Cyclic octapeptide neuromedin B receptor antagonists
First Claim
1. A cyclic octapeptide of the formula:
- ##STR3## wherein;
A1 is D-Nal or D-Trp;
A3 is Phe, F5 -Phe, or X-Phe wherein X is a halogen, NO2, CH3, or OH;
A5 is --NH--CH(Y)--CO-- wherein Y is (CH2)m --R4 --N(R5)(R6) or (CH2)n --R4 --NH--C(R7)--N(R5) (R6);
A6 is the D-- or L-- isomer of an amino acid selected from the group consisting of Thr, Leu, Ile, Nle, Val, and Abu;
A8 is Nal or Trp;
m is 1, 2, or 3;
n is 1, 2, 3, 4 or 5;
each of R1 and R2, independently, is H, E, COE, or COOE wherein E is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, phenyl, naphthyl, C7-12 phenylalkyl or alkylphenyl, C8-12 phenylalkenyl or alkenylphenyl, C8-12 phenylalkynyl or alkynylphenyl, C11-20 naphthylalkyl or alkylnaphthyl, C12-20 naphthylalkenyl or alkenylnaphthyl, or C12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R1 or R2 is COE or COOE, the other must be H;
R4 is C6 H4 or absent;
R7 is ═
NR8, ═
S, or ═
O; and
each of R3, R5, R6, and R8, independently, is H or E.
3 Assignments
0 Petitions
Accused Products
Abstract
A cyclic octapeptide of the formula: ##STR1## wherein: A1 is D-Nal or D-Trp;
A3 is Phe, F5 -Phe, or X-Phe wherein X is a halogen, NO2, CH3, or OH;
A5 is --NH--CH(Y)--CO-- wherein Y is (CH2)m --R4 --N(R5)(R6) or (CH2)n --R4 --NH--C(R7)--N(R5) (R6);
A6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;
A8 is Nal or Trp;
m is 1, 2, or 3;
n is 1, 2, 3, 4 or 5;
each of R1 and R2, independently, is H, E, COE, or COOE wherein E is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, phenyl, naphthyl, C7-12 phenylalkyl or alkylphenyl, C8-12 phenylalkenyl or alkenylphenyl, C8-12 phenylalkynyl or alkynylphenyl, C11-20 naphthylalkyl or alkylnaphthyl, C12-20 naphthylalkenyl or alkenylnaphthyl, or C12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R1 or R2 is COE or COOE, the other must be H;
R4 is C6 H4 or absent;
R7 is ═NR8, ═S, or ═O; and
each of R3, R5, R6, and R8, independently, is H or E.
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Citations
24 Claims
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1. A cyclic octapeptide of the formula:
- ##STR3## wherein;
A1 is D-Nal or D-Trp;A3 is Phe, F5 -Phe, or X-Phe wherein X is a halogen, NO2, CH3, or OH; A5 is --NH--CH(Y)--CO-- wherein Y is (CH2)m --R4 --N(R5)(R6) or (CH2)n --R4 --NH--C(R7)--N(R5) (R6); A6 is the D-- or L-- isomer of an amino acid selected from the group consisting of Thr, Leu, Ile, Nle, Val, and Abu; A8 is Nal or Trp; m is 1, 2, or 3; n is 1, 2, 3, 4 or 5; each of R1 and R2, independently, is H, E, COE, or COOE wherein E is C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, phenyl, naphthyl, C7-12 phenylalkyl or alkylphenyl, C8-12 phenylalkenyl or alkenylphenyl, C8-12 phenylalkynyl or alkynylphenyl, C11-20 naphthylalkyl or alkylnaphthyl, C12-20 naphthylalkenyl or alkenylnaphthyl, or C12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R1 or R2 is COE or COOE, the other must be H; R4 is C6 H4 or absent; R7 is ═
NR8, ═
S, or ═
O; andeach of R3, R5, R6, and R8, independently, is H or E. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
- ##STR3## wherein;
Specification
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- Resources
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Current AssigneeAdministrators Of The Tulane Educational Fund (ADMINISTRATORS|DAVID H. COY), Blomeasure, Inc., Societe de Conseils de Recherches et d'Applications Scientifiques
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Original AssigneeAdministrators Of The Tulane Educational Fund (ADMINISTRATORS|DAVID H. COY), Biomeasure, Inc. (Ipsen Sa)
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InventorsTaylor, John E., Coy, David H.
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Primary Examiner(s)DAVENPORT, AVIS MICHELLE
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Application NumberUS08/352,392Time in Patent Office691 DaysField of Search530/311, 530/328, 530/317, 514/15, 514/16, 514/17US Class Current530/311CPC Class CodesA61K 38/31 SomatostatinsA61P 43/00 Drugs for specific purposes...C07K 14/6555 at least 1 amino acid in D-...
