Patent US4148788A successfully refreshed from Google Patents.
US4148788A
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Synthesis of thymosin α1
Assignee: Sciclone Pharmaceuticals LLC
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Filing: 1978-06-19
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Granted: 1979-04-10
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Expires: 1998-06-19
Abstract
Abstract Thymosin α 1 , was chemically synthesized by the fragment condensation of the protected amino terminal tetradecapeptide with the protected carboxyl terminal tetradecapeptide and by solid phase peptide synthesis. Thymosin α 1 is active as an agent which affects regulation, differentiation and function of thymus dependent lymphocytes (T cells).
Inventors
- 👤 Su-Sun Wang
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 09:55
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/57581; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06034; C07K5/06043; C07K5/06052; C07K5/0606; C07K5/06069; C07K5/06086; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0819; C07K5/10; C07K5/1002; C07K5/1005; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/18
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
103 words
Ac-Ser(R 1 )-Asp(OR 2 )-Ala-Ala-Val-Asp(OR 2 )-Thr(R 3 )-Ser(R 1 )-Ser(R 1 )-Glu(OR 4 )-Ile-Thr(R 3 )-Thr(R 3 )-Lys(R 5 )-Asp(OR 2 )-Leu-Lys(R 5 )-Glu(OR 4 )-Lys(R 5 )-Lys(R 5 )-Glu(OR.sup.4)-Val-Val-Glu(OR 4 )-Glu(OR 4 )-Ala-Glu(OR 4 )-Asn-OR 6 wherein Ac is acetyl; R 1 is a conventional protecting group for the hydroxyl group of the serine residue; R 2 is a conventional carboxyl protecting group; R 3 is a conventional protecting group for the hydroxyl group of threonine; R 4 is a conventional carboxyl protecting group; R 5 is a conventional ω-amino protecting group; and R 6 is a conventional carboxyl protecting group.
Claim 2
Dependent Claim
103 words
Ac-Ser(R 1 )-Asp(OR 2 )-Ala-Ala-Val-Asp(OR 2 )-Thr(R 3 )-Ser(R 1 )-Ser(R 1 )-Glu(OR 4 )-Ile-Thr(R 3 )-Thr(R 3 )-Lys(R 5 )-Asp(OR 2 )-Leu-Lys(R 5 )-Glu(OR 4 )-Lys(R 5 )-Lys(R 5 )-Glu(OR.sup.4)-Val-Val-Glu(OR 4 )-Glu(OR 4 )-Ala-Glu(OR 4 )-Asn-OR 6 wherein Ac is acetyl; R 1 is a conventional protecting group for the hydroxyl group of the serine residue; R 2 is a conventional carboxyl protecting group; R 3 is a conventional protecting group for the hydroxyl group of threonine; R 4 is a conventional carboxyl protecting group; R 5 is a conventional ω-amino protecting group; and R 6 is a conventional carboxyl protecting group.
Claim 3
Dependent Claim
31 words
The compound of claim 1 wherein R 1 is benzyl, R 2 is benzyl, R 3 is benzyl, R 4 is benzyl, R 5 is benzyloxycarbonyl and R 6 is benzyl.
Claim 4
Dependent Claim
6 words
Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys and pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
6 words
Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys and pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
6 words
Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
6 words
Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim
6 words
Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim
6 words
Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
6 words
Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim
6 words
Glu-Val-Val-Glu-Glu-Ala-Glu-Asn and pharmaceutically acceptable salts thereof.
Claim 12
Dependent Claim
15 words
H-Asp(OBzl)-Leu-Lys(Z)-Glu(OBzl)-Lys(Z)-Lys(Z)-Glu(OBzl)-Val-Val-Glu(OBzl)-Glu(OBzl)-Ala-Glu(OBzl)-Asn-OBzl and the trifluoroacetic acid salt thereof, wherein Bzl is benzyl and Z is benzyloxycarbonyl.
Claim 13
Dependent Claim
15 words
H-Asp(OBzl)-Leu-Lys(Z)-Glu(OBzl)-Lys(Z)-Lys(Z)-Glu(OBzl)-Val-Val-Glu(OBzl)-Glu(OBzl)-Ala-Glu(OBzl)-Asn-OBzl and the trifluoroacetic acid salt thereof, wherein Bzl is benzyl and Z is benzyloxycarbonyl.
Claim 14
Dependent Claim
12 words
Ac-Ser(Bzl)-Asp(OBzl)-Ala-Ala-Val-Asp(OBzl)-Thr(Bzl)-Ser(Bzl)-Ser(Bzl)-Glu-(OBzl)-Ile-Thr(Bzl)-Thr(Bzl)-Lys(Z)-OH wherein Ac is acetyl, Bzl is benzyl and Z is benzyloxycarbonyl.
Claim 15
Dependent Claim
12 words
Ac-Ser(Bzl)-Asp(OBzl)-Ala-Ala-Val-Asp(OBzl)-Thr(Bzl)-Ser(Bzl)-Ser(Bzl)-Glu-(OBzl)-Ile-Thr(Bzl)-Thr(Bzl)-Lys(Z)-OH wherein Ac is acetyl, Bzl is benzyl and Z is benzyloxycarbonyl.
Claim 16
Dependent Claim
113 words
Ac-Ser(R 1 )-Asp(OR 2 )-Ala-Ala-Val(OR 2 )-Asp(OR 2 )-Thr(R 3 )-Ser(R 1 )-Ser(R 1 )-Glu (OR 4 )-Ile-Thr(R 3 )-Thr(R 3 )-Lys(R 5 )-Asp(OR 2 )-Leu-Lys(R 5 )-Glu(OR 4 )-Lys(R 5 )-Lys (R 5 )-Glu(OR 4 )-Val-Val-Glu(OR 4 )-Glu(OR 4 )-Ala-Glu(OR.sup.4)-Asp-(CONH-CH(C 6 H 5 )- ##STR2## Resin)-OR 2 wherein Ac is acetyl; R 1 is a conventional protecting group for the hydroxyl group of the serine residue; R 2 is a conventional carboxyl protecting group; R 3 is a conventional protecting group for the hydroxyl group of threonine; R 4 is a conventional carboxyl protecting group; R 5 is a conventional ω-amino protecting group and R 6 is a conventional carboxyl protecting group.
Claim 17
Dependent Claim
113 words
Ac-Ser(R 1 )-Asp(OR 2 )-Ala-Ala-Val(OR 2 )-Asp(OR 2 )-Thr(R 3 )-Ser(R 1 )-Ser(R 1 )-Glu (OR 4 )-Ile-Thr(R 3 )-Thr(R 3 )-Lys(R 5 )-Asp(OR 2 )-Leu-Lys(R 5 )-Glu(OR 4 )-Lys(R 5 )-Lys (R 5 )-Glu(OR 4 )-Val-Val-Glu(OR 4 )-Glu(OR 4 )-Ala-Glu(OR.sup.4)-Asp-(CONH-CH(C 6 H 5 )- ##STR2## Resin)-OR 2 wherein Ac is acetyl; R 1 is a conventional protecting group for the hydroxyl group of the serine residue; R 2 is a conventional carboxyl protecting group; R 3 is a conventional protecting group for the hydroxyl group of threonine; R 4 is a conventional carboxyl protecting group; R 5 is a conventional ω-amino protecting group and R 6 is a conventional carboxyl protecting group.
Claim 18
Dependent Claim
31 words
The compound of claim 9 wherein R 1 is benzyl, R 2 is benzyl, R 3 is benzyl, R 4 is benzyl, R 5 is 2,4-dichlorobenzyloxycarbonyl and R 6 is benzyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-09 | 1982-10-09 | 1983-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-09 | 1986-10-09 | 1987-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-09 | 1990-10-09 | 1991-04-10 | $7700.00 | Window Closed / Lapsed |