62 results about "Orphan receptor" patented technology

The present invention relates to bispecific antigen binding molecules specific for both the receptor tyrosine kinase-like orphan receptor 1 (ROR1) and the epidermal growth factor receptor (EGFR), as well as related fusion proteins and conjugates. In another aspect, the invention relates to conjugated immunoglobulin-like shark variable neoantigen receptors (VNARs).

The invention discloses an anti-receptor tyrosine kinase-like orphan receptor 1 antibody and a conjugate of the anti-receptor tyrosine kinase-like orphan receptor 1 antibody and a small molecule drug. Also disclosed is the use of the ligand-cytotoxic drug conjugate and a pharmaceutical composition comprising the same in the preparation of a medicament for the treatment of cancer.

Provided are an antibody targeting receptor tyrosine kinase-like orphan receptor 1 and a use thereof. Further provided is a pharmaceutical composition comprising the antibody and a use thereof. The provided antibody achieves excellent anti-tumor activity and / or good safety. The provided antibody can be used for the treatment of tumors.

The present invention relates to receptor tyrosine kinase-like orphan receptor 1 (ROR1) specific antigen binding molecules and associated fusion proteins and conjugates. In a further aspect, the present invention relates to conjugated immunoglobulin-like shark variable novel antigen receptors (VNARs).

The present invention relates to the use of an ROR inverse agonist or a pharmaceutically acceptable salt thereof for the preparation of a medicament for modulating ROR in a patient and / or for controlling autoimmune diseases and antibody-mediated rejection in a patient. The ROR-mediated diseases or autoimmune diseases include HIV, cancer, celiac disease, type 1 diabetes, Graves' disease (Graves' disease), inflammatory bowel disease, multiple sclerosis, psoriasis, rheumatoid arthritis, systemic lupus erythematosus, asthma, dermatitis, fatty liver disease, Crohn's disease (Crohn's disease), cardiovascular disease, inflammatory disease, nervous system disorders, multiple sclerosis, and the like. Acute respiratory distress syndrome and arteriosclerosis.

The present invention relates to: a receptor tyrosine kinase-like orphan receptor 1 (ROR1) antibody or an antigen-binding fragment thereof; a nucleic acid encoding the same; a recombinant expression vector carrying the nucleic acid; a host cell transfected with the recombinant expression vector; a method for preparing the antibody or the antigen-binding fragment thereof; a bispecific or multispecific antibody carrying the antibody or the antigen binding fragment thereof; the immune cells are connected with bispecific or multispecific antibodies; an antibody-drug conjugate (ADC), wherein the antibody or antigen-binding fragment thereof binds to a drug; a chimeric antigen receptor (CAR) comprising the scFv of the antibody as the antigen binding site of the extracellular domain; an immune cell having a chimeric antigen receptor introduced therein; a composition for combination therapy including the antibody or an antigen-binding fragment thereof; a pharmaceutical composition for preventing or treating cancer; and a method for preventing or treating cancer.

The present invention relates to bi-specific antigen binding molecules with specificity for both receptor tyrosine kinase-like orphan receptor 1 (ROR1) and epidermal growth factor receptor (EGFR) and associated fusion proteins and conjugates. In a further aspect, the present invention relates to conjugated immunoglobulin-like shark variable novel antigen receptors (VNARs).

The present disclosure relates to antibodies and antibody conjugates, for instance antibody drug conjugates, with binding specificity for receptor tyrosine kinase orphan receptor 1 (ROR1) and its isoforms and homologs, and compositions comprising the antibodies or antibody conjugates, including pharmaceutical compositions. Also provided are methods of producing the antibodies and antibody conjugates and compositions thereof as well as methods of using the antibodies and antibody conjugates and compositions thereof, such as in therapeutic and diagnostic methods.

The present invention relates to receptor tyrosine kinase-like orphan receptor 2 (ROR2) inhibitors which are fused to IgG2-Fc domains.

ROR1-specific antigen-binders, and multispecific antibodies are provided, which contains one or more ROR1-specific antigen-binding sites and at least one antigen-specific binding site for an activation receptor (such as CD3) on an immune cell, wherein various configurations are presented of new VHH-based anti-ROR1 sequences in relation to the antigen-specific binding site for the immune cell activation receptor, as well as to a scaffolding segment forming a constant region of the antibodies. These multispecific antibodies have been demonstrated to bind to ROR1-positive cancer cells, induce immune cell-mediated cytotoxicity against ROR1-positive target cells, and to inhibit growth of tumor size in animals.

The present disclosure provides novel 4-substituted-phenyl acetamide and arylurea derivatives that act as agonists against GPR88. The compounds of the present disclosure are believed to be useful for the treatment of diseases and conditions caused by physiological processes implicating the orphan receptor GPR88, including diverse brain and behavioral functions such as cognition, mood, movement control, and reward-based learning. GPR88 is emerging as a novel drug target for central nervous system disorders including schizophrenia, Parkinson's disease, anxiety, and addiction. One particular indication for which GPR88 agonists hold promise is alcohol use disorder (AUD).

To provide an ophthalmic formulation for treating or preventing glaucoma or pathogenic intraocular pressure.SOLUTION: The ophthalmic formulation comprises a Wnt receptor inhibitor that specifically inhibits expression of a Wnt receptor selected from among frizzled-2 (FZD2), frizzled-5 (FZD5), and receptor tyrosine kinase like orphan receptor 1 (ROR1) through genetic manipulation.SELECTED DRAWING: None

The present application relates to an isolated antigen binding protein capable of binding to ROR1 (Receptor Tyrosine Kinase Orphan Receptor 1), said isolated antigen protein comprising CDR1, CDR2 and CDR3. The present application also provides a method for preparing said isolated antigen binding protein and uses thereof.

The invention encompasses the novel class of compounds represented by the Formula (I), (II), (III) and (IV) below, which are modulators of RORγt:The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing autoimmune diseases and antibody mediated rejection in a patient in need thereof.

The invention provides a method for determining an endogenous ligand of an orphan receptor and application of the method. Particularly, the endogenous ligand of GPR50 is identified, and the function of the endogenous ligand is characterized. The ligand-receptor pairing screening platform established by the invention has high sensitivity and wide generalizability.

Provided herein are, inter alia, antibodies (e.g., humanized antibodies, monoclonal antibodies), antibody fragments (e.g., scFvs), and antibody compositions (e.g., chimeric antigen receptors, bispecific antibodies) that bind to human tyrosine kinase-like orphan receptor 2 (ROR2) with high efficiency and specificity and are useful, inter alia, for the diagnosis and treatment of cancer and other ROR2-associated diseases.

Provided are a fusion polypeptide, an expression cassette comprising a coding gene thereof, a gene delivery vector, a pharmaceutical composition, and uses thereof. Specifically, the invention provides a fusion polypeptide, which comprises a secretion signal peptide and an afbercept polypeptide, and the secretion signal peptide is selected from any one of a human albumin secretion signal peptide, a human Opticin protein secretion signal peptide, a human interleukin-2 secretion signal peptide and a mouse receptor tyrosine kinase-like orphan receptor 1 secretion signal peptide. According to the fusion polypeptide, the polynucleotide for encoding the fusion polypeptide, the gene expression cassette containing the polynucleotide and the gene delivery vector containing the expression cassette, the expression of the aflibercept can be improved, and the effect of treating eye diseases by using the aflibercept can be improved.

The invention discloses application of an orphan receptor GPR88 as a target spot in developing or preparing a medicine for treating neuropathic pain. The invention proposes that the orphan receptor GPR88 is a target of a medicine for treating neuropathic pain for the first time, the expression characteristic of the orphan receptor GPR88 at the spinal cord level is verified for the first time, the pain behavior of a mouse is observed through intrathecal administration of a GPR88 receptor agonist, the definite analgesic effect after the GPR88 receptor is activated is verified, and the effect is possibly generated by inhibiting a cAMP / PKA / CREB signal channel, so that the effect is obvious. And thinking and theoretical basis are provided for research and development of analgesic drugs for targeting the spinal cord GPR88 receptor.

The invention belongs to the technical field of fluorescent probes, and particularly discloses a novel fluorescent compound capable of being combined with a retinoic acid receptor related orphan receptor gamma normal site and application of the novel fluorescent compound serving as a fluorescent probe to inhibitor screening, imaging and the like. Compounds P1-P11 conforming to the general formula (I) are synthesized, a novel ROR gamma normal inhibitor screening platform can be established on the basis of a fluorescence polarization probe system constructed by the compounds according to a competitive ligand replacement principle, and the technical scheme breaks through the limitation of a traditional activity detection method and has a wide application prospect. An activity evaluation tool with economical efficiency, timeliness and reliability is provided for research and development of drugs targeting ROR gamma normal sites, and the lead compound discovery and structure optimization process can be accelerated.

The invention discloses a GPR21 expression vector and a construction method and application of a recombinant HEK293 cell based on the GPR21 expression vector, and belongs to the technical field of biology. PGMLV-CMV-HGPR21-EF1-ZsGreen1-T2A-Puro plasmids are constructed on the basis of a seamless cloning technology and are packaged into a lentivirus system for infecting HEK293 cells, puromycin is used for screening to obtain a genetic engineering cell line GPR21-HEK293 of stably transfected full-length GRP21, and the cell line is proved to be capable of improving the protein expression of the full-length GPR21 by 2.5 times, so that the gene engineering cell line GPR21-HEK293 can be used for efficiently expressing the full-length GPR21. The cell with high GPR21 expression provides a technical means for research on a ligand of a GRP21 orphan receptor and screening of drugs for treating inflammation, immunity, metabolism related diseases and the like by taking GRP21 as a target.

The application belongs to the technical field of pharmaceutical chemistry, and discloses a phenothiazine sulfonamide compound shown in a general formula (I) or a salt thereof, a preparation method and application thereof. The compound, a pharmaceutically acceptable salt, an isomer, a prodrug, a co-crystal complex, a hydrate or a solvate thereof can be used as an agonist of a retinoic acid receptor-related orphan receptor-gamma t (RORgamma t).

The present disclosure relates to antibodies and antibody conjugates, for instance antibody drug conjugates, with binding specificity for receptor tyrosine kinase orphan receptor 1 (ROR1) and its isoforms and homologs, and compositions comprising the antibodies or antibody conjugates, including pharmaceutical compositions. Also provided are methods of producing the antibodies and antibody conjugates and compositions thereof as well as methods of using the antibodies and antibody conjugates and compositions thereof, such as in therapeutic and diagnostic methods.

The invention encompasses the novel class of compounds represented by the Formula (I), (II), (III) and (IV) below, which are modulators of RORγtThe invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing autoimmune diseases and antibody mediated rejection.

The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and / or disorder, in particular their use in diseases and / or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

The present disclosure provides novel 4-substituted-phenyl acetamide and arylurea derivatives that act as agonists against GPR88. The compounds of the present disclosure are believed to be useful for the treatment of diseases and conditions caused by physiological processes implicating the orphan receptor GPR88, including diverse brain and behavioral functions such as cognition, mood, movement control, and reward-based learning. GPR88 is emerging as a novel drug target for central nervous system disorders including schizophrenia, Parkinson's disease, anxiety, and addiction. One particular indication for which GPR88 agonists hold promise is alcohol use disorder (AUD).

There is described Receptor Tyrosine Kinase Like Orphan Receptor 1 (ROR1) antibodies that specifically bind a ROR1 polypeptide, and their use. In particular, isolated monoclonal antibodies are described and their use in a number of applications, including in the detection, prevention and treatment of cancer.

The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and / or disorder, in particular their use in diseases and / or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

In one aspect, the present disclosure describes compounds that may be used to modulate the activity of an estrogen receptor-related orphan receptor (EER). Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

The application belongs to the technical field of drug research and development, and particularly relates to a compound, a preparation method and application of the compound as an agonist of orphan receptor GPR99. The application first discovers and identifies a small-molecule compound capable of specifically activating the orphan receptor GPR99, and systematically clarifies the mechanism of the small-molecule compound in the regulation of vascular smooth muscle cell (VSMC) contraction and the improvement of pathological vascular dilation. The discovery not only fills the blank of GPR99 agonists in the field of treatment of rosacea, but also provides a new molecular target and a drug research and development direction for precise treatment of diseases related to abnormal vascular function.