Abstract

Provided is a camptothecin compound, which is a compound represented by structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof. An antibody-drug conjugate comprising the camptothecin compound is also provided. Provided is a camptothecin compound, which is a compound represented by structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof. An antibody-drug conjugate comprising the camptothecin compound is also provided.

IPC Classes  ?

• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61P 35/00 - Antineoplastic agents
• C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Abstract

Provided is the use of an anti-human interleukin-11 antibody or an antigen-binding fragment thereof in the preparation of a drug for treating tumors related to IL-11 expression. Experiments demonstrate that the anti-human interleukin-11 antibody or the antigen-binding fragment thereof can bind to IL-11 so as to block the formation of an IL-11/IL-11Rα/GP130 ternary complex and/or block the activation of an STAT3 signalling pathway, thereby achieving an obvious inhibitory effect on tumor growth.

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

A pharmaceutical composition containing an anti-Nectin4 antibody-drug conjugate and an anti-PD-1 antibody and a use thereof in preventing or treating cancer. The pharmaceutical composition has good safety, and has a stronger anti-tumor effect than using a drug alone. The pharmaceutical composition shows a synergistic tumor inhibitory effect. The present invention also relates to a kit of parts containing the pharmaceutical composition.

IPC Classes  ?

• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed is an anti-interleukin 11 (IL-11) antibody or a fragment thereof, which has high affinity for antigen IL-11, can block the formation of an IL-11/IL-11 R/GP130 ternary complex and inhibit the activation of the STAT3 signal pathway. Therefore, the anti-interleukin 11 antibody or the fragment thereof can effectively neutralize the activity of IL-11, and can be used for preventing, treating and/or improving diseases or conditions related to IL-11 expression (including overexpression).

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

Abstract

The present invention relates to a nucleic acid encoding ATP7B, an adeno-associated virus vector, and a use thereof in preparing a drug for preventing and treating Wilson's disease. Provided is an ATP7B GOI vector that can be packaged into an adeno-associated virus having cellular activity, relatively high yield and good integrity, which can be used in AAV gene therapy for WD. By means of using an engineered tissue-specific promoter and a truncated natural ATP7B gene having a unique sequence, the sequence length is suitable for packaging into an active adeno-associated virus particle, potential side effects caused by gene expression in tissues other than the liver are minimized, and it is expected to have better in vivo safety.

IPC Classes  ?

• C12N 15/55 - Hydrolases (3)
• C12N 9/14 - Hydrolases (3.)
• C12N 15/86 - Viral vectors
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy

Abstract

The present invention relates to a method for preparing an antibody-drug conjugate. According to the method, a highly homogeneous antibody conjugate molecule is obtained by means of a specific chemical site-directed conjugation method, and the proportion of a DAR2 main peak thereof reaches 99% or above. The preparation method of the present invention has few steps, and is easy to operate, and is thus beneficial for industrial scaled-up production. In addition, the prepared product has few impurities and a high purity, the medication safety is obviously improved, and the production cost is also reduced.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

Provided are an antibody and an antigen-binding fragment that specifically bind to Nectin-4, and a test kit containing the antibody or antigen-binding fragment. Also provided are a nucleic acid encoding the antibody, a host cell containing the nucleic acid, and a method for preparing the antibody. Also provided are uses of the antibody specifically binding to Nectin-4 in diagnosis and prognosis.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• G01N 33/53 - ImmunoassayBiospecific binding assayMaterials therefor
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G01N 33/577 - ImmunoassayBiospecific binding assayMaterials therefor involving monoclonal antibodies
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

A series of novel anti-B7-H3 antibodies. The antibodies have high affinity to B7-H3 and have stable structures. Also provided is an antibody drug conjugate prepared by using said antibody. The antibody drug conjugate uses a camptothecin compound having a specific structure as a toxic molecule, has significant tumor inhibition activity, and has a bystander killing effect.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• A61P 35/00 - Antineoplastic agents

Abstract

A method for synthesizing 5,8-diamino-3,4-dihydro-2H-1-naphthalenone (Compound I), which method comprises: subjecting 2,5-diprotected aminophenylbutyric acid to the Friedel-Crafts reaction for ring closure, and then removing a protecting group on the amino group to obtain Compound I.

IPC Classes  ?

• C07C 227/44 - StabilisationUse of additives
• B01J 27/125 - HalogensCompounds thereof with scandium, yttrium, aluminium, gallium, indium or thallium
• B01J 27/16 - PhosphorusCompounds thereof containing oxygen
• B01J 31/22 - Organic complexes
• B01J 31/24 - Phosphines
• C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
• C07C 227/06 - Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
• C07C 229/54 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
• C07C 233/83 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton

Abstract

Provided are an anti-VEGF antibody and a method for treating ocular fundus vascular lesions by using same. The antibody can be administered at a specific dosage and administration frequency to patients with ocular fundus vascular lesions.

IPC Classes  ?

• C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 27/02 - Ophthalmic agents

Abstract

An antibody-drug conjugate targeting a poliovirus receptor-like molecule 4 (Nectin-4). The antibody-drug conjugate can be used for preparing a drug for treating Nectin-4-related diseases. The antibody-drug conjugate has strong targeting properties to Nectin-4 and a strong endocytosis effect via the target, and has an excellent tumor-killing effect.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an antibody that specifically recognizes FRα or an antigen-binding fragment thereof, as well as a corresponding nucleic acid, a host cell, a drug, treatment and diagnosis methods, or a use.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 1/15 - Fungi Culture media therefor modified by introduction of foreign genetic material
• C12N 1/19 - YeastsCulture media therefor modified by introduction of foreign genetic material
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12N 15/06 - Animal cells
• C12N 15/09 - Recombinant DNA-technology
• C12N 15/13 - Immunoglobulins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G01N 33/82 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving vitamins

Goods & Services

Retail services for pharmaceutical, veterinary and sanitary preparations and medical supplies; wholesale services for pharmaceutical, veterinary and sanitary preparations and medical supplies; business auditing. Preparations for destroying noxious animals; dressings, medical; dental abrasives; biochemical drug; medicines for human purposes; biological preparations for medical purposes; pharmaceutical preparations; dietetic foods adapted for medical purposes; depuratives; medicines for veterinary purposes. Quality control; geological research; chemical research; biological research; material testing; packaging design; electronic data storage; clinical trials; technological research.

Goods & Services

Wholesale services for pharmaceutical, veterinary and sanitary preparations and medical supplies; advertising; sales promotion for others; provision of an online marketplace for buyers and sellers of goods and services; personnel management consultancy; updating and maintenance of data in computer databases; business auditing; sponsorship search; retail or wholesale services for pharmaceutical preparations; marketing. Biochemical drug; medicines for human purposes; biological preparations for medical purposes; pharmaceutical preparations; chemico-pharmaceutical preparations; drugs for medical purposes; chemical preparations for pharmaceutical purposes; chemical preparations for medical purposes. Quality control; geological research; chemical research; biological research; material testing; packaging design; architectural services; electronic data storage; clinical trials; technological research.

Abstract

The present invention provides a preparation containing an anti-Nectin-4 antibody drug conjugate (ADC) and a use thereof. The preparation comprises an ADC, a buffering agent and an excipient. The anti-Nectin-4 ADC in the preparation exists stably, proteins do not aggregate after long-term storage, small molecule drugs are not prone to becoming detached, the osmotic pressure of the preparation is close to isotonic, and targeted therapy of Nectin-4 related diseases is facilitated.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides an antibody binding a human tumor-associated calcium signal sensor 2 (Trop-2) protein or fragments thereof, and use of the antibody or fragments thereof in preventing or treating diseases. The antibody or fragments thereof of the present invention can effectively bind to the human Trop-2 protein, and have internalization activity, and the internalization activity is enhanced after ADC drug labeling, and the in vivo efficacy and safety of a mouse model are not lower than those of a control antibody.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided are an antibody and a preparation method therefor. The antibody is, such as a humanized anti-human CD47 monoclonal antibody or fragment thereof, and a bispecific antibody targeting PD-L1 and CD47 or an antigen-binding fragment thereof. The bispecific antibody comprises two heavy chains and two light chains, variable regions of the two heavy chains are heterologous, and variable regions of the two light chains have similar sequences. The provided bispecific antibody has the light chains having the similar sequences, thus solving the technical problem of light and heavy chain mismatch during an assembly process of bispecific antibodies.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61P 35/00 - Antineoplastic agents

Abstract

Provided in the present invention are an anti-human CD24 antibody or a fragment thereof and the use thereof. The anti-human CD24 antibody of the present invention specifically binds to human CD24, has significant complement-dependent cytotoxic (CDC) activity and antibody-dependent cytotoxic (ADCC) activity on the cell expressing the target, can regulate and control macrophage-mediated anti-tumor immune response, and can be used for tumor immunotherapy.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• G01N 33/577 - ImmunoassayBiospecific binding assayMaterials therefor involving monoclonal antibodies

Abstract

A preparation method for a bis-substituted bridging antibody-drug conjugate, comprising: hydrolyzing an antibody coupling product obtained by coupling an antibody to a compound as represented by formula I. Also provided is an antibody coupling product obtained by the preparation method. A preparation method for a bis-substituted bridging antibody-drug conjugate, comprising: hydrolyzing an antibody coupling product obtained by coupling an antibody to a compound as represented by formula I. Also provided is an antibody coupling product obtained by the preparation method.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment

Abstract

In view of the technical problem that TGF-β RH and a fusion protein thereof are prone to degradation and breakage during the process of recombinant expression, provided are a TGF-β RII mutant and a fusion protein thereof. Compared with the extracellular region of the wild-type TGF-β RII of SEQ ID NO: 6, the TGF-β RII mutant has a mutation selected from Gln at position 6, Asp at position 12 and Gly at position 20. The TGF-β RII mutant is capable of binding to TGF-β. Compared to wild-type TGF-β RII, the TGF-β RII mutant has less breakage and/or degradation during recombination expression. It is convenient for large-scale production of antibodies/the TGF-β RII bifunctional protein with a more stable quality.

IPC Classes  ?

• C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61P 35/00 - Antineoplastic agents
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression

Abstract

Disclosed in the present invention are a liquid antibody composition and the use thereof. The liquid antibody composition comprises a bispecific antibody targeting PD-L1 and CD47, an acidic buffer solution, a saccharide stabilizer and a polysorbate surfactant, and has a pH of 5.5-6.5, preferably 5.5-6.0. The composition has a good stability under the conditions of a high-concentration bispecific antibody.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a single variable domain antibody targeting a human programmed death ligand 1 (PD-L1) and a derivative thereof. A single variable domain antibody 2-2F2 specific for human PD-L1 is identified and obtained by extracting PBMCs from a camel immunized with human PD-L1, constructing a phage surface displayed VHH antibody library, and screening said VHH antibody library. On said basis, a chimeric antibody chF2 and a humanized modified antibody hzF2 variant are prepared. The hzF2 variant possesses affinity comparable or even superior to that of the original single variable domain antibody 2-2F2, can block the binding of PD-1 to PD-L1 in vitro, and can inhibit tumor growth in an in vivo experiment on tumor-bearing mice.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61P 35/00 - Antineoplastic agents

Abstract

Provided is an antibody molecule that binds to human Nectin-4 or a fragment thereof. The antibody is obtained by means of hybridoma screening and humanization techniques, and is used for the prevention or treatment of a cancer, and may be used as a clinical lead drug molecule.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives

Abstract

Embodiments of the present disclosure provide an antibody that binds to human Claudin 18.2 or a fragment thereof, as well as encoded nucleic acids and the like thereof. The anti-human Claudin 18.2 antibody of embodiments of the present disclosure has strong affinity to an antigen Claudin 18.2 and significant complement-dependent cytotoxicity (CDC) activity and antibody-dependent cytotoxicity (ADCC) activity to target expression cells, and exhibits high specificity to human CLDN 18.2.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a drug combination for treating tumors. The drug combination comprises: an anti-IL-11 antibody or a fragment thereof; and an anti-tumor drug, wherein the anti-tumor drug can cause local IL-11 expression up-regulation and/or signaling pathway activation in a tumor microenvironment by killing tumor cells. The present invention also provides a synergistic drug administration method for the anti-IL-11 antibody or the fragment thereof and the anti-tumor drug.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed is an anti-interleukin 11 (IL-11) antibody or a fragment thereof, which has high affinity for antigen IL-11, can block the formation of an IL-11/IL-11 Rα/GP130 ternary complex and inhibit the activation of the STAT3 signal pathway. Therefore, the anti-interleukin 11 antibody or the fragment thereof can effectively neutralize the activity of IL-11, and can be used for preventing, treating and/or improving diseases or conditions related to IL-11 expression (including overexpression).

IPC Classes  ?

• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided are an anti-ST2 antibody or a fragment thereof. The antibody or the fragment thereof can be specifically bound to human ST2, for inhibiting combination of IL-33 and human ST2, blocking an IL-33/ST2 intracellular signaling pathway, and inhibiting the promoting effect of different forms of IL-33 in cell-derived IL5, IL6 and 118 production. Compared with a known anti-ST2 antibody, this anti-ST2 antibody has higher biological activity, and can be used for preventing, treating or alleviating diseases related to ST2 expression or IL-33/ST2 pathway disorders.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided is a camptothecin compound, which is a compound represented by structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof. An antibody-drug conjugate comprising the camptothecin compound is also provided.

IPC Classes  ?

• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

Provided is a camptothecin compound, which is a compound represented by structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof. An antibody-drug conjugate comprising the camptothecin compound is also provided.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Abstract

The present invention provides an antibody binding to programmed cell death protein 1 (PD-1) or a fragment thereof and a use of the antibody or a fragment thereof in preventing or treating a tumor or cancer. The antibody or a fragment thereof of the present invention can effectively block the interactions of PD-1/PD-L1 and PD-1/PD-L2 and has a unique antigen binding epitope and unique properties in terms of efficacy and safety.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents

Abstract

A method for synthesizing 5,8-diamino-3,4-dihydro-2H-1-naphthalenone (compound I), which method comprises: subjecting 2,5-diprotected aminophenylbutyric acid to the Friedel-Crafts reaction for ring closure, and then removing a protecting group on the amino group to obtain compound I.

IPC Classes  ?

• C07C 49/613 - Unsaturated compounds containing a keto group being part of a ring polycyclic
• C07C 13/28 - Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof
• C07C 233/15 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings

Abstract

An anti-suppression of tumorigenicity 2 (ST2) antibody or a fragment thereof. The anti-ST2 antibody or the fragment thereof can block the binding of IL-33 to a ST2 protein, and inhibit a downstream signaling pathway thereof, thereby exerting a therapeutic effect in diseases associated with IL-33/ST2 signaling pathway activation. In addition, a stable liquid antibody preparation containing the anti-ST2 antibody or the fragment thereof is further provided.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

Provided is the use of a new anti-tumor inhibin 2 (ST2) antibody in the preparation of a drug for preventing or treating inflammatory, allergic or autoimmune diseases. The anti-ST2 antibody can bind to human ST2 with a high affinity, and can block the binding of human ST2 and human IL-33, thereby being capable of effectively inhibiting IL-33/ST2 signaling pathways. The anti-ST2 antibody has the effects of positively preventing and treating inflammatory, allergic or autoimmune diseases.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 37/02 - Immunomodulators
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 11/06 - Antiasthmatics

Abstract

A bispecific molecule targeting LAG-3 and PD-L1 and the use thereof. On the basis of a humanized antibody against human LAG-3, an anti-PD-L1 nano-antibody is linked to the C terminal of the heavy chain of the antibody by means of a linker. The method of linking the nano-antibody to the C-terminal of the heavy chain of the antibody by means of the above-mentioned linker not only reduces the function of the effector of Fc and avoids the clearance of activated T cells, but also makes the structure of the bispecific antibody more stable and the assembly efficiency of recombinant expression higher. Moreover, the bispecific molecule can simultaneously inhibit a PD-1/PD-L1 signal pathway and a LAG-3/MHCII and LAG3/signal pathway, achieve the bridging of LAG-3 positive cells and PD-L1 positive cells, and cluster disinhibited T cells around tumor cells expressing PD-L1, which has a good effect when inhibiting tumors.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a single-domain antibody that targets human programmed death ligand 1 (PD-L1) and a derivative protein thereof. A recombinant human PD-L1 protein is used as an immunogen, and PBMCs are separated to construct a single-domain antibody heavy chain variable region phage surface display antibody library; the recombinant human PD-L1 protein is subjected to solid-phase screening, so as to obtain phage display of camelid single-domain antibody VHH-B6, which can bind to the recombinant human PD-L1 protein; human-camelid chimeric antibody chB6 is prepared and humanized, and hzB6 is obtained; affinity maturation is performed on the basis of hzB6, and variants of 27 humanized single-domain antibodies are obtained and screened to obtain a humanized single-domain antibody variant having high affinity for human PD-L1, strong blocking activity for the binding of human PD-L1 with receptor PD-1, long in vivo half life, and good tumor treatment effects in an animal model.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

An antibody-drug conjugate targeting a poliovirus receptor-like molecule 4 (Nectin-4). The antibody-drug conjugate can be used for preparing a drug for treating Nectin-4-related diseases. The antibody-drug conjugate has strong targeting properties to Nectin-4 and a strong endocytosis effect via the target, and has an excellent tumor-killing effect.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61P 35/00 - Antineoplastic agents

Abstract

An antibody-drug conjugate targeting a poliovirus receptor-like molecule 4 (Nectin-4). The antibody-drug conjugate can be used for preparing a drug for treating Nectin-4-related diseases. The antibody-drug conjugate has strong targeting properties to Nectin-4 and a strong endocytosis effect via the target, and has an excellent tumor-killing effect.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• C12N 15/13 - Immunoglobulins
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells

Abstract

Provided are an antibody that binds to Staphylococcus aureus alpha-hemolysin or a fragment thereof, and the use of the antibody or the fragment thereof for preventing or treating Staphylococcus aureus infections. The antibody is obtained through screening by means of the strategies of attenuated immunity and virulent screening of alpha-hemolysin, and the antibody has high affinity to alpha-hemolysin, can effectively block the hemolysis effect of alpha-hemolysin, has proved significant protective or therapeutic effects in the alpha-hemolysin sepsis model, MRSA bacteremia model and MRSA lung infection model, and has a synergistic effect with antibiotics, which is a beneficial supplement to existing antibiotic therapy for Staphylococcus aureus.

IPC Classes  ?

• C07K 16/12 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from bacteria
• A61P 31/04 - Antibacterial agents

Abstract

Provided are antibodies and antibody fragments specifically binding LAG-3, and pharmaceutical compositions containing the antibodies or the antibody fragments. A nucleic acid encoding the antibodies, a host cell comprising the nucleic acid, and a method for preparing the antibodies are provided. Further provided are therapeutic and diagnostic uses of the antibodies binding LAG-3.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Goods & Services

Biochemical drug; medicines for human purposes; biological preparations for medical purposes; pharmaceutical preparations; chemico-pharmaceutical preparations; drugs for medical purposes; chemical preparations for pharmaceutical purposes; chemical preparations for medical purposes. Wholesale services for pharmaceutical, veterinary and sanitary preparations and medical supplies; advertising; sales promotion for others; provision of an online marketplace for buyers and sellers of goods and services; personnel management consultancy; updating and maintenance of data in computer databases; business auditing; sponsorship search; retail or wholesale services for pharmaceutical preparations; marketing. Quality control; geological research; chemical research; biological research; material testing; packaging design; architectural services; electronic data storage; clinical trials; technological research.

Abstract

Provided are an anti-human B7-H3 monoclonal antibody and an application thereof. By using a recombinant human B7-H3 extracellular region as an immunogen, a murine anti-human B7-H3 monoclonal antibody can be prepared by means of a hybridoma technology, and a murine anti-human B7-H3 antibody can bind to various domains of the B7-H3 extracellular region. A human-mouse chimeric antibody constructed on the basis of a murine antibody can specifically bind to B7-H3 of a cell surface. A humanized antibody prepared by means of CDRs transplantation and CDRs region mutation retains the ability to specifically bind to the human B7-H3 extracellular region and cell membrane surface B7-H3, and can be mediated for internalization by the cell membrane surface B7-H3.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 15/13 - Immunoglobulins
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an anti-human B7-H3 monoclonal antibody and an application thereof. By using a recombinant human B7-H3 extracellular region as an immunogen, a murine anti-human B7-H3 monoclonal antibody can be prepared by means of a hybridoma technology, and a murine anti-human B7-H3 antibody can bind to various domains of the B7-H3 extracellular region. A human-mouse chimeric antibody constructed on the basis of a murine antibody can specifically bind to B7-H3 of a cell surface. A humanized antibody prepared by means of CDRs transplantation and CDRs region mutation retains the ability to specifically bind to the human B7-H3 extracellular region and cell membrane surface B7-H3, and can be mediated for internalization by the cell membrane surface B7-H3.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided are an antibody and a preparation method therefor. The antibody is, such as a humanized anti-human CD47 monoclonal antibody or fragment thereof, and a bispecific antibody targeting PD-L1 and CD47 or an antigen-binding fragment thereof. The bispecific antibody comprises two heavy chains and two light chains, variable regions of the two heavy chains are heterologous, and variable regions of the two light chains have similar sequences. The provided bispecific antibody has the light chains having the similar sequences, thus solving the technical problem of light and heavy chain mismatch during an assembly process of bispecific antibodies.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• C12N 15/13 - Immunoglobulins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression

Abstract

A preparation method for a bis-substituted bridging antibody-drug conjugate, comprising: hydrolyzing an antibody coupling product obtained by coupling an antibody to a compound as represented by formula I. Also provided is an antibody coupling product obtained by the preparation method.

IPC Classes  ?

• C07D 207/456 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
• A61P 35/00 - Antineoplastic agents
• C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
• C07K 5/06 - Dipeptides

Goods & Services

Preparations for destroying noxious animals; dressings, medical; dental abrasives; biochemical drug; medicines for human purposes; biological preparations for medical purposes; pharmaceutical preparations; dietetic foods adapted for medical purposes; depuratives; medicines for veterinary purposes. Retail services for pharmaceutical, veterinary and sanitary preparations and medical supplies; wholesale services for pharmaceutical, veterinary and sanitary preparations and medical supplies; business auditing. Quality control; geological research; chemical research; biological research; material testing; packaging design; electronic data storage; clinical trials; technological research.

Abstract

In view of the technical problem that TGF-β RII and a fusion protein thereof are prone to degradation and breakage during the process of recombinant expression, provided are a TGF-β RII mutant and a fusion protein thereof. Compared with the extracellular region of the wild-type TGF-β RII of SEQ ID NO: 6, the TGF-β RII mutant has a mutation selected from Gln at position 6, Asp at position 12, and Gly at position 20. The TGF-β RII mutant is capable of binding to TGF-β. Compared to wild-type TGF-β RII, the TGF-β RII mutant has less breakage and/or degradation during recombinant expression. It is convenient for large-scale production of antibodies/the TGF-β RII bifunctional protein with a more stable quality.

IPC Classes  ?

• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• C07K 19/00 - Hybrid peptides
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to an antibody binding to human PD-1 or a fragment thereof, and a composition containing the anti-human PD-1 antibody or the fragment thereof, the composition preferably being an injection preparation. The anti-human PD-1 antibody performs screening by using a hybridoma technology to obtain an antibody molecule 317 having high affinity binding to both a human PD-1 extracellular region domain recombinant protein and a cell surface human PD-1 and capable of specifically blocking binding of receptors and ligands of PD-1/PD-L1 and PD-1/PD-L2, and a humanized antibody h317 having unchanged affinity and specificity is further obtained by means of a humanization technology is further obtained. According to structural analysis of an antigen-antibody compound crystal, mutants of h317 light and heavy chain CDR regions are constructed, so that a 317-series derivative antibody is obtained. On the basis of the anti-human PD-1 antibody h317, an antibody stabilized preparation provided by means of three rounds of component selection and concentration optimization improves the storage stability and temperature adaptability of the antibody, and prolongs the storage life of the antibody preparation especially an injection.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an antibody binding to Staphylococcus aureus α-hemolysin, or a fragment thereof, and a composition comprising the antibody against Staphylococcus aureus α-hemolysin or the fragment thereof. The composition preferably is a water injection preparation. Provided is an antibody stabilizing preparation.

IPC Classes  ?

• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• A61K 39/40 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum bacterial
• A61P 31/04 - Antibacterial agents
• A61K 47/06 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite

Abstract

On the basis of light and heavy chain amino acid sequences of an antibody against NKG2A reported in the prior art, by means of a mutant antibody having improved affinity and/or an improved dissociation constant obtained by constructing a light chain and heavy chain mutant antibody library for affinity maturation, a human Fab heavy chain gene expression vector and a mammalian cell expression vector containing a human κ subgroup light chain constant region gene are constructed using CDRs of the mutant antibody; crossover is carried out on a heavy chain vector and a light chain vector of the affinity-matured antibody; a mutant Fab antibody against NKG2A is obtained by screening; and a Fc fragment of a human antibody is bonded. A second antigen binding molecule (such as an antibody against PD-L1) is bonded to a C end of the Fc fragment by means of a linker to obtain a bispecific antibody.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

Provided is an antibody molecule that binds human Nectin-4 or a fragment thereof. The antibody is obtained by means of hybridoma screening and humanization techniques, and is used for the prevention or treatment of a cancer, and may be used as a clinical lead drug molecule.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

A fully human monoclonal antibody or a fragment thereof. The monoclonal antibody is a fully human antibody that is obtained by cloning a single B cell isolated from a blood sample in a recovery stage of a COVID-19 patient and specifically binds to a RBD region of SARS-CoV-2 S protein. The monoclonal antibody has no ADE effect on SARS-CoV-2 infected THP-1 cells and K562 cells. The monoclonal antibody has high affinity with a SARS-CoV-2 S protein RBD, and the KD value is 5.0×10 -9M or below; in addition, the monoclonal antibody has blocking activity on the binding of the SARS-CoV-2 S protein RBD to ACEII, and the IC50 value is less than 50 nM.

IPC Classes  ?

• C07K 14/165 - Coronaviridae, e.g. avian infectious bronchitis virus
• C12N 15/50 - Coronaviridae, e.g. infectious bronchitis virus, transmissible gastroenteritis virus
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
• A61K 39/42 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum viral
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Provided is an antibody molecule that binds human Nectin-4 or a fragment thereof. The antibody is obtained by means of hybridoma screening and humanization techniques, and is used for the prevention or treatment of a cancer, and may be used as a clinical lead drug molecule.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 38/00 - Medicinal preparations containing peptides
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a single variable domain antibody targeting a human programmed death ligand 1 (PD-L1) and a derivative thereof. A bacteriophage surface display VHH antibody library is constructed from PBMCs extracted from a camel immune to human PD-L1, and a single variable domain antibody 2-2F2 specific for anti-human PD-L1 is obtained by screening and identification, and on said basis, a chimeric antibody chF2 and a humanized modified antibody hzF2 mutant are prepared. The affinity of the hzF2 mutant may reach or even exceed that of an initial single variable domain antibody 2-2F2. The mutant may block the binding of PD-1 and PD-L1 in vitro, and inhibit tumor growth in an in vivo experiment on tumor-bearing mice.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an anti-ST2 antibody or a fragment thereof. The antibody or the fragment thereof can be specifically bound to human ST2, for inhibiting combination of IL-33 and human ST2, blocking an IL-33/ST2 intracellular signaling pathway, and inhibiting the promoting effect of different forms of IL-33 in cell-derived IL-5, IL-6 and Il-8 production. Compared with a known anti-ST2 antibody, this anti-ST2 antibody has higher biological activity, and can be used for preventing, treating, or alleviating diseases related with ST2 expression or IL-33/ST2 pathway disorders.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• C07K 19/00 - Hybrid peptides
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 37/02 - Immunomodulators
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• G01N 33/577 - ImmunoassayBiospecific binding assayMaterials therefor involving monoclonal antibodies

Abstract

Provided are an anti-ST2 antibody or a fragment thereof. The antibody or the fragment thereof can be specifically bound to human ST2, for inhibiting combination of IL-33 and human ST2, blocking an IL-33/ST2 intracellular signaling pathway, and inhibiting the promoting effect of different forms of IL-33 in cell-derived IL-5, IL-6 and Il-8 production. Compared with a known anti-ST2 antibody, this anti-ST2 antibody has higher biological activity, and can be used for preventing, treating, or alleviating diseases related with ST2 expression or IL-33/ST2 pathway disorders.

IPC Classes  ?

• A61P 37/02 - Immunomodulators
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided is an antibody or a fragment thereof to an activated receptor (OX40) expressed on the surfaces of CD4+T and CD8+T activated cells, and use of the antibody or the fragment thereof in preventing or treating diseases. The antibody has a high affinity for OX40 and has an obvious effect of activating the OX40 signaling pathway, and has a relatively broad spectrum of immune-enhancing effects, can enhance T cell response to immune memory, achieve better tumor inhibition and killing effects in in-vivo experiments on animal models, and thus has good clinical application prospect.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

Provided in the present invention are an antibody against PD-L1 or a fragment thereof, a nucleic acid encoding the antibody or the fragment thereof, a composition containing the antibody or the fragment thereof and the use thereof in the treatment of diseases. The antibody or the fragment thereof provided in the present invention can specifically bind to human PD-L1, block the binding of PD-L1 and PD-1, have a strong ADCC effect on target cells and significantly inhibit tumor growth.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 19/00 - Hybrid peptides
• C12N 15/13 - Immunoglobulins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides an antibody binding a human tumor-associated calcium signal sensor 2 (Trop-2) protein or fragments thereof, and use of the antibody or fragments thereof in preventing or treating diseases. The antibody or fragments thereof of the present invention can effectively bind to the human Trop-2 protein, and have internalization activity, and the internalization activity is enhanced after ADC drug labeling, and the in vivo efficacy and safety of a mouse model are not lower than those of a control antibody.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells

Abstract

The present invention provides an antibody binding a human tumor-associated calcium signal sensor 2 (Trop-2) protein or fragments thereof, and use of the antibody or fragments thereof in preventing or treating diseases. The antibody or fragments thereof of the present invention can effectively bind to the human Trop-2 protein, and have internalization activity, and the internalization activity is enhanced after ADC drug labeling, and the in vivo efficacy and safety of a mouse model are not lower than those of a control antibody.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 15/09 - Recombinant DNA-technology
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides an antibody that binds to human Claudin 18.2 or a fragment thereof, as well as encoded nucleic acids and the like thereof. The anti-human Claudin 18.2 antibody of the present invention has strong affinity to an antigen Claudin 18.2 and significant complement-dependent cytotoxicity (CDC) activity and antibody-dependent cytotoxicity (ADCC) activity to target expression cells, and exhibits high specificity to human CLDN 18.2.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61P 35/00 - Antineoplastic agents
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

The present invention provides an antibody that binds to human Claudin 18.2 or a fragment thereof, as well as encoded nucleic acids and the like thereof. The anti-human Claudin 18.2 antibody of the present invention has strong affinity to an antigen Claudin 18.2 and significant complement-dependent cytotoxicity (CDC) activity and antibody-dependent cytotoxicity (ADCC) activity to target expression cells, and exhibits high specificity to human CLDN 18.2.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided are an antibody that binds to Staphylococcus aureus alpha-hemolysin or a fragment thereof, and the use of the antibody or the fragment thereof for preventing or treating Staphylococcus aureus infections. The antibody is obtained through screening by means of the strategies of attenuated immunity and virulent screening of alpha-hemolysin, and the antibody has high affinity to alpha-hemolysin, can effectively block the hemolysis effect of alpha-hemolysin, has proved significant protective or therapeutic effects in the alpha-hemolysin sepsis model, MRSA bacteremia model and MRSA lung infection model, and has a synergistic effect with antibiotics, which is a beneficial supplement to existing antibiotic therapy for Staphylococcus aureus.

IPC Classes  ?

• A61P 31/04 - Antibacterial agents
• C07K 16/12 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from bacteria

Abstract

Provided are an antibody that binds to Staphylococcus aureus alpha-hemolysin or a fragment thereof, and the use of the antibody or the fragment thereof for preventing or treating Staphylococcus aureus infections. The antibody is obtained through screening by means of the strategies of attenuated immunity and virulent screening of alpha-hemolysin, and the antibody has high affinity to alpha-hemolysin, can effectively block the hemolysis effect of alpha-hemolysin, has proved significant protective or therapeutic effects in the alpha-hemolysin sepsis model, MRSA bacteremia model and MRSA lung infection model, and has a synergistic effect with antibiotics, which is a beneficial supplement to existing antibiotic therapy for Staphylococcus aureus.

IPC Classes  ?

• C07K 16/12 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from bacteria
• A61K 39/40 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum bacterial
• A61P 31/04 - Antibacterial agents

Abstract

The present invention provides an antibody binding to programmed cell death protein 1 (PD-1) or a fragment thereof and a use of the antibody or a fragment thereof in preventing or treating a tumor or cancer. The antibody or a fragment thereof of the present invention can effectively block the interactions of PD-1/PD-L1 and PD-1/PD-L2 and has a unique antigen binding epitope and unique properties in terms of efficacy and safety.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins

Abstract

The present invention provides an antibody binding to programmed cell death protein 1 (PD-1) or a fragment thereof and a use of the antibody or a fragment thereof in preventing or treating a tumor or cancer. The antibody or a fragment thereof of the present invention can effectively block the interactions of PD-1/PD-L1 and PD-1/PD-L2 and has a unique antigen binding epitope and unique properties in terms of efficacy and safety.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

IPC Classes  ?

• A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
• A61K 31/402 - 1-aryl-substituted, e.g. piretanide
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 207/456 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
• A61K 31/365 - Lactones
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam

Abstract

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. The di-substituted maleic amide linker is represented by Formula la,(see formula Ia)wherein R is X or ArS-; X is selected from halogen, preferably bromine or iodine; Ar is selected from the group consisting of substituted or unsubstituted C6-C10 aryl and substituted or unsubstituted 5-12 membered heteroaryl; Ar' is selected from the group consisting of substituted or unsubstituted C6-C10 arylene, and substituted or unsubstituted 5-12 membered heteroarylene; L1 is -O(CH2CH2O)n- linked to Ar', in which n is any integer between 1 and 20.The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. Also provided are antibody drug conjugates using the di-substituted maleic amide linkers, compositions comprising the conjugates, uses thereof and methods of making thereof.

IPC Classes  ?

• A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07D 207/456 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 491/18 - Bridged systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
• C07K 7/02 - Linear peptides containing at least one abnormal peptide link