application Number:09/536,785
Patent Claims:1. A human parathyroid hormone hPTH-(1-31) analogue in which position 27 is Lys or has been substituted by Ala, Tyr or Gln, and which has been cyclized between Glu.sup.22 and Lys.sup.26 to form a lactam.

2. An analogue according to claim 1, having either a C-terminal amide ending or a C-terminal carboxyl ending.

3. A composition for administration to a warm-blooded animal in need thereof, comprising a human parathyroid hormone (hPTH)-(1-31) analogue according to claim 1, in association with a pharmaceutically acceptable carrier or excipient.

4. A method of treating a warm-blooded animal in need of such treatment, comprising administering to such warm-blooded animal, a therapeutically effective amount of a human parathyroid hormone (hPTH)-(1-31) analogue according to claim 1.

5. A human parathyroid hormone hPTH analogue and pharmaceutically acceptable salts thereof, having the amino acid sequence R--NH-R1-Val-Ser-Glu-Ile-Gln-Leu-R2-His-Asn-Leu-Gly-Lys-R3-R4-R5-R6-R7-Glu- Arg-Val-R8--Trp-Leu-R9-R10-R11-Leu-R12-Asp-Y (SEQ ID NO: 23)

wherein, R=hydrogen, R1=Ser, R2=Met, R3=His or Lys, R4=Leu or Lys, R5=Asn or Lys, R6=Ser or Lys, R7=Met, R8=Glu or Lys, R9=Arg, R10=Glu or Lys provided that R8 and R10 are not both Glu and are not both Lys, R11=Lys or Leu, R12=Gln, X=OH, or NH.sub.2, and Y=Val-X (SEQ ID NO: 36), Val-His-X (SEQ ID NO: 37), Val-His-Asn-X (SEQ ID NO: 38) or Val-His-Asn-Phe-X (SEQ ID NO: 24) cyclized in the form of a lactam between amino acid pair 22 and 26, excluding when R=H, R1=Ser, R2=Met, R3=His, R4=Leu, R5=Asn, R6=Ser, R7=Met, R8=Glu, R9=Arg, R10=Lys, R11=Leu, R12=Gln, X=OH or NH.sub.2, and Y=Val-X together.

6. An analogue according to claim 5, wherein the lactam is a Glu22-Lys26 lactam.

7. An analogue according to claim 5, wherein R is H and X is NH.sub.2.

8. An analogue according to claim 7, wherein R2 is Met, R7 is Met, R8 is Glu, and R10 is Lys.

9. An analogue according to claim 8, wherein Y=Val-X.

10. An analogue according to claim 8, wherein Y=Val-His-Asn-Phe-X (SEQ ID NO:24).

11. An analogue having the SEQ ID NO: 9.

12. An analogue having the SEQ ID NO: 10.

13. An analogue having the SEQ ID NO: 11.

14. An analogue having the SEQ ID NO: 13.

15. An analogue having the SEQ ID NO: 14.

16. An analogue having the SEQ ID NO: 16.

17. An analogue having the SEQ ID NO: 18.

18. An analogue having the SEQ ID NO: 19.

Details for Patent 6,541,450

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 001 2015-01-23   Start Trial National Research Council of Canada (Ontario, CA) 2014-06-20 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 002 2015-01-23   Start Trial National Research Council of Canada (Ontario, CA) 2014-06-20 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 003 2015-01-23   Start Trial National Research Council of Canada (Ontario, CA) 2014-06-20 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

McKesson
Johnson and Johnson
Harvard Business School
AstraZeneca
Boehringer Ingelheim
McKinsey

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.