3451 results about "Heterocyclic compound" patented technology

Disclosed in the present invention is a novel fused heterocyclic compound having CDK target inhibitory activity. Specifically disclosed are a compound having a structure as shown in formula (I) and serving as a CDK target inhibitor, or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer thereof.

Provides heterocyclic compounds and use thereof, specially relates to a compound represented by Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof, further relates to a PROTAC comprising a compound of Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof. The heterocyclic compounds can be used for preventing or treating a SOS l-associated disease.

Provided herein are compounds having the following structure (I), wherein the substituents are as defined herein, compositions comprising a compound, and methods for modulating the activity of KRAS G12D.

The invention discloses an oxygen-containing heterocyclic compound salt, and a crystal form and application thereof. The oxygen-containing heterocyclic compound salt disclosed by the invention has a structure as shown in a formula II. The oxygen-containing heterocyclic compound salt and the crystal form thereof provided by the invention have one or more improved characteristics, which are represented by extremely high water solubility, and high dissolution rate and high solubility in physiological related medium simulated gastrointestinal fluid, so that the stability of the oxygen-containing heterocyclic compound under an oxidation condition is remarkably improved, and the stability of the oxygen-containing heterocyclic compound is improved. Low hygroscopicity and good crystal form stability are achieved, and oral absorption and long-term storage of the medicine are facilitated; and the preparation method is simple and suitable for industrial production. # imgabs0 #

Provided herein are compounds having the following structure (I), wherein the substituents are as defined herein, compositions comprising a compound, and methods for modulating the activity of KRAS G12D and / or G12V.

Provided is a compound useful as an active ingredient in a pharmaceutical composition for treating cancer.　The present inventors have examined a compound useful as an active ingredient in a pharmaceutical composition for cancer treatment, and have completed the present invention by finding that: a heterocyclic compound represented by formula (I) and formula (I-I) has excellent an action of inducing degradation of a mutant KRAS protein and a wild-type KRAS protein, and in particular, an action of inducing degradation of a KRAS protein having a G12C mutation, G12D mutation, G12V mutation, or G13D mutation; and said heterocyclic compound has mutant KRAS inhibition and the inhibitory activity of KRAS amplified by a wild-type KRAS gene, and in particular, inhibitory activity of KRAS having a G12C mutation, G12D mutation, G12V mutation, or G13D mutation. The heterocyclic compound according to the present invention or a salt thereof can be used as a therapeutic agent for cancer.

Provided is an antibody-drug conjugate for use in the treatment of cancer in which one or more KRAS mutants, particularly a KRAS G12V mutant, a KRAS G12D mutant, and a KRAS G12C mutant, are expressed. Also provided are a drug and a drug-linker conjugate for use in the antibody-drug conjugate.　The present inventors have produced an antibody-drug conjugate with which a heterocyclic compound represented by formula (II) and having an activity of inducing the decomposition of KRAS mutant proteins can be delivered to cancer in which EGFRs are expressed, the production being achieved by linking the compound to an anti-EGFR antibody. The present inventors have also discovered a drug-linker conjugate for use in the antibody-drug conjugate or a salt thereof. In cancer in which EGFRs are expressed, the antibody-drug conjugate induces the decomposition of one or more KRAS mutants, particularly a KRAS G12V mutant protein, a KRAS G12D mutant protein, and a KRAS G12C mutant protein, thereby inhibiting the KRAS mutants and exhibiting an anti-tumor effect.

Disclosed in the present invention is a new substituted heterocyclic compound having GSPT1 degradation activity, and particularly disclosed is a compound having the structure as shown in formula (I) as a GSPT1 degradation agent, or a pharmaceutically acceptable salt, a solvate, a hydrate, an isotope substitute or an isomer thereof. The compound can be used for preventing or treating diseases related to GSPTs / MYC targets or signaling pathways.

A compound, as shown in Formula I, is a multi-heterocyclic compound. It has been verified that the compound provided by this invention integrates a novel compound targeting the calcitonin gene-related peptide (CGRP) based on ephedrine. Upon contact with the skin, due to photoactivated cell biological function regulation and the blocking effect of the multi-heterocyclic compound I structure on serotonin receptors, it achieves therapeutic effects on cutaneous vascular malformations and telangiectasia, improves the effectiveness of phototherapy in improving chronic cutaneous vascular diseases, and promotes skin wound healing.

The present invention provides a heterocyclic compound for inducing degradation of mutant KRAS protein, a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, as shown in formula (I), and the definition of each group in the formula is detailed in the specification. In addition, the invention also discloses a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in preparation of a kit for treating cancers, immune diseases or prognosis evaluation of cancer patients. # imgabs0 #

The invention provides a boron-nitrogen heterocyclic compound as well as an intermediate and a preparation method thereof, the boron-nitrogen heterocyclic compound has a structure as shown in a general formula (1), and is prepared by taking compounds as shown in a formula A, a formula B and a formula C as intermediates. Compared with similar carbon skeleton molecules, the boron-nitrogen heterocyclic compound provided by the invention shows an excellent narrow-band luminescence property. The half-peak width of the emission spectrum of the boron-aza compound is as low as 6.4 nm, and meanwhile, the fluorescence quantum yield is as high as 97%.

The invention belongs to the field of medical chemistry, and particularly relates to a crystal form of a heterocyclic compound and a pharmaceutical composition thereof. Specifically, the invention relates to a crystal form of 4-((2R, 3S, 5R)-3-(3, 4-difluoro-2-methoxyphenyl)-5-methyl-5-(trifluoromethyl) thiacyclopentane-2-formamido) pyridine-2-formamide and a pharmaceutical composition of the crystal form of 4-((2R, 3S, 5R)-3-(3, 4-difluoro-2-methoxyphenyl)-5-methyl-5-(trifluoromethyl) thiacyclopentane-2-formamido) pyridine-2-formamide. The crystal form is good in crystallinity, excellent in chemical stability and crystal form stability, high in process safety and capable of playing a good drug effect in various animal models.

The invention provides a pyrimidino heterocyclic compound as well as a pharmaceutical composition and application thereof. The invention provides a pyrimidino heterocyclic compound as shown in a formula I, and a stereoisomer, a tautomer, an atropisomer or a pharmaceutically acceptable salt of the pyrimidino heterocyclic compound. The compound disclosed by the invention has good proliferation inhibition activity on NCI-H358 cells, AsPC-1 cells and Capan-1 cells containing KRAS mutation, and has relatively weak proliferation inhibition activity on PC-9 cells wild in KRAS. # imgabs0 #

The present specification relates to a heterocyclic compound of chemical formula 1, an organic light-emitting device comprising same, and a composition for forming an organic material layer of the organic light-emitting device.

The present invention discloses a series of fluorine-substituted heterocyclic compounds, specifically, compounds represented by formula (XII) and pharmaceutically acceptable salts thereof. 【Chemical 1】 JPEG2025516367000403.jpg44170

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.

The present invention relates to a heterocyclic compound represented by chemical formula 1, and an organic light-emitting device and a composition for an organic layer, each comprising same.

The present invention relates to a novel heterocyclic compound, which is a compound having FGFR3 protein activity. Specifically, the invention relates to a compound as shown in formula (I), or pharmaceutically acceptable salts, solvates, polymorphic substances or isomers thereof, and application of the compound in preparation of medicines for treating diseases related to FGFR3 (Fibroblast Growth Factor Receptor 3). # imgabs0 #

The present invention relates to heterocyclic compound. These heterocyclic compounds are useful as TEAD binders and / or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and / or treatment of cancer and other severe disorders and diseases.

The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

The present application discloses substituted polycyclic heterocycles compound of Formula (I), pharmaceutically acceptable salt and / or solvate and pharmaceutical compositions thereof useful in the treatment of proliferative disease or condition characterized by a dysregulation of the RAS-ERK pathway such as neoplasm disease or disorder, inflammatory disease or immune system disorder.

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit Human Respiratory Syncytial Virus (HRSV) or Human Metapneumovirus (HMPV) inhibitors. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HRSV or HMPV infection. The invention also relates to methods of treating an HRSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.