US 2003/0144210 A1Published application

Gamma-carboxyglutamate containing conopeptides

OwnerBaldomero M. Olivera, J. Michael McIntosh +4inventors

InventorsBaldomero M. Olivera, J. Michael McIntosh, James E. Garrett, Craig S. Walker, Maren Watkins, Robert M. Jones

Life of this patent

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Abstract

The invention relates to γ-carboxyglutamate containing conopeptides, derivatives or pharmaceutically acceptable salts thereof, and uses thereof, including the treatment of neurologic and psychiatric disorders, such as anticonvulsant agents, as neuroprotective agents or for the management of pain. The invention further relates to nucleic acid sequences encoding the conopeptides and encoding propeptides, as well as the propeptides.

Claims24

Dependent claims

An isolated peptide selected from the group consisiting of:

Conopeptide JG001:
Gly-Xaa1-Asp-Xaa1-Val-Ser-Gln-Met-Ser-Xaa2-Xaa1-Ile-Leu-Arg-Xaa1-Leu-Glu-Leu -Gln-Xaa2 (SEQ ID NO:
1);
Conantokin-G[L5Y]:
Gly-Xaa1-Xaa1-Xaa1-Xaa3-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaal-Xaa2-Ser-Asn (SEQ ID NO:
2);
Conantokin-G[G1A]:
Ala-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
3);
Conantokin-G[L11A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Ala-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
4);
Conantokin-G[L11A, 112A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Ala-Ala-Arg -Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
5);
Conantokin-G[I12A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1Leu-Ala-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
6);
Conantokin-G[S16A, N17A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg -Xaa1-Xaa2-Ala-Ala (SEQ ID NO:
7);
Conantokin-G[E2D]:
Gly-Asp-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
8);
Conantokin-G[E2dD]:
Gly-D-Asp-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
9);
Conantokin-G-desG1:
Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
10);
Conantokin-G-desG1/E2:
Xaa1-Xaa1-Leu-Gln-Xaa2-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
11);
Conantokin-G[E2Q]:
Gly-Gln-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
12);
Conantokin-G[G1S]:
Ser-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1 -Xaa2-Ser-Asn (SEQ ID NO:
13);
Conantokin-G[K15A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Ala -Ser-Asn (SEQ ID NO:
14);
Conantokin-G[L5V, K15A]:
Gly-Xaa1-Xaa1-Xaa1-Val-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg -Xaa1-Ala-Ser-Asn (SEQ ID NO:
15);
Conopeptide-A:
Gly-Glu-Asp-Xaa1-Val-Ser-Gln-Met-Ser-Xaa2-Xaa1-Ile-Leu-Arg-Xaa1-Leu-Xaa2-Xaa2 ,-Xaa2-Xaa2 (SEQ ID NO:
16);
Conopeptide-R2:
Xaa3-Xaa3-Xaa1-Xaa1-Asp-Arg-Leu-Arg-Arg-Xaa4-Leu-Ala-Asn-Ser-Xaa2-Xaa2 (SEQ ID NO:
17);
Conopeptide-O1:
Ile-Xaa1-Xaa1-Gly-Leu-Ile-Xaa1-Asp-Leu-Xaa1-Thr-Ala-Arg-Xaa1-Arg-Asn-Ser (SEQ ID NO:
18);
Conopeptide-O1A:
Ile-Xaa1-Xaa1-Gly-Leu-Ile-Xaa1-Asp-Leu-Xaa1-Thr-Val-Arg-Xaa1-Arg-Asn-Ser (SEQ ID NO:
19);
Conopeptide-O2:
Arg-Asp-Xaa1-Xaa1-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Ile-Leu-Xaa1-Leu-Glu-Arg-Asn (SEQ ID NO:
20);
Conopeptide-O2A:
Ser-Asp-Xaa1-Xaa1-Leu-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Val-Leu-Xaa1-Leu-Glu-Arg -Asn (SEQ ID NO:
21);
Conopeptide-O2B:
Arg-Asp-Xaa1-Xaa1-Leu-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Ile-Leu-Xaa1-Leu-Glu-Arg -Asn (SEQ ID NO:
22);
Conopeptide-Ar:
Gly-Phe-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Leu-Ala-Asn-Xaa1-Leu-Xaa1-Xaa1,-Ile (SEQ ID NO:
23);
Conopeptide-Lv1:
Gly-Asn-Xaa1-Asp-His-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Ile-Arg-Xaa1-Leu-Gln-Val-Leu-Leu-Xaa2Xaa1-Xaa2-Asp (SEQ ID NO:
24);
Conopeptide-Lv2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Asn-Ile-Xaa1-Leu-Asp-Val -Ala-Gly-Xaa2-Xaa1-Asn-Asp (SEQ ID NO:
25);
Conopeptide-Lv3:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Asn-Ile-Arg-Xaa1-Leu-Gln -Val-Gln-Xaa1-Xaa2-Xaa1-Asn-Asp (SEQ ID NO:
26);
Conopeptide-Qc2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Val-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Val-Ala (SEQ ID NO:
27);
Conopeptide-Im1:
Gly-Xaa3-Xaa1-Xaa1-Xaa1-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1 -Leu-Xaa1-Xaa1-Ala (SEQ ID NO:
28);
Conopeptide-Im2:
Gly-Xaa4-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ile (SEQ ID NO:
29);
Conopeptide-Im3:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Leu-Xaa1-Thr-Val-Ser-Xaa1-Leu-Xaa1-Xaa1-Ile (SEQ ID NO:
30);
Conopeptide-Em:
Gly-Xaa3-Xaa1-Xaa1-Xaa1-Arg-Xaa1-Val-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ala (SEQ ID NO :31);
Conopeptide-Ca3:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Ile-Asn-Xaa1-Leu-Asp-Xaa1-Ile (SEQ ID NO:
32);
Conopeptide-Ca4:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Ile-Asn-Xaa1-Leu-Asp-Xaa2-Ile (SEQ ID NO:
33);
Conopeptide-Ca5:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Met-Asn-xaa1-Leu-Asp-Xaa2-Ile (SEQ ID NO:
34);
Conopeptide-Vr1:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Val-Ala (SEQ ID NO:
35);
Conopeptide-Vr2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ala (SEQ ID NO:
36);
Conopeptide-Cn:
Gly-Xaa1-Xaa1-Xaa1-Val-Gly-Asn-Ile-Xaa5-Xaa1-Ile-Val-Arg-Gln-Gln-Xaa1-Cys-Ile -Arg-Asn-Asn-Asn-Asn-Arg-Xaa5-Xaa4-Cys-Xaa5-Xaa2 (SEQ ID NO:
37);
Conopeptide-Cn2:
Gly-Xaa1-Xaa1-Xaa1-Val-Gly-Asn-Ile-Xaa5-Xaa1-Ile-Val-Arg-Gln-Gln-Xaa1-Cys -Ile-Arg-Asn-Asn-Asn-Asn-Arg-Xaa5-Xaa4-Cys-Xaa5-Xaa2 (SEQ ID NO:
38);
Conopeptide-Cj1:
Asp-Xaa1-Xaa5-Xaa1-Xaa3-Ala-Xaa1-Ala-Ile-Arg-Xaa1-Xaa3-Gln-Leu -Xaa2-Xaa3-Gly-Xaa2-Ile (SEQ ID NO:
39);
Conopeptide-Cj2:
Gly-Xaa1-Asp-Xaa1-Xaa3-Ala-Xaa1-Gly-Ile-Arg-Xaa1-Xaa3-Gln-Leu-Ile-His -Gly-Xaa2-Ile (SEQ ID NO:
40);
and
Conopeptide-Cx:
Gly-Xaa1-Xaa1-Xaa1-Val-Ala-Xaa2-Met-Ala-Ala-Xaa1-Ile-Ala-Arg-Xaa1-Asn-Ala-Ala -Xaa1 (SEQ ID NO:
41);
wherein Xaa1 is Glu or γ-carboxyglutamic acid (Gla);
Xaa2 is Lys, nor-Lys, N-methyl-Lys, N,N-dimethyl-Lys or N,N,N-trimethyl-Lys;
Xaa3 is Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr or nitro-Tyr;
Xaa4 is Trp (D or L) or halo-Trp (D or L);
and Xaa5 is Pro or hydroxy-Pro. The halo is preferably chlorine, bromine or iodine, more preferably iodine for Tyr and bromine for Trp

125 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/207,780Filed 31 Jul 2002
Priority: 10 Sep 1999
Published: 31 Jul 2003
Term ends: Not estimatedThe source records don’t support an estimate.

Classification28 codes

C07K 7/08
Linear peptides containing only normal peptide links: having 12 to 20 amino acids
A61P 3/08
Drugs for disorders of the metabolism: for glucose homeostasis
A61P 9/00
Drugs for disorders of the cardiovascular system
A61P 9/10
Drugs for disorders of the cardiovascular system: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary…

Family

Application60/153,034Us provisional application · filed 10 Sep 1999
Application60/219,673Us provisional application · filed 21 Jul 2000
Application09/658,603Continuation · filed 8 Sep 2000
Application10/207,780Continuation · filed 31 Jul 2002
US 2003/0144210 A1This patent

From the US filing history. Foreign family members aren’t listed.

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Abstract

An isolated peptide selected from the group consisiting of:

Conopeptide JG001:
Gly-Xaa1-Asp-Xaa1-Val-Ser-Gln-Met-Ser-Xaa2-Xaa1-Ile-Leu-Arg-Xaa1-Leu-Glu-Leu -Gln-Xaa2 (SEQ ID NO:
1);
Conantokin-G[L5Y]:
Gly-Xaa1-Xaa1-Xaa1-Xaa3-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaal-Xaa2-Ser-Asn (SEQ ID NO:
2);
Conantokin-G[G1A]:
Ala-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
3);
Conantokin-G[L11A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Ala-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
4);
Conantokin-G[L11A, 112A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Ala-Ala-Arg -Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
5);
Conantokin-G[I12A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1Leu-Ala-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
6);
Conantokin-G[S16A, N17A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg -Xaa1-Xaa2-Ala-Ala (SEQ ID NO:
7);
Conantokin-G[E2D]:
Gly-Asp-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
8);
Conantokin-G[E2dD]:
Gly-D-Asp-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
9);
Conantokin-G-desG1:
Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
10);
Conantokin-G-desG1/E2:
Xaa1-Xaa1-Leu-Gln-Xaa2-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2 -Ser-Asn (SEQ ID NO:
11);
Conantokin-G[E2Q]:
Gly-Gln-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Xaa2-Ser-Asn (SEQ ID NO:
12);
Conantokin-G[G1S]:
Ser-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1 -Xaa2-Ser-Asn (SEQ ID NO:
13);
Conantokin-G[K15A]:
Gly-Xaa1-Xaa1-Xaa1-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Ala -Ser-Asn (SEQ ID NO:
14);
Conantokin-G[L5V, K15A]:
Gly-Xaa1-Xaa1-Xaa1-Val-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg -Xaa1-Ala-Ser-Asn (SEQ ID NO:
15);
Conopeptide-A:
Gly-Glu-Asp-Xaa1-Val-Ser-Gln-Met-Ser-Xaa2-Xaa1-Ile-Leu-Arg-Xaa1-Leu-Xaa2-Xaa2 ,-Xaa2-Xaa2 (SEQ ID NO:
16);
Conopeptide-R2:
Xaa3-Xaa3-Xaa1-Xaa1-Asp-Arg-Leu-Arg-Arg-Xaa4-Leu-Ala-Asn-Ser-Xaa2-Xaa2 (SEQ ID NO:
17);
Conopeptide-O1:
Ile-Xaa1-Xaa1-Gly-Leu-Ile-Xaa1-Asp-Leu-Xaa1-Thr-Ala-Arg-Xaa1-Arg-Asn-Ser (SEQ ID NO:
18);
Conopeptide-O1A:
Ile-Xaa1-Xaa1-Gly-Leu-Ile-Xaa1-Asp-Leu-Xaa1-Thr-Val-Arg-Xaa1-Arg-Asn-Ser (SEQ ID NO:
19);
Conopeptide-O2:
Arg-Asp-Xaa1-Xaa1-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Ile-Leu-Xaa1-Leu-Glu-Arg-Asn (SEQ ID NO:
20);
Conopeptide-O2A:
Ser-Asp-Xaa1-Xaa1-Leu-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Val-Leu-Xaa1-Leu-Glu-Arg -Asn (SEQ ID NO:
21);
Conopeptide-O2B:
Arg-Asp-Xaa1-Xaa1-Leu-Leu-Arg-Xaa1-Asp-Val-Xaa1-Thr-Ile-Leu-Xaa1-Leu-Glu-Arg -Asn (SEQ ID NO:
22);
Conopeptide-Ar:
Gly-Phe-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Leu-Ala-Asn-Xaa1-Leu-Xaa1-Xaa1,-Ile (SEQ ID NO:
23);
Conopeptide-Lv1:
Gly-Asn-Xaa1-Asp-His-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Ile-Arg-Xaa1-Leu-Gln-Val-Leu-Leu-Xaa2Xaa1-Xaa2-Asp (SEQ ID NO:
24);
Conopeptide-Lv2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Asn-Ile-Xaa1-Leu-Asp-Val -Ala-Gly-Xaa2-Xaa1-Asn-Asp (SEQ ID NO:
25);
Conopeptide-Lv3:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Asn-Ile-Arg-Xaa1-Leu-Gln -Val-Gln-Xaa1-Xaa2-Xaa1-Asn-Asp (SEQ ID NO:
26);
Conopeptide-Qc2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Val-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Val-Ala (SEQ ID NO:
27);
Conopeptide-Im1:
Gly-Xaa3-Xaa1-Xaa1-Xaa1-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1 -Leu-Xaa1-Xaa1-Ala (SEQ ID NO:
28);
Conopeptide-Im2:
Gly-Xaa4-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ile (SEQ ID NO:
29);
Conopeptide-Im3:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Leu-Xaa1-Thr-Val-Ser-Xaa1-Leu-Xaa1-Xaa1-Ile (SEQ ID NO:
30);
Conopeptide-Em:
Gly-Xaa3-Xaa1-Xaa1-Xaa1-Arg-Xaa1-Val-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ala (SEQ ID NO :31);
Conopeptide-Ca3:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Ile-Asn-Xaa1-Leu-Asp-Xaa1-Ile (SEQ ID NO:
32);
Conopeptide-Ca4:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Ile-Asn-Xaa1-Leu-Asp-Xaa2-Ile (SEQ ID NO:
33);
Conopeptide-Ca5:
Cys-Leu-Xaa1-Xaa1-Val-Leu-Xaa1-Ile-Val-Xaa1-Thr-Met-Asn-xaa1-Leu-Asp-Xaa2-Ile (SEQ ID NO:
34);
Conopeptide-Vr1:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Val-Ala (SEQ ID NO:
35);
Conopeptide-Vr2:
Gly-Xaa3-Xaa1-Xaa1-Asp-Arg-Xaa1-Ile-Ala-Xaa1-Thr-Val-Arg-Xaa1-Leu-Xaa1-Xaa1-Ala (SEQ ID NO:
36);
Conopeptide-Cn:
Gly-Xaa1-Xaa1-Xaa1-Val-Gly-Asn-Ile-Xaa5-Xaa1-Ile-Val-Arg-Gln-Gln-Xaa1-Cys-Ile -Arg-Asn-Asn-Asn-Asn-Arg-Xaa5-Xaa4-Cys-Xaa5-Xaa2 (SEQ ID NO:
37);
Conopeptide-Cn2:
Gly-Xaa1-Xaa1-Xaa1-Val-Gly-Asn-Ile-Xaa5-Xaa1-Ile-Val-Arg-Gln-Gln-Xaa1-Cys -Ile-Arg-Asn-Asn-Asn-Asn-Arg-Xaa5-Xaa4-Cys-Xaa5-Xaa2 (SEQ ID NO:
38);
Conopeptide-Cj1:
Asp-Xaa1-Xaa5-Xaa1-Xaa3-Ala-Xaa1-Ala-Ile-Arg-Xaa1-Xaa3-Gln-Leu -Xaa2-Xaa3-Gly-Xaa2-Ile (SEQ ID NO:
39);
Conopeptide-Cj2:
Gly-Xaa1-Asp-Xaa1-Xaa3-Ala-Xaa1-Gly-Ile-Arg-Xaa1-Xaa3-Gln-Leu-Ile-His -Gly-Xaa2-Ile (SEQ ID NO:
40);
and
Conopeptide-Cx:
Gly-Xaa1-Xaa1-Xaa1-Val-Ala-Xaa2-Met-Ala-Ala-Xaa1-Ile-Ala-Arg-Xaa1-Asn-Ala-Ala -Xaa1 (SEQ ID NO:
41);
wherein Xaa1 is Glu or γ-carboxyglutamic acid (Gla);
Xaa2 is Lys, nor-Lys, N-methyl-Lys, N,N-dimethyl-Lys or N,N,N-trimethyl-Lys;
Xaa3 is Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr or nitro-Tyr;
Xaa4 is Trp (D or L) or halo-Trp (D or L);
and Xaa5 is Pro or hydroxy-Pro. The halo is preferably chlorine, bromine or iodine, more preferably iodine for Tyr and bromine for Trp

125 more elements

Facts

Application

10/207,780Filed 31 Jul 2002

Priority

10 Sep 1999

Published

31 Jul 2003

Term ends

Not estimatedThe source records don’t support an estimate.

Classification28 codes

C07K 7/08
Linear peptides containing only normal peptide links: having 12 to 20 amino acids
A61P 3/08
Drugs for disorders of the metabolism: for glucose homeostasis
A61P 9/00
Drugs for disorders of the cardiovascular system
A61P 9/10
Drugs for disorders of the cardiovascular system: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary…

Family

Application60/153,034Us provisional application · filed 10 Sep 1999

Application60/219,673Us provisional application · filed 21 Jul 2000

Application09/658,603Continuation · filed 8 Sep 2000

Application10/207,780Continuation · filed 31 Jul 2002

US 2003/0144210 A1This patent

From the US filing history. Foreign family members aren’t listed.