Abstract

The present disclosure relates to an antibody or antigen-binding fragment thereof that is specific for transmembrane and coiled-coil domain family 3 (TMCC3). The present disclosure also relates to a pharmaceutical composition for treating and/or preventing a disease related to a TMCC3-mediated signal in a subject in need thereof, and a method for detecting TMCC3, a cancer stem cell or a cancer in a sample.

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 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 38/00 - Medicinal preparations containing peptides
• 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
• C12N 5/078 - Cells from blood or from the immune system
• C12N 5/095 - Stem cellsProgenitor cells
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• G01N 33/575 -
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

Disclosed herein are a messenger RNA (mRNA) comprising an open reading frame (ORF) encoding a protein of interest, a heterologous 5' untranslated region (UTR) and/or a heterologous 3' UTR for highly expressing the protein of interest. A method for synthesizing the mRNA and uses of the mRNA are also provided.

IPC Classes  ?

• C12N 15/67 - General methods for enhancing the expression
• C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• A61K 38/44 - Oxidoreductases (1)
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 9/51 - Nanocapsules
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• C12N 9/12 - Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)

Abstract

Disclosed herein is a double stranded RNA (dsRM A) molecule for RNA interference. A method for inhibiting the expression of complement factor B (CFB) and a method for treating a complement-related disease are also provided.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/7115 - Nucleic acids or oligonucleotides having modified bases, i.e. other than adenine, guanine, cytosine, uracil or thymine
• A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
• 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

Abstract

A lipid is represented by Formula (I), wherein each of the substituents in Formula (I) is given the definition as set forth in the Specification and Claims. A lipid nanoparticle including the lipid, a helper lipid, a steroid, a PEGylated lipid, a branched-chain ionizable cationic lipidoid with five hydroxyl groups, and a nucleic acid is also provided. A method for delivering a nucleic acid to a subject using a pharmaceutical composition including the lipid nanoparticle, and a pharmaceutical composition for delivering a nucleic acid to a subject are also provided.

IPC Classes  ?

• A61K 9/51 - Nanocapsules
• A61K 31/70 - CarbohydratesSugarsDerivatives thereof
• A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides

Abstract

Disclosed herein are a messenger RNA (mRNA) comprising an open reading frame (ORF) encoding a protein of interest, a heterologous 5′ untranslated region (UTR) and/or a heterologous 3′ UTR for highly expressing the protein of interest. A method for synthesizing the mRNA and uses of the mRNA are also provided.

IPC Classes  ?

• C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
• A61K 38/00 - Medicinal preparations containing peptides
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• C12N 9/90 - Isomerases (5.)
• C12P 19/34 - Polynucleotides, e.g. nucleic acids, oligoribonucleotides

Abstract

Disclosed herein are recombinant antibodies specific to programmed death 1 (PD-1), chimeric antigen receptors (CARs) and genetically modified cells configured to express the CARs on their surfaces and secret the recombinant antibodies specific to PD-1. Also disclosed herein is a method of treating cancer by administering the genetically modified cells to a subject afflicted with cancer.

IPC Classes  ?

• A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
• A61K 40/11 - T-cells, e.g. tumour infiltrating lymphocytes [TIL] or regulatory T [Treg] cellsLymphokine-activated killer [LAK] cells
• A61K 40/15 - Natural-killer [NK] cellsNatural-killer T [NKT] cells
• A61K 40/17 - MonocytesMacrophages
• A61K 40/31 - Chimeric antigen receptors [CAR]
• A61K 40/42 - Cancer antigens
• A61P 35/00 - Antineoplastic agents
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C07K 14/725 - T-cell receptors
• 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

Disclosed herein are recombinant antibodies specific to programmed death 1 (PD-1), chimeric antigen receptors (CARs) and genetically modified cells configured to express the CARs on their surfaces and secret the recombinant antibodies specific to PD-1. Also disclosed herein is a method of treating cancer by administering the genetically modified cells to a subject afflicted with cancer.

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 5/0783 - T cellsNK cellsProgenitors of T or NK cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells

Goods & Services

Adjuvants, other than for medical or veterinary purposes; biochemical catalysts; chemical preparations for scientific purposes, other than for medical or veterinary use; sulphides; carbides; carbonic hydrates; ferments for chemical purposes, namely, fermentation extract; biological preparations for use in industry and science, other than for medical or veterinary purposes; benzene derivatives, namely, benzene-based acids; protein in raw material form for scientific and medical research; chemicals for science; aromatic compounds, namely aromatic hydrocarbons; enzyme reagent for scientific and research use; chemical reagents for non-medical purposes; active chemical ingredients for use in the manufacture of pharmaceuticals; chemical substances for analyses in laboratories, other than for medical or veterinary purposes; proteins for use in manufacture; chemical analytical reagent for tests, other than for medical or veterinary purpose; chemical reagents, other than for medical or veterinary purposes; glycoprotein; biological preparations for use in industry and science; polymers and polymeric additives for use in the manufacture of pharmaceutical preparations, plastics, cosmetics, personal care products, coatings, adhesives, and lubricants; proteins for use in the manufacture of drugs Immunostimulants; chemical preparations for medical purposes, namely, for prevention and treatment of cancer; enzyme preparations for medical purposes; ferments for pharmaceutical purposes; adjuvants for medical purposes; chemical reagents for medical purposes; anti-cancer drug preparations; medicines to treat cancers for human purposes; medicinal preparations for treating cancer in humans; antiviral drug; biological preparations for medical purposes, namely, for the treatment of cancer; chemico-pharmaceutical preparations, namely, for the prevention and treatment of cancer; protein preparations for medical purposes, namely, biological therapeutics for cancer; chemical preparations for pharmaceutical purposes, namely, for the prevention and treatment of cancer; pharmaceutical drugs, namely, pharmaceutical preparations for the prevention and treatment of cancer; pharmaceutical preparations for the prevention and treatment of cancer; biological reagent for medical purposes; enzymes for medical purposes; western medicine, namely, pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; biological preparations for the treatment of cancer; medicinal preparations for the treatment of infectious diseases and for use in oncology; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment and prevention of cancer; pharmaceutical preparations for use in chemotherapy; pharmaceutical products for the prevention and treatment of cancer; pharmaceutical products for the treatment of cancer; pharmaceutical products for the treatment of viral and infectious diseases, for the treatment of cancer; ferments for chemical purposes, namely, ferments for pharmaceutical purposes; enzyme reagents for medical purposes; chemical reagents for medical purposes; chemical analytical reagent for tests, for medical purposes. Chemical analysis; biological research; scientific laboratory services; scientific research; chemistry research services; scientific laboratory services, namely, clinical laboratory testing of medical reagent; scientific research in the nature of conducting clinical trials for others; biochemical research and analysis of medical reagent; providing scientific research and development; research and development of new products for others; technological research in the field of biotechnology and biopharmaceuticals; conducting technical project studies, namely, technical research in the field of pharmaceutical studies; technological consultancy in the field of biotechnology; scientific and technological research in the field of biopharmaceuticals; culturing of cells for others for scientific research purposes; biological research and analysis; chemical research and analysis; chemical research services; medical and scientific research in the field of cancer treatment and diagnosis; medical research in the field of oncology; medical research services; medical research services in the field of cancer; pharmaceutical research and development; providing information about medical research in the field of oncology; providing laboratory research services in the field of gene expression, namely, cancer biology; research and development of pharmaceuticals for the treatment of age-related diseases and cancer; scientific research and development; technical research in the field of pharmaceutical studies. Health care; hospitals; medical services, namely medical treatment of cancer; pathological examination for medical diagnosis and treatment; preparation of prescriptions by pharmacists; alternative medicine services; medical assistance; occupational therapy; drug screening for medical diagnosis and treatment; cancer screening services; health care services for treating cancer; providing health information in the field of cancer prevention and treatment; providing information in the field of cancer prevention, screening, diagnosis and treatment; medical laboratory analysis services, namely, clinical laboratory testing of medical reagents for the treatment of persons; medical laboratory analysis services, namely, analysis of medical reagents for the treatment of persons.

Goods & Services

Adjuvants, other than for medical or veterinary purposes; biochemical catalysts; chemical preparations for scientific purposes, other than for medical or veterinary use; sulphides; carbides; carbonic hydrates; ferments for chemical purposes; biological preparations, other than for medical or veterinary purposes; benzene derivatives; protein [raw material]; chemicals for science; aromatic compounds; enzyme reagent; chemical reagents; active chemical ingredients for use in the manufacture of pharmaceuticals; chemical substances for analyses in laboratories, other than for medical or veterinary purposes; proteins for use in manufacture; chemical analytical reagent for tests; chemical reagents, other than for medical or veterinary purposes; glycoprotein; biological preparations for use in industry and science; polymers and polymeric additives for use in the manufacture of pharmaceutical preparations, plastics, cosmetics, personal care products, coatings, adhesives, and lubricants; protein in raw material form for scientific and medical research; proteins for use in the manufacture of drugs. Immunostimulants; chemical preparations for medical purposes; enzyme preparations for medical purposes; ferments for pharmaceutical purposes; adjuvants for medical purposes; chemical reagent for medical purposes; anticancer drug; medicines for human purposes; medicinal agent for human use; antiviral drug; biological preparations for medical purposes; chemico-pharmaceutical preparations; albuminous preparations for medical purposes; chemical preparations for pharmaceutical purposes; pharmaceutical drugs; pharmaceutical preparations; biological reagent for medical purposes; enzymes for medical purposes; medicated preparations of western medicine; anti- cancer preparations; tumor suppressing agents; biological preparations for the treatment of cancer; medicinal preparations for the treatment of infectious diseases and for use in oncology; pharmaceutical preparations for suppressing tumors; pharmaceutical preparations for the treatment and prevention of cancer; pharmaceutical preparations for use in chemotherapy; pharmaceutical products for the prevention and treatment of cancer; pharmaceutical products for the treatment of cancer; pharmaceutical products for the treatment of viral and infectious diseases, for the treatment of cancer. Chemical analysis; biological research; scientific laboratory services; scientific research; chemistry services; clinical lab test of medical reagent; clinical trials; research and analysis of medical reagent; providing research and development; research and development of new products for others; technological research; conducting technical project studies; technological consultancy; scientific research and technological research; culturing of cells for scientific research purposes; biological research and analysis; chemical research and analysis; chemical research services; medical and scientific research in the field of cancer treatment and diagnosis; medical research in the field of oncology; medical research services; medical research services in the field of cancer; pharmaceutical research and development; providing information about medical research in the field of oncology; providing laboratory research services in the field of gene expression, namely, cancer biology; research and development of pharmaceuticals for the treatment of age-related diseases and cancer; scientific research and development; technical research in the field of pharmaceutical studies. Health care; hospitals; therapy services; pathological examinations; preparation of prescriptions by pharmacists; alternative medicine services; medical assistance; occupational therapy; drug screening for medical diagnosis and treatment; cancer screening services; health care services for treating cancer; providing health information in the field of cancer prevention and treatment; providing information in the field of cancer prevention, screening, diagnosis and treatment.

Abstract

Disclosed are compounds of formula (I) below and tautomers, stereoisomers, isotopologues, solvates, polymorphs, or pharmaceutically acceptable salts thereof: in which each of variables R1, R2, R3, R4, R5, R6 and L is defined herein. Also disclosed are a method for treating disease or disorder mediated by formyl peptide receptor with the compound of formula (I) or a tautomer, stereoisomer, isotopologue, solvate, polymorph, or salt thereof, and a pharmaceutical composition containing same.

IPC Classes  ?

• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
• A61K 31/33 - Heterocyclic compounds

Abstract

Disclosed herein is a recombinant antibody or a fragment thereof exhibiting binding affinity and specificity toward B7-H3. According to some embodiments of the present disclosure, the recombinant antibody or its fragment comprises a heavy chain variable (VH) domain and a light chain variable (VL) domain respectively having the amino acid sequences of SEQ ID NOs: 7 and 8. Also disclosed herein are an immunoconjugate comprising the recombinant antibody or its fragment, and a method of treating cancers by use of the present immunoconjugate.

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 16/46 - Hybrid immunoglobulins
• 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
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed herein is a recombinant antibody or a fragment thereof exhibiting binding affinity and specificity toward B7-H3. According to some embodiments of the present disclosure, the recombinant antibody or its fragment comprises a heavy chain variable (VH) domain and a light chain variable (VL) domain respectively having the amino acid sequences of SEQ ID NOs: 7 and 8. Also disclosed herein are an immunoconjugate comprising the recombinant antibody or its fragment, and a method of treating cancers by use of the present immunoconjugate.

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 39/00 - Medicinal preparations containing antigens or antibodies
• 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 51/10 - Antibodies or immunoglobulinsFragments thereof
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a novel antibody, an antigen-binding fragment thereof and the uses of the antibody and fragment, wherein the antibody and the fragment comprise specific complementarity-determining regions (CDRs) and/or specifically bind to human CD73 at specific epitopes.

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 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed herein are novel single-stranded anti-sense oligonucleotides (ASOs) capable of reducing the transcription of thioredoxin domain containing protein 5 (TXNDC5) mRNA. Also disclosed is use of the single-stranded ASOs as disclosed herein for manufacturing medicaments suitable for treating a disease associated with upregulation of TXNDC5. Accordingly, a pharmaceutical composition comprising the disclosed ASO molecules is provided; as well as a method of treating a subject suffering from TXNDC5-mediated disease via administering to the subject the disclosed single-stranded ASO molecules.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61P 11/00 - Drugs for disorders of the respiratory system

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• 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

Abstract

A humanized anti-neurotensin receptor 1 (NTSR1) antibody or an antigen-binding fragment thereof. Also, a method for treating, prophylactic treating and/or preventing diseases and/or disorders caused by or related to NTSR1 activity and/or signaling, and a method or kit for detecting NTSR1 in a sample.

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
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression

Abstract

The present disclosure relates to a humanized anti-neurotensin receptor 1 (NTSR1) antibody or an antigen-binding fragment thereof. The present disclosure also relates to a method for treating, prophylactic treating and/or preventing diseases and/or disorders caused by or related to NTSR1 activity and/or signaling, and a method or kit for detecting NTSR'l in a sample.

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 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

IPC Classes  ?

• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C07K 14/735 - Fc receptors
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• C07K 16/46 - Hybrid immunoglobulins

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
• C07K 16/46 - Hybrid immunoglobulins
• C12N 15/64 - General methods for preparing the vector, for introducing it into the cell or for selecting the vector-containing host
• C12N 15/79 - Vectors or expression systems specially adapted for eukaryotic hosts
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

The present disclosure relates to a fusion protein comprising a Gas6 binding portion and an antigen binding portion comprising an anti-PD-L1 antibody or antigen-binding fragment thereof. The present disclosure also relates to a method for treating and/or detecting a cancer in a subject in need, and a kit for detecting a cancer in a sample.

IPC Classes  ?

• C12N 9/12 - Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
• A61K 38/00 - Medicinal preparations containing peptides
• 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
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

The present disclosure relates to an antibody or antigen-binding fragment thereof that is specific for transmembrane and coiled-coil domain family 3 (TMCC3). The present disclosure also relates to a pharmaceutical composition for treating and/or preventing a disease related to a TMCC3-mediated signal in a subject in need thereof, and a method for detecting TMCC, a cancer stem cell or a cancer in a sample.

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
• C07K 16/46 - Hybrid immunoglobulins
• C12N 15/64 - General methods for preparing the vector, for introducing it into the cell or for selecting the vector-containing host
• C12N 15/79 - Vectors or expression systems specially adapted for eukaryotic hosts
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

The present disclosure relates to a fusion protein comprising a GasS binding portion and an antigen binding portion comprising an anti-PD-Ll antibody or antigen-binding fragment thereof. The present disclosure also relates to a method for treating and/or detecting a cancer in a subject in need, and a kit for detecting a cancer in a sample.

IPC Classes  ?

• C07K 14/735 - Fc receptors
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• C07K 16/46 - Hybrid immunoglobulins
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure relates to an anti-PD-L1 antibody or an antigen-binding fragment thereof, comprising: a heavy chain variable region sequence comprising the three CDRs with the sequences of SEQ ID NOs: 2 to 4, or 6 to 8; and a light chain variable region sequence comprising the three CDRs with the sequences of SEQ ID NOs: 10 to 12, or 14 to 16. The present disclosure also relates to a pharmaceutical composition and a method for detecting expression of PD-L1 in a sample.

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 39/00 - Medicinal preparations containing antigens or antibodies
• 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
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed herein is a chimeric antigen receptor (CAR) comprising a single-chain variable fragment specific to Globo H, a hinge and transmembrane domain, a co-stimulatory molecule, and a cytoplasmic domain. According to some embodiments of the present disclosure, the CAR further comprises a single-chain variable fragment specific to PD-L1, and optionally, a fragment crystallizable region of an immunoglobulin. Also disclosed herein are isolated nucleic acids encoding the CAR pharmaceutical kits comprising the isolated immune cells expressing the C AR, and methods of treating cancers by using isolated immune cells.

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
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C12N 15/90 - Stable introduction of foreign DNA into chromosome
• C07K 14/005 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from viruses
• C12N 9/12 - Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
• C12N 15/86 - Viral vectors

Abstract

Disclosed herein is a chimeric antigen receptor (CAR) comprising a single-chain variable fragment specific to Globo H, a hinge and transmembrane domain, a co-stimulatory molecule, and a cytoplasmic domain. According to some embodiments of the present disclosure, the CAR further comprises a single-chain variable fragment specific to PD-L1, and optionally, a fragment crystallizable region of an immunoglobulin. Also disclosed herein are isolated nucleic acids encoding the CAR pharmaceutical kits comprising the isolated immune cells expressing the CAR, and methods of treating cancers by using isolated immune cells.

IPC Classes  ?

• A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61P 35/00 - Antineoplastic agents
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• 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

The present disclosure relates to an anti-PD-L1 antibody or an antigen-binding fragment thereof, comprising: a heavy chain variable region sequence comprising the three CDRs with the sequences of SEQ, ID NOs: 2 to 4, or 6 to 8; and a light chain variable region sequence comprising the three CDRs with the sequences of SEQ ID NOs: 10 to 12, or 14 to 16. The present disclosure also relates to a pharmaceutical composition and a method for detecting expression of PD-L1 in a sample.

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 5/0783 - T cellsNK cellsProgenitors of T or NK cells
• A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes

IPC Classes  ?

• A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
• 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 5/0783 - T cellsNK cellsProgenitors of T or NK cells

Abstract

The present invention relates to a novel antibody, an antigen-binding fragment thereof and the uses of the antibody and fragment, wherein the antibody and the fragment comprise specific complementarity-determining regions (CDRs) and/or specifically bind to human CD73 at specific epitopes.

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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention relates to a novel antibody, an antigen-binding fragment thereof and the uses of the antibody and fragment, wherein the antibody and the fragment comprise specific complementarity-determining regions (CDRs) and/or specifically bind to human CD73 at specific epitopes.

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
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• 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
• C12N 9/16 - Hydrolases (3.) acting on ester bonds (3.1)

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 16/30 - 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 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• C12N 9/16 - Hydrolases (3.) acting on ester bonds (3.1)

IPC Classes  ?

• A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
• A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
• A61P 19/00 - Drugs for skeletal disorders
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 35/00 - Antineoplastic agents
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

TXNDC5TXNDC5) mRNA. Also disclosed is use of the single-stranded ASOs as disclosed herein for manufacturing medicaments suitable for treating a disease associated with upregulation of TXNDC5. Accordingly, a pharmaceutical composition comprising the disclosed ASO molecules is provided; as well as a method of treating a subject suffering from TXNDCS-mediated disease via administering to the subject the disclosed single-stranded ASO molecules.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
• A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof

Abstract

The present disclosure provides a bifunctional compound of formula (I): RB-Linker-ULM (I), which binds more preferentially to mutant KRAS proteins than to wild KRAS protein and promotes degradation of KRAS protein via recruitment of an E3 ubiquitin ligase. Pharmaceutical compositions comprising the bifunctional compound and uses thereof are also provided.

IPC Classes  ?

• 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
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents

Abstract

A compound, which can act as inhibitors of protein kinases, especially Class III RTKs such as FLT3, PDGFRα, c-KIT and/or CSF-1R kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a binder of a Proteolysis-Targeting Chimera (PROTAC) thereof. The compound can be used in the treatments of diseases or conditions mediated by FLT3, PDGFR, c-KIT, and/or CSF-1R kinases, or mediated by a mutant kinase of FLT3, PDGFR, c-KIT, and/or CSF-1R kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• 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

Abstract

An antibody, or an antigen-binding fragment thereof, that binds specifically to human CSF-1R includes a heavy chain variable domain that contains a HCDR1 region having the sequence of SEQ ID NO: 4, a HCDR2 region having the sequence of SEQ ID NO: 5, and a HCDR3 region having the sequence of SEQ ID NO: 6; and a light chain variable domain that contains a LCDR1 region having the sequence of SEQ ID NO: 7, a LCDR2 region having the sequence of SEQ ID NO: 8, and a LCDR3 region having the sequence of SEQ ID NO: 9. The heavy chain variable domain comprises the sequence of SEQ ID NO: 2, and wherein the light chain variable domain comprises the sequence of SEQ ID NO: 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
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure provides an immunoconjugate includes an antibody comprising an antigen-binding fragment that specifically binds to an epitope in mesothelin, N-glycan binding domain and an N-glycan; a linker linking to the N-glycan; and a payload A and a payload B conjugated to the linker, respectively; wherein the payload A and the payload B are the same or different. A pharmaceutical composition comprises the immunoconjugate and a method for treating cancer are also provided in the disclosure.

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
• 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

Abstract

The present disclosure provides an immunoconjugate includes an antibody comprising an antigen-binding fragment that specifically binds to an epitope in mesothelin, an N-glycan binding domain and an N-glycan; a linker linking to the N-glycan; and a payload A and a payload B conjugated to the linker, respectively; wherein the payload A and the payload B are the same or different. A pharmaceutical composition comprises the immunoconjugate and a method for treating cancer are also provided in the disclosure.

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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

Abstract

The present disclosure provides an immunoconjugate includes an antibody comprising an antigen-binding fragment that specifically binds to an epitope in mesothelin, an N-glycan binding domain and an N-glycan; a linker linking to the N-glycan; and a payload A and a payload B conjugated to the linker, respectively; wherein the payload A and the payload B are the same or different. A pharmaceutical composition comprises the immunoconjugate and a method for treating cancer are also provided in the disclosure.

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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• C07K 16/46 - Hybrid immunoglobulins

Abstract

The present invention provides a compound of formula (I): RB-Linker-ULM which binds wild-type and mutant RAS proteins and promotes degradation via recruitment of an E3 ubiquitin ligase. Pharmaceutical compositions comprising the compound and uses thereof are also provided.

IPC Classes  ?

• A61K 31/404 - Indoles, e.g. pindolol
• 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
• 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

Abstract

An anti-PD-L1 antibody, or an antigen-binding fragment thereof, comprising: a heavy chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 2-4, 6-8, 10-12, 14-16, or 18-20; and/or a light chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 22-24, 26-28, 30-32, 34-36, or 38-40, wherein the antibody is a chimeric, humanized, composite, or human 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 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

A compound, which can act as inhibitors of protein kinases, especially Class III RTKs such as FLT3, PDGFRa, c-KIT and/or CSF-1R kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a binder of a Proteolysis-Targeting Chimera (PROTAC) thereof. The compound can be used in the treatments of diseases or conditions mediated by FLT3, PDGFR, c-KIT, and/or CSF-1R kinases, or mediated by a mutant kinase of FLT3, PDGFR, c-KIT, and/or CSF-1R kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/422 - Oxazoles not condensed and 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 31/454 - 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 31/506 - 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 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61P 35/00 - Antineoplastic agents
• C07D 495/04 - Ortho-condensed 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

Abstract

A compound, which can act as inhibitors of protein kinases, especially Class III RTKs such as FLT3, PDGFRa, c-KIT and/or CSF-1R kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a binder of a Proteolysis-Targeting Chimera (PROTAC) thereof. The compound can be used in the treatments of diseases or conditions mediated by FLT3, PDGFR, c-KIT, and/or CSF-1R kinases, or mediated by a mutant kinase of FLT3, PDGFR, c-KIT, and/or CSF-1R kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed 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
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone

Abstract

An immunoconjugate having the Formula Ab-[L1-(A-L2-B)m]n, wherein: (a) Ab is an antibody or a binding fragment thereof; (b) L1 and L2 are each independently a linker, wherein L1 and L2 are the same or different and wherein L1 links to L2; (c) A is a target-protein ligand/binder; (d) B is a ubiquitin ligase ligand/binder, and (e) n and m are independently integers from 1 to 8. The target protein includes kinase, G protein-coupled receptors, transcription factor, phosphatases, and RAS superfamily members.

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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are compounds of formula (I) below and tautomers, stereoisomers, isotopologues, or pharmaceutically acceptable salts thereof: 1, ring A, L, W, V, and G is defined herein. Also disclosed are a method for treating disease or disorder mediated by Tyro3, Axl, and/or Mer kinase with a compound of formula (I) or a tautomer, stereoisomer, isotopologue, or salt thereof and a pharmaceutical composition containing same.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids

Abstract

Disclosed herein are novel inhibitors of CD73. More specifically, the novel CD73 inhibitors are derived from benzothiadiazine. Further, the present disclosure is related to the use of said benzothiadiazine derivatives in the treatment of diseases and/or disorders mediated by adenosine, such as AIDS, an autoimmune disease, atherosclerosis, a cancer, an infectious disease, ischemia-reperfusion injury and pre-cancerous syndrome. Also encompassed in the present disclosure are pharmaceutical compositions comprising said benzothiadiazine derivatives.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 498/04 - Ortho-condensed systems

Abstract

A chimeric signal peptide for protein expression includes an N-region, a hydrophobic region, and a C-region, wherein the N-region and the C-region are from a same signal peptide of a first protein and the hydrophobic region is from a signal peptide of a second protein, wherein the first protein is different from the second protein. The first and second protein are independently selected from the group consisting of BM40, IL2, HA, Insulin, CD33, IFNA2, IgGK leader, AZU, and SEAP.

IPC Classes  ?

• C07K 7/04 - Linear peptides containing only normal peptide links
• C07K 14/17 - Porcine transmissible gastroenteritis virus
• C12N 15/62 - DNA sequences coding for fusion proteins

Abstract

An antibody, or an antigen-binding fragment thereof, that binds specifically to human CSF-1R includes a heavy chain variable domain that contains a HCDR1 region having the sequence of SEQ ID NO: 4, a HCDR2 region having the sequence of SEQ ID NO: 5, and a HCDR3 region having the sequence of SEQ ID NO: 6; and a light chain variable domain that contains a LCDR1 region having the sequence of SEQ ID NO: 7, a LCDR2 region having the sequence of SEQ ID NO: 8, and a LCDR3 region having the sequence of SEQ ID NO: 9. The heavy chain variable domain comprises the sequence of SEQ ID NO: 2, and wherein the light chain variable domain comprises the sequence of SEQ ID NO: 3.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• 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

Abstract

An immunoconjugate, comprising an anti-EGFR antibody or a binding fragment thereof, and a kinase inhibitor.

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
• 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 38/00 - Medicinal preparations containing peptides
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

A process for modifying glycoproteins is provided. The invention also provides a process for producing glycoprotein-payload conjugates, as well as the conjugates produced thereby.

IPC Classes  ?

• C12P 21/00 - Preparation of peptides or proteins
• 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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

Abstract

The present invention provides a compound of formula (1): 2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention rurthe r provides a process for preparing the compound.

IPC Classes  ?

• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
• C07D 239/48 - Two nitrogen atoms
• 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 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 403/04 - 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 directly linked by a ring-member-to-ring- member bond
• A61P 35/00 - Antineoplastic agents
• C07D 239/38 - One sulfur atom
• 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 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

A humanized anti-Globo H antibody, or an scFv or Fab fragment thereof, comprising a heavy-chain variable domain having three complementary regions consisting of HCDR1, HCDR2, and HCDR3 and a light-chain variable domain having three complementary regions consisting of LCDR1, LCDR2, and LCDR3, wherein the sequence of HCDR1 is GYISSDQILN (SEQ ID NO:4), the sequence of HCDR2 is RIYPVTGVTQYXHKFVG (SEQ ID NO:5, wherein X is any amino acid), and the sequence of HCDR3 is GETFDS (SEQ ID NO:6), wherein the sequence of LCDR1 is KSNQNLLX′SGNRRYZLV (SEQ ID NO:7, wherein X′ is F, Y, or W, and Z is C, G, S or T), the sequence of LCDR2 is WASDRSF (SEQ ID NO:8), and the sequence of LCDR3 is QQHLDIPYT (SEQ ID NO:9).

IPC Classes  ?

• C07K 16/34 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against blood group antigens

Abstract

An anti-PD-L1 antibody, or an antigen-binding fragment thereof, comprising: a heavy chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 2-4, 6-8, 10-12, 14-16, or 18-20; and/or a light chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 22-24, 26-28, 30-32, 34-36, or 38-40, wherein the antibody is a chimeric, humanized, composite, or human antibody.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• 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
• 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
• A61K 38/395 -
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

A humanized anti-human T-cell immunoglobulin domain and mucin domain 3 (TIM-3) antibody, or a binding fragment thereof, wherein the antibody or the binding fragment includes a heavy-chain variable domain that comprises framework region sequences derived from a human immunoglobulin and the following complementarity determining region (CDR) sequences: HCDRI (SEQ ID NO: 3), HCDR2 (SEQ ID NO: 4), HCDR3 (SEQ ID NO: 5), and a light-chain variable domain that includes framework region sequences from a human immunoglobulin and the following CDR sequences: LCDR1 (SEQ ID NO: 6), LCDR2 (SEQ ID NO: 7), and LCDR3 (SEQ ID NO: 8).

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C12N 15/13 - Immunoglobulins
• 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

Abstract

A regioselective one-step process for the synthesis of 2-hydroxyquinoxaline of Formula (1) or tautomers thereof: comprising reacting 1,2-phenylenediamine of Formula (2): with an excess amount of glyoxylic acid, glyoxylic acid monohydrate, or a 2,2-dialkoxyacetic acid of Formula (3): 2 are as defined in the specification.

IPC Classes  ?

• C07D 241/52 - Oxygen atoms
• C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring

Abstract

An antibody, or an antigen-binding fragment there, binding human ENO1 (GenBank: AAH506421.1) is provided. Methods for treating an ENO1 protein-related disease or disorder, inhibiting cancer invasion and diagnosis of cancer are also provided.

IPC Classes  ?

• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• A61P 35/00 - Antineoplastic agents
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

A compound, capable of inhibiting kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof. The compound can be used in the treatments of diseases or conditions mediated by CSF-1R, c-KIT, FLT3, or PDGFR kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• A61P 35/00 - Antineoplastic agents
• C07D 241/40 - Benzopyrazines
• C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring
• 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 401/12 - 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 241/52 - Oxygen 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 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 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
• 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 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 403/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 405/12 - 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 chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• 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

Abstract

An immunoconjugate having the Formula Ab-[L1-(A-L2-B)m]n, wherein: (a) Ab is an antibody or a binding fragment thereof; (b) L1 and L2 are each independently a linker, wherein L1 and L2 are the same or different and wherein L1 links to L2; (c) A is a target-protein ligand/binder; (d) B is a ubiquitin ligase ligand/binder, and (e) n and m are independently integers from 1 to 8. The target protein includes kinase, G protein-coupled receptors, transcription factor, phosphatases, and RAS superfamily members.

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
• 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

An immunoconjugate having the Formula Ab-[L1-(A-L2mnn, wherein: (a) Ab is an antibody or a binding fragment thereof; (b) L1and L2are each independently a linker, wherein L1and L2are the same or different and wherein L1links to L2; (c) A is a target-protein ligand/binder; (d) B is a ubiquitin ligase ligand/binder, and (e) n and m are independently integers from 1 to 8. The target protein includes kinase, G protein-coupled receptors, transcription factor, phosphatases, and RAS superfamily members.

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 16/30 - 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
• A61P 35/00 - Antineoplastic agents

Abstract

A 3D organoid is used for diagnosis or assay, wherein the 3D organoid is constructed from a tumor cell. The tumor cell in the 3D organoid is from a cell line, from circulating tumor cells isolated from a patient, or from a tumor tissue. The 3D organoid is constructed using an aqueous gel material and an adhesion molecule. The aqueous gel material is hydrogel. The adhesion molecule is ICAM-1 or galectin-3. The 3D organoid is constructed by forming a scaffold with an aqueous gel material, followed by adding a mixture of the tumor cell and an adhesion molecule.

IPC Classes  ?

• C12N 5/09 - Tumour cells
• A61L 27/24 - Collagen
• A61L 27/52 - Hydrogels or hydrocolloids

Abstract

An antigenic short peptide includes 11 to 15 amino-acid residues and has an ability to induce antibody against influenza virus. The sequence of the antigenic peptide is selected from hemagglutinin (HA). The antigenic peptide includes the sequence of JJ (SEQ ID NO:2), JJ-1 (SEQ ID NO:3), JJ-2 (SEQ ID NO:4), JJ-3 (SEQ ID NO:5) or JJ-4 SEQ ID NO:6). A method for inducing a broad-spectrum immunity against influenza viruses includes administering a vaccine to a subject, wherein the vaccine comprises one of the above antigenic peptide.

IPC Classes  ?

• A61K 39/145 - Orthomyxoviridae, e.g. influenza virus
• C07K 14/11 - Orthomyxoviridae, e.g. influenza virus
• C07K 16/10 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from viruses from RNA viruses

Abstract

A host cell for protein expression having a lower expression level of a gene, as compared to a wild-type cell, wherein the gene is selected from HDAC8, Dab2, Caspase3, Sys1, Ergic3, Grasp, Trim 23, or a combination thereof. The host cells are CHO cells. The lower expression level of the gene results from RNA interference, which may be achieved by transfecting a vector that contains an shRNA targeting the gene.

IPC Classes  ?

• C12N 15/09 - Recombinant DNA-technology
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• C12N 5/06 -
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

Disclosed are compounds of formula (I) below and tautomers, stereoisomers, isotopologues, or pharmaceutically acceptable salts thereof: in which each of variables R1, ring A, L, W, V, and G is defined herein. Also disclosed are a method for treating disease or disorder mediated by Tyro3, Axl, and/or Mer kinase with a compound of formula (I) or a tautomer, stereoisomer, isotopologue, or salt thereof and a pharmaceutical composition containing same.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups

Abstract

A method for predicting therapeutic efficacy of a drug includes analyzing a panel of genes to derive information for predicting whether a patient will respond to the drug. The analyzing a panel of genes includes analysis of gene mutations, copy number variations, and/or expression levels. The panel of genes comprises PIK3CA, KRAS, PTEN, BRAF, and CSF-1R. The gene mutations include E542K, E545K, and H1047R mutations in PIK3CA, G12C, G12D, G12V, G13D mutations in KRAS, R130G and C71F/Y mutations or deletion in PTEN, V600E mutation in BRAF, and H362R mutation in CSF-1R. The drug is a CSF-IR inhibitor.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12Q 1/6806 - Preparing nucleic acids for analysis, e.g. for polymerase chain reaction [PCR] assay
• C12Q 1/6811 - Selection methods for production or design of target specific oligonucleotides or binding molecules
• C12Q 1/6813 - Hybridisation assays
• C12Q 1/6827 - Hybridisation assays for detection of mutation or polymorphism

Abstract

Disclosed is an embedded nasal filtering apparatus, comprising a support body, an air permeable sac and a filtering element. The support body comprises a frame portion corresponding to the position of a nostril, and the frame portion defines a telescoping direction. The air permeable sac is connected to the frame portion, and the air permeable sac can be adjusted from a folded state to an unfolded state along the telescoping direction. When in the unfolded state, the air permeable sac forms an opening and an accommodating space which are mutually connected. The position of the filtering element corresponds to the frame portion. By means of the described design, the present invention can adapt to users having different intranasal space sizes.

Abstract

m, wherein Ab is the anti-Globo H antibody or the binding fragment thereof, L is a linker or a direct bond, D is the therapeutic agent or the label, and m is an integer from 1 to 8. The antibody may be a monoclonal antibody, which may be a humanized antibody. A method for treating a cancer includes administering to a subject in need of such treatment a pharmaceutically effective amount of an immunoconjugate containing an antibody against Globo H, or a binding fragment thereof, and a therapeutic agent covalently conjugated with the antibody.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• 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 49/00 - Preparations for testing in vivo
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• 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
• 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

Abstract

The present invention relates to xin yi extracts and a method for preparing the same. The treatment of periodontitis by using the xin yi extracts is also provided.

IPC Classes  ?

• A61K 36/57 - Magnoliaceae (Magnolia family)
• A61K 36/575 - Magnolia
• C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography

Abstract

Crassocephalum crepidioides extract. The use of the extract and the composition/combination comprising the extract in the prevention or treatment of cancer is also provided.

IPC Classes  ?

• A61K 36/28 - Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• A61K 36/00 - Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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
• A61K 9/14 - Particulate form, e.g. powders

Abstract

The present invention relates to an antibody or antigen-binding fragment thereof that bind human vascular endothelial growth factor receptor 2 (VEGFR-2). The present invention also relates to a method for inhibiting VEGFR-2-mediated signaling in a subject in need, a method for treating diseases and/or disorders caused by or related to VEGFR-2 activity and/or signaling in a subject afflicted with the diseases and disorders, a method for treating tumor in a subject afflicted with the tumor, a method for inhibiting cell proliferation of endothelial cells in a subject in need, and a method for detecting human vascular endothelial growth factor receptor in a sample.

IPC Classes  ?

• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• 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
• A61K 33/24 - Heavy metalsCompounds thereof

Abstract

An asymmetric heterodimeric antibody includes a knob structure formed in a CH3 domain of a first heavy chain; a hole structure formed in a CH3 domain of a second heavy chain, wherein the hole structure is configured to accommodate the knob structure so that a heterodimeric antibody is formed; and a T-cell targeting domain fused to the CH3 domain of the first heavy chain or the second heavy chain, wherein the T-cell targeting domain binds specifically to an antigen on the T-cell. The T-cell targeting domain is a ScFv or Fab derived from an anti-CD3 antibody. The asymmetric heterodimeric antibody may have L234A and L235A mutations or L235A and G237A such that its effector binding is compromised.

IPC Classes  ?

• A61K 47/66 - 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 a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
• 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
• 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 16/46 - Hybrid immunoglobulins

Abstract

A bispecific anti-Globo H antibody includes an anti-Globo H antibody that binds specifically to Globo H; and a T-cell targeting domain fused to a CH3 domain of a heavy chain of the anti-Globo H antibody, wherein the T-cell targeting domain binds specifically to an antigen on T-cells; and wherein the anti-Globo H antibody comprises mutations at an effector binding site such that the bispecific anti-Globo H antibody has a diminished effector function. The T-cell targeting domain is a ScFv or Fab from an anti-CD3 antibody.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• 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 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes

Abstract

An asymmetric heterodimeric antibody includes a knob structure formed in a CH3 domain of a first heavy chain; a hole structure formed in a CH3 domain of a second heavy chain, wherein the hole structure is configured to accommodate the knob structure so that a heterodimeric antibody is formed; and a T-cell targeting domain fused to the CH3 domain of the first heavy chain or the second heavy chain, wherein the T-cell targeting domain binds specifically to an antigen on the T-cell. The T-cell targeting domain is a ScFv or Fab derived from an anti-CD3 antibody. The asymmetric heterodimeric antibody may have L234A and L235A mutations or L235A and G237A such that its effector binding is compromised.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• 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 16/46 - Hybrid immunoglobulins
• 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

A bispecific anti-Globo H antibody includes an anti-Globo H antibody that binds specifically to Globo H; and a T-cell targeting domain fused to a CH3 domain of a heavy chain of the anti-Globo H antibody, wherein the T-cell targeting domain binds specifically to an antigen on T-cells; and wherein the anti-Globo H antibody comprises mutations at an effector binding site such that the bispecific anti-Globo H antibody has a diminished effector function. The T-cell targeting domain is a ScFv or Fab from an anti-CD3 antibody.

IPC Classes  ?

• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• 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
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes

Abstract

An immunoconjugate includes an anti-Globo H antibody, or a binding fragment thereof, and a therapeutic agent or a label, having the formula: Ab-(L-D)m, wherein Ab is the anti-Globo H antibody or the binding fragment thereof, L is a linker or a direct bond, D is the therapeutic agent or the label, and m is an integer from 1 to 8. The antibody may be a monoclonal antibody, which may be a humanized antibody. A method for treating a cancer includes administering to a subject in need of such treatment a pharmaceutically effective amount of an immunoconjugate containing an antibody against Globo H, or a binding fragment thereof, and a therapeutic agent covalently conjugated with the antibody.

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
• A61K 49/00 - Preparations for testing in vivo
• 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
• 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

An immunoconjugate includes an anti-Globo H antibody, or a binding fragment thereof, and a therapeutic agent or a label, having the formula: Ab-(L-D)m, wherein Ab is the anti-Globo H antibody or the binding fragment thereof, L is a linker or a direct bond, D is the therapeutic agent or the label, and m is an integer from 1 to 8. The antibody may be a monoclonal antibody, which may be a humanized antibody. A method for treating a cancer includes administering to a subject in need of such treatment a pharmaceutically effective amount of an immunoconjugate containing an antibody against Globo H, or a binding fragment thereof, and a therapeutic agent covalently conjugated with the antibody.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
• 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
• 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
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

A humanized anti-Globo H antibody, or an scFv or Fab fragment thereof, comprising a heavy-chain variable domain having three complementary regions consisting of HCDR1, HCDR2, and HCDR3 and a light -chain variable domain having three complementary regions consisting of LCDR1, LCDR2, and LCDR3, wherein the sequence of HCDR1 is GYISSDQILN (SEQ ID NO:4), the sequence of HCDR2 is RIYPVTGVTQYXHKFVG (SEQ ID NO:5, wherein X is any amino acid), and the sequence of HCDR3 is GETFDS (SEQ ID NO:6), wherein the sequence of LCDR1 is KSNQNLLX' SGNRRYZLV (SEQ ID NO: 7, wherein X' is F, Y, or W, and Z is C, G, S or T), the sequence of LCDR2 is WASDRSF (SEQ ID NO:8), and the sequence of LCDR3 is QQHLDIPYT (SEQ ID NO:9).

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 16/44 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere

Abstract

A humanized anti-Globo H antibody, or an scFv or Fab fragment thereof, comprising a heavy-chain variable domain having three complementary regions consisting of HCDRl, HCDR2, and HCDR3 and a light -chain variable domain having three complementary regions consisting of LCDRl, LCDR2, and LCDR3, wherein the sequence of HCDRl is GYISSDQILN (SEQ ID NO:4), the sequence of HCDR2 is RIYPVTGVTQYXHKFVG (SEQ ID NO:5, wherein X is any amino acid), and the sequence of HCDR3 is GETFDS (SEQ ID NO:6), wherein the sequence of LCDRl is KSNQNLLX' SGNRRYZLV (SEQ ID NO: 7, wherein X' is F, Y, or W, and Z is C, G, S or T), the sequence of LCDR2 is WASDRSF (SEQ ID NO:8), and the sequence of LCDR3 is QQHLDIPYT (SEQ ID NO:9).

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 16/44 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere

Abstract

A compound for inhibiting BMI-l/MCL-1 having a structure of Formula (I), wherein the various groups are as described. A pharmaceutical composition for treating cancer includes an effective amount of a compound of Formula (I).

IPC Classes  ?

• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• 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

Abstract

A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) 7 are defined herein. Compounds of formula (I) are useful for inhibition of protein kinases. Methods of using compounds of formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

IPC Classes  ?

• C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring
• 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
• A61P 35/00 - Antineoplastic agents
• 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 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
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

A process for modifying glycoproteins is provided. The invention also provides a process for producing glycoprotein-payload conjugates, as well as the conjugates produced thereby.

IPC Classes  ?

• 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
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• C12P 21/00 - Preparation of peptides or proteins

Abstract

A recombinant protein drug includes a parent protein drug coupled with a modified kininogen-1 peptide. The modified kininogen-1 peptide has the sequence of SEQ ID NO:2 or a homolog having a sequence identity of 80% or higher. The parent protein drug is a bispecific antibody having a first targeting domain linked by a bridging domain with a second targeting domain. The modified kininogen-1 peptide is fused between the first targeting domain and the bridging domain, or between the bridging domain and the second targeting domain. A method for increasing the serum half-life of a protein drug includes constructing a fusion protein comprising the protein drug coupled with a modified kininogen-1 peptide.

IPC Classes  ?

• 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
• A61K 47/55 - 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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds

Abstract

A process for modifying glycoproteins is provided. The invention also provides a process for producing glycoprotein-payload conjugates, as well as the conjugates produced thereby.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 16/46 - Hybrid immunoglobulins
• C12P 21/00 - Preparation of peptides or proteins
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• C12P 21/08 - Monoclonal antibodies

Abstract

The present invention relates to an antibody or antigen-binding fragment thereof that bind human vascular endothelial growth factor receptor 2 (VEGFR-2). The present invention also relates to a method for inhibiting VEGFR-2-mediated signaling in a subject in need, a method for treating diseases and/or disorders caused by or related to VEGFR-2 activity and/or signaling in a subject afflicted with the diseases and disorders, a method for treating tumor in a subject afflicted with the tumor, a method for inhibiting cell proliferation of endothelial cells in a subject in need, and a method for detecting human vascular endothelial growth factor receptor in a sample.

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
• G01N 33/74 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving hormones
• A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
• 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
• C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• 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 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 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

An antibody prodrug capable of being selectively activated in a central nervous system (CNS) by protease KLK6 includes an antibody for treating a disease or disorder in the CNS; a KLK6 cleavable peptide fused to an N-terminus of a heavy chain and/or a light chain of the antibody; and a blocker fused to an N-terminus of the KLK6 cleavable peptide. The disease or disorder is a cancer, inflammatory disease, autoimmune disease, infectious disease, or neuron degeneration disease.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/46 - Hybrid immunoglobulins
• C07K 19/00 - Hybrid peptides
• C12N 15/09 - Recombinant DNA-technology

Abstract

An anti-human T-cell immunoglobulin domain and mucin domain 3 (TIM-3) antibody, can bind the peptides, comprising the amino-acid sequence RKGDVSL (SEQ ID NO: 9) and/or EKFNLKL (SEQ ID NO: 10) of human TIM-3 protein. The antibody can regulate immune cell activity. The antibody or binding fragment thereof is useful in diagnosis, prognosis, and treatment of cancers that have been reported to express cell-surface TIM-3 such as lung, liver, esophageal cancer and solid tumors.

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

Described herein are specific CHO genomic sites for targeted insertion of exogenous genes. The sites are located within a sequence selected from SEQ ID NOs: 1-16.

IPC Classes  ?

• C12N 15/64 - General methods for preparing the vector, for introducing it into the cell or for selecting the vector-containing host
• C12N 15/67 - General methods for enhancing the expression
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• C12N 15/90 - Stable introduction of foreign DNA into chromosome

Abstract

An immunoconjugate, comprising an anti-EGFR antibody or a binding fragment thereof, and a kinase inhibitor.

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
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 47/50 - 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
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole

Abstract

The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, R1, R2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention further provides a process for preparing the compound.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms

Abstract

Anti-TMCC3 immunoconjugates are provided. The invention also provides methods of using the immunoconjugates in the treatment or detection of TMCC3-pocitive cancers.

IPC Classes  ?

• A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
• 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

A compound, capable of inhibiting kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof. The compound can be used in the treatments of diseases or conditions mediated by CSF-IR, c-KIT, FLT3, or PDGFR kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• C07D 241/40 - Benzopyrazines
• C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring
• 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

Abstract

A compound, capable of inhibiting kinases, for the treat- ments of diseases or disorders mediated by such kinases, has a structure of formula (I) or a stereoisomer, a tautomer, a pharmaceutically accept- able salt thereof. The compound can be used in the treatments of diseases or conditions mediated by CSF-IR, c-KIT, FLT3, or PDGFR kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

IPC Classes  ?

• C07D 241/40 - Benzopyrazines
• C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring
• 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

Abstract

The present invention provides a modified antigen-binding Fab fragment. An antigen-binding molecule comprising the antigen-binding Fab fragment and a composition comprising the molecule are also provided.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/46 - Hybrid immunoglobulins
• C12N 15/62 - DNA sequences coding for fusion proteins
• C12N 15/64 - General methods for preparing the vector, for introducing it into the cell or for selecting the vector-containing host
• C12N 15/66 - General methods for inserting a gene into a vector to form a recombinant vector using cleavage and ligationUse of non-functional linkers or adaptors, e.g. linkers containing the sequence for a restriction endonuclease
• C12N 15/86 - Viral vectors

Abstract

The present invention provides a process for the preparation of a Crassocephalum crepidioides extract, and the extract prepared thereby. The present invention further relates to a pharmaceutical composition/combination comprising the Crassocephalum crepidioides extract. The use of the extract and the composition/combination comprising the extract in the prevention or treatment of cancer is also provided.

IPC Classes  ?

• A61K 36/28 - Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to an antibody or antigen-binding fragment thereof that bind human vascular endothelial growth factor receptor 2 (VEGFR-2). The present invention also relates to a method for inhibiting VEGFR-2-mediated signaling in a subject in need, a method for treating diseases and/or disorders caused by or related to VEGFR-2 activity and/or signaling in a subject afflicted with the diseases and disorders, a method for treating tumor in a subject afflicted with the tumor, a method for inhibiting cell proliferation of endothelial cells in a subject in need, and a method for detecting human vascular endothelial growth factor receptor in a sample.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• 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
• C12N 15/13 - Immunoglobulins

Abstract

Hedychium coronarium Koenig and its use in lowering blood glucose, increasing insulin levels and treating and/or preventing diabetes.

IPC Classes  ?

• A61K 36/906 - Zingiberaceae (Ginger family)

Abstract

A humanized antibody, or a binding fragment thereof, wherein the humanized antibody binds human ENOl (GenBank: AAH50642.1), wherein the antibody comprises a light chain variable region (VL) domain comprising a CDR1 having the amino acid sequence LCDR1 (RASENIYSYLT; SEQ ID NO:6) and a CDR2 having the amino acid sequence LCDR2 (NAKTLPE; SEQ ID NO:7) and a CDR3 having the amino acid sequence LCDR3 (QHHYGTPYT; SEQ ID NO: 8) and an antibody heavy chain variable region (VH) domain comprising a CDR1 having the amino acid sequence HCDR1 (GYTFTSCVMN; SEQ ID NO:3), a CDR2 having the amino acid sequence HCDR2 (YINPYNDGTKYNEKFKG; SEQ ID NO:4) and a CDR3 having the amino acid sequence HCDR3 (EGFYYGNFDN; SEQ ID NO: 5), wherein framework regions in the light chain variable region (VL) domain and the heavy chain variable region (VH) domain comprise amino acid sequences from a human immunoglobulin.

IPC Classes  ?

• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

Abstract

A humanized antibody, or a binding fragment thereof, wherein the humanized antibody binds human ENOl (GenBank: AAH50642.1), wherein the antibody comprises a light chain variable region (VL) domain comprising a CDR1 having the amino acid sequence LCDR1 (RASENIYSYLT; SEQ ID NO:6) and a CDR2 having the amino acid sequence LCDR2 (NAKTLPE; SEQ ID NO:7) and a CDR3 having the amino acid sequence LCDR3 (QHHYGTPYT; SEQ ID NO: 8) and an antibody heavy chain variable region (VH) domain comprising a CDR1 having the amino acid sequence HCDR1 (GYTFTSCVMN; SEQ ID NO:3), a CDR2 having the amino acid sequence HCDR2 (YINPYNDGTKYNEKFKG; SEQ ID NO:4) and a CDR3 having the amino acid sequence HCDR3 (EGFYYGNFDN; SEQ ID NO: 5), wherein framework regions in the light chain variable region (VL) domain and the heavy chain variable region (VH) domain comprise amino acid sequences from a human immunoglobulin.

IPC Classes  ?

• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

Abstract

A method for specific linkage to a glycoprotein includes obtaining a glycoprotein having a monoglycan or diglycan attached thereto; producing a reactive functional group on a sugar unit on the glycoprotein; and coupling a linker or a payload to the reactive functional group on the glycoprotein.

IPC Classes  ?

• C07K 1/08 - General processes for the preparation of peptides using protecting groups or activating agents using activating agents
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans

Abstract

A humanized antibody, or a binding fragment thereof, wherein the humanized antibody binds human ENO1 (GenBank: AAH50642.1), wherein the antibody comprises a light chain variable region (VL) domain comprising a CDR1 having the amino acid sequence LCDR1 (RASENIYSYLT; SEQ ID NO: 6) and a CDR2 having the amino acid sequence LCDR2 (NAKTLPE; SEQ ID NO: 7) and a CDR3 having the amino acid sequence LCDR3 (QHHYGTPYT; SEQ ID NO: 8) and an antibody heavy chain variable region (VH) domain comprising a CDR1 having the amino acid sequence HCDR1 (GYTFTSCVMN; SEQ ID NO: 3), a CDR2 having the amino acid sequence HCDR2 (YINPYNDGTKYNEKFKG; SEQ ID NO: 4) and a CDR3 having the amino acid sequence HCDR3 (EGFYYGNFDN; SEQ ID NO: 5), wherein framework regions in the light chain variable region (VL) domain and the heavy chain variable region (VH) domain comprise amino acid sequences from a human immunoglobulin.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.

IPC Classes  ?

• 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
• 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 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
• 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 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 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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