US4093713A
Expired / Lapsed
US
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Dipeptide derivatives with central nervous system activity and preparation thereof
Assignee: Wyeth Canada Inc
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Filing: 1977-02-28
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Granted: 1978-06-06
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Expires: 1997-02-28
Abstract
Abstract The dipeptide derivatives of formula I H-L-Pro-N(R1)CH(R2)CO-NHR3(I) in which R1, R2 and R3 each independently is lower alkyl and a method for their preparation are disclosed. The dipeptide derivatives of formula I possess central nervous system activity and methods for their use are given.
Inventors
- 👤 Kazimir Sestanj
- 👤 Hans Ueli Immer
- 👤 Manfred Karl Gotz
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 07:28
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06139; C07K5/06165
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
30 words
A compound of formula I h--l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (I) in which R 1 , R 2 and R 3 each independently is lower alkyl, or a therapeutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
30 words
A compound of formula I h--l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (I) in which R 1 , R 2 and R 3 each independently is lower alkyl, or a therapeutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
45 words
A compound of formula I h--l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (I) in which R 1 and R 3 each independently is lower alkyl containing 1 to 2 carbon atoms and R 2 is lower alkyl containing 1 to 4 carbon atoms, or a therapeutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
45 words
A compound of formula I h--l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (I) in which R 1 and R 3 each independently is lower alkyl containing 1 to 2 carbon atoms and R 2 is lower alkyl containing 1 to 4 carbon atoms, or a therapeutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
7 words
L-Prolyl-L-N-methyl-leucine ethylamide, as claimed in claim 2.
Claim 6
Dependent Claim
7 words
L-Prolyl-D-N-methyl-leucine ethylamide, as claimed in claim 2.
Claim 7
Dependent Claim
9 words
The sulfate salt of the compound of claim 3.
Claim 8
Dependent Claim
9 words
The sulfate salt of the compound of claim 4.
Claim 9
Dependent Claim
31 words
A compound of formula II r.sup.4 --l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (II) in which R 1 , R 2 and R 3 each independently is lower alkyl and R 4 is an α-amino protecting group.
Claim 10
Dependent Claim
31 words
A compound of formula II r.sup.4 --l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (II) in which R 1 , R 2 and R 3 each independently is lower alkyl and R 4 is an α-amino protecting group.
Claim 11
Dependent Claim
8 words
t-Butoxycarbonyl-L-prolyl-L-N-methyl leucine ethylamide, as claimed in claim 7.
Claim 12
Dependent Claim
7 words
t-Butoxycarbonyl-L-prolyl-D-N-methyl-leucine ethylamide, as claimed in claim 7.
Claim 13
Dependent Claim
41 words
A method of treating or managing central nervous system disorders in a mammal which comprises administering to said mammal an effective amount of a compound of formula I, as claimed in claim 1, or a therapeutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim
13 words
The method as claimed in claim 10 wherein said compound is L-prolyl-L-N-methyl-leucine ethylamide.
Claim 15
Dependent Claim
13 words
The method as claimed in claim 10 wherein said compound is L-prolyl-D-N-methyl-leucine ethylamide.
Claim 16
Dependent Claim
27 words
A pharmaceutical composition comprising a compound of formula I or a therapeutically acceptable acid addition salt thereof, as claimed in claim 1, and a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim
14 words
The pharmaceutical composition as claimed in claim 13 wherein said compound is L-prolyl-L-N-methyl-leucine ethylamide.
Claim 18
Dependent Claim
14 words
The pharmaceutical composition as claimed in claim 13 wherein said compound is L-prolyl-D-N-methyl-leucine ethylamide.
Claim 19
Dependent Claim
43 words
A pharmaceutical composition in unit dosage form for treating Parkinson's disease comprising a combination of a compound of formula I of claim 1, or a therapeutically acceptable acid addition salt thereof, together with a therapeutic dose of levodopa and a pharmaceutically acceptable carrier.
Claim 20
Dependent Claim
14 words
The pharmaceutical composition as claimed in claim 16 wherein said compound is L-prolyl-L-N-methyl-leucine ethylamide.
Claim 21
Dependent Claim
14 words
The pharmaceutical composition as claimed in claim 16 wherein said compound is L-prolyl-D-N-methyl-leucine ethylamide.
References Cited (Backward Citations)
US4018912A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-06-05 | 1981-12-05 | 1982-06-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-06-05 | 1985-12-05 | 1986-06-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-06-05 | 1989-12-05 | 1990-06-06 | $7700.00 | Window Closed / Lapsed |