38 results about "Receptor binding sites" patented technology

The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula wherein: R1, R2, and R3 are as defined herein and pharmaceutically acceptable acid addition salts thereof. These compounds have high affinity and selectivity for GABA A α5 receptor binding sites. The invention also relates to methods for enhancing cognition and treating cognitive disorders like Alzheimer's disease.

The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formulawhereinR1,R2, andR3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention pertains to the provision of trimeric binding units which bind to trimeric cytokines. In particular there is provided a trimeric polypeptide comprising a trimerising domain and three monomers with binding members capable of binding a trimeric cytokine. Preferably , the trimeric binding units bind in a manner such that upon binding, all receptor binding sites of the trimeric cytokine are substantially blocked, and hence the potential biological activity of the trimeric cytokine is suppressed. In one aspect the invention relates to trimeric binders capable of binding to trimeric cytokines of the Tumor necrosis factor ligand superfamily, such as TNF, TRAIL, RANKL, TWEAK, APRIL and BAFF.

The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defmed in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The invention relates to a graphene oxide targeted drug carrier material. The graphene oxide targeted drug carrier material contains RGDF polypeptide molecules, a graphene oxide material and an anti-tumor drug loaded by graphene oxide, wherein the RGDF polypeptide molecules and the graphene oxide material are linked through covalent bonds; active functional groups of graphene oxide include amino and / or hydroxy, carboxyl and epoxy group; and the graphene oxide material is a product prepared by carrying out amidation reaction on the RGDF polypeptide molecules and aminated graphene oxide. A drugcarrier provided by the invention has biocompatibility, small toxic and side effects, good dissolving property and high drug loading ratio; after entering a human body, the carrier loading the anti-tumor drug can stably circulate in the human body, and the anti-tumor drug can be enriched at tumor cells by virtue of the polypeptide molecules, so that the targeting property is realized; and besides,receptor binding sites on polypeptide are not exposed outside, so that the stability of the anti-tumor polypeptide molecules in the human body is improved.

The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula I wherein R1, R2, and R3 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. These compounds have a high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention pertains to the provision of trimeric binding units which bind to trimeric cytokines. In particular there is provided a trimeric polypeptide comprising a trimerising domain and three monomers with binding members capable of binding a trimeric cytokine. Preferably, the trimeric binding units bind in a manner such that upon binding, all receptor binding sites of the trimeric cytokine are substantially blocked, and hence the potential biological activity of the trimeric cytokine is suppressed. In one aspect the invention relates to trimeric binders capable of binding to trimeric cytokines of the Tumor necrosis factor ligand superfamily, such as TNF, TRAIL, RANKL, TWEAK, APRIL and BAFF.

The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula IwhereinR1, R2, and R3 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. These compounds have a high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

A method for detecting cancer in a patient. The method comprises the steps of introducing labeled antibodies or labeled AFP to a biological sample of the patient so the labeled antibodies or labeled AFP will react with the AFP receptor binding sites in the biological sample. Next there is the step of identifying AFP receptor binding sites in the biological material which are reacted with the labeled antibodies or labeled AFP to determine the presence of cancer. Preferably, before the introducing step, there is the step of obtaining a biological sample from a body of a patient. A method for treating cancer cells in a patient. The method comprises the steps of introducing AFP receptor antibodies to cancer cells in the patient. Then there is the step of reacting the AFP receptor antibodies with the AFP receptor of the cancer cells to inhibit growth of the cancer cells or kill the cancer cells. A method for monitoring a patient. The method comprises the steps of treating the patient for cancer. Then there is the step of testing the patient at predetermined intervals after the treatment for AFP receptor site levels. A method for treating a patient. The method comprises the steps of testing the patient for AFP receptor. Then there is the step of introducing AFP receptor antibodies or AFP into the patient to react with cancer cells in the patient if the testing indicates AFP receptors are in the patient. A method for treating cancer cells in a patient. The method comprises the steps of introducing modified AFP to cancer cells in the patient. Then there is the step of reacting the modified AFP with the AFP receptor of the cancer cells to inhibit growth of the cancer cells or kill the cancer cells.

The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I:whereinR1 to R6 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The invention discloses an application of specific antibodies in the preparation of biological products for controlling virus infection based on virus acceptor binding site selection. The heavy chain variable gene VH of the specific antibodies comprises one or more CDRs in amino acid sequences containing GYNFASEW, IYPGDSDT and ARQNHYGSGSYFYRTAYYYAMDV, the heavy chain variable gene VL of the specific antibodies comprises one or more CDRs in amino acid sequences containing QSISSY, AAS and QQSYNTPFT, and the specific antibodies having above amino acid sequence are selectively combined with gp41MPER. According to the invention, the specific antibodies having specific sequences are selectively combined with the gp41MPER, so the antibodies and viruses undergo a good neutral reaction, thereby the antibodies play good roles in the control of the virus infection.

The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formulawhereinR1,R2, andR3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formulawherein the definition of substituents is described in the claims. This class of compounds shows high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula Iwherein R1 to R5 are as described in the specification and pharmaceutically acceptable salt thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites, being useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

A screening method directed towards; (1) specifying a receptor binding site by introduction of mutation, and (2) specifying a binding site-specific peptide motif on the basis of an amino acid selection ratio by contrast between a peptide motif bound to a wild-type subunit and a peptide motif bound to a mutant functionally deficient in the binding site according to a peptide library method. A peptide which inhibits a toxin whose receptor binding portion has a subunit structure is screened. Accordingly, an STX2 inhibitor in which an STX2 inhibiting peptide is incorporated in a molecular nuclear structure portion having three molecules of lysine (Lys) peptide-linked thereto and which is easy to synthesize and can inhibit verotoxin is provided.

The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I:whereinR1 to R5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula IwhereinR1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA Aα5 mediated diseases, including Alzheimer's disease.

The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula IwhereinR1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′;R2 is hydrogen or methyl;R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy;R′ is hydrogen or lower alkyl;R″ is hydrogen, hydroxy or lower alkyl;n is 0, 1 or 2;m is 1, 2 or 3; ando is 1 or 2;and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.

The present disclosure is directed to individual peptide immunogen constructs targeting portions of the Interleukin-6 (IL-6) protein, compositions containing the constructs, antibodies elicited by the constructs, and methods for making and using the constructs and compositions thereof. The disclosed IL-6 peptide immunogen constructs contain a B cell epitope from IL-6 linked to a heterologous T helper cell (Th) epitope directly or through an optional heterologous spacer. The IL-6 peptide immunogen constructs stimulate the generation of highly specific antibodies directed to the IL-6 receptor (IL-6R) binding site for the prevention and / or treatment of diseases impacted by IL-6 dysregulation.