15 results about "Dual inhibitor" patented technology

Disclosed are tricyclic fused heterocyclic compounds with PDE3 / 4 dual inhibition effect shown in formula (I), and stereoisomers, solvates, or pharmaceutically acceptable salts thereof, and use thereof in the preparation of drugs for treating / preventing PDE3 / 4 mediated diseases, wherein the groups in formula (I) are as defined in the specification.

Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1 / Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.

A tricyclic fused heterocyclic PDE3 / 4 dual inhibitor, a method for preparing the inhibitor, and use thereof are disclosed. Specifically, a compound of Formula I, or a pharmaceutically acceptable form thereof is provided, wherein each substituent is as defined in the specification. The compound or pharmaceutically acceptable form thereof may be used as a phosphodiesterase inhibitor, and exhibits high activity.

Aspects of the application provide dual inhibitor anti-trypsin 1 / trypsin 2 antibodies and methods of using the same for treating pancreatitis. Other aspects of the application provide engineered non-human organisms encoding a human trypsin 1 protein.

This invention relates to the field of medicinal chemistry, specifically disclosing 4-(2-fluoro-4-iodophenoxy)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline, its preparation method, and its applications. A novel N-[4-(quinazoline-4-yl)oxyphenyl]biarylsulfonamide compound prepared from this intermediate is a dual inhibitor targeting EGFR and c-Met. The quinazoline core and sulfonamide biaryl side chain in its molecular structure can specifically recognize and bind to mutant EGFR and abnormally activated c-Met, significantly enhancing its selective killing effect on tumor cells. Pharmacodynamic studies show that it exhibits excellent inhibitory activity against the human lung cancer cell line (NCI-H1975) at the cellular level, with an IC50 of [missing information - likely an IC50 value] against p-EGFR. 50 A value of 1.56 nM for p-Met IC 50 The value is 1.8nM.

Provided in the present invention are a small molecule compound, which is the compound represented by formula (I), or a stereoisomer, a geometric isomer, a tautomer, a hydrate, a solvate, and a pharmaceutically acceptable salt or a prodrug thereof, where R1 to R4 are each independently selected from C or N, and wherein R is selected from a cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl. The small molecule compound of the present disclosure can inhibit a JAK kinase, and more particularly is used as a JAK1 / Tyk2 dual inhibitor and a Tyk2 specific inhibitor.

A tricyclic fused heterocyclic PDE3 / 4 dual inhibitor, and a preparation method and application thereof are disclosed. Specifically provided is a compound with a structural formula (I) or a pharmaceutically acceptable form thereof, wherein each substituent is defined in the description. The compound or the pharmaceutically acceptable form thereof can be used as a phosphodiesterase inhibitor and has high activity.

The present application provides a phosphodiesterase inhibitor compound and a preparation method and application thereof, in particular, the present application provides a compound with structural formula (I) or a pharmaceutically acceptable form thereof, wherein each substituent is defined in the description. The compound of the present application or the pharmaceutically acceptable form thereof can be used as a phosphodiesterase inhibitor and has high activity.

The invention discloses a tricyclic fused heterocyclic PDE3 / 4 dual inhibitor, and a preparation and use therefor. Specifically provided is a compound having structural formula (I) or a pharmaceutically acceptable form thereof, wherein each substituent is as defined in the description, respectively. The compound or the pharmaceutically acceptable form thereof can be used as a phosphodiesterase inhibitor and has high activity.

Provided are a salt form and a crystal form of a pyrazole substituted imidazo[1,2-a]quinoxaline derivative, and a preparation method therefor. Specifically disclosed are a salt form and a crystal form of a compound of formula (I), and a preparation method therefor and the use thereof in the preparation of drugs related to dual inhibitors of spleen tyrosine kinase (Syk) and vascular endothelial growth factor 2 (VEGFR2).

A tricyclic fused heterocyclic PDE3 / 4 dual inhibitor, its preparation method, and its application are disclosed. Specifically, a compound having structural formula (I) or a pharmaceutically acceptable form thereof is provided, wherein each substituent is as defined in the specification. The compound or its pharmaceutically acceptable form can function as a phosphodiesterase inhibitor with high activity.

The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.

Disclosed are a tricyclic fused heterocyclic compound having a PDE3 / 4 dual inhibitory effect represented by formula (I), a stereoisomer, a solvate, or a pharmaceutically acceptable salt thereof, and the use thereof in the preparation of a drug for treating / preventing PDE3 / 4-mediated diseases. Each group in formula (I) is as defined in the description.

Disclosed in the present invention is a 1-thienyl-β-carboline-based IDO1 and TDO dual inhibitor, selected from a 1-thienyl-β-carboline derivative having a structure as represented by formula I or a pharmaceutically acceptable salt thereof. R1 is hydrogen, fluorine, chlorine or bromine, R2 is hydrogen, methyl or trifluoromethyl, R3 is methyl, and R4 is C1-C4 linear or branched alkyl. Disclosed in the present invention is a use of the 1-thienyl-β-carboline derivative or the pharmaceutically acceptable salt thereof in the preparation of a IDO1 and TDO dual inhibitor. Disclosed in the present invention is a use of the 1-thienyl-β-carboline derivative or the pharmaceutically acceptable salt thereof in the preparation of a medicament for treating IDO1- and TDO-mediated diseases. The IDO1- and TDO-mediated diseases are central nervous system diseases associated with IDO1- and TDO-mediated tryptophan-kynurenine metabolic pathway abnormalities, specifically including depression, anxiety, Parkinson's disease and Alzheimer's disease.

A nanosystem and methods of treating, including prophylactically, coronavirus infections, such as those caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), by administering such nanosystem to a patient is presented. The nanosystem may be comprised of a single or a combination of therapeutic agents, optionally encapsulated in a nanoparticle having a targeting moiety directed to the particular coronavirus. For CoV-2 infections, at least one therapeutic agent, such as the dual DPP4 / ACE2 inhibitor sitagliptin, may optionally be encapsulated within a nanoparticle having a fatty acid such as linoleic acid, as the targeting moiety. Administration can occur intranasally prior to infection for prophylactic treatment or post-infection for treatment of the viral infection.