US4008209A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Nonapeptide amide analogs of luteinizing releasing hormone
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1975-07-11
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Granted: 1977-02-15
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Expires: 1995-07-11
Abstract
Abstract The novel nonapeptide amide derivatives of the formula (Pyr)Glu-His-Trp-Ser-R1-R2-R3-Arg-Pro-NH-R4 wherein R1 is Tyr or Phe; R2 is D-Leu, D-Ile, D-Nle, D-Val, D-NVa, D-Abu, alpha -Aibu, D-Phe, D-Phg, D-Ser, D-Thr or D-Met; R3 is Leu, Ile or Nle and R4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl group have a strong ovulation inducing activity.
Inventors
- 👤 Masahiko Fujino
- 👤 Tsunehiko Fukuda
- 👤 Susumu Shinagawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 15:44
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/23; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1005; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/13
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
50 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 1 is Tyr or Phe, R 2 is D-Nle, D-Nva, D-Abu, α-Aibu, D-Phe or D-Ser, R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl.
Claim 2
Dependent Claim
50 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 1 is Tyr or Phe, R 2 is D-Nle, D-Nva, D-Abu, α-Aibu, D-Phe or D-Ser, R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl.
Claim 3
Dependent Claim
31 words
A compound according to claim 1 wherein R 2 is D-Nva, D-Abu, α-Aibu, D-Phg or D-Ser, R 3 is Leu, and R 4 is alkyl of 1 to 3 carbon atoms.
Claim 4
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is α-Aibu, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 5
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Phg, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 6
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Ser, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 7
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Abu, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 8
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Nva, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 9
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Phe, R 2 is D-Nva, R 3 is Leu, and R 4 is -C 3 H 7 .
Claim 10
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Abu, R 3 is Leu, and R 4 is -CH(CH 3 ) 2 .
Claim 11
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Tyr, R 2 is D-Nle, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 12
Dependent Claim
28 words
A compound according to claim 1 wherein R 1 is Phe, R 2 is D-Phe, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 13
Dependent Claim
46 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 1 is Tyr or Phe, R 2 is D-Thr or D-Met, R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl.
Claim 14
Dependent Claim
46 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 1 is Tyr or Phe, R 2 is D-Thr or D-Met, R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl.
Claim 15
Dependent Claim
28 words
A compound according to claim 12 wherein R 1 is Tyr, R 2 is D-Thr, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 16
Dependent Claim
28 words
A compound according to claim 12 wherein R 1 is Tyr, R 2 is D-Met, R 3 is Leu, and R 4 is -C 2 H 5 .
Claim 17
Dependent Claim
32 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-Phe-D-Leu-R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted by hydroxyl.
Claim 18
Dependent Claim
32 words
A compound of the formula (Pyr)Glu-His-Trp-Ser-Phe-D-Leu-R.sub.3 -Arg-Pro-NH-R.sub.4 wherein R 3 is Leu, Ile or Nle, and R 4 is alkyl of 1 to 3 carbon atoms which may be substituted by hydroxyl.
Claim 19
Dependent Claim
20 words
A compound according to claim 15 wherein R 3 is Leu, and R 4 is -C 2 H 5 .
References Cited (Backward Citations)
US3853837A
Cited
US3914412A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-02-15 | 1980-08-16 | 1981-02-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-02-15 | 1984-08-16 | 1985-02-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-02-15 | 1988-08-16 | 1989-02-15 | $7700.00 | Window Closed / Lapsed |