Provided are an antibody specifically binding to PD-L1 and an antigen-binding fragment thereof. The antibody and the antigen-binding fragment thereof have high specificity and stability, can specifically block a PD-L1-SIPRα pathway, do not cause hemagglutination within a certain concentration range, and thus can significantly suppress tumor growth in vivo.
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 39/00 - Medicinal preparations containing antigens or antibodies
The present invention provides an anti-PD-L1/anti-CD47 bispecific antibody and a preparation method therefor. The antibody has characteristics of a natural IgG, and is a highly stable heterodimeric form without heavy and light chain mismatching. The bispecific antibody can bind two target molecules at the same time and has a smaller side effect.
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
Provided are an anti-PD-L1/anti-4-1BB natural antibody structure-like heterodimeric form bispecific antibody and a preparation thereof. Specifically, provided are an anti-PD-L1/anti-4-1BB bispecific antibody that has natural IgG features, that has no mismatch between heavy and light chains and that is in the form of a highly stable heterodimer, as well as a preparation method therefor. The bispecific antibody can simultaneously bind two target molecules and is more effective in treating complex diseases and has fewer side effects.
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
Provided are formulations for anti-PD-L1/anti-4-1BB bispecific antibodies and methods of making and using the same. In one aspect, provided is a stable aqueous pharmaceutical formulation comprising an anti-PD-L1/anti-4-1BB bispecific antibody or antigen-binding fragment thereof.
The present invention relates to formulations comprising an anti-PD-1/HER2 bispecific antibody, and in particular to a pharmaceutical formulation comprising the anti-PD-1/HER2 bispecific antibody, a buffer, a stabilizer and a surfactant. Furthermore, the present invention also relates to therapeutic or prophylactic use of these formulations.
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 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 9/00 - Medicinal preparations characterised by special physical form
Provided are an anti-PD-L1/anti-4-1BB natural antibody structure-like heterodimeric form bispecific antibody and a preparation thereof. Specifically, provided are an anti-PD-L1/anti-4-1BB bispecific antibody that has natural IgG features, that has no mismatch between heavy and light chains and that is in the form of a highly stable heterodimer, as well as a preparation method therefor. The bispecific antibody can simultaneously bind two target molecules and is more effective in treating complex diseases and has fewer side effects.
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
The present invention provides an anti-PD-1/anti-CD47 bispecific antibody and a preparation method therefor. The antibody has characteristics of a natural IgG, and is a highly stable heterodimeric form without heavy and light chain mismatching. The bispecific antibody can bind two target molecules at the same time and has a smaller side effect.
Provided are an antibody specifically binding to CD47 and an antigen-binding fragment thereof The antibody and the antigen-binding fragment thereof have high specificity and stability, can specifically block a CD47-SIPRα pathway, do not cause hemagglutination within a certain concentration range, and thus can significantly suppress tumor growth in vivo.
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
An antibody specifically binding with PD-L1 and an antigen-binding fragment of the antibody. The antibody specifically binding with PD-L1 and the antigen-binding fragment of the antibody have high specificity and stability, are capable of enhancing the secretion of IFN-γ, provide strong T cell function regulation activity, and are capable of significantly suppressing the growth of a tumor in the body.
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
Provided are an anti-PD-L1/anti-4-1BB natural antibody structure-like heterodimeric form bispecific antibody and a preparation thereof. Specifically, provided are an anti-PD-L1/anti-4-1BB bispecific antibody that has natural IgG features, that has no mismatch between heavy and light chains and that is in the form of a highly stable heterodimer, as well as a preparation method therefor. The bispecific antibody can simultaneously bind two target molecules and is more effective in treating complex diseases and has fewer side effects.
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
11.
ANTIBODY SPECIFICALLY BINDING TO 4-1BB AND ANTIGEN-BINDING FRAGMENT OF ANTIBODY
Provided are an antibody specifically binding to 4-1BB and an antigen-binding fragment of the antibody. The antibody specifically binding to 4-1BB and the antigen-binding fragment of the antibody have high specificity, and after being binded to an antigen, the antibody and the antigen-binding fragment thereof can enhance an immune killing function of T cells, can induce activation of immune cells and promote secretion of cytokines, and can significantly inhibit the growth of tumors in the body.
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
Provided are an anti-TNFα/anti IL-17A natural antibody structure-like heterodimer form of a bispecific antibody and a preparation method therefor, wherein the antibody can bind two target molecules simultaneously, and can be used for treating complex diseases.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
Provided are an anti-PD-L1/anti-CD47 bispecific antibody that has natural IgG characteristics and is in a highly stable heterodimer form without the heavy chain and light chain being mismatched, and a preparation method therefor. Either the first Fc chain or second Fc chain of the bispecific antibody comprises amino acid substitutions at positions 366 and 399, and the other comprises amino acid substitutions at positions 351, 407 and 409.
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
An anti-PD-1/anti-VEGF natural antibody structure-like heterodimeric form bispecific antibody and preparation thereof. Provided are a highly stable, heterodimeric form anti-PD-1/anti-VEGF bispecific antibody having natural IgG characteristics and free of mismatched heavy and light chains and preparation method for the antibody. The bispecific antibody is capable of simultaneously binding with two target molecules and provides improved efficacy in treating a complicated disease.
C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
The present invention relates to formulations comprising an anti-PD-1/HER2 bispecific antibody, and in particular to a pharmaceutical formulation comprising the anti-PD-1/HER2 bispecific antibody, a buffer, a stabilizer and a surfactant. Furthermore, the present invention also relates to therapeutic or prophylactic use of these formulations.
The present invention relates to a preparation comprising an anti-PD-1/HER2 bispecific antibody, and in particular, relates to a pharmaceutical preparation comprising an anti-PD-1/HER2 bispecific antibody, a buffering agent, a stabilizing agent, and a surfactant. In addition, the present invention further relates to use of these preparations in the treatment or prevention of diseases.
Provided are an anti-PD-1/anti-HER2 natural antibody structural heterodimeric bispecific antibody and a method of preparing the same. More particularly, provided are a highly stable heterodimeric anti-PD-1/anti-HER2 bispecific antibody having natural IgG characteristics without mismatch between a heavy chain and a light chain, and a method of preparing the same. The bispecific antibody may bind to two target molecules simultaneously and has excellent effects in treatment of a complex disease.
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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/00 - Medicinal preparations containing antigens or antibodies
18.
ANTI-TNF.ALPHA./ANTI IL - 17A NATURAL ANTIBODY STRUCTURE-LIKE HETERODIMER FORM OF BISPECIFIC ANTIBODY AND PREPARATION METHOD THEREFOR
Provided are an anti-TNFa/anti IL-17A natural antibody structure-like heterodimer form of a bispecific antibody and a preparation method therefor, wherein the antibody can bind two target molecules simultaneously, and can be used for treating complex diseases.
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
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
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
Provided are an anti-TNFα/anti IL-17A natural antibody structure-like heterodimer form of a bispecific antibody and a preparation method therefor, wherein the antibody can bind two target molecules simultaneously, and can be used for treating complex diseases.
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 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
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
The present invention relates to a compound inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (particularly humans). The compound has a structural formula I.
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
21.
Anti-PD-1/anti-HER2 natural antibody structural heterodimeric bispecific antibody and method of preparing the same
Provided are an anti-PD-1/anti-HER2 natural antibody structural heterodimeric bispecific antibody and a method of preparing the same. Specifically, provided are a highly stable anti-PD-1/anti-HER2 heterodimeric bispecific antibody having characteristics of a natural IgG and having no mismatched heavy chain and light chain, and a method of preparing the same. The bispecific antibody may bind to both of two kinds of target molecules, and thus may be more effective in treating complex diseases.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
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
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
The present invention provides a method for production of stable and highly specific heterodimeric immunoglobulin constructs, e.g., bispecific antibodies, retaining desirable properties of native IgG and lacking undesirable heavy chain-light chain mispairing, that can simultaneously bind two target molecules and are more potent in the treatment of complex diseases.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
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
An anti-PD-1/anti-VEGF natural antibody structure-like heterodimeric form bispecific antibody and the preparation thereof. Provided are a highly stable, heterodimeric form anti-PD-1/anti-VEGF bispecific antibody having natural IgG characteristics and free of mismatched heavy and light chains and a preparation method for the antibody. The bispecific antibody is capable of simultaneously binding with two target molecules and provides improved efficacy in treating a complicated disease.
The present invention provides an anti-PD-1/anti-HER2 natural antibody structural heterodimeric bispecific antibody and a method of preparing the same. More particularly, the present invention provides a highly stable heterodimeric anti-PD-1/anti-HER2 bispecific antibody having natural IgG characteristics without mismatch between a heavy chain and a light chain and a method of preparing the same.
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
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
The present invention provides an anti-PD-1/anti-HER2 natural antibody structural heterodimeric bispecific antibody and a method of preparing the same. More particularly, the present invention provides a highly stable heterodimeric anti-PD-1/anti-HER2 bispecific antibody having natural IgG characteristics without mismatch between a heavy chain and a light chain and a method of preparing the same.
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
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
An anti-PD-1/anti-VEGF natural antibody structure-like heterodimeric form bispecific antibody and the preparation thereof. Provided are a highly stable, heterodimeric form anti-PD-1/anti-VEGF bispecific antibody having natural IgG characteristics and free of mismatched heavy and light chains and a preparation method for the antibody. The bispecific antibody is capable of simultaneously binding with two target molecules and provides improved efficacy in treating a complicated disease.
Provided are an anti-PD-1/anti-HER2 natural antibody structure-like bispecific antibody in heterodimeric form and a preparation method therefor. The antibody can bind two target molecules simultaneously, and can be used for treating complex diseases.
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
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
Provided are an anti-PD-L1/anti-CD47 bispecific antibody that has natural IgG characteristics and is in a highly stable heterodimer form without the heavy chain and light chain being mismatched, and a preparation method therefor. Either the first Fc chain or second Fc chain of the bispecific antibody includes amino acid substitutions at positions 366 and 399, and the other includes amino acid substitutions at positions 351, 407 and 409.
Provided are an anti-PD-L1/anti-CD47 bispecific antibody that has natural IgG characteristics and is in a highly stable heterodimer form without the heavy chain and light chain being mismatched, and a preparation method therefor. Either the first Fc chain or second Fc chain of the bispecific antibody includes amino acid substitutions at positions 366 and 399, and the other includes amino acid substitutions at positions 351, 407 and 409.
Disclosed are a compound related to inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (especially humans). The compound has a structural formula I.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
31.
ANTI-PD-1/ANTI-HER2 NATURAL ANTIBODY STRUCTURE-LIKE BISPECIFIC ANTIBODY OF HETERODIMERIC FORM AND PREPARATION THEREOF
Provided are an anti-PD-1/anti-HER2 bispecific antibody of a heterodimeric form having the characteristics of a natural IgG and a preparation method therefor. The antibody binds both target molecules simultaneously, and can be used to treat complex diseases.
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
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
Provided are an anti-PD-1/anti-HER2 bispecific antibody of a heterodimeric form having the characteristics of a natural IgG and a preparation method therefor. The antibody binds both target molecules simultaneously, and can be used to treat complex diseases.
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
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
Provided is a method for production of stable and highly specific heterodimeric immunoglobulin constructs, e.g., bispecific antibodies, retaining desirable properties of native IgG and lacking undesirable heavy chain-light chain mispairing, that can simultaneously bind two target molecules and are more potent in the treatment of complex diseases.
Provided is a method for production of stable and highly specific heterodimeric immunoglobulin constructs, e.g., bispecific antibodies, retaining desirable properties of native IgG and lacking undesirable heavy chain-light chain mispairing, that can simultaneously bind two target molecules and are more potent in the treatment of complex diseases.
The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I).
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for human purposes; pharmaceutical preparations;
drugs for medical purposes; biological preparations for
medical purposes; biochemical drug; dietetic foods adapted
for medical purposes; pharmaceutical preparations in the
form of injection; pharmaceutical raw material; nutritional
supplements; dietetic substances adapted for medical use.
37.
N-benzoate group substituted benzopyrroline-2-one derivative and use thereof
Disclosed are a compound, a stereisomer and a tautomer thereof, a pharmaceutically acceptable salt thereof, and a solvate or a prodrug thereof, which can be used for preventing or treating a RORγ mediated disease. The compound has the structural formula (I).
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for human purposes, pharmaceutical preparations, drugs for medical purposes, biological preparations for medical purposes, biochemical drugs, and pharmaceutical preparations in the form of injection, each of which being, namely, for treating one or more of autoimmune diseases, immune response against grafts, allergic reactions, neurodegenerative diseases, neoplastic diseases and cellular proliferative disorders, arthritis, rheumatoid arthritis, psoriasis, multiple sclerosis (MS), ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE), glomerulonephritis, dilated cardiomyopathy-like diseases, Sjogren's syndrome, allergic contact dermatitis, polymyositis, scleroderma, periarteritis nodosa, rheumatic fever, vitiligo, insulin-dependent diabetes mellitus, Behcet's syndrome, chronic thyroiditis, Parkinson's disease, Huntington's disease, Machado-Joseph disease, amyotrophic lateral sclerosis (ALS), Creutzfeldt - Jakob disease, leukemia, lymphoma, myeloma, brain tumors, head and neck squamous cell carcinoma, non-small cell lung cancer (NSCLC), nasopharyngeal cancer, esophageal cancer, stomach cancer, pancreatic cancer, gallbladder cancer, liver cancer, colorectal cancer, breast cancer, ovarian cancer, cervical cancer, endometrial cancer, uterine sarcoma, prostate cancer, bladder cancer, renal cell carcinoma, melanoma, and combinations thereof; nutritional supplements and dietetic substances adapted for medical use, namely, dietetic foods adapted for medical use and dietetic beverages adapted for medical use
The present invention relates to a compound inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (particularly humans). The compound has a structural formula I.
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
Disclosed are a compound related to inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (especially humans). The compound has a structural formula I.
The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I).
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
42.
N-BENZOATE GROUP SUBSTITUTED BENZOPYRROLINE-2-ONE DERIVATIVE AND USE THEREOF
Disclosed are a compound, a stereisomer and a tautomer thereof, a pharmaceutically acceptable salt thereof, and a solvate or a prodrug thereof, which can be used for preventing or treating a RORγ mediated disease. The compound has the structural formula (I).
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
Provided are oxyntomodulin (OXM) analogs having GLP-1 receptor antagonist activity and GCG receptor antagonist activity. Also provided are pharmaceutical compositions comprising the OXM analogs, and a use thereof.
Disclosed are a bifunctional fusion protein comprising an extracellular domain of a CTLA4 molecule and a functional fragment with neutralized IL6 activity, a coding gene of the bifunctional fusion protein, a carrier comprising the gene, a host cell comprising the carrier, and a pharmaceutical composition comprising the fusion protein. The functional fragment with the neutralized IL6 activity is a monoclonal antibody against IL6. The extracellular domain of the CTLA4 molecule is located at an N end of a heavy chain of the monoclonal antibody against IL6, and is connected by using a connecting peptide. The bifunctional fusion protein in the present invention can simultaneously block B7/CD28 and IL6/IL6R/GP130 signal paths, so as to suppress an inflammatory reaction.
C12N 15/62 - DNA sequences coding for fusion proteins
C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
The present application relates to a compound usable as a retinoic acid related orphan receptor γ(RORγ) modifier, pharmaceutical composition thereof, use thereof in drug preparation, and method of treating or preventing diseases mediated by RORγ in mammals(especially humans) using the compound. The compound has a structure of formula I:
C07D 403/10 - 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 carbon chain containing aromatic 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 209/02 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
C07D 231/54 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
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
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to a compound which can be used as a retinoid-related orphan receptor γ (RORγ) modifier, a pharmaceutical composition of said compound, the use of said compound in the manufacture of pharmaceuticals, and a method for using said compound for treatment and/or prophylaxis of a RORγ-mediated disease in a mammal (especially a human). The compound has the structural formula I.
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 247/02 - Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups having the nitrogen atoms in positions 1 and 3
C07D 401/06 - 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 carbon chain containing only aliphatic 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 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
47.
BIFUNCTIONAL FUSION PROTEIN, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention provides a bifunctional fusion protein comprising the extracellular region of CTLA4 and an anti-IL-17 antibody, a gene encoding the protein, a vector comprising the gene, a host cell comprising the vector, and a pharmaceutical composition containing the protein.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
C12N 15/62 - DNA sequences coding for fusion proteins
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 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A particle composition and a preparation method therefor. The particle composition comprises montelukast sodium particles and levocetirizine particles. The montelukast sodium particles comprise montelukast sodium, a filler, a stabilizer, and an adhesive. The levocetirizine particles comprise levocetirizine, a filler, a stabilizer, and an adhesive. The stabilizers are meglumine, and the adhesives are hydroxypropyl-β-cyclodextrin.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I). (see formula I)
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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
50.
COMPOUND INHIBITING ACTIVITIES OF BTK AND/OR JAK3 KINASES
The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I).
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A compound capable of inhibiting kinase activities of BTK and/or JAK3, a pharmaceutical composition, and applications in preparing a medicament. The compound is as represented by structural formula I, where the definitions of the substituents are as presented in the description.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group 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 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur 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
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 35/02 - Antineoplastic agents specific for leukemia
52.
BIFUNCTIONAL FUSION PROTEIN, PREPARATION METHOD THEREFOR, AND USE THEREOF
Provided are a bifunctional fusion protein having a CTLA4 molecule extracellular region, an Fc fragment, and a functional fragment that neutralizes TNFα activity, a gene for encoding the bifunctional fusion protein, a carrier having the gene, a host cell having the carrier, and a pharmaceutical composition having the bifunctional fusion protein. The functional fragment that neutralizes TNFα activity is a TNFR2 molecule extracellular region or an anti-TNFα single-chain antibody, wherein the CTLA4 molecule extracellular region is located at the N-terminus of the bifunctional protein, and the TNFR2 molecule extracellular region or the anti-TNFα scFv is located in the middle or the C-terminus of the bifunctional protein. The bifunctional fusion protein can simultaneously block the signal pathways of B7/CD28 and TNFα/TNFR, thereby inhibiting inflammation reactions. Comparing to single-function proteins, the present invention can lower the production cost, reduce clinically administered medicine volume and frequency, and enhance compliance of the test subjects.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12N 15/62 - DNA sequences coding for fusion proteins
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
53.
Method for treating cancer using an interferon alpha conjugate
A method for preventing or treating a cancer includes administering an anti-cancer pharmaceutical composition including an interferon alpha or a polymer conjugate thereof. The pharmaceutical composition can be co-administered with anti-cancer agents. The interferon alpha conjugate shows a longer in vivo half-life and a more excellent anti-cancer activity than the conventional interferon alpha, and in particular, its co-administration with an anti-cancer agent such as gemcitabine has synergistic inhibitory effects on cancer cell growth and proliferation so as to exhibit a remarkably excellent anti-cancer activity. Further, the anti-cancer pharmaceutical composition has excellent in vivo half-life and anti-cancer activity to greatly reduce administration frequency. Co-administration of an anti-cancer agent and the interferon alpha conjugate having excellent anti-cancer activity reduces administration dose of anti-cancer agent so as to reduce side effects of anti-cancer agent and increase treatment compliance of patient.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 9/00 - Medicinal preparations characterised by special physical form
54.
Glucose dependent insulinotropic polypeptide analogs, pharmaceutical compositions and use thereof
The present invention provides a GIP analog, which is derived from GIP (1-29, SEQ ID NO: 1), has both GLP-1 agonist activity and GIPR stimulation activity, and comprises an amino acid sequence represented by the following formula I: Tyr-A2-A3-Gly-Thr-Phe-A7-Ser-Asp-Tyr-Ser-A12-A13-A14-A15-Lys-A17-A18-A19-A20-A21-A22-A23-A24-Trp-Leu- A27-A28-A29-Y. The present invention also provides a pharmaceutical composition comprising the GIP analog and use thereof.
Disclosed is a compound of formula (I), wherein R1, R2, L, Rm and Rn are as defined herein. The compound of formula (I) may be used in preventing and/or treating acyl CoA-diacylglycerol acyltransferase 1(DGAT-1) related diseases, such as obesity, coronary disease, hypertension, hyperlipidemia, arteriosclerosis, type II diabetes, stroke, hepatitis C, and the like.
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 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 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur 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
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
The present invention relates to an anti-cancer pharmaceutical composition comprising an interferon alpha or a polymer congugate thereof and use thereof in the treatment of cancer by co-administration with anti-cancer agents. The interferon alpha conjugate of the present invention shows a longer in vivo half-life and a more excellent anti-cancer activity than the conventional interferon alpha, and in particular, its co-administration with an anti-cancer agent such as gemcitabine has synergistic inhibitory effects on cancer cell growth and proliferation so as to exhibit a remarkably excellent anti-cancer activity. Further, the anti-cancer pharmaceutical composition of the present invention has excellent in vivo half-life and anti-cancer activity to greatly reduce administration frequency. Co-administration of an anti-cancer agent and the interferon alpha conjugate having excellent anti-cancer activity reduces administration dose of anti-cancer agent so as to reduce side effects of anti-cancer agent and increase treatment compliance of patient.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 47/30 - Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
The present invention relates to a coumarin derivative of formula (I): wherein X, Y1, Y2, Y3, R1, R2, R3 and R4 are as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising the compound of the present invention, and use of the compound of the present invention in treating tumor and/or inflammation.
C07D 311/08 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention provides a GIP analog, which is derived from GIP (1-29, SEQ ID NO: 1), has both GLP-1 agonist activity and GIPR stimulation activity, and comprises an amino acid sequence represented by the following formula I: Tyr-A2-A3-Gly-Thr-Phe-A7-Ser-Asp-Tyr-Ser-A12-A13- A14-A15-Lys-A17-A18-A19-A20-A21 -A22-A23-A24-Trp-Leu-A27-A28-A29-Y. The present invention also provides a pharmaceutical composition comprising the GIP analog and use thereof.
Compounds of formula I as inhibitors and their process of preparation are disclosed. The compounds can be used to inhibit Hedgehog pathway and can be used as new medicine for treating cancer. Pharmaceutical compositions as inhibitors containing the said compounds which are used as Hedgehog pathway inhibitors for treating cancer are disclosed. The use of said compounds in the manufacture of medicaments of the Hedgehog pathway inhibitors is disclosed.
C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
