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Histidine derivatives

Assignee: Reckitt Benckiser Healthcare UK Ltd
•
Filing: 1976-02-20
•
Granted: 1977-11-29
•
Expires: 1996-02-20
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Abstract

Abstract Compounds of the formula ##STR1## wherein R, R 1 , R 2 , R 3 and R 4 represent certain specified substituent groups. The compounds exhibit activity in the reserpine induced hypothermia test.

Inventors

  • 👤 Barry A. Morgan
  • 👤 Derek J. Schafer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 20:26
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0821; C07K5/0825

Claims Analysis

Total Claims: 24
Claim 1
Independent Claim 56 words
Compounds of the formula: ##STR5## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl or alkoxy C 1-3 ; R 2 is hydrogen, alkyl or alkoxy C 1-3 ; R 3 is hydrogen, alkyl C 1-6 , or cycloalkyl C 3-6 ; and R 4 is hydrogen or alkyl C 1-6 .
Claim 2
Dependent Claim 56 words
Compounds of the formula: ##STR5## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl or alkoxy C 1-3 ; R 2 is hydrogen, alkyl or alkoxy C 1-3 ; R 3 is hydrogen, alkyl C 1-6 , or cycloalkyl C 3-6 ; and R 4 is hydrogen or alkyl C 1-6 .
Claim 3
Dependent Claim 33 words
Compounds of the formula: ##STR6## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl or alkoxy C 1-3 ; R 2 is hydrogen, alkyl or alkoxy C 1-3 .
Claim 4
Dependent Claim 33 words
Compounds of the formula: ##STR6## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl or alkoxy C 1-3 ; R 2 is hydrogen, alkyl or alkoxy C 1-3 .
Claim 5
Dependent Claim 53 words
Compounds of the formula: ##STR7## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl C 1-3 ; R 2 is hydrogen or alkyl C 1-3 ; R 3 is hydrogen, alkyl C 1-6 , or cycloalkyl C 3-6 ; and R 4 is hydrogen or alkyl C 1-6 .
Claim 6
Dependent Claim 53 words
Compounds of the formula: ##STR7## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl C 1-3 ; R 2 is hydrogen or alkyl C 1-3 ; R 3 is hydrogen, alkyl C 1-6 , or cycloalkyl C 3-6 ; and R 4 is hydrogen or alkyl C 1-6 .
Claim 7
Dependent Claim 40 words
A compound of Formula I as claimed in claim 3 wherein R is hydrogen or methyl; R 1 is methyl or ethyl; R 2 is hydrogen of methyl; R 3 is hydrogen, hexyl or cyclohexyl; and R 4 is hydrogen.
Claim 8
Dependent Claim 22 words
A pharmaceutical composition which comprises a compound of Formula I as claimed in claim 3 and a pharmaceutically acceptable diluent or carrier.
Claim 9
Dependent Claim 30 words
Compounds of the formula: ##STR8## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl C 1-3 ; R 2 is hydrogen or alkyl C 1-3 .
Claim 10
Dependent Claim 30 words
Compounds of the formula: ##STR8## wherein R is hydrogen or alkyl C 1-3 ; R 1 is alkyl C 1-3 ; R 2 is hydrogen or alkyl C 1-3 .
Claim 11
Dependent Claim 29 words
A compound of Formula Ia as claimed in claim 6 wherein R is hydrogen or methyl; R 1 is methyl or ethyl; and R 2 is hydrogen or methyl.
Claim 12
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolineamide.
Claim 13
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolineamide.
Claim 14
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-ethyl-dl-prolineamide.
Claim 15
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-ethyl-dl-prolineamide.
Claim 16
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-3,3-dimethyl-dl-prolineamide.
Claim 17
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-3,3-dimethyl-dl-prolineamide.
Claim 18
Dependent Claim 2 words
L-Pyroglutamyl-N.sup.α -methyl-L-histidyl-trans-3-methyl-L-prolineamide.
Claim 19
Dependent Claim 2 words
L-Pyroglutamyl-N.sup.α -methyl-L-histidyl-trans-3-methyl-L-prolineamide.
Claim 20
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolinecyclohexylamide.
Claim 21
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolinecyclohexylamide.
Claim 22
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolinehexylamide.
Claim 23
Dependent Claim 1 words
L-Pyroglutamyl-L-histidyl-trans-3-methyl-L-prolinehexylamide.
Claim 24
Dependent Claim 25 words
A pharmaceutical composition as claimed in claim 5 in unit dosage form for oral administration which comprises from 1 to 100 mg of said compound.

References Cited (Backward Citations)

US3931139A Cited
US3959248A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-11-28 1981-05-30 1981-11-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-11-28 1985-05-30 1985-11-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-11-28 1989-05-30 1989-11-29 $7700.00 Window Closed / Lapsed

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