17 results about "Integrin ligand" patented technology

The present invention refers to: a) at least one peptide recognizing tumor endothelial cell markers, the peptide being preferably: —an αv-integrin ligand, preferably a ligand of αvβ3, βvβ5, αvβ8, α5β1 and / or αvβ6 integrin, more preferably the peptide includes a sequence having a RGD motif or of a CgA sequence or—a ligand of CD 13 receptor, more preferably the ligand includes a sequence having a NGR motif or functional fragments or derivatives or a biologically active variant thereof and b) saporin or functional fragments, derivatives or a biologically active variant thereof.

The invention discloses a CAIX targeted degradation agent. The CAIX targeted degradation agent comprises a CAIX target protein ligand, an integrin ligand and a connector, the CAIX target protein ligand and the integrin ligand are connected through the connecting body. As the carbonic anhydrase IX is enriched in the tumor region, the CAIX targeted degradation agent can specifically target the tumor region; the compound can effectively induce degradation of CAIX and inhibit survival of tumor cells under the hypoxia condition, has the functions of targeting a tumor area and degrading carbonic anhydrase IX by utilizing integrin and lysosome, further changes hypoxia and subacid environments of the internal environment of a tumor patient, and plays a role in inhibiting survival of hypoxia tumor cells; the tumor targeting property is high, the toxic and side effects on normal cells are relatively small, and a relatively good effect can be obtained by using a relatively small dosage.

The present invention relates to an integrin ligand key intermediate and a preparation method therefor, and specifically provides a new process for synthesizing target compound (7). Compared with existing synthesis processes, the new synthesis process can avoid racemic intermediate compound resolution, improve yields and reduce costs, thereby strongly supporting cost reduction and large-scale production of an αvβ6 integrin ligand.

Provided herein are compounds including delivery moieties for the selective delivery of a therapeutic and / or an oligonucleotide to the lungs. Also provided herein are compounds including a single delivery moiety for the selective delivery of a therapeutic and / or oligonucleotide to the lungs. Also disclosed herein are novel αvβx integrin ligands, such as ligands that associate with αvβ5, αvβ6, and / or αvβ8 integrins.

The invention provides a compound as shown in the following formula I, a tautomer or pharmaceutically acceptable salt thereof, and the compound has serum stability and affinity to integrin alpha v beta 6, has a better alpha v beta 6 integrin inhibition effect, and further has an inhibition effect on tumor growth.

The present invention relates to an integrin ligand and the use thereof. Specifically, provided is a compound represented by formula I or a stereoisomer thereof or a pharmaceutically acceptable salt thereof, or an αvβ6 integrin ligand comprising the compound represented by formula I or the stereoisomer thereof or the pharmaceutically acceptable salt thereof. The compound or the αvβ6 integrin ligand has a good serum stability and affinity for integrin αvβ6, and can be used for delivering a cargo molecule (such as an RNAi agent) or other oligonucleotide-based compounds to cells expressing integrin αvβ6, thereby promoting the uptake of the cargo molecule by these cells.

The invention provides a ligand compound targeting integrin, which can be conjugated with a small nucleic acid drug molecule in a covalent coupling manner to realize in vivo delivery of the small nucleic acid drug molecule, especially for non-hepatocyte delivery. The invention also provides an RNAi agent comprising the integrin ligand compound.

To provide methods of treating disease.SOLUTION: Synthetic αvβ6 integrin ligands of Formula I having serum stability and affinity for integrin αvβ6, which is a receptor expressed in a variety of cell types, are described. The described ligands are useful for delivering cargo molecules, such as RNAi agents or other oligonucleotide-based compounds, to cells that express integrin αvβ6, and thereby facilitating the uptake of the cargo molecules into these cells. Compositions that include αvβ6 integrin ligands and methods of use are also described.SELECTED DRAWING: None

The present invention provides double stranded ribonucleic acid (dsRNA) agents for inhibiting expression of a target gene, comprising an antisense strand which is complementary to the target gene; a sense strand which is complementary to the antisense strand and forms a double stranded region with the antisense strand; and at least one alpha-v-beta-6 (αvβ6) integrin targeting ligand that mediates delivery to an extrahepatic tissues, e.g., muscle tissue, e.g., skeletal muscle tissue and / or cardiac muscle tissue, or lung tissue, conjugated to at least one strand, compositions comprising such dsRNA agents, and methods of use thereof for treating a subject having a disorder that would benefit from reduction in expression of the target gene. The dsRNA may optionally contain an in vivo delivery enhancing agent.

Provided herein are α4β1 / 7 integrin receptor ligand-containing compounds, methods of delivering said compounds, and methods of treating diseases, disorders, and symptoms (e.g., central nervous system diseases, disorders, and symptoms) in a subject using said compounds.

This document provides compounds comprising a delivery portion for selectively delivering a therapeutic agent and / or oligonucleotide to the lungs. This document also provides compounds comprising a single delivery portion for selectively delivering a therapeutic agent and / or oligonucleotide to the lungs. This document also discloses novel α- v β x Integrin ligands, such as those with α v β5, α v β6 and / or α v Ligands that bind to β8 integrin.

The invention relates to an integrin ligand and application thereof, and particularly provides a compound shown in a formula I or a stereoisomer thereof or a pharmaceutically acceptable salt thereof, or an alpha v beta 6 integrin ligand which comprises the compound shown in the formula I or the stereoisomer thereof or the pharmaceutically acceptable salt thereof. The compounds or the [alpha] v [beta] 6 integrin ligands have good serum stability and affinity for integrin [alpha] v [beta] 6, and can be used to deliver transported molecules, such as RNAi agents, or other oligonucleotide-based compounds to cells expressing integrin [alpha] v [beta] 6, thereby promoting ingestion of the transported molecules to the cells.

The present invention provides: a double-stranded ribonucleic acid (dsRNA) agent for inhibiting the expression of a target gene, comprising an antisense strand complementary to the target gene; a sense strand complementary to the antisense strand and forming a double strand region with the antisense strand; and at least one alpha-v-beta-6 (alphavbeta6) integrin targeting ligand bound to the at least one strand that mediates delivery to extrahepatic tissue, such as muscular tissue, such as skeletal muscle tissue and / or cardiac muscle tissue, or lung tissue; compositions comprising such dsRNA agents; and methods of using the same to treat an individual having a condition that would benefit from reduced expression of the gene of interest.

The present invention provides double stranded ribonucleic acid (dsRNA) agents for inhibiting expression of a target gene, comprising an antisense strand which is complementary to the target gene; a sense strand which is complementary to the antisense strand and forms a double stranded region with the antisense strand; and at least one alpha-v-beta-6 (αvβ6) integrin targeting ligand that mediates delivery to an extrahepatic tissues, e.g., muscle tissue, e.g., skeletal muscle tissue and / or cardiac muscle tissue, or lung tissue conjugated to at least one strand, compositions comprising such dsRNA agents, and methods of use thereof for treating a subject having a disorder that would benefit from reduction in expression of the target gene.

To provide integrin ligands having serum stability and affinity for αvβ6 integrins.SOLUTION: Disclosed are peptide-based alpha-v beta-6 (αvβ6) integrin ligands useful in targeting αvβ6 integrin and / or targeting cells that express αvβ6 integrin. The αvβ6 integrin ligands can be conjugated to one or more cargo molecules to facilitate the delivery of the cargo molecules to cells expressing αvβ6 integrin, such as epithelial cells.SELECTED DRAWING: None

The present invention provides double stranded ribonucleic acid (dsRNA) agents for inhibiting expression of a target gene, comprising an antisense strand which is complementary to the target gene; a sense strand which is complementary to the antisense strand and forms a double stranded region with the antisense strand; and at least one alpha-v-beta-6 (αvβ6) integrin targeting ligand that mediates delivery to an extrahepatic tissues, e.g., muscle tissue, e.g., skeletal muscle tissue and / or cardiac muscle tissue, or lung tissue, conjugated to at least one strand, compositions comprising such dsRNA agents, and methods of use thereof for treating a subject having a disorder that would benefit from reduction in expression of the target gene. The dsRNA may optionally contain an in vivo delivery enhancing agent.

Integrin ligands having serum stability and affinity for avß6 integrins are described. Compositions comprising avß6 integrin ligands having serum stability and having affinity for avß6 integrins and methods of using them are also described. 20 24 20 26 95 24 A pr 2 02 4 A B S T R A C T 2 0 2 4 2 0 2 6 9 5 2 4 2 0 2 4 A p r