Provided is a use of an antibody targeting an antigenic epitope polypeptide or an antigen-binding fragment thereof in the preparation of an antibody-drug conjugate. An antigenic epitope polypeptide is differentially expressed on tumor cells/cancer cells and normal human cells. The antibody or the antigen-binding fragment thereof can target and bind to the antigenic epitope polypeptide to show an antibody internalization function, and thus can be applied to the preparation of an antibody-drug conjugate and play a tumor treatment effect.
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 39/00 - Medicinal preparations containing antigens or antibodies
Provided are a bispecific antibody and use thereof. The bispecific antibody provided can specifically bind to TGF-β, GARP, or GARP-TGF-β complex individually or simultaneously, and can also specifically bind to PD-L1. The bispecific antibody provided exhibits high affinity and specificity for the antigens, has a tumor-killing effect, and can be applied to the treatment of 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
3.
CRYSTAL FORM OF BICYCLIC COMPOUND AND PREPARATION METHOD THEREFOR
The present invention relates to a crystal form of compound 1, a pharmaceutical composition comprising the crystal form, and a use of the pharmaceutical composition in treating diseases. The present invention further relates to a preparation method for compound 1 and the crystal form thereof.
C07D 243/36 - Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
4.
SALT AND CRYSTAL FORM OF EGFR INHIBITOR, AND COMPOSITION AND USE THEREOF
The present invention relates to salt and crystal form of an EGFR inhibitor, and a composition and the use thereof. The salt and crystal form of the EGFR inhibitor as represented by formula I of the present invention can be used for treating or preventing epidermal growth factor receptor-mediated diseases or medical conditions (such as L858R activation mutants, exon 19 deletion activation mutants, T790M resistance mutants and C797S resistant mutants) in certain mutant forms.
The present invention relates to salt and crystal form of an EGFR inhibitor, and a composition and the use thereof. The salt and crystal form of the EGFR inhibitor as represented by formula I of the present invention can be used for treating or preventing epidermal growth factor receptor-mediated diseases or medical conditions (such as L858R activation mutants, exon 19 deletion activation mutants, T790M resistance mutants and C797S resistant mutants) in certain mutant forms.
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Embodiments of the present application provide Ensartinib or a salt thereof and a use of a composition containing Ensartinib or the salt thereof in treatment of a disease carrying MET 14 exon skipping mutation.
A compound of formula I and a use thereof as an MALT1 inhibitor, and a pharmaceutical composition containing the compound. The compound can be used to treat diseases or disorders such as cancer.
A compound of formula I and a use thereof as an MALT1 inhibitor, and a pharmaceutical composition containing the compound. The compound can be used to treat diseases or disorders such as cancer.
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 31/167 - 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 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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 31/444 - 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 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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
C07C 237/40 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to a carbon atom of a six-membered aromatic ring
C07C 311/32 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 323/33 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to a carbon atom of the same non-condensed six-membered aromatic ring
C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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 401/06 - 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 405/12 - 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 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 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 413/04 - 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
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Provided are an anti-PD-L1 nanobody and use thereof. The anti-PD-L1 nanobody comprises a CDR1, a CDR2, and a CDR3, wherein the CDR1 comprises a sequence selected from SEQ ID NOs: 1, 5, and 9; the CDR2 comprises a sequence selected from SEQ ID NOs: 2, 6, and 10; and the CDR3 comprises a sequence selected from SEQ ID NOs: 3, 7, 11, and 14. The antibody can block the PD-1/PD-L1 and CD-80/PD-L1 signaling pathways, inhibit the growth of tumor cells, and exhibit a therapeutic effect against 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
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
8.
BRM INHIBITOR AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
The present invention relates to a BRM inhibitor, a composition, and a use thereof. In particular, the present invention relates to a compound as shown in formula (I), a pharmaceutical composition containing the compound of the present invention, and a use thereof as a BRM inhibitor in treatment of cancer-related diseases.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present invention provides an application of a compound in the preparation of drug for treating myelofibrosis and the related symptoms/signs thereof, and a use of the compound. The compound is selected form one or more of a compound having a structure as shown in formula I, and a pharmaceutically-acceptable salt, prodrug, solvate and hydrate thereof.
The present invention provides an application of a compound in the preparation of drug for treating myelofibrosis and the related symptoms/signs thereof, and a use of the compound. The compound is selected form one or more of a compound having a structure as shown in formula I, and a pharmaceutically-acceptable salt, prodrug, solvate and hydrate thereof.
Provided are a multispecific antibody and the use thereof. The provided antibody can specifically bind to TGF-β, GARP, or GARP-TGF-β complex individually or simultaneously, same can also specifically bind to VEGF, and can further selectively specifically bind to PD-L1. The provided multispecific antibody exhibits high affinity and specificity to an antigen, has a tumor killing efficacy, and can be used 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 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Provided are an anti-TT3 humanized antibody and the use thereof. The antibody provided has a heavy chain variable region as shown in SEQ ID NO: 1, 2 or 3 and a light chain variable region as shown in SEQ ID NO: 4, 5 or 6. The antibody provided can specifically recognize and bind to a TT3 antigen.
Disclosed are a polymorph of (S)-1-(2-((S)-3-cyclopropyl-5-isopropyl-2,4-dioxoimidazolidin-1-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)pyrrolidine-2-carboxamide, a composition comprising the polymorph, a use method therefor and a preparation method therefor.
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
Provided are a humanized anti-CD3 antibody and the use thereof. The provided antibody has a heavy chain variable region shown as SEQ ID NO: 1, 2 or 3 and a light chain variable region shown as SEQ ID NO: 4, 5, 6, 7 or 8. The provided antibody can specifically recognize and bind to CD3.
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 compound targeting a pan-KRAS protein degradation agent and a use thereof, relating to the technical field of medicines. Provided are a compound having an F-L-M structure, or a tautomer, racemate, enantiomer, or diastereomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, wherein the F is a KRAS protein binding fragment; the L is a linking unit for linking the F and the M; and the M is a VHL binding fragment. The compound can be used for treating diseases caused by KRAS mutations or amplifications.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a crystalline form and/or maleate, phosphate, L-tartrate, and adipate of the compound represented by the structural formula I, and various crystalline forms of various salt forms, and preparation methods and applications thereof.
The present invention relates to a crystalline form and/or maleate, phosphate, L-tartrate, and adipate of the compound represented by the structural formula I, and various crystalline forms of various salt forms, and preparation methods and applications thereof.
The present invention belongs to the field of medicine, and in particular relates to a heteroarylopiperidine derivative, and a pharmaceutical composition and the use thereof. The heteroarylopiperidine as represented by formula (I) provided in the present invention can not only be prepared into an oral preparation, but also has good properties, which are especially embodied in the aspects of pharmacokinetic properties, blood-brain barrier penetration abilities and cardiac safety.
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
A method for diagnosing and/or treating a disease is provided, which comprises at least the following steps: evaluating the anaplastic lymphoma kinase (ALK) gene rearrangement, anaplastic lymphoma kinase phosphorylation levels, and RNase1 expression levels of a subject; if the evaluation result for ALK gene rearrangement is negative, and the ALK phosphorylation levels and the RNase1 expression levels are both higher than levels of a reference population, then defining the disease as a disease caused by RNase1-driven ALK activation (an RDAA positive disease), and administering an ALK inhibitor to the subject, wherein the RDAA positive disease is RDAA positive non-small cell lung cancer, and the ALK inhibitor does not comprise ensartinib.
The present invention relates to a macrocyclic inhibitor, a composition, and a use thereof. In particular, the present invention relates to a compound represented by formula (I), a pharmaceutical composition containing said compound, and a use of same as an EGFR inhibitor in the treatment of a cancer-related disease.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
The present invention relates to a macrocyclic inhibitor, a composition and a use thereof. In particular, the present invention relates to a compound as shown in formula (I), a pharmaceutical composition comprising the compound of the present invention, and a use thereof as an EGFR inhibitor in the treatment of cancer-related diseases.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
The present invention provides a method for treatment of a disease, at least comprising the following steps: administering an anaplastic lymphoma kinase (ALK) inhibitor to a patient suffering from an RDAA-positive disease, wherein the RDAA-positive disease is defined as a disease caused by ALK activation driven by RNase1, a sample from the patient suffering from the RDAA-positive disease has a negative ALK gene rearrangement test result, a RNase1 expression level of 418 ng/ml or above in blood plasma or a positive immunohistochemical staining result against RNase1, and a positive immunohistochemical staining result against ALK phosphorylation, the RDAA-positive disease is RDAA-positive non-small cell lung cancer, and the ALK inhibitor is ensartinib.
Provided in the present disclosure is a method for treating diseases, which at least comprises the following step: administering an anaplastic lymphoma kinase (ALK) inhibitor to a patient suffering from an RDAA-positive disease, the RDAA-positive disease being defined as a disease caused by RNase1 driven ALK activation, wherein a specimen from the patient suffering from the RDAA positive disease has an ALK gene rearrangement detection result that is negative, has an Rnase1 expression level in plasma that is ≥ 418 ng/mL or has an Rnase1-targeted immunohistochemical staining result that is positive, and has an ALK-phosphorylation-targeted immunohistochemical staining result that is positive, and the patient suffering from the RDAA-positive disease is not a patient with non-small cell lung cancer.
Provided are a compound of formula (I), and a stereoisomer, tautomer, deuterated product or pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and an application thereof as a medicament for the treatment and/or prevention of diseases mediated by KRAS.
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 471/02 - 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 in which the condensed system contains two hetero rings
C07D 471/12 - 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 in which the condensed system contains three hetero rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to a compound represented by general formula (I), a stereoisomer, a tautomer, a deuterated compound or a pharmaceutically acceptable salt thereof, which has therapeutic activity against cancer. The present invention also relates to a method for preparing the compounds and a pharmaceutical composition containing same.
The present invention relates to compounds of Formula (I), pharmaceutical compositions comprising such compounds and use thereof. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer.
The present invention relates to compounds of Formula (I), pharmaceutical compositions comprising such compounds and use thereof. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer.
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 403/06 - 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 only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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 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
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 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
C07C 237/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
Provided is a compound having a structure of formula (I), which has cancer treatment activity. Further provided are a preparation method for the compound of formula (I), and a pharmaceutical composition comprising the compound.
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 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 407/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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
A compound (as represented by formula I) serving as an Src homology region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitor, as well as a pharmaceutical composition thereof, a preparation method therefor, and a use in treating an SHP2 mediation diseases. The compounds of formula I exerts an effect by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis.
A compound (as represented by formula I) serving as an Src homology region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitor, as well as a pharmaceutical composition thereof, a preparation method therefor, and a use in treating an SHP2 mediation diseases. The compounds of formula I exerts an effect by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis.
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 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 405/14 - 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 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition comprising the compound.
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition comprising the compound.
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
28.
MUTANT IDH1 AND IDH2 INHIBITOR AND APPLICATION THEREOF
Disclosed are a compound represented by formula (I) as a mutant isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) inhibitor, a preparation method therefor, and a pharmaceutical composition thereof. Also disclosed is a use of the described compound or the pharmaceutical composition thereof in the treatment of mutant IDH1 and IDH2-mediated diseases.
C07D 251/18 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
The present invention relates to a crystal form of a pyridazine derivative 5-(6-chloro-5-((1S,2S)-2-phenylcyclopropyl)pyridazin-3-yl)pyrimidine-2,4(1H,3H)-dione free base or a salt thereof, and a preparation method therefor and a use thereof.
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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
The present invention relates to a pharmaceutical composition comprising a compound as shown in formula (I), and use of the pharmaceutical composition in treating diseases. The present invention also relates to a method for preparing the compound as shown in formula I.
Disclosed are a compound having an X-Y-Z structure, and a tautomer, a deuterated compound or a pharmaceutical salt thereof. X is a KRAS protein binding ligand compound, Z is an E3 ligase binding ligand compound, and Y is a linking chain for linking X to Z. The compound has KRAS G12D regulation activity. In addition, the present invention also relates to a method for preparing the compound and a pharmaceutical composition comprising same.
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 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a compound as represented by formula (I). The present invention also provides compositions and formulations containing such compounds, and methods for using and preparing such compounds.
The present invention relates to a compound as represented by formula (I). The present invention also provides compositions and formulations containing such compounds, and methods for using and preparing such compounds.
C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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 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 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 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
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
Provided in the present invention is the use of at least one of a compound of formula I, a stereoisomer thereof, a tautomer thereof, a polymorph thereof, a solvate thereof and a pharmaceutically acceptable salt thereof, or a composition containing at least one of same, a stereoisomer thereof, a tautomer thereof, a polymorph thereof, a solvate thereof and a pharmaceutically acceptable salt thereof in the treatment of leukemia.
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound. (I)
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound. (I)
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 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 451/04 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring system
The present invention relates to a novel compound (formula I), which has cancer treatment activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound.
The present invention relates to a novel compound (formula I), which has cancer treatment activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
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 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated 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
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
The present invention relates to a crystal form of a compound as represented in formula I, various salt types and crystal forms thereof, and further relates to a preparation method for the crystal form of the compound as represented in formula I, various salt types and crystal forms thereof, and a pharmaceutical composition containing the crystal form, various salt types and crystal forms thereof, and the use thereof in the preparation of a drug for treating diseases, disorders or conditions, or a treatment method for treating the diseases, disorders or conditions.
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
Provided is a compound shown in formula (I), a stereoisomer, tautomer, deuterated substance or medicinal salt thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and a use thereof as a drug for treating and/or preventing KRAS-mediated diseases.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/553 - 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
The present invention relates to a compound as shown in formula (I). The present invention also provides a composition and preparation containing the compound, and a method for using and preparing the compound.
C07D 243/36 - Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system
The present invention relates to a compound as shown in formula (I). The present invention also provides a composition and preparation containing the compound, and a method for using and preparing the compound.
C07D 243/36 - Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
41.
EGFR INHIBITOR, COMPOSITION, AND METHOD FOR PREPARATION THEREOF
Provided are the compounds of Formula I, a method for using these compounds as an EGFR inhibitor, and a pharmaceutical composition comprising the compounds. The compound is used for treatment, prevention or amelioration of diseases or conditions such as cancer or infection.
Provided are the compounds of Formula I, a method for using these compounds as an EGFR inhibitor, and a pharmaceutical composition comprising the compounds. The compound is used for treatment, prevention or amelioration of diseases or conditions such as cancer or infection.
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
Provided are compounds represented by formula (I) having KRAS G12D modulating activity, a preparation method for said compounds, pharmaceutical compositions comprising said compounds, and a use thereof in the preparation of a medicament for treating or preventing diseases mediated by KRAS G12D.
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 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
The present invention relates to a compound of formula (I), a method for using the compound as an EGFR inhibitor, and a pharmaceutical composition comprising the compound. The compound can be used for treatment, prevention or alleviation of diseases or disorders such as cancer or infection.
The present invention relates to a compound of formula (I), a method for using the compound as an EGFR inhibitor, and a pharmaceutical composition comprising the compound. The compound can be used for treatment, prevention or alleviation of diseases or disorders such as cancer or infection.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 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
Provided are a bispecific antibody and use thereof. The bispecific antibody provided can specifically bind to TGF-?, GARP, or GARP-TGF-? complex individually or simultaneously, and can also specifically bind to PD-L1. The bispecific antibody provided exhibits high affinity and specificity for the antigens, has a tumor-killing effect, and can be applied to the treatment of tumors.
C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A bispecific antibody and an application thereof are provided. The provided bispecific antibody can specifically bind to TGF-β, GARP or a GARP-TGF-β complex individually or simultaneously, and can also specifically bind to PD-L1. The provided bispecific antibody exhibits high affinity and specificity to an antigen, has tumor killing effects, and can be applied to treat tumors.
C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Provided are compounds of formula (I), which have KRAS mutation tumor regulating activity. Also provided are a method for providing these compounds and a pharmaceutical composition comprising the same.
Provided are compounds of formula (I), which have KRAS mutation tumor regulating activity. Also provided are a method for providing these compounds and a pharmaceutical composition comprising the same.
An imidazolidinone compound represented by formula (I), or a stereoisomer thereof, a geometric isomer thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, a synthesis method therefor and use thereof.
An imidazolidinone compound represented by formula (I), or a stereoisomer thereof, a geometric isomer thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, a synthesis method therefor and use thereof.
The present invention relates to a salt and crystal form of an EGFR inhibitor, and a composition and the use thereof. The salt and crystal form of the EGFR inhibitor as represented by formula I of the present invention can be used for treating or preventing epidermal growth factor receptor-mediated diseases or medical conditions (such as L858R activation mutants, exon 19 deletion activation mutants, T790M resistance mutants and C797S resistant mutants) in certain mutant forms.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Embodiments of the present application provide Ensartinib or a salt thereof and a use of a composition containing Ensartinib or the salt thereof in treatment of a disease carrying MET 14 exon skipping mutation.
The present invention relates to a pharmaceutical composition, containing befotertinib or a pharmaceutically acceptable salt thereof and icotinib or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of EGFR-mediated diseases.
Provided are an anti-PD-L1 nanobody and the use thereof. The anti-PD-L1 nanobody contains CDR1, CDR2 and CDR3, wherein CDR1 contains a sequence selected from SEQ ID NOs: 1, 5 and 9, CDR2 contains a sequence selected from SEQ ID NOs: 2, 6 and 10, and CDR3 contains a sequence selected from SEQ ID NOs: 3, 7, 11 and 14. The antibody can block signaling pathways of PD-1/PD-L1 and CD-80/PD-L1, inhibit the growth of tumor cells, and exhibit a tumor treatment effect.
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
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
C12N 15/62 - DNA sequences coding for fusion proteins
The invention relates to a bromodomain inhibitor. The invention also provides compositions and formulations comprising such compounds, and methods of using and preparing such compounds.
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
A compound of formula I and a use thereof as an MALT1 inhibitor, and a pharmaceutical composition containing the compound. The compound can be used to treat diseases or disorders such as cancer.
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 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 413/14 - 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 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
The present invention provides an application of a compound in the preparation of drug for treating myelofibrosis and related symptoms/signs thereof, and a use of the compound. The compound is selected from one or more of a compound having a structure as shown in formula I, and a pharmaceutically-acceptable salt, prodrug, solvate, and hydrate thereof.
The present invention relates to the compounds of Formula I, methods of using these compounds as EGFR inhibitors, and pharmaceutical compositions comprising compounds thereof. The compounds are used for treating, preventing or ameliorating diseases or disorders such as cancer or infections.
The present invention relates to the compounds of Formula I, methods of using these compounds as EGFR inhibitors, and pharmaceutical compositions comprising compounds thereof. The compounds are used for treating, preventing or ameliorating diseases or disorders such as cancer or infections.
A compound of formula (I), a tautomer, a deuterated product, or pharmacologically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a drug for treating a cancer.
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
Disclosed are a polymorph of (S)-1-(2-((S)-3-cyclopropyl-5-isopropyl-2,4-dioxoimidazolidin-1-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)pyrrolidine-2-carboxamide, a composition comprising the polymorph, a use method therefor and a preparation method therefor.
Disclosed are a polymorph of (S)-1-(2-((S)-3-cyclopropyl-5-isopropyl-2,4-dioxoimidazolidin-1-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)pyrrolidine-2-carboxamide, a composition comprising the polymorph, a use method therefor and a preparation method therefor.
The present invention relates a novel compound having cancer treatment activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound.
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
Compounds of formula A, a method for using said compounds as an EGFR inhibitor, and a pharmaceutical composition comprising said compounds. The compounds can be used to treat, prevent or ameliorate diseases or conditions such as cancers or infections.
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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
Disclosed are a pharmaceutical combination, a kit containing same, and the use thereof in the preparation of a drug for treating breast cancer. The pharmaceutical combination comprises a first active ingredient and a second active ingredient, wherein the first active ingredient is any one of or more of a compound having a structure represented by structural formula I, a stereoisomer thereof, a tautomer thereof, a polymorph thereof, a solvate thereof and a pharmaceutically acceptable salt thereof; and the second active ingredient is an estrogen receptor antagonist or an aromatase inhibitor. The above-mentioned first active ingredient and second active ingredient are co-administered in combination, the achieved co-treatment activity has a prominent improvement effect with respect to the separate administration of each active ingredient, and the synergistic effect is achieved.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 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 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 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
64.
USE OF ICOTINIB IN POSTOPERATIVE ADJUVANT THERAPY FOR NON-SMALL CELL LUNG CANCER
The use of icotinib in postoperative adjuvant therapy for non-small cell lung cancer. The curative effect of icotinib in postoperative adjuvant therapy for NSCLC patients with an EGFR gene-sensitive mutation is significantly better than that of standard adjuvant chemotherapy. In addition, the safety of postoperative adjuvant therapy is better than that of standard adjuvant chemotherapy, that is, the icotinib adjuvant therapy can provide safe and effective treatment options for patients with stage II-IIIA NSCLC.
The present invention belongs to the field of medicine, and in particular relates to a heteroarylpiperidine derivative, a pharmaceutical composition and use thereof. The heteroarypiperidine derivative as shown in formula (I) provided by the present invention can be prepared into oral formulations, and has good pharmacokinetic properties.
The present invention belongs to the field of medicine, and in particular relates to heteroarylopiperidine derivative, and a pharmaceutical composition thereof and the use thereof. The heteroarylopiperidine derivative as shown in formula (I) provided by the present invention can not only be prepared into an oral preparation, but also has good pharmacokinetic properties and blood brain barrier penetration capabilities.
A61K 31/4355 - 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 oxygen as a ring hetero atom
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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 31/4545 - 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 compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
C07F 9/6512 - Six-membered rings having the nitrogen atoms in positions 1 and 3
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention relates to a salt of a Compound 1 and polymorphs thereof, and pharmaceutical compositions containing the same, wherein the salt is preferably hydrochloride, phosphate, tosilate, benzene sulfonate, succinate, sulfate, monohydrobromate, dihydrobromate, etc. The present invention further relates to methods for preparing the described substances, their uses, and pharmaceutical preparations containing these salts and crystalline forms.
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
69.
Polymorphs of a Kinase Inhibitor, Pharmaceutical Compositions Containing Such a Compound, Preparation Methods, and Applications
The University of North Carolina at Chapel Hill (USA)
Betta Pharmaceuticals Co., Ltd. (China)
Inventor
Wang, Xiaodong
Zhang, Weihe
Liu, Xiangyong
Han, Changlong
Li, Zongquan
Abstract
The invention relates to new crystal forms of compound (trans)-4-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) cyclohexanol trihydrochloride, its hydrate, or solvate, as shown in Formula I. The invention also relates to methods for preparation of the described compound, crystal form, and related intermediate compounds, as well as pharmaceutical compositions containing the compounds. Further described is, the use of the compounds or crystal forms in the production of a medicament for the treatment of a disease, symptom, or condition, or the use in treatment of a disease, symptom or condition.
The invention relates to new crystal forms of compound (trans)-4-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) cyclohexanol trihydrochloride, its hydrate, or solvate, as shown in Formula I. The invention also relates to methods for preparation of the described compound, crystal form, and related intermediate compounds, as well as pharmaceutical compositions containing the compounds. Further described is, the use of the compounds or crystal forms in the production of a medicament for the treatment of a disease, symptom, or condition, or the use in treatment of a disease, symptom or condition.
The present invention relates to a compound as shown in formula (I) serving as a mutant isocitrate dehydrogenase 1 (IDH1) and 2 (IDH2) inhibitor, a preparation method therefor and a pharmaceutical composition thereof. The present invention also relates to use of the compound or the pharmaceutical composition thereof in treating mutant IDH1 and IDH2-mediated diseases.
C07D 251/18 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
C07D 251/26 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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
The present invention relates to compounds which have cancer treatment activity, and also relates to a preparation method for such compounds and a pharmaceutical composition comprising same.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 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
A novel compound with cancer therapeutic activity. The present invention also relates to a method for preparing these compounds and a pharmaceutical composition containing same. (I)
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
Provided herein are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
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 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
The present invention relates to compounds represented by formula (I). Further provided are a composition that comprises said type of compound and a preparation, and a method for using and preparing such compounds.
C07D 209/52 - 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 condensed with a ring other than six-membered
75.
CD73 INHIBITOR AND APPLICATION THEREOF IN MEDICINE
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition comprising the compound.
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
76.
CD73 INHIBITOR AND APPLICATION THEREOF IN MEDICINE
The present invention relates to a novel compound, which has cancer therapeutic activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition comprising the compound.
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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Provided are compounds having a structure of formula (I), pharmaceutical compositions comprising such compounds and use thereof. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer.
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 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/444 - 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 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 31/4545 - 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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl 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 401/10 - 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 aromatic rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/04 - 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 403/06 - 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 only aliphatic carbon atoms
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 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
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 475/10 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with an aromatic or hetero-aromatic ring directly attached in position 2
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Provided are compounds having a structure of formula (I), pharmaceutical compositions comprising such compounds and use thereof. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
Provided herein is compounds of Formula I, methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Provided herein is compounds of Formula I, methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
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 413/06 - 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 carbon chain containing only aliphatic carbon atoms
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
C07D 417/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
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 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
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61P 37/00 - Drugs for immunological or allergic disorders
a compound (as represented by formula I) serving as an Src homology region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitor, as well as a pharmaceutical composition thereof, a preparation method therefor, and a use in treating an SHP2 mediation disease. The compound of formula I exerts an effect by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis.
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 413/14 - 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 is a novel compound, having curative activity for cancer. Also provided is a preparation method for the compound and a pharmaceutical composition containing the compound.
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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
Disclosed is a compound as a fibroblast growth factor receptor 4 (FGFR4) inhibitor (as shown in formula (I)), and a pharmaceutical composition thereof and a preparation method therefor, as well as the use of same in the treatment of FGFR4-mediated diseases. The above-mentioned compounds act by participating in a number of processes, such as regulating cell proliferation, apoptosis, migration, neovascularization.
Disclosed is a compound as a fibroblast growth factor receptor 4 (FGFR4) inhibitor (as shown in formula (I)), and a pharmaceutical composition thereof and a preparation method therefor, as well as the use of same in the treatment of FGFR4-mediated diseases. The above-mentioned compounds act by participating in a number of processes, such as regulating cell proliferation, apoptosis, migration, neovascularization.
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
The present invention relates to compounds of Formula I, methods of using the compounds as Trk inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
The present invention relates to compounds of Formula I, methods of using the compounds as Trk inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
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
A compound as represented by formula (I), a composition and formulation comprising such compound, and a method for using and preparing such compound. The compound is used for treating diseases mediated by HIF-2α.
C07C 49/755 - Unsaturated compounds containing a keto group being part of a ring containing ether groups, groups, groups, or groups a keto group being part of a condensed ring system with two or three rings, at least one ring being a six-membered aromatic ring
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/085 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
Provided are a bicyclic compound as represented by formula (I), a composition and a preparation comprising the compound, a method for using the compound, and a method for preparing the compound.
Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated 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
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
89.
SALT FORM, CRYSTAL FORM, PHARMACEUTICAL COMPOSITION AND USE OF TYROSINE KINASE INHIBITOR
A salt form of a compound represented by structural formula I, various crystal forms of phosphate, and a preparation method therefor and application thereof.
The present invention relates to a compound as represented by formula (I). Also provided are a composition and a preparation containing the compound, and a method for using and preparing the compound.
C07D 243/36 - Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
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 invention relates to a compound as represented by formula (I). Also provided are a composition and a preparation containing the compound, and a method for using and preparing the compound.
C07D 243/36 - Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
The present invention provides a bromodomain inhibitor. The present invention also provides a composition and a preparation containing such a compound, a method for using such a compound, and a method for preparing such a compound.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present invention relates to a compound (as represented by formula I) serving as an Src homology region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitor, a pharmaceutical composition thereof, a preparation method therefor, and the use thereof in the treatment of SHP2-mediated diseases. The compound has an effect by means of participating in the regulation of multiple processes, such as cell proliferation, apoptosis, migration and angiogenesis.
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 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
The present invention relates to a novel compound (formula I), which has cancer treatment activity. The present invention also relates to a preparation method for the compound and a pharmaceutical composition containing the compound.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
C07D 471/22 - 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 in which the condensed systems contains four or more hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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
Provided herein are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
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 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
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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention relates to compounds of Formula (I), methods of using the compounds as ENPP1 inhibitors, and pharmaceutical compositions comprising such compounds.The compounds are useful in treating cancers and infectious diseases.
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 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 215/44 - Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
98.
SALT AND CRYSTALLINE FORMS OF FGFR4 INHIBITOR AND USES THEREOF
The present invention relates to a crystalline form and/or maleate, phosphate, L-tartrate, and adipate of the compound represented by the structural formula I, and various crystalline forms of various salt forms, and preparation methods and applications thereof.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
The present invention relates to a salt form of (R)—N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(6-fluoro-1-methyl-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridin-8-yl)pyrimidin-2-amine (compound I) as shown in structural formula (I) or a crystal form thereof, and also relates to a method for preparing the salt form of compound I and/or the crystal form thereof, a pharmaceutical composition containing the salt form and/or the crystal form, and the use of same in the preparation of drugs for treating diseases, illnesses or conditions, or a method for treating diseases, illnesses or conditions.
Disclosed are a compound (as shown in formula I) as an extracellular signal-regulated kinase (ERK) inhibitor, a pharmaceutical composition thereof, a preparation method therefor, and use thereof in treating ERK-mediated diseases. Said compound plays a role by regulating a plurality of processes such as cell proliferation, apoptosis, migration and angiogenesis.
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 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 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
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
patents
