US5204326A
Expired / Lapsed
US
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Polypeptide derivatives and calcium metabolism improving agent
Assignee: Otsuka Pharmaceutical Co Ltd
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Filing: 1990-03-14
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Granted: 1993-04-20
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Expires: 2010-03-14
Abstract
Abstract Novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, having the activities for inhibiting bone calcium absorption, for lowering the blood level of calcium, as analgesics, for inhibiting secretion of the gastric juice. Pharmaceutical composition can be prepared by formulating, at least one of the novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, together with a proteolytic enzyme inhibitors and/or pharmaceutically acceptable acids. The pharmaceutical composition are quite effective as agents for curing hypercalcemia, for curing Peget's disease, for curing osteoporosis, analgetic agent, anti-ulcerative agent and the like.
Inventors
- 👤 Setsuro Fujii, deceased
- 👤 successor by Keiko Fujii
- 👤 successor by Shinichiro Fujii
- 👤 successor by Kaoruko Takada
- 👤 Yoshihito Yamamoto
- 👤 Fumio Shimizu
- 👤 Masatoshi Inai
- 👤 Naosumi Kinoshita
- 👤 Shizuo Nakamura
- 👤 Mitsuru Hirohashi
- 👤 Takashi Sakamoto
- 👤 Kazuhiko Tsutsumi
- 👤 Tetsuhiko Shirasaka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 13:11
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/585; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
171 words
Polypeptide derivatives, acid-addition salts thereof and complexes thereof represented by the general formula (1) ##STR110## wherein (A) is a lower alkylene group; (B) is --NHCO--, --S-- or an oxyphenylene group; (D) is a lower alkylene group; (E) is a valine residue, a glycine residue or an isoleucine residue; (F) is a histidine residue, an asparagine residue, a glycine residue, an alanine residue, a serine residue, a leucine residue or a glutamine residue; and (G) is an arginine residue or a glutamine residue, respectively; l, m and n are each 0 or 1; provided that when l is 0 and (A) is a methylene group, then (D) is a methylene group or an ethylene group; or represented by the general formula (2) ##STR111## wherein (A') is a lower alkylene group; (B') is --NHCO--; (D') is a lower alkylene group; (G') is a histidine residue, a asparagine residue or a glycine o residue; and (H') is an arginine residue or a glutamine residue, respectively; and p and q are each 0 or 1.
Claim 2
Dependent Claim
171 words
Polypeptide derivatives, acid-addition salts thereof and complexes thereof represented by the general formula (1) ##STR110## wherein (A) is a lower alkylene group; (B) is --NHCO--, --S-- or an oxyphenylene group; (D) is a lower alkylene group; (E) is a valine residue, a glycine residue or an isoleucine residue; (F) is a histidine residue, an asparagine residue, a glycine residue, an alanine residue, a serine residue, a leucine residue or a glutamine residue; and (G) is an arginine residue or a glutamine residue, respectively; l, m and n are each 0 or 1; provided that when l is 0 and (A) is a methylene group, then (D) is a methylene group or an ethylene group; or represented by the general formula (2) ##STR111## wherein (A') is a lower alkylene group; (B') is --NHCO--; (D') is a lower alkylene group; (G') is a histidine residue, a asparagine residue or a glycine o residue; and (H') is an arginine residue or a glutamine residue, respectively; and p and q are each 0 or 1.
Claim 3
Dependent Claim
42 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 1, wherein the polypeptide derivatives are represented by the general formula (1) ##STR112## wherein (A), (B), (D), (E), (F), (G), l, m and n are the same as defined above.
Claim 4
Dependent Claim
40 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 1, wherein the polypeptide derivatives are represented by the general formula (2) ##STR113## wherein (A'), (B'), (D'), (G'), (H'), p and q are the same as defined above.
Claim 5
Dependent Claim
73 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 2, wherein the polypeptide derivatives are represented by the general formula (3) ##STR114## wherein (A) is a lower alkylene group; (B') is --NHCO--; (D) is a lower alkylene group; (F') is a histidine residue, an asparagine residue or a glycine residue; (G) is an arginine residue or a glutamine residue, respectively; and l, m and n are each 0 or 1.
Claim 6
Dependent Claim
21 words
The polypeptide derivative, acid-addition salt thereof and complex thereof according to claim 2, wherein the polypeptide is the formula of: ##STR115##
Claim 7
Dependent Claim
21 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 2, wherein the polypeptide derivatives are formulas of: ##STR116##
Claim 8
Dependent Claim
21 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 2, wherein the polypeptide derivatives are formulas of: ##STR117##
Claim 9
Dependent Claim
22 words
The polypeptide derivative, acid-addition salt thereof and complex thereof according to claim 2, wherein the polypeptide derivative is the formula of: ##STR118##
Claim 10
Dependent Claim
22 words
The polypeptide derivative, acid-addition salt thereof and complex thereof according to claim 2, wherein the polypeptide derivative is the formula of: ##STR119##
Claim 11
Dependent Claim
22 words
The polypeptide derivative, acid-addition salt thereof and complex thereof according to claim 2, wherein the polypeptide derivative is the formula of: ##STR120##
Claim 12
Dependent Claim
22 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 2, wherein the polypeptide derivatives are the formulas of: ##STR121##
Claim 13
Dependent Claim
22 words
The polypeptide derivatives, acid-addition salts thereof and complexes thereof according to claim 3, wherein the polypeptide derivatives are the formulas of: ##STR122##
Claim 14
Dependent Claim
74 words
Polypeptide derivatives, and their blocked derivatives of which the side chain functional group is protected, acid-addition salts thereof and complexes thereof represented by the general formula (3) ##STR123## wherein (A') is a lower alkylene group; (B') is --NHCO--; and (D') is a lower alkylene group, respectively; and R is an activated carboxyl group or hydroxyl group, or a group of the formula -Val-Leu-Gly-R', wherein R' is an activated carboxyl group or a hydroxyl group.
Claim 15
Dependent Claim
74 words
Polypeptide derivatives, and their blocked derivatives of which the side chain functional group is protected, acid-addition salts thereof and complexes thereof represented by the general formula (3) ##STR123## wherein (A') is a lower alkylene group; (B') is --NHCO--; and (D') is a lower alkylene group, respectively; and R is an activated carboxyl group or hydroxyl group, or a group of the formula -Val-Leu-Gly-R', wherein R' is an activated carboxyl group or a hydroxyl group.
Claim 16
Dependent Claim
30 words
A pharmaceutical composition for lowering blood serum calcium which comprises a polypeptide derivative, acid-addition salt thereof or complex thereof as claimed in claim 1, together with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim
47 words
A pharmaceutical composition for lowering blood serum calcium wherein the active ingredients, at least one polypeptide derivative, acid-addition salt thereof or complex thereof represented by the general formula (1) or (2) as claimed in claim 1, together with a proteolytic enzyme inhibitor and/or a pharmaceutically acceptable acid.
Claim 18
Dependent Claim
29 words
A pharmaceutical composition for treating hypercalcemia by using polypeptide derivative, acid-addition salt thereof or complex thereof selected from the group consisting of: ##STR124## together with a pharmaceutically acceptable carrier.
Claim 19
Dependent Claim
29 words
A pharmaceutical composition for treating hypercalcemia by using polypeptide derivative, acid-addition salt thereof or complex thereof selected from the group consisting of: ##STR124## together with a pharmaceutically acceptable carrier.
Claim 20
Dependent Claim
39 words
A method for lowering blood calcium serum, which comprises administering to a host an effective amount of a polypeptide derivative, acid-addition salt thereof or complex thereof represented by the general formula (1) or (2) as claimed in claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-04-19 | 1996-10-19 | 1997-04-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-04-19 | 2000-10-19 | 2001-04-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-04-19 | 2004-10-19 | 2005-04-20 | $7700.00 | Window Closed / Lapsed |