- SUBSTITUTED IMIDAZOQUINOXALINE COMPOUNDS AND USES THEREOF
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The disclosure provides substituted imidazo [1, 5-a] quinoxaline and related compounds as kinase inhibitors, and their uses. Specifically, the disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof or prodrugs thereof, wherein, A 1-A 3, Cy and R 1-R 2 are defined herein. The compounds of Formula I are kinase inhibitors. Therefore, the compounds of the disclosure can be used to treat clinical conditions caused by DDR function defects, such as cancers. (I)
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- Double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as preparation method and application thereof, pharmaceutical composition and medicament
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The invention discloses a double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as a preparation method and application thereof, a pharmaceutical composition and a medicament, and belongs to the
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- SUBSTITUTED FUSED HETEROARYL COMPOUND SERVING AS A KINASE INHIBITOR, AND APPLICATIONS THEREOF
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The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
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- TRI-SUBSTITUTED IMIDAZOLES FOR THE INHIBITION OF TGF BETA AND METHODS OF TREATMENT
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Pharmaceutical compounds, their methods of manufacture, and methods of treatment of mammals with pharmaceutical compounds are provided.
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Paragraph 0094
(2019/01/17)
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- NOVEL 6-6 BICYCLIC AROMATIC RING SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
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The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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- Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
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- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 73-74
(2016/07/05)
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- COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
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- COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
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Paragraph 0175
(2014/05/24)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions c
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Paragraph 0289
(2013/03/28)
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- Certain Chemical Entities, Compositions, and Methods
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Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
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Paragraph 0473
(2013/03/26)
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Chemical entities that are quinoxaline kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
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Paragraph 0187; 0271
(2013/08/15)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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- SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES
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The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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Page/Page column 131
(2012/06/16)
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- Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives
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The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3′-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.
- Nishimura, Nobuko,Siegmund, Aaron,Liu, Longbin,Yang, Kevin,Bryan, Marian C.,Andrews, Kristin L.,Bo, Yunxin,Booker, Shon K.,Caenepeel, Sean,Freeman, Daniel,Liao, Hongyu,McCarter, John,Mullady, Erin L.,San Miguel, Tisha,Subramanian, Raju,Tamayo, Nuria,Wang, Ling,Whittington, Douglas A.,Zalameda, Leeanne,Zhang, Nancy,Hughes, Paul E.,Norman, Mark H.
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p. 4735 - 4751
(2011/09/20)
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- PYRAZOLYL QUINAZOLINE KINASE INHIBITORS
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The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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Page/Page column 181
(2011/11/13)
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- SUBSTITUTED AMINOQUINOXALINES AS TYROSINE THREONINE KINASE INHIBITORS
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The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
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Page/Page column 57
(2011/04/14)
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- QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS
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Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.
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Page/Page column 26; 27-28
(2009/01/20)
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- NOVEL CHEMICAL COMPOUNDS
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This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.
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Page/Page column 34
(2010/11/26)
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- THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS
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Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, ne
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Page/Page column 45-46
(2008/06/13)
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- NOVEL CHEMICAL COMPOUNDS
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This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.
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Page/Page column 30
(2010/11/25)
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- FUSED PYRAZOLE DERIVATIVES AS TGF-BETA SIGNAL TRANSDUCTION INHIBITORS FOR THE TREATMENT OF FIBROSIS AND NEOPLASMS
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The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.
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Page/Page column 26
(2010/02/14)
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- NOVEL COMPOUNDS AS PHARMACEUTICAL AGENTS
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The current invention relates to compounds of the formula:(Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
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