US4301045A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Synthesis of peptides
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1977-05-02
•
Granted: 1981-11-17
•
Expires: 1997-05-02
Abstract
Abstract Resin peptides useful in the preparation of peptides having biological activity, and particularly such resin peptides containing Pro--Asp--CH 2 -- or Pro--Asn--CH 2 -- at one end of an amino acid chain, being the resin and Pro, Asp and Asn being the residues of the amino acids proline, aspartic acid and asparagine; and processes for the preparation of such resin peptides.
Inventors
- 👤 Emil Kaiser
- 👤 Robert L. Colescott
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 13:12
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/695; C07K1/00; C07K1/04; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
24 words
A resin peptide having the structure: ##STR24## in which R is a crosslinked polystyrene resin, and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl.
Claim 2
Dependent Claim
24 words
A resin peptide having the structure: ##STR24## in which R is a crosslinked polystyrene resin, and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl.
Claim 3
Dependent Claim
29 words
A resin peptide having the structure: ##STR25## in which R is a crosslinked polystyrene resin, Bz is benzyl, P-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl, and Y is H or Bz.
Claim 4
Dependent Claim
29 words
A resin peptide having the structure: ##STR25## in which R is a crosslinked polystyrene resin, Bz is benzyl, P-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl, and Y is H or Bz.
Claim 5
Dependent Claim
38 words
A resin peptide having the structure: ##STR26## in which R is a crosslinked polystyrene resin and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl, Y is H or Bz and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 6
Dependent Claim
38 words
A resin peptide having the structure: ##STR26## in which R is a crosslinked polystyrene resin and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, P-nitrobenzyl or benzhydryl, Y is H or Bz and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 7
Dependent Claim
51 words
A resin peptide having the structure: ##STR27## in which R is a crosslinked polystyrene resin, and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, p-nitrobenzyl or benzhydryl, Y is H or Bz, T is tosyl or nitro, W is carbobenzyloxy, tosyl, dinitrophenyl, Bz or H, and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 8
Dependent Claim
51 words
A resin peptide having the structure: ##STR27## in which R is a crosslinked polystyrene resin, and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, p-nitrobenzyl or benzhydryl, Y is H or Bz, T is tosyl or nitro, W is carbobenzyloxy, tosyl, dinitrophenyl, Bz or H, and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 9
Dependent Claim
11 words
A peptide having the structure: ##STR28## in which TFA is trifluoroacetyl.
Claim 10
Dependent Claim
11 words
A peptide having the structure: ##STR28## in which TFA is trifluoroacetyl.
Claim 11
Dependent Claim
18 words
A resin peptide having the structure: NH.sub.2 --Pro--Asn--CH.sub.2 -- R in which R is a crosslinked polystyrene resin.
Claim 12
Dependent Claim
18 words
A resin peptide having the structure: NH.sub.2 --Pro--Asn--CH.sub.2 -- R in which R is a crosslinked polystyrene resin.
Claim 13
Dependent Claim
21 words
A resin peptide having the structure: ##STR29## in which R is a crosslinked polystyrene resin, and Y is H or Bz.
Claim 14
Dependent Claim
21 words
A resin peptide having the structure: ##STR29## in which R is a crosslinked polystyrene resin, and Y is H or Bz.
Claim 15
Dependent Claim
50 words
A resin peptide having the structure: ##STR30## in which R is a crosslinked polystyrene resin, Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, p-nitrobenzyl or benzhydryl, Y is H or Bz, T is tosyl or nitro, W is carbobenzyloxy, tosyl, dinitrophenyl, Bz or H, and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 16
Dependent Claim
50 words
A resin peptide having the structure: ##STR30## in which R is a crosslinked polystyrene resin, Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, p-nitrobenzyl or benzhydryl, Y is H or Bz, T is tosyl or nitro, W is carbobenzyloxy, tosyl, dinitrophenyl, Bz or H, and V is carbobenzyloxy, 2-chlorocarbobenzyloxy, 2-bromocarbobenzyloxy, dichlorocarbobenzyloxy or trifluoroacetyl.
Claim 17
Dependent Claim
11 words
A peptide having the structure: ##STR31## in which TFA is trifluoroacetyl.
Claim 18
Dependent Claim
11 words
A peptide having the structure: ##STR31## in which TFA is trifluoroacetyl.
Claim 19
Dependent Claim
48 words
In a process for synthesizing a resin peptide, the step of coupling L-Pro-P with the reactant NH.sub.2 --Asn--CH.sub.2 -- R or an active ester or an azide thereof, said coupling being conducted in the presence of a diimide unless said reactant is an active ester or an azide.
Claim 20
Dependent Claim
48 words
In a process for synthesizing a resin peptide, the step of coupling L-Pro-P with the reactant NH.sub.2 --Asn--CH.sub.2 -- R or an active ester or an azide thereof, said coupling being conducted in the presence of a diimide unless said reactant is an active ester or an azide.
References Cited (Backward Citations)
US3531258A
Cited
US3743628A
Cited
US3912711A
Cited
US3886132A
Cited
US3987014A
Cited
US3915949A
Cited
US3917579A
Cited
US3988307A
Cited
US4002740A
Cited
US4022760A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-11-16 | 1985-05-18 | 1985-11-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-11-16 | 1989-05-18 | 1989-11-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-11-16 | 1993-05-18 | 1993-11-17 | $7700.00 | Window Closed / Lapsed |