254 results about "Dual inhibitor" patented technology

The invention belongs to the technical field of medicines, and particularly relates to an imidazo quinoline PI3K and mTOR (mammalian target of rapamycin) dual inhibitor disclosed in a general formula (I) and clinically-acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R3', R4, R4', R5 and X are defined as in a specification. The invention also relates to a preparation method of the compounds, a medicine preparation containing the compounds and the application of the compounds in preparing medicines capable of treating and/ or preventing proliferative diseases.

The present invention provides compounds of Formula (I):

or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R³ and R¹¹ are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that 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 specifically relates to a preparation method for a dual inhibitor LCZ696 of angiotensin II receptor and neprilysin, which belongs to the technical field of drug synthesis. The preparation method comprises the following steps: preparing valsartan and AHU-377 or AHU-377 calcium salt at first; and then mixing valsartan with AHU-377 or AHU-377 calcium salt under stirring so as to prepare LCZ696. The LCZ696 prepared in the invention has good quality and high purity; and the preparation method has the advantages of simplicity, low energy consumption, low cost and suitability for large batch production.

The invention discloses a making method of compound I and drug composition and application to treat tumour, which is 3-cyano quinoline derivant (I) as dual-inhibitor protein kinase of tyrosine and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z and n are defined as instruction.

This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.

The invention which belongs to the technical field of medicines concretely relates to dual PI3K and mTOR inhibitor compounds with a general formula represented by formula (I), pharmaceutically acceptable salts thereof, or stereoisomers thereof. In the formula (I), R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, X and Y are defined in the specification. The invention also relates to a preparation method of the compounds, medicinal preparations containing the compounds, medicinal compositions containing the compounds, and an application of the compounds in the preparation of medicines for treating and/or preventing proliferative diseases.

The invention discloses a making method of compound I and drug composition and application to treat tumour, which is 3-nitrile quinoline derivant (I) as dual-inhibitor protein kinase of tyrosine and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z and n are defined as instruction.

The invention belongs to the field of pharmaceutical chemistry, and in particular relates to a HDM2 and HDMX dual inhibitor 3-nitrile quinoline derivative and a preparation method and application thereof. The invention provides the quinoline derivative whose structure is shown in formula (I) or a pharmaceutically acceptable salt thereof. The compound provided by the invention can inhibit the respective ability of combining with p53 specificity of HDM2 and HDMX, can be used as an anti-tumor drug, and has a wide clinical application prospect.

This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

The invention relates to naturally or artificially synthesized iso-thiocyanates i.e. JC-5411 compounds and their use in treating and preventing malignant tumor, wherein the compounds can directly suppress the methylation of the gene promoter / 5-UTR area CpG DNA, directly inhibit the reactivity of histone deacethylases (HADC), selectively promote histone acetylation and methylation, then further recover the expression of genes with important functions that are shut abnormally in cancer cells, thus control the malignant proliferation of cancer cells.

This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and bone metastases, with a dual inhibitor of MET and VEGF.

The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and a pharmaceutical formulation of one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and B-RAF and MEK inhibitors.

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts 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 discloses a novel dual inhibitor of deoxyribonucleic acid (DNA) topoisomerase I and DNA topoisomerase II. Mononuclear ruthenium (II) complexes containing a plurality of hydroxy ligands are synthesized, the complexes are stable in structure, the water-solubility of the complexes is better than that of normal organic small molecule inhibitors, and the complexes have dual poison effect for I type DNA topoisomerase and II type DNA topoisomerase and can inhibit body cancer cell growth obviously.

This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.

The present invention provides compounds of Formula (I):

or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L₁, M and R¹¹ are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that 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.

3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and derivatives thereof are provided for use as dual inhibitors of the Raf/MEK/ERK and PI3K/Akt pathways and for use in the treatment of cancer.

The invention provides a small molecular compound, The small molecular compound is characterized by having a structure as shown in the following molecular general formula, wherein X1 and X2 are selected from carbon or nitrogen, G1 is a carbon ring or a heterocyclic ring with aromaticity, any one or more hydrogen atoms on the G1 ring are substituted by R1, wherein R1 is selected from nitrogen-containing groups. The small molecule compound can be used as an efficient and specific JAK kinase inhibitor, especially a Tyk2 inhibitor, and/or a JAK1 inhibitor, and/or a JAK1/Tyk2 dual inhibitor, or a Tyk2/JAK1 dual inhibitor or a Tyk2/Jak2 dual inhibitor.

This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.