Patent US4423037A successfully refreshed from Google Patents.
US4423037A
Expired / Lapsed
US
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Inhibitors of peptide hormone action
Assignee: General Hospital Corp
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Filing: 1982-05-13
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Granted: 1983-12-27
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Expires: 2002-05-13
Abstract
Abstract The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein the three N-terminal amino acids are removed and zero or more of the next four N-terminal amino acids are removed sequentially from the N-terminus.
Inventors
- 👤 Michael Rosenblatt
- 👤 John T. Potts, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 12:16
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/635; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 65
Claim 1
Independent Claim
117 words
A parathyroid hormone analogue, comprising: a parathyroid peptide fragment wherein the three N-terminal amino acids and zero or more of the next four N-terminal amino acids are absent from a parathyroid hormone (PTH), from a parathyroid hormone fragment comprising at least the first 34 amino acids of said PTH, or from said parathyroid hormone or said parathyroid hormone fragment in which amino acid #34 is replaced with D- or L-tyrosine or in which amino acids #8 and #18 are each replaced with norleucine and amino acid #34 is replaced with D- or L-tyrosine, wherein the carboxy-terminal of said peptide fragment is optionally an amide, and wherein the N-terminal of said peptide fragment is optionally a D-amino acid.
Claim 2
Dependent Claim
117 words
A parathyroid hormone analogue, comprising: a parathyroid peptide fragment wherein the three N-terminal amino acids and zero or more of the next four N-terminal amino acids are absent from a parathyroid hormone (PTH), from a parathyroid hormone fragment comprising at least the first 34 amino acids of said PTH, or from said parathyroid hormone or said parathyroid hormone fragment in which amino acid #34 is replaced with D- or L-tyrosine or in which amino acids #8 and #18 are each replaced with norleucine and amino acid #34 is replaced with D- or L-tyrosine, wherein the carboxy-terminal of said peptide fragment is optionally an amide, and wherein the N-terminal of said peptide fragment is optionally a D-amino acid.
Claim 3
Dependent Claim
12 words
The analogue of claim 1 wherein said PTH is bovine PTH (bPTH).
Claim 4
Dependent Claim
15 words
The analogue of claim 2 wherein said hormone fragment comprises amino acids 1-34 (bPTH (1-34)).
Claim 5
Dependent Claim
18 words
The analogue of claim 2 or 3 wherein amino acid #34 is replaced by either D- or L-tyrosine.
Claim 6
Dependent Claim
20 words
The analogue of claim 2 or 3 wherein the N-terminal amino acid of said peptide fragment is a D-amino acid.
Claim 7
Dependent Claim
19 words
The analogue of claim 2 or 3 wherein the carboxy-terminal amino acid of said peptide fragment is an amide.
Claim 8
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [L-Tyr-34] bPTH (4-34) amide.
Claim 9
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [L-Tyr-34] bPTH (5-34) amide.
Claim 10
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [L-Tyr-34] bPTH (6-34) amide.
Claim 11
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [L-Tyr-34] bPTH (7-34) amide.
Claim 12
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [D-Tyr-34] bPTH (4-34) amide.
Claim 13
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [D-Tyr-34] bPTH (5-34) amide.
Claim 14
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [D-Tyr-34] bPTH (6-34) amide.
Claim 15
Dependent Claim
13 words
The analogue of claim 1 wherein said analogue is [D-Tyr-34] bPTH (7-34) amide.
Claim 16
Dependent Claim
15 words
The analogue of claim 1 wherein said analogue is [Nle-8, Nle-18, Tyr-34] bPTH (4-34) amide.
Claim 17
Dependent Claim
12 words
The analogue of claim 1 wherein said PTH is human PTH (hPTH).
Claim 18
Dependent Claim
15 words
The analogue of claim 16 wherein said hormone fragment comprises amino acids 1-34 (hPTH (1-34)).
Claim 19
Dependent Claim
18 words
The analogue of claim 16 or 17 wherein amino acid #34 is replaced by either D- or L-tyrosine.
Claim 20
Dependent Claim
20 words
The analogue of claim 16 or 17 wherein the N-terminal amino acid of said peptide fragment is a d-amino acid.
Claim 21
Dependent Claim
19 words
The analogue of claim 16 or 17 wherein the carboxy-terminal amino acid of said peptide fragment is an amide.
Claim 22
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [L-Tyr-34] hPTH (4-34) amide.
Claim 23
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [L-Tyr-34] hPTH (5-34) amide.
Claim 24
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [L-Tyr-34] hPTH (6-34) amide.
Claim 25
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [L-Tyr-34] hPTH (7-34) amide.
Claim 26
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [D-Tyr-34] hPTH (4-34) amide.
Claim 27
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [D-Tyr-34] hPTH (5-34) amide.
Claim 28
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [D-Tyr-34] hPTH (6-34) amide.
Claim 29
Dependent Claim
13 words
The analogue of claim 16 wherein said analogue is [D-Tyr-34] hPTH (7-34) amide.
Claim 30
Dependent Claim
15 words
The analogue of claim 16 wherein said analogue is [Nl3-8, Nle-18, Tyr-34] hPTH (4-34) amide.
Claim 31
Dependent Claim
24 words
A method of inhibiting the action of parathyroid hormone, comprising: administering a therapeutically effective amount of an analogue of claim 1 to a vertebrate.
Claim 32
Dependent Claim
10 words
The method of claim 30 wherein said hormone is bPTH.
Claim 33
Dependent Claim
10 words
The method of claim 30 wherein said hormone is hPTH.
Claim 34
Dependent Claim
19 words
The method of claim 30, wherein said hormone fragment comprises the N-terminal 34 amino acids of a parathyroid hormone.
Claim 35
Dependent Claim
17 words
The method of claim 33 wherein said hormone fragment comprises the N-terminal 34 amino acids of bPTH.
Claim 36
Dependent Claim
17 words
The method of claim 33 wherein said hormone fragment comprises the N-terminal 34 amino acids of hPTH.
Claim 37
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] bPTH (4-34) amide.
Claim 38
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] bPTH (5-34) amide.
Claim 39
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] bPTH (6-34) amide.
Claim 40
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] bPTH (7-34) amide.
Claim 41
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [D-Tyr-34] bPTH (4-34) amide.
Claim 42
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [D-Tyr-34] bPTH (5-34) amide.
Claim 43
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [D-Tyr-34] bPTH (6-34) amide.
Claim 44
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [D-Tyr-34] bPTH (7-34) amide.
Claim 45
Dependent Claim
16 words
The method of claim 30 wherein said peptide fragment is [Nle-8, Nle-18, Tyr-34] bPTH (4-34) amide.
Claim 46
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (4-34) amide.
Claim 47
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (5-34) amide.
Claim 48
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (6-34) amide.
Claim 49
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (7-34) amide.
Claim 50
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (4-34) amide.
Claim 51
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (5-34) amide.
Claim 52
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (6-34) amide.
Claim 53
Dependent Claim
14 words
The method of claim 30 wherein said peptide fragment is [L-Tyr-34] hPTH (7-34) amide.
Claim 54
Dependent Claim
16 words
The method of claim 30 wherein said peptide fragment is [Nle-8, Nle-18, Tyr-34] hPTH (4-34) amide.
Claim 55
Dependent Claim
28 words
An in vitro bioassy of parathyroid hormone, wherein a measured amount of the analogue of claim 1 inhibits binding a parathyroid hormone to a PTH receptor in vitro.
Claim 56
Dependent Claim
14 words
The method of claim 30, wherein said administering is for the treatment of hypercalcemia.
Claim 57
Dependent Claim
16 words
The method of claim 30, wherein said administering is for the diagnosing or treating of hyperparathyroidism.
Claim 58
Dependent Claim
13 words
The method of claim 56, wherein the hyperparathyroidism results in a hypercalcemic crisis.
Claim 59
Dependent Claim
12 words
The method of claim 56, wherein the hyperparathyroidism results in renal failure.
Claim 60
Dependent Claim
13 words
The method of claim 56, wherein a tumor produces a parathyroid hormone-like substance.
Claim 61
Dependent Claim
16 words
The method of claim 30, wherein said administering is for the treatment of an immune disease.
Claim 62
Dependent Claim
11 words
The method of claim 60, wherein the immune disease comprises inflammation.
Claim 63
Dependent Claim
13 words
The method of claim 60, wherein the immune disease comprises an allergic response.
Claim 64
Dependent Claim
12 words
The method of claim 60, wherein the immune disease comprises hyperactive lymphocytes.
Claim 65
Dependent Claim
14 words
The method of claim 30, wherein said administering is for the treatment of hypertension.
References Cited (Backward Citations)
US3886132A
Cited
US4086196A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-12-26 | 1987-06-27 | 1987-12-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-12-26 | 1991-06-27 | 1991-12-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-12-26 | 1995-06-27 | 1995-12-27 | $7700.00 | Window Closed / Lapsed |