A method for preparing a benzofuran derivative. Specifically, the present invention relates to a method for preparing a benzofuran derivative represented by formula L The preparation method greatly improves yield and has good application prospects.
C07D 405/14 - 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 three or more hetero rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The present invention relates to the use of an EZH2 inhibitor in the preparation of a drug for treating T-cell lymphoma. Specifically, the present invention relates to the use of a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating T-cell lymphoma.
The present invention relates to the use of an EZH2 inhibitor in the preparation of a drug for treating T-cell lymphoma. Specifically, the present invention relates to the use of a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating T-cell lymphoma.
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The present invention provides a pharmaceutical composition comprising a CD40 antibody or an antigen-binding fragment thereof and an acetic acid-sodium acetate buffer solution, and a use thereof. The pharmaceutical composition may further contain sugar, a non-ionic surfactant, and other excipients. The pharmaceutical composition of the present invention shows good antibody stability.
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 9/19 - Particulate form, e.g. powders lyophilised
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
4.
Antibody capable of binding to thymic stromal lymphopoietin and use thereof
Disclosed are an antibody capable of binding to thymic stromal lymphopoietin and the use thereof. Disclosed are an anti-TSLP antibody, comprising a murine antibody, chimeric antibody and humanized antibody of the light chain and heavy chain variable regions of the anti-TSLP antibody and antigen-binding fragments thereof, or a pharmaceutically acceptable salt or solvent compound thereof, and the use thereof as a medicament for treating asthma, especially the use thereof in the preparation of a drug for treating TSLP-positive diseases or conditions.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
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 9/00 - Medicinal preparations characterised by special physical form
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
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention relates to an echinocandin analogue and a preparation method therefor. The compound can be used for preventing or treating fungal infection, or for preventing, stabilizing or inhibiting fungal growth or killing fungi. An exemplary compound is represented by formula I, wherein the definitions of R1, R2, R3 and G groups are as described in the description.
The present invention relates to an echinocandin analogue and a preparation method therefor. The compound can be used for preventing or treating fungal infection, or for preventing, stabilizing or inhibiting fungal growth or killing fungi. An exemplary compound is represented by formula I, wherein the definitions of R1, R2, R3 and G groups are as described in the description.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
The present disclosure relates to a drug conjugate of an Eribulin derivative, a preparation method therefor and an application thereof in medicine. Specifically, provided is an antibody-drug conjugate, which contains an Eribulin derivative drug portion. The present disclosure further relates to a method for treating cancer by administering the antibody-drug conjugate provided herein.
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 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
8.
TRICYCLIC TETRAHYDROISOQUINOLINE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF IN MEDICINE
The present disclosure relates to a tricyclic tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, the present disclosure relates to a tricyclic tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a pharmaceutical composition comprising said derivative, a use thereof as an estrogen receptor modulator, and a use thereof in preparing a drug for treating estrogen receptor-mediated or dependent diseases or disorders. The substituents in general formula (I) are the same as those defined in the description.
The present disclosure relates to a tricyclic tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, the present disclosure relates to a tricyclic tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a pharmaceutical composition comprising said derivative, a use thereof as an estrogen receptor modulator, and a use thereof in preparing a drug for treating estrogen receptor-mediated or dependent diseases or disorders. The substituents in general formula (I) are the same as those defined in the description.
The present invention relates to an anti-ANGPTL3 antibody and a use thereof. In particular, the present invention relates to the anti-ANGPTL3 antibody and an antigen-binding fragment thereof, or a pharmaceutically acceptable salt or solvent thereof, and a use thereof as a medicine, in particular a use in the preparation of a medicine for treating hyperlipidemia.
The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 235/12 - Radicals substituted by oxygen atoms
C07D 235/14 - Radicals substituted by nitrogen atoms
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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 409/04 - 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 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
The present disclosure relates to a new polypeptide complex. Specifically, the present disclosure relates to a domain engineered antibody. At least one of the constant region domains CH1 and/or CL of the antibody is replaced, and the domain CH1/CL is replaced by a Titin T chain/Obscurin-O chain or by a Titin T chain/Obscurin-like-O chain.
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
12.
CEPHALOSPORIN ANTIBACTERIAL COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
Provided are a cephalosporin compound represented by formula I-1, I-2, or I-3, a pharmaceutical composition comprising same, and use thereof as an antibacterial agent.
Provided are a cephalosporin compound represented by formula I-1, I-2, or I-3, a pharmaceutical composition comprising same, and use thereof as an antibacterial agent.
C07D 501/46 - Methylene radicals, substituted by nitrogen atomsLactams thereof with the 2-carboxyl groupMethylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atomQuaternary compounds thereof with the 7-amino radical acylated by carboxylic acids containing hetero rings
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
Provided in the present invention are an anti-TROP-2 antibody-exatecan analog conjugate and the medical use thereof. Specifically, provided in the present invention is an anti-TROP-2 antibody-exatecan analog conjugate represented by the general formula (Pc-L-Y-D), wherein Pc is an anti-TROP-2 antibody or an antigen-binding fragment thereof.
Provided in the present invention are an anti-TROP-2 antibody-exatecan analog conjugate and the medical use thereof. Specifically, provided in the present invention is an anti-TROP-2 antibody-exatecan analog conjugate represented by the general formula (Pc-L-Y-D), wherein Pc is an anti-TROP-2 antibody or an antigen-binding fragment thereof.
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
An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CRaRb)m—CR1R2—C(O)—, —O—CR1R2—(CRaRb)m—, —O—CR1R2—, —NH—(CRaRb)m—CR1R2—C(O)—, and —S—(CRaRb)m—CR1R2—C(O); and n is a decimal or integer from 1 to 10.
An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CRaRb)m—CR1R2—C(O)—, —O—CR1R2—(CRaRb)m—, —O—CR1R2—, —NH—(CRaRb)m—CR1R2—C(O)—, and —S—(CRaRb)m—CR1R2—C(O); and n is a decimal or integer from 1 to 10.
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
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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
The present disclosure relates to a crystal form of a pyridopyrimidine derivative and a preparation method thereof, and specifically relates to the crystal form of the compound of formula (I) and a preparation method thereof. The new crystal form has good physical and chemical properties, thereby facilitating clinical treatments.
An anti-claudin antibody-drug conjugate and a pharmaceutical use thereof, specifically relating to a ligand-drug conjugate represented by general formula (Pc-L-Y-D), wherein Pc is an anti-claudin 18.2 antibody or an antigen-binding fragment thereof, and L, Y, and n are as defined in the description.
An anti-claudin antibody-drug conjugate and a pharmaceutical use thereof, specifically relating to a ligand-drug conjugate represented by general formula (Pc-L-Y-D), wherein Pc is an anti-claudin 18.2 antibody or an antigen-binding fragment thereof, and L, Y, and n are as defined in the description.
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
A JAK kinase inhibitor pharmaceutical composition, containing (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide or a pharmaceutically acceptable salt thereof and a co-processed excipient, such as cellulose-lactose. The present invention has good stability, dissolution and bioavailability, and the preparation process thereof is simple and convenient.
Disclosed is a pyrazolo-heteroaryl derivative, a preparation method therefor, and medical use thereof. In particular, the present invention relates to a pyrazolo-heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and a use thereof as a therapeutic agent, particularly as ATR kinase inhibitor and in the preparation of drugs for the treatment and/or prevention of hyperproliferative diseases. The definition of each group in the general formula (I) is identical as in the specification.
Disclosed is a pyrazolo-heteroaryl derivative, a preparation method therefor, and medical use thereof. In particular, the present invention relates to a pyrazolo-heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and a use thereof as a therapeutic agent, particularly as ATR kinase inhibitor and in the preparation of drugs for the treatment and/or prevention of hyperproliferative diseases. The definition of each group in the general formula (I) is identical as in the specification.
Provided is an anti-CEA antibody comprising a heavy chain variable region and a light chain variable region, a drug conjugate thereof, and a composition containing the anti-CEA antibody or the drug conjugate thereof, and an application thereof as a drug.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
20.
BIFUNCTIONAL FUSION PROTEIN AND PHARMACEUTICAL USE THEREOF
Provided are a bifunctional fusion protein and pharmaceutical use thereof. Specifically, provided are a bifunctional fusion protein comprising an SIRPγ peptide variant and an anti-human PD-L1 antibody, an SIRPγ peptide variant, and pharmaceutical use thereof. The bifunctional fusion protein can specifically bind PD-L1 and CD47 to block the binding of PD-L1 or CD47 to a receptor or ligand thereof. In addition, also provided are preparation and application of the bifunctional fusion protein, and treatment of cancers and immune-related diseases.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
An acid addition salt of a RORγ regulator. Specifically relating to the acid addition salt of the compound of formula II. More specifically relating to benzoate, oxalate, methanesulfonate, maleate, hydrobromate, hydrochloride salt, and acetate of the compound of formula II and the benzoate crystal form, benzoate amorphous form, oxalate crystal form, oxalate amorphous form, methanesulfonate amorphous form, maleate B crystal form, maleate C crystal form, maleate D crystal form, hydrobromate I crystal form, hydrochloride salt α crystal form, hydrochloride salt β crystal form, hydrochloride salt γ crystal form, and acetate crystal form of the compound of formula II.
An acid addition salt of a RORγ regulator. Specifically relating to the acid addition salt of the compound of formula II. More specifically relating to benzoate, oxalate, methanesulfonate, maleate, hydrobromate, hydrochloride salt, and acetate of the compound of formula II and the benzoate crystal form, benzoate amorphous form, oxalate crystal form, oxalate amorphous form, methanesulfonate amorphous form, maleate B crystal form, maleate C crystal form, maleate D crystal form, hydrobromate I crystal form, hydrochloride salt α crystal form, hydrochloride salt β crystal form, hydrochloride salt γ crystal form, and acetate crystal form of the compound of formula II.
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A compound represented by formula II or a pharmaceutically acceptable salt thereof, and a preparation method therefor. The compound represented by formula II is an antagonist of a neurokinin-1 receptor, can be used for treating diseases related to the neurokinin-1 receptor, and can avoid hemolytic effects of drugs and reduce the side effects of drug administration.
A compound represented by formula II or a pharmaceutically acceptable salt thereof, and a preparation method therefor. The compound represented by formula II is an antagonist of a neurokinin-1 receptor, can be used for treating diseases related to the neurokinin-1 receptor, and can avoid hemolytic effects of drugs and reduce the side effects of drug administration.
Provided are an IL-5 antibody, an antigen binding fragment thereof, and a medical application therefor. The present invention comprises a mouse-derived antibody containing an IL-5 antibody CDR region, a chimeric antibody, a humanized antibody, and a pharmaceutical composition comprising said IL-5 antibody and said antigen binding fragment thereof, as well as the use of the pharmaceutical composition as a drug.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
24.
ANTIBODY CAPABLE OF BINDING TO THYMIC STROMAL LYMPHOPOIETIN AND USE THEREOF
Disclosed are an antibody capable of binding to thymic stromal lymphopoietin and the use thereof. Disclosed are an anti-TSLP antibody, comprising a murine antibody, chimeric antibody and humanized antibody of the light chain and heavy chain variable regions of the anti-TSLP antibody and antigen-binding fragments thereof, or a pharmaceutically acceptable salt or solvent compound thereof, and the use thereof as a medicament for treating asthma, especially the use thereof in the preparation of a drug for treating TSLP-positive diseases or conditions.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
Provided are an anti-CTGF antibody comprising variable regions of a light chain and a heavy chain and a use thereof as a drug. The antibody may be used to prepare drugs for treating CTGF-related diseases or conditions.
The present application provides an anti-CD38 antibody, an antigen-binding fragment thereof, and pharmaceutical use. Specifically, the present application provides a murine-derived antibody, a chimeric antibody or a humanized antibody comprising a CDR region of the anti-CD38 antibdoy, a pharmaceutical composition comprising the anti-CD38 antibody or the antigen-binding fragment thereof, and an application thereof as a drug. In particular, the present application provides an application of a humanized anti-CD38 antibody in preparing a drug for treating a CD38 positive disease or disorder.
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
An indazole derivative, a preparation method therefor, and a pharmaceutical application thereof. In particular, the present invention relates to an indazole derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use of the derivative as an estrogen receptor modulator in the prevention and/or treatment of an estrogen receptor mediated or dependent disease or condition, the disease being particularly preferably breast cancer. The definition of each substituent in the general formula (I) is the same as that in the description.
An indazole derivative, a preparation method therefor, and a pharmaceutical application thereof. In particular, the present invention relates to an indazole derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use of the derivative as an estrogen receptor modulator in the prevention and/or treatment of an estrogen receptor mediated or dependent disease or condition, the disease being particularly preferably breast cancer. The definition of each substituent in the general formula (I) is the same as that in the description.
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 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 405/14 - 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 three or more hetero rings
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
28.
METHOD FOR TREATING AUTOIMMUNE DISEASE BY IL-17 ANTAGONIST
The present application relates to a method for treating an autoimmune disease by an IL-17 antagonist. The present application relates to an application of an IL-17A binding agent in preparation of a drug for treating an autoimmune disease, such as rheumatoid arthritis, ankylosing spondylitis, and psoriasis, in particular, provides a method for treating inflammation or an autoimmune disease, comprising administering an effective amount of an IL-17 binding agent to a patient, wherein the administration frequency is less than once a week.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
The present disclosure provides the use of an anti-PD-1 antibody in combination with famitinib in the preparation of a drug for treating tumors. In the present technical solution, toxicity is controllable and tolerable. At the same time, the described drug combination effectively reduces adverse reactions to the anti-PD-1 antibody, such as the occurrence of reactive capillary endothelial proliferation.
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 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 39/00 - Medicinal preparations containing antigens or antibodies
Disclosed are a sustained-release lipid composition and a preparation method therefore. Specifically, the present invention relates to a solid composition containing lipids and a liposome composition obtained therefrom, wherein the liposomes have improved release properties.
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 31/4515 - Non-condensed piperidines, e.g. piperocaine having a butyrophenone group in position 1, e.g. haloperidol
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
The present disclosure relates to a CD3 antibody and a pharmaceutical use thereof. Specifically, the present disclosure relates to forming a multi-specificity antibody by using CD3 antibody and binding molecules of another target. The multi-specificity antibody may simultaneously bind to CD3 and another tumor-associated antigen, and bind and activate CD3-positive T cells while binding tumor-associated antigen-expressing cells, thereby promoting T cells specifically killing tumor cells that express tumor-associated antigens. In addition, the present disclosure also provides a preparation and application of a multi-specific antibody.
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
Solid dispersion and a preparation method therefor. In a specific embodiment, the solid dispersion contains an active ingredient (R)-4-amino-1-(1-(but-2-ynyl)pyrrolidin-3-yl))-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one or a salt thereof, and a carrier material, and the pH value is adjusted; employing a method that adds an appropriate amount of acid effectively inhibits an emulsification phenomenon in a reverse solvent process, thereby obtaining solid dispersion having a moderate particle size and uniform content.
Provided are an anti-CD73 antibody, an antigen-binding fragment thereof, and an application thereof. Specifically, provided are a murine, chimeric or humanized anti-CD73 antibody comprising a specific CDR region and an antigen-binding fragment thereof. Also provided are a pharmaceutical composition comprising the anti-CD73 antibody or the antigen-binding fragment thereof and the use thereof as a diagnostic agent and a therapeutic agent for CD73-related diseases.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are a thienoheterocyclic derivative, a preparation method therefor and the medical use thereof. In particular, provided are a thienoheterocyclic derivative represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, the use of same as a therapeutic agent, particularly as an ERK inhibitor, and the use of same in the preparation of a drug for treating or preventing cancers, inflammation or other proliferative diseases, wherein each substituent of formula (I) is the same as defined in the description.
Provided are a thienoheterocyclic derivative, a preparation method therefor and the medical use thereof. In particular, provided are a thienoheterocyclic derivative represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, the use of same as a therapeutic agent, particularly as an ERK inhibitor, and the use of same in the preparation of a drug for treating or preventing cancers, inflammation or other proliferative diseases, wherein each substituent of formula (I) is the same as defined in the description.
Disclosed are a nitrogen-containing bridged heterocyclic compound, a preparation method therefor, and a medical application thereof. Specifically, disclosed are a nitrogen-containing bridged heterocyclic compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a therapeutic agent, particularly, use as a complement factor (Factor B) inhibitor and use in preparing a drug for treatment and/or prevention of Factor B-mediated diseases or disorders.
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 401/02 - 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
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
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
36.
PURINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF IN MEDICINE
A purinone derivative represented by general formula (IG), a preparation method therefor, a pharmaceutical composition containing said derivative, and uses thereof as a therapeutic agent, particularly a use as a DNA-PK inhibitor and a use in preparing a pharmaceutical for treating and/or preventing a cancer; wherein groups in the general formula (IG) are as defined in the description.
C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
Provided are a complex of an anti-IL-4R antibody or an antigen-binding fragment thereof, and a medical use thereof. Specifically, provided are a complex of an antibody that specifically binds to IL-4R or an antigen-binding fragment thereof covalently linked to a toxin, a pharmaceutical composition comprising the complex, and a use thereof in the preparation of a drug for treating IL-4R-mediated diseases or disorders, especially a use in the preparation of an anti-cancer drug.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C12N 15/62 - DNA sequences coding for fusion proteins
A purinone compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, and in particular a use in preparation of a DNA-PK inhibitor and a use in preparation of a drug for treating and/or preventing a cancer.
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
The present disclosure relates to a crystal form of a pyrimido five-membered nitrogen heterocyclic derivative and a preparation method therefor. Specifically, the present disclosure relates to different crystal forms of the compound shown in formula (I) and a preparation method therefor. The crystal forms of the compound of formula (I) provided by the present disclosure have good stability and can be better used for clinical treatment.
C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
The present disclosure relates to the use of an NK1 antagonist prodrug compound and a 5-HT3 receptor antagonist. In particular, the present disclosure relates to the use of a compound represented by formula (I) or a pharmaceutically acceptable salt thereof in combination with a 5-HT3 receptor antagonist in the preparation of a drug for preventing or treating nausea and/or vomiting.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
Provided are a pharmaceutically acceptable salt of an indazole derivative, and a crystalline form and a preparation method therefor. Particularly, provided are a crystal form of a pharmaceutically acceptable salt of a compound represented by formula (I), and a preparation method therefor. The provided crystal form of the pharmaceutically acceptable salt of the compound represented by formula (I) has good stability and can be better used for clinical treatment.
C07D 413/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero 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
The present disclosure relates to an anti-Claudin 18.2 antibody and an application thereof. Specifically, the present invention relates to an anti-Claudin 18.2 antibody; a mouse-derived antibody, chimeric antibody, humanized antibody and antigen-binding fragment thereof which contain a CDR of the anti-Claudin 18.2 antibody, and a use thereof as a medicine. In particular, the present disclosure relates to a use of the anti-Claudin 18.2 antibody in the preparation of a drug for treating Claudin 18.2 positive diseases or 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
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
The present application provides a pyrroloheterocyclic derivative, a preparation method therefor, and an application thereof in medicine. Specifically, the present application provides a novel pyrroloheterocyclic derivative as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and an application of the derivative as a therapeutic agent, particularly as an ERK inhibitor, wherein substituents in the formula have the same definitions as those in the description.
The present application provides a pyrroloheterocyclic derivative, a preparation method therefor, and an application thereof in medicine. Specifically, the present application provides a novel pyrroloheterocyclic derivative as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and an application of the derivative as a therapeutic agent, particularly as an ERK inhibitor, wherein substituents in the formula have the same definitions as those in the description.
Provided is an application of a JAK inhibitor in kidney disease. Specifically, provided is a use of a JAK inhibitor in the preparation of a drug for treating or preventing kidney disease.
A dry powder particle for pulmonary delivery, comprising an active agent, phospholipid, and other pharmaceutically acceptable excipients. A mass median aerodynamic diameter of the particle is less than 5 microns, a volume median geometric diameter thereof is less than 5 microns, and the active agent mass accounts for more than 85% of the total mass of the particles. The particles have a high drug loading capacity and have higher pulmonary delivery efficiency, and can be used for inhalation therapy of pulmonary diseases.
A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 33/14 - Alkali metal chloridesAlkaline earth metal chlorides
A61P 11/00 - Drugs for disorders of the respiratory system
46.
BISPECIFIC ANTIBODY SPECIFICALLY BOUND TO VEGF AND ANG2
The present disclosure provides a bispecific antibody specifically bound to VEGF and ANG2, comprising an anti-VEGF antibody or antigen-binding fragment thereof that specifically binds to VEGF, and an anti-ANG2 single-domain antibody that specifically binds to ANG2, wherein the anti-ANG2 single domain antibody is directly or indirectly connected to the anti-VEGF antibody or an antigen-binding fragment thereof. The present disclosure further provides an anti-ANG2 single domain antibody and an antigen-binding fragment thereof, as well as a preparation and application of said antibody.
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
A machine learning-based peptide immunogenicity prediction and identification system and method. Said system comprises: a data coding module, a neural network training module, an integrated learning training module, and an immunogenicity prediction and/or identification module.
G16B 40/00 - ICT specially adapted for biostatisticsICT specially adapted for bioinformatics-related machine learning or data mining, e.g. knowledge discovery or pattern finding
G16B 5/00 - ICT specially adapted for modelling or simulations in systems biology, e.g. gene-regulatory networks, protein interaction networks or metabolic networks
Provided is a pharmaceutical composition comprising an anti-connective tissue growth factor antibody. In another aspect, further provided is a use of the pharmaceutical composition comprising an anti-connective tissue growth factor antibody.
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
Provided is a multispecific antigen binding protein. Provided is a multispecific antigen binding protein comprising one or more amino acid substitutions at CH1 and CL, a composition comprising same, a preparation method therefor, and a medical use thereof. The specific antigen binding protein effectively reduces the mismatching of light chains.
Provided are a pharmaceutical composition comprising an anti-TSLP antibody and the use thereof. The pharmaceutical composition comprises an anti-TSLP antibody and a buffer.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
The present invention relates to an antibody capable of binding to thymic stromal lymphopoietin, and the use thereof. In particular, the present invention relates to an anti-TSLP antibody, a pharmaceutical composition thereof, and the use thereof as a drug for treating asthma.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
52.
PYRIMIDINEDIONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
Provided are a pyrimidinedione derivative shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and a use thereof as a therapeutic agent, in particular the use thereof in the preparation of a Myosin inhibitor and the use thereof in the preparation of drugs for the treatment of hypertrophic cardiomyopathy (HCM) or heart disease with pathophysiological features related to HCM.
C07D 405/02 - 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
C07D 405/14 - 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 three or more hetero rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
53.
METHOD FOR PREPARING ACYLATED DERIVATIVE OF INSULIN OR OF ANALOG THEREOF
The present disclosure provides a method for preparing an acylated derivative of insulin or of an analog thereof, comprising the step of reacting insulin or an analog thereof with the compound of formula (I), and also provides the compound of formula (I) and a method for preparation thereof. The method of the present disclosure has a high yield and a stable process, can significantly reduce the cost of production of acylated derivatives of insulin or its analogs, and enables commercial production on a large scale.
The present invention relates to a fused tricyclic compound, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a fused tricyclic compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as a TLR7/8/9 inhibitor and a use in preparing a drug for the treatment and/or prevention of inflammatory and autoimmune diseases. The definition of each group in general formula (I) is as defined in the description.
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
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
A61K 31/435 - 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
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention relates to a nitrogen-containing heterocyclic derivative, and a preparation method therefor and a medical application thereof. Specifically, the present invention relates to a nitrogen-containing heterocyclic derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and use thereof as a therapeutic agent, in particular the use thereof as a TYK2 inhibitor and in the preparation of a drug for treating and/or preventing inflammatory and autoimmune diseases.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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 401/14 - 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 405/14 - 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 three or more hetero rings
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
Provided are a triazine dione derivative, a preparation method therefor and an application thereof in medicine. Specifically, provided are a triazine dione derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative and a use thereof as a therapeutic agent, particularly a use in preparing a myosin inhibitor and a use in preparing a drug for treating hypertrophic cardiomyopathy (HCM) or heart diseases having pathophysiological features related to HCM.
C07D 407/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
57.
6-OXO-1,6-DIHYDROPYRIDAZINE PRODRUG DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF IN MEDICINE
Specifically, the present invention relates to the 6-oxo-1,6-dihydropyridazine prodrug derivative shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, a use thereof as a NaV inhibitor, and a use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases.
Specifically, the present invention relates to the 6-oxo-1,6-dihydropyridazine prodrug derivative shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, a use thereof as a NaV inhibitor, and a use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases.
The present application provides a pharmaceutical composition of a prolyl hydroxylase inhibitor and a preparation method therefor. In particular, the present application provides a composition comprising a compound represented by formula (I) or a pharmacologically acceptable salt thereof and at least one water-soluble filler. The composition provided by the present application has a rapid dissolution rate and good stability.
The present application provides a pharmaceutical composition of a prolyl hydroxylase inhibitor and a preparation method therefor. In particular, the present application provides a composition comprising a compound represented by formula (I) or a pharmacologically acceptable salt thereof and at least one water-soluble filler. The composition provided by the present application has a rapid dissolution rate and good stability.
The present disclosure relates to a pharmaceutical composition comprising a human IL-2 variant or derivative and use thereof. In particular, the disclosure relates to a pharmaceutical composition comprising an IL-2 variant or derivative and a pharmaceutically acceptable excipient. The pharmaceutical composition has improved high temperature stability, freeze-thaw stability and normal temperature stability as well as appearance formulation reproducibility.
Provided are a human GCGR antibody, a GLP-1 peptid and a mutant thereof, as well as a bispecific protein formed by fusion of the GCGR antibody and the GLP-1 peptide and a preparation method thereof, which can be used for weight loss and diabetes treatment.
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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Provided are a pharmaceutical composition comprising a human interleukin 2 (IL-2) variant or derivative thereof and use thereof. In particular, provided are a pharmaceutical composition including a human interleukin 2 variant or derivative thereof and a pharmaceutically acceptable excipient. The pharmaceutical composition has improved high temperature, freezing and thawing, room-temperature stability, and appearance formulation reproducibility.
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
62.
PHARMACEUTICAL COMPOSITION CONTAINING ANTIBODY AGAINST IL-5 AND USE THEREOF
Disclosed in the present application are a pharmaceutical composition containing an antibody against IL-5 and use thereof. In particular, disclosed in the present application is a pharmaceutical composition, which contains an IL-5 antibody or an antigen binding fragment thereof in a buffer solution. In addition, the pharmaceutical composition further contains a saccharide and a nonionic surfactant.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
The present disclosure relates to use of a composition containing a CDK4/6 inhibitor in combination with anastrozole in preparation of a medicament for treating tumor diseases. Specifically, the CDK4/6 inhibitor involved in the application is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
The present disclosure relates to use of a composition containing a CDK4/6 inhibitor in combination with anastrozole in preparation of a medicament for treating tumor diseases. Specifically, the CDK4/6 inhibitor involved in the application is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
A GLP1-GCGR antibody fusion protein variant and a composition comprising same, specifically relating to a variant of a GLP1-GCGR antibody fusion protein, and in particular, to a glycosylated variant, a composition comprising a GLP1-GCGR antibody fusion protein and a variant thereof, preparation and characterization methods for the composition, and use of the composition.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 1/15 - Fungi Culture media therefor modified by introduction of foreign genetic material
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
A61K 9/00 - Medicinal preparations characterised by special physical form
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
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/00 - Medicinal preparations containing antigens or antibodies
66.
ANTI-HER3 ANTIBODY AND ANTI-HER3 ANTIBODY-DRUG CONJUGATE AND MEDICAL USE THEREOF
Provided are an anti-HER3 antibody and an anti-HER3 antibody-drug conjugate and a medical use thereof, specifically, the anti-HER3 antibody, and the anti-HER3 antibody-drug conjugate as represented by general formula (Pc-L-Y-D), wherein Pc is an anti-HER3 antibody, and L, Y and n are as defined in the description.
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 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Provided are a pharmaceutical composition comprising an antibody-drug conjugate, and use of the pharmaceutical composition. Specifically provided is a pharmaceutical composition, comprising an anti-claudin antibody-drug conjugate.
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
Provided are a crystal form of a pyrrolo heterocyclic derivative and a preparation method therefor. Specifically, the present invention relates to a crystal form of a pharmaceutically acceptable salt of a compound as represented by formula (I) and a preparation method therefor. The provided crystal form of the pharmaceutically acceptable salt of the compound as represented by formula (I) has a good stability and can be better used in clinical treatment.
Provided are a 6-oxo-1,6-dihydropyridazin derivative, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a 6-oxo-1,6-dihydropyridazin derivative as shown by general formula (I), a preparation method therefor, a pharmaceutical composition containing said derivative, and same serving as a therapeutic agent, particularly a use in preparing a drug for treating and/or preventing a disease regulated by a thyroid hormone.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 253/075 - Two hetero atoms, in positions 3 and 5
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
70.
ANTI-PD-1 ANTIBODY, ANTIGEN-BINDING FRAGMENT THEREOF AND PHARMACEUTICAL USE THEREOF
Provided are an anti-PD-1 antibody, an antigen-binding fragment thereof, and a pharmaceutical use thereof. Specifically, provided are a humanized anti-PD-1 antibody containing a specific CDR region and an antigen-binding fragment thereof, a pharmaceutical composition containing the anti-PD-1 antibody and the antigen-binding fragment thereof, and a used thereof as medicament. In particular, provided is a use of the humanized anti-PD-1 antibody in the preparation of the medicament for treating PD-1 associated diseases or 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
A percutaneously absorbable pharmaceutical composition containing amide local anaesthetics, a preparation method therefor, and a use thereof, specifically relating to a percutaneously absorbable pharmaceutical composition, containing a skin adhesion layer, wherein the skin adhesion layer contains amide local anaesthetics, a silicone pressure-sensitive adhesive, and an additive; and the pharmaceutical composition has improved release characteristics and rheological properties.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention relates to a bispecific antigen binding molecule, comprising a first antigen-binding domain specifically binding to ANG-2, and a second antigen-binding domain specifically binding to VEGF. At the same time, the present invention also relates to a monoclonal antibody specifically binding to ANG-2, the preparation of the antibody and an application thereof.
The present invention provides a crystal form of a 1,2,3-triazolo[1,5-a]pyrazines derivative and a preparation method for the crystal form. Specifically, the present invention provides a crystal form of a compound (S)-N5-(3,4-difluorophenyl)-6-methyl-N3-((R)-1,1,1-trifluoropropan-2-yl)-6,7-dihydro-[1,2,3]triazolo[1,5-c]pyrazine-3,5(4H)-dimethylformamide and a preparation method for the crystal form. The prepared crystal form has good stability and clinical application value.
A dosing regimen of a bicyclic substituted pyrazolone azo derivative. In particular, the present invention relates to a method for treating a disease, comprising administering to a patient an effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein the interval between administration and food intake is at least 2 hours.
Provided are a SIRPγ variant and a fusion protein thereof. Moreover, also provided are preparation for a polypeptide containing the SIRPγ variant, and an application of the polypeptide.
A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a Nav inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description.
A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a Nav inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description.
A drug-loaded macromolecule and a preparation method therefor, the macromolecule specifically being a dendritic polymer loaded with a drug and a pharmacokinetic modifier, and relating in particular to connecting the drug to the dendritic polymer by means of a specific linker. The present macromolecule can be used to regulate the release speed of the drug, specifically by means of the selection of linker.
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 47/62 - 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
A61K 47/60 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
Disclosed is an application of a combination of a fusion protein of TGF-β receptor and multi-targeted tyrosine kinase inhibitor in preparing an anti-tumor drug.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention relates to a signal peptide for reducing the end heterogeneity of a heterologous polypeptide. Specifically, the present invention relates to a signal peptide for protein expression. The present invention further relates to a recombinant polypeptide, a preparation method therefor, and a composition containing a recombinant polypeptide.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C07K 14/00 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
C12N 15/00 - Mutation or genetic engineeringDNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purificationUse of hosts therefor
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Provided is a human interleukin-2 (IL-2) variant having one or more amino acid mutations or a derivative thereof. The IL-2 variant or derivative thereof has increased stability compared to wild-type IL-2 and improved properties as an immunotherapeutic agent. Also disclosed are an immunoconjugate and a pharmaceutical composition which comprise the human IL-2 variant or derivative thereof, a polynucleotide molecule encoding same, a vector, a host cell and a preparation method therefor, as well as the pharmaceutical uses of the IL-2 variant or derivative thereof and the immunoconjugate or pharmaceutical composition comprising the L-2 variant or derivative thereof.
A61K 47/60 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
81.
PRODRUG OF SELECTIVE NAV INHIBITOR AND CRYSTAL FORM THEREOF
VV inhibitor and a crystal form thereof, i.e., a compound represented by general formula (A), the crystal form A and the crystal form B of a compound represented by formula (I), and preparation methods therefor.
The present disclosure relates to the use of BTK inhibitors in the treatment of diseases. Specifically, the present disclosure relates to the use of BTK inhibitors in the preparation of drugs for the prevention or treatment of neuromyelitis optica spectrum disorders.
A fused tricyclic derivative as shown in general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use thereof as a therapeutic agent, particularly a use as a TLR7/8/9 inhibitor and a use in preparation of a medication for treating and/or preventing inflammatory and autoimmune diseases.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 37/00 - Drugs for immunological or allergic disorders
85.
INDOLE FUSED RING DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF IN MEDICINE
The present disclosure relates to an indole fused ring derivative, a preparation method therefor and the use thereof in medicine. Specifically, the present disclosure relates to an indole fused ring derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, in particular the use thereof as a TLR7/8/9 inhibitor and in the preparation of a drug for treating and/or preventing inflammatory and autoimmune diseases.
Disclosed are a method for preparing triazolo[1,5-a]pyrazine and the use thereof. The preparation method comprises the step of reacting a compound of formula C with a diphenylphosphine azide compound so as to form a compound of formula D, wherein R1is selected from hydrogen or an alkyl group, and R2 is selected from an alkyl group and a cycloalkyl group. The method is simple to operate and has a high yield, and a sample obtained thereby is of good quality. The method is suitable for large-scale production.
Disclosed are an oxa-azaspiro derivative, a preparation method therefor and a pharmaceutical use thereof. In particular, disclosed are an oxa-azaspiro derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, especially the use thereof as a PI3Kδ inhibitor and the use thereof in the preparation of a drug for treating diseases or conditions improved by means of inhibiting PI3Kδ.
The present disclosure relates to an anti-PD-1 antibody pharmaceutical composition and use thereof. Specifically, the present disclosure provides a pharmaceutical composition, comprising an anti-PD-1 antibody and a buffer solution.
A fused pyridazine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative and use thereof as a therapeutic agent, in particular use thereof as an SOS1 inhibitor and use thereof in the preparation of a medicament for treating conditions or disorders which are ameliorated by the inhibition of SOS1.
The present application relates to a sulfur-containing isoindoline derivative, and a preparation method therefor and medical use thereof. In particular, the present application relates to a sulfur-containing isoindoline derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and use thereof as a therapeutic agent, particularly use thereof as a Cereblon modulator in the field of treatment of multiple myeloma.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/454 - 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
Disclosed is use of a TIM-3 antibody in preparation of medicines for treating tumors. Specifically, provided is use of the TIM-3 antibody or an antigen-binding fragment thereof in preparation of medicines for treating non-small cell lung cancer, the TIM-3 antibody containing a heavy chain variable region shown in SEQ ID NO: 33 and a light chain variable region shown in SEQ ID NO: 36. Further, also provided is use of the TIM-3 antibody or the antigen-binding fragment thereof and a PD-1 antibody or an antigen-binding fragment thereof in joint preparation of medicines for treating tumors.
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
Disclosed in the present disclosure are a TGF-β receptor fusion protein pharmaceutical composition and a use thereof. Specifically, the pharmaceutical composition comprises a TGF-β receptor fusion protein in a sodium citrate buffer, and the TGF-β receptor fusion protein comprises a PD-L1 antibody targeting portion and a TGF-βRII extracellular region. In addition, the pharmaceutical composition may also comprise a sugar and a non-ionic surfactant.
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention relates to a sulfonylurea derivative and medical uses thereof, specifically relating to the sulfonylurea derivative shown in general formula (I), a preparation method thereof, a pharmaceutical composition containing same, and a use of same for treating diseases and disorders affected by neuronal damage, for example: cerebral stroke, brain damage, neuropathic pain, migraines, inflammatory pain, chronic pain, or depression. The definition of each group in general formula (I) is the same as that in the description.
C07C 311/59 - Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea having sulfur atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings having nitrogen atoms of the sulfonylurea groups bound to carbon atoms of rings other than six-membered aromatic rings
A61K 31/64 - Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
94.
TRANSDERMAL PREPARATION CONTAINING ANESTHETIC DRUG ACTIVE INGREDIENT AND PREPARATION METHOD THEREFOR
The present disclosure relates to a transdermal preparation containing an anesthetic drug active ingredient and a preparation method therefor. The transdermal preparation contains an anesthetic active ingredient and an organosilicon elastomer mixture. The transdermal preparation has the characteristics of good stability and being fast acting.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
95.
OXA-AZABICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
The present disclosure relates to an oxa-azabicyclic derivative, a preparation method therefor, and the medical use thereof. In particular, the present disclosure relates to an oxa-azabicyclic derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, especially the use thereof as a PI3Kδ inhibitor and the use thereof in the preparation of a drug for treating conditions or symptoms improved by means of inhibiting PI3Kδ.
Provided are a sulfonylbenzamide derivative and a conjugate thereof, a preparation method therefor, and the use thereof. In particular, provided is a sulfonylbenzamide derivative having a structure as represented by formula (D), a conjugate thereof, a preparation method therefor, a pharmaceutical composition containing same, and the use thereof in the preparation of a drug for treating cancers by means of receptor regulation. Each substituent in general formula (D) is as defined in the description.
C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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
Disclosed are fused imidazole derivatives, preparation methods therefor and medical uses thereof. Specifically, the present disclosure relates to a fused imidazole derivative as shown in general formula (IM), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of same as a therapeutic agent, in particular the use thereof as a GLP-1 receptor agonist, and the use thereof in the preparation of drugs for the treatment and/or prevention of diabetes.
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 405/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
98.
LAG-3 antibody, antigen-binding fragment thereof, and pharmaceutical application thereof
Provided are a LAG-3 antibody, an antigen-binding fragment thereof, and a pharmaceutical application thereof. Further, provided are a chimeric antibody comprising a CDR of the LAG-3 antibody, a humanized antibody, a pharmaceutical composition comprising the LAG-3 antibody and the antigen-binding fragment thereof, and an application of the pharmaceutical composition as an antineoplastic drug. Particularly, provided is an application of a humanized LAG-3 antibody in preparation of drugs for treatment of diseases involving immune cells.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
99.
QUICK-ACTING INSULIN COMPOSITION AND MEDICAL USE THEREOF
Disclosed are a quick-acting insulin composition and the medical use thereof, the composition containing: 1) insulin aspart, and 2) at least one of iloprost and tafluprost. The composition has faster pharmacokinetics, better stability, and causes less irritation to an injection site than commercial preparations of existing insulin analog products.
The present disclosure relates to an imidazopyrimidine derivative, a preparation method therefor, and the medical use thereof. In particular, the present disclosure relates to an imidazopyrimidine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, particularly the use thereof as an ATR kinase inhibitor and the use thereof in the preparation of a drug for treating and/or preventing hyperproliferative diseases.
