US3853837A
Expired / Lapsed
US
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Novel nonapeptide amide analogs of luteinizing hormone releasing factor
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1973-04-25
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Granted: 1974-12-10
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Expires: 1993-04-25
Abstract
Abstract The present invention relates to nonapeptide amide derivatives of the formula: L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-A1-glycyl-A2-Larginyl-L -prolyl-Y (wherein A1 is L-tyrosyl or L-phenylalanyl; A2 is L-leucyl, Lisoleucyl, L-norleucyl, L-valyl, L-norvalyl, L-methionyl or Lphenylalanyl, Y represents NHR in which R is a straight or branched alkyl group of one to three carbon atoms which may be substituted by hydroxy or alternatively Y represents pyrrolidino), AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF. The subject peptides have strong ovulation inducing activity.
Inventors
- 👤 M Fujino
- 👤 S Shinagawa
- 👤 T Fukuda
- 👤 S Kobayashi
- 👤 M Obayashi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:19
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07K; C07K7/00; C07K7/04; C07K7/06; C07K7/23; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/13
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
62 words
A NONAPEPTIDE AMIDE DERIVATIVE SHOWN BY THE GENERAL FORMULA: L-PYROGLUTAMYL-L-HISTIDYL-L-TRYTOPHYL-L-SERYL-A1-GLYCYLA2-L-ARGINYL-L-PROYL -Y WHEREIN A1 IS L-TYROSYL OR L-PHENYLALANYL; A2 IS L-LEUCYL, L-ISOLEUCYL, L-NORLEUCYL, L-VALYL, L-NORVALYL, L-METHIONYL OR L-PHENYLALANYL, Y REPRESENTS NHR IN WHICH R IS A STRAIGHT OR BRANCHED ALKYL GROUP OF ONE TO THREE CARBON ATOMS WHICH MAY BE SUBSTITUTED BY HYDROXTY OR ALTERNATIVELY Y REPRESENTS PYRROLIDINO, AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF.
Claim 2
Dependent Claim
62 words
A NONAPEPTIDE AMIDE DERIVATIVE SHOWN BY THE GENERAL FORMULA: L-PYROGLUTAMYL-L-HISTIDYL-L-TRYTOPHYL-L-SERYL-A1-GLYCYLA2-L-ARGINYL-L-PROYL -Y WHEREIN A1 IS L-TYROSYL OR L-PHENYLALANYL; A2 IS L-LEUCYL, L-ISOLEUCYL, L-NORLEUCYL, L-VALYL, L-NORVALYL, L-METHIONYL OR L-PHENYLALANYL, Y REPRESENTS NHR IN WHICH R IS A STRAIGHT OR BRANCHED ALKYL GROUP OF ONE TO THREE CARBON ATOMS WHICH MAY BE SUBSTITUTED BY HYDROXTY OR ALTERNATIVELY Y REPRESENTS PYRROLIDINO, AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF.
Claim 3
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is NHCH2CH3.
Claim 4
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is NHCH2CH2OH.
Claim 5
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is NHCH3.
Claim 6
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-phenylalanyl, A2 is L-isoleucyl and Y is NHCH2CH3.
Claim 7
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is pyrrolidino.
Claim 8
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is N(CH3)2.
Claim 9
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl and Y is NHCH(CH3)2.
Claim 10
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-norleucyl and Y is NHCH2CH3.
Claim 11
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-methionyl and Y is NHCH2CH3.
Claim 12
Dependent Claim
20 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-phenylalanyl, A2 is L-leucyl and Y is NHCH2CH3.
Claim 13
Dependent Claim
16 words
A nonapeptide amide derivative as claimed in claim 1, wherein A1 is L-tyrosyl, A2 is L-leucyl.
Claim 14
Dependent Claim
12 words
A nonapeptide derivative as claimed in claim 1 wherein Y represents NHR.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1977-12-09 | 1978-06-10 | 1978-12-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1981-12-09 | 1982-06-10 | 1982-12-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1985-12-09 | 1986-06-10 | 1986-12-10 | $7700.00 | Window Closed / Lapsed |