130 results about "Dual inhibitor" patented technology

The present invention relates to novel compounds which are capable of inhibiting semicarbazide-sensitive amine oxidase and myeloperoxidase. These compounds are useful for the treatment of a variety of inflammatory indications, e.g., autoimmune diseases, respiratory disease, fibrosis, vasculitis, neurological diseases or disorders, and the complications resulting from infectious disease, obesity, diabetes / metabolic syndrome and / or cardiovascular disease in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

The invention provides a tricyclic fused heterocyclic PDE3 / 4 dual inhibitor as well as a preparation method and application thereof, and particularly provides a compound with a structural formula I or a pharmaceutically acceptable form thereof, and each substituent group is defined in the specification. The compound or the pharmaceutically acceptable form of the compound can be used as a phosphodiesterase inhibitor and has relatively high activity. # imgabs0 #

The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as V-domain immunoglobulin suppressor of T-cell activation (VISTA) inhibitors or as dual inhibitors of VISTA and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by VISTA and its ligands, PD-1, PD-L1, and / or PD-L2.

The present invention relates, in part, to methods, compounds, and compositions of KRAS G12D inhibitors in combination with dual RAF / MEK inhibitors for the treatment of abnormal cell growth (e.g., cancer).

The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) inhibitors or as dual inhibitors of TIM-3 and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by TIM-3, PD-1, PD-L1, and / or PD-L2.

The invention provides a tricyclic fused heterocyclic PDE3 / 4 dual inhibitor as well as a preparation method and application thereof, and particularly provides a compound with a structural formula I or a pharmaceutically acceptable form thereof, and each substituent group is defined in the specification. The compound or the pharmaceutically acceptable form of the compound can be used as a phosphodiesterase inhibitor and has relatively high activity. # imgabs0 #

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 in the present invention is a small molecule compound, which is characterized in that it is a compound or a stereoisomer, geometric isomer, tautomer, racemate, hydrate, solvate, metabolite, and pharmaceutically acceptable salt or prodrug of the compound as represented by the following structural formula: formula (I). The small molecule compound of the present invention is applicable as a highly efficient and specific JAK kinase inhibitor, specifically a Tyk2 inhibitor and / or a JAK1 inhibitor, and / or a JAK1 / Tyk2 dual inhibitor.

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.

Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

Disclosed are direct-binding dual hypoxia-inducible factor (HIF) inhibitors and their use for treating cancer, including, but not limited to, breast, colorectal, lung, melanoma, pancreatic, and prostate cancer as a monotherapy and in combination with anti-CTLA-4 or anti-PD-1 immunotherapies. The dual HIF inhibitors also can be used for treating diseases, disorders, or conditions associated with ocular neovascularization, including, but not limited to, diabetic macular edema, diabetic retinopathy, and other ischemic retinopathies (including, but not limited to retinal vein occlusion, sickle cell retinopathy, retinopathy of prematurity, Norrie's disease, and Coat's disease), corneal neovascularization, and the treatment or prevention of neurovascular (wet-type) age-related macular degeneration.

The invention provides a dihydrofuro-indole compound with a structure as shown in a formula I, or a derivative thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug molecule thereof, or a deuteride thereof, or a tritide thereof, and application of the dihydrofuro-indole compound or the derivative thereof, or the stereoisomer thereof, or the pharmaceutically acceptable salt thereof, or the solvate thereof, or the prodrug molecule thereof, or the deuteride thereof, or the tritide thereof. The dihydrofuro-indole compound or the derivative thereof provided by the invention is a compound with a novel structure, and the compound has relatively good inhibitory activity on urate oxidase and urate transporter protein, realizes XOR / URAT1 dual inhibition, has a good uric acid reducing effect, is good in safety, has a very good pharmacokinetic property, and can be used for preparing a medicine for treating uric acid. The compound is high in druggability, can be used for preparing uric acid reducing medicines, and is used for preventing and / or treating gout or hyperuricemia. # imgabs0 #

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.

Compounds (I) are provided, where R1 and R2 are H or (C1-C3)-alkyl; X is a linear methylene chain of formula —[CH2]n— with n=0, 1 or 2, or a biradical from a branched saturated (C2-C4)-alkylene chain; and A is either a C-radical from a non-aromatic polycyclic 6- to 15-membered carbocyclic ring system, or a C-radical from a polycyclic 6- to 15-membered heterocyclic ring system having one or two O, S or N; wherein the C-radicals are unsubstituted or substituted. Compounds (I) are simultaneously inhibitors of soluble epoxide hydrolase and inhibitors of glutaminyl cyclase. Besides, they reduce the levels of pro-inflammatory cytokines in LPS stimulated BV2 cells, display low cytotoxicity, and have good BBB permeability. Thus, they are useful as multitarget compounds for the prevention or treatment of Alzheimer's disease.

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more compounds of Formula I compounds, and methods for using the compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Provided are methods and compositions for treating solid tumors in patients carrying an IDH1 and / or IDH2 mutation using a combination of a dual inhibitor of a mutant IDH1 or IDH2 enzyme and a DNA demethylating agent.

The invention discloses a hydantoin thiourea compound with dual inhibition effects of an androgen receptor and histone deacetylase 6, and further discloses a pharmaceutically acceptable salt of the hydantoin thiourea compound with the dual inhibition effects of the androgen receptor and the histone deacetylase 6. The invention further discloses application of the compound in preparation of a dual inhibitor serving as an androsinesin receptor and histone deacetylase 6. The invention also discloses application of the compound in preparation of drugs for treating tumors related to androgen receptors and histone deacetylase 6. The medicine prepared from the compound has an anti-prostatic cancer effect, provides a new direction for the research of the anti-prostatic cancer medicine, and is of great significance to the development of the anti-prostatic cancer medicine.

The present invention provides compounds of Formula (I):or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.

The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure and an application of the TRPV1 / URAT1 dual inhibitor. The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure, and the structural formula of the TRPV1 / URAT1 dual inhibitor is as follows: # imgabs0 #. The compound is unique and novel in structure, a preparation method of the compound is researched and provided, the compound has high inhibitory activity as a TRPV1 / URAT1 dual inhibitor, IC50 to TRPV1 is smaller than or equal to 100 nM, IC50 to URAT1 is smaller than or equal to 1 mu M, and inhibitory activity IC50 to an hERG channel is larger than 30 mu M; the traditional Chinese medicine composition has an excellent treatment effect on hyperuricemia, gout, inflammatory pain and the like, also has a better analgesic effect, and can be used as an analgesic medicine, a medicine for treating gout or hyperuricemia and the like.

The present invention relates to a pharmaceutical composition comprising a metabolite of enavogliflozin, and a use thereof. An enavogliflozin M1 metabolite of chemical formula 1 is a SGLT1 / SGLT2 dual inhibitor and exhibits a different pharmacological mechanism from enavogliflozin which is a SGLT2 selective inhibitor. A pharmaceutical composition comprising, as an active ingredient, the enavogliflozin M1 metabolite that is a SGLT1 / SGLT2 dual inhibitor can be useful in the prevention or treatment of diabetes or heart failure.

The present invention relates to a tricyclic compound, and a preparation method therefor and a use thereof. The structural formula of the tricyclic compound of the present invention is as shown in formula (I), wherein R1, R2, R3, R4, R5, R6, R7, E, X, and Y are as stated in the description. The compound of the present invention can simultaneously inhibit PDE3 and PDE4. Moreover, compared with existing PDE3 and PDE4 dual inhibitors, the compound of the present invention has a better effect.

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.

The present invention relates to the technical field of compound synthesis, and in particular, to a compound capable of enhancing the permeability of the blood-brain barrier, a preparation method thereof, and an application thereof. The compound capable of enhancing the permeability of the blood-brain barrier has the following structural formula: wherein X represents a halogen, R1 represents a C1-C5 alkyl, and R represents a substituted or unsubstituted alkyl and a substituted or unsubstituted phenyl. The compound has a high blood-brain barrier permeability, and can then enter the brain more quickly, which is beneficial for the compound to exert its pharmacological effect. At the same time, the compound can simultaneously inhibit ALK and EGFR, and can serve as a dual inhibitor of ALK and EGFR, and has a good therapeutic effect on cancers such as non-small cell lung cancer, anaplastic lymphoma, lung adenocarcinoma, and glioma.

The application discloses a tricyclic fused heterocyclic compound with PDE3 / 4 dual inhibition effect, and a stereoisomer, a solvate or a pharmaceutically acceptable salt of the compound, and a use of the compound in preparation of a medicine for treating and preventing PDE3 / 4-mediated diseases.

Aspects of the application provide dual inhibitor anti-KLK5 / KLK7 antibodies and methods of using the same for promoting barrier function and reducing inflammation, and treating conditions such as Netherton syndrome, eosinophilic esophagitis and atopic dermatitis.

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.

The invention discloses a novel medical application of low-medium glycans in American ginseng and a medicinal preparation of the low-medium glycans in American ginseng. The invention provides low-medium glycans separated from American ginseng. The low-medium glycans are mainly formed by polymerizing 2-15 hexose molecules. The hexose molecule is composed of glucose and fructose. The American ginseng low-medium glycan component provided by the invention not only can down-regulate the expression level of PD-L1 in tumor cells, but also can reduce the expression level of PD-1 in immune cells such as T cells, effectively activate the T cells and hinder tumor immune escape, has the application of preparing a PD-L1 inhibitor, a PD-1 inhibitor, a PD-L1 and PD-1 dual inhibitor or an anti-tumor drug, and can be used for preparing the anti-tumor drug. The compound can be used for immunotherapy of various cancers such as lung cancer, breast cancer, colon cancer, melanoma and the like, and has an application prospect in the aspect of tumor immunotherapy.