Patent classifications
C07K7/083
Macrocyclic compounds and methods of preventing or treating pain
The present invention provides a macrocyclic compound of formula (I) ##STR00001## compositions and kits comprising this compound and their use for preventing or treating pain, or inducing hypothermia or hypotension.
PEPTIDE COMPOUNDS AND PEPTIDE CONJUGATES FOR THE TREATMENT OF CANCER THROUGH RECEPTOR-MEDIATED CHEMOTHERAPY
The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer. For example, the compounds can comprise compounds of formula
TABLE-US-00001 X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (I) (SEQ ID NO: 1) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (II) (SEQ ID NO: 2) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (III) (SEQ ID NO: 3) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (IV) (SEQ ID NO: 4) IKLSGGVQAKAGVINMDKSESM (V) (SEQ ID NO: 5) IKLSGGVQAKAGVINMFKSESY (VI) (SEQ ID NO: 6) IKLSGGVQAKAGVINMFKSESYK (VII) (SEQ ID NO: 7) GVQAKAGVINMFKSESY (VIII) (SEQ ID NO: 8) GVRAKAGVRNMFKSESY (IX) (SEQ ID NO: 9) GVRAKAGVRN(Nle)FKSESY (X) (SEQ ID NO: 10) YKSLRRKAPRWDAPLRDPALRQLL (XI) (SEQ ID NO: 11) YKSLRRKAPRWDAYLRDPALRQLL (XII) (SEQ ID NO: 12) YKSLRRKAPRWDAYLRDPALRPLL (XIII) (SEQ ID NO: 13) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end.
CHIMERIC POLYPEPTIDES AND USES THEREOF
The present invention relates to a nucleic acid molecule encoding a chimeric polypeptide comprising a peptide of interest fused to one or more heterologous moieties, wherein at least one of the heterologous moieties is a ligand of the Sortilin receptor. The invention also relates to a chimeric polypeptide encoded by said nucleic acid molecule and uses thereof.
DUAL AGONIST GLP-1 AND NEUROTENSIN FUSION PEPTIDE
The present invention relates to a polypeptide comprising a first peptide linked to a second peptide, optionally via a linker molecule, which first peptide comprises an appetite regulating hormone peptide, e.g. glucagon like peptide 1 (GLP-1), such as amino acids 7-37 of the initial GLP-1 product (1-37), and a Neurotensin (NT) like peptide, targeting both the GLP-1 receptor (GLP-1R) and NT receptors (NTR1-3) and display an increased effect on decrease of appetite and food intake and body weight compared to simultaneous administration of both peptides.
Activated neurotensin molecules and the uses thereof
The present invention relates to activated neurotensin, pharmaceutical compositions comprising the same, and the uses thereof. The compounds and compositions of the invention may be used, e.g., to reduce body temperature, attenuate or halt seizures, reduce excitotoxicity, promote neuroprotection, reduce neuroinflammation and aberrant axonal sprouting or reduce pain.
Neurotensin analogues for radioisotope targeting to neurotensin receptor-positive tumors
The invention relates to a new neurotensin analogue, or a salt thereof, useful for targeting to neurotensin receptor-positive tumors, like ductal pancreatic adenocarcinoma, exocrine pancreatic cancer, invasive ductal breast cancers, colon adenocarcinoma, small cell lung carcinoma, Ewing sarcoma, meningioma, medulloblastoma and astrocytoma.
METHODS AND COMPOUNDS FOR TARGETING SORTILIN RECEPTORS AND INHIBITING VASCULOGENIC MIMICRY
The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treatment of cancer or aggressive cancer. For example, the compounds can comprise compounds of formula X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (I) (SEQ ID NO: 1) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (II) (SEQ ID NO: 2) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (III) (SEQ ID NO: 3) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (IV) (SEQ ID NO: 4) IKLSGGVQAKAGVINMDKSESM (V) (SEQ ID NO: 5) IKLSGGVQAKAGVINMFKSESY (VI) (SEQ ID NO: 6) IKLSGGVQAKAGVINMFKSESYK (VII) (SEQ ID NO: 7) GVQAKAGVINMFKSESY (VIII) (SEQ ID NO: 8) GVRAKAGVRNMFKSESY (IX) (SEQ ID NO: 9) GVRAKAGVRN(Nle)FKSESY (X) (SEQ ID NO: 10) YKSLRRKAPRWDAPLRDPALRQLL (XI) (SEQ ID NO: 11) YKSLRRKAPRWDAYLRDPALRQLL (XII) (SEQ ID NO: 12) YKSLRRKAPRWDAYLRDPALRPLL (XIII) (SEQ ID NO: 13) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end, for use in inhibiting vasculogenic mimicry and/or for treating a cancer.
Peptide compounds and peptide conjugates for the treatment of cancer through receptor-mediated chemotherapy
The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer. For example, the compounds can comprise compounds of formula TABLE-US-00001 X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (SEQ ID NO: 1) (I) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (SEQ ID NO: 2) (II) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (SEQ ID NO: 3) (III) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (SEQ ID NO: 4) (IV) IKLSGGVQAKAGVINMDKSESM (SEQ ID NO: 5) (V) IKLSGGVQAKAGVINMFKSESY (SEQ ID NO: 6) (VI) IKLSGGVQAKAGVINMFKSESYK (SEQ ID NO: 7) (VII) GVQAKAGVINMFKSESY (SEQ ID NO: 8) (VIII) GVRAKAGVRNMFKSESY (SEQ ID NO: 9) (IX) GVRAKAGVRN(Nle)FKSESY (SEQ ID NO: 10) (X) YKSLRRKAPRWDAPLRDPALRQLL (SEQ ID NO: 11) (XI) YKSLRRKAPRWDAYLRDPALRQLL (SEQ ID NO: 12) (XII) YKSLRRKAPRWDAYLRDPALRPLL (SEQ ID NO: 13) (XIII) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end.
CONJUGATED OLIGONUCLEOTIDES AND USES THEREOF
Disclosed herein are compounds that comprise an oligonucleotide, a conjugate linker, and a conjugate moiety capable of interacting with a cell surface moiety, wherein the oligonucleotide and the conjugate moiety are connected via the conjugate linker. The conjugate moiety may comprise a cell-targeting moiety and a peptide extender. In general, peptide extenders have sufficient length and/or structure to reduce or prevent interaction between the oligonucleotide and the cell-targeting moiety. Such compounds are useful to treat, prevent or ameliorate a condition or disease in an individual with limited off-target effects.
PEPTIDE ANALOGS
Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulatng activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.