- Benzimidazolone derivatives organic light emitting compound and organic electroluminescent device including the same
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Provided is a benzo imidazolone derivative organic electroluminescent compound represented by chemical formula a. Chemical Formula a. The benzo imidazolone derivative organic light emitting compound is suitable for inclusion in an organic electroluminescent device. Both electrochemical stability and thermal stability can be satisfactorily met.
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Paragraph 0135-0139
(2021/04/20)
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- KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
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Disclosed are kinase inhibitor compounds having the following structure: (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3,R4, R5, R6, N-Ar, X, Y, Z, and AA are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
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Paragraph 0170; 0315; 0319
(2020/07/21)
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- KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
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Disclosed herein are kinase inhibitor compounds having structure (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, X, Y, Z, and (AA) are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
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Paragraph 0314; 0318
(2020/07/21)
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- Bipolar material and organic light emitting diode element
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The invention provides a bipolar material in which carbazole is linked with benzimidazole carbon nitrogen and an organic light emitting diode element utilizing the bipolar material. The organic lightemitting diode element comprises a substrate, a first conducting layer, an electric hole transfer layer, a light emitting layer, an electronic transfer layer and a second conducting layer, wherein thefirst conducting layer is arranged on the substrate; the electric hole transfer layer is arranged on the first conducting layer; the light emitting layer is arranged on the electric hole transfer layer and comprises the bipolar material in which carbazole is linked with benzimidazole carbon nitrogen; and the electronic transfer layer is arranged on the electronic transfer layer.
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Paragraph 0032
(2019/04/14)
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- Dual inhibitors of RAF-MEK-ERK and PI3K-PDK1-AKT pathways: Design, synthesis and preliminary anticancer activity studies of 3-substituted-5-(phenylamino) indolone derivatives
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The dysfunction and mutual compensatory activation of RAF-MEK-ERK and PI3K-PDK1-AKT pathways have been demonstrated as the hallmarks in several primary and recurrent cancers. The strategy of concurrent blocking of these two pathways shows clinical merits on effective cancer therapy, such as combinatory treatments and dual-pathway inhibitors. Herein, we report a novel prototype of dual-pathway inhibitors by means of merging the core structural scaffolds of a MEK1 inhibitor and a PDK1 inhibitor. A library of 43 compounds that categorized into three series (Series I–III) was synthesized and tested for antitumor activity in lung cancer cells. The results from structure-activity relationship (SAR) analysis showed the following order of antitumor activity that 3-hydroxy-5-(phenylamino) indolone (Series III) > 3-alkenyl-5-(phenylamino) indolone (Series I) > 3-alkyl-5-(phenylamino) indolone (Series II). A lead compound 9za in Series III showed most potent antitumor activity with IC50 value of 1.8 ± 0.8 μM in A549 cells. Moreover, antitumor mechanism study demonstrated that 9za exerted significant apoptotic effect, and cellular signal pathway analysis revealed the potent blockage of phosphorylation levels of ERK and AKT in RAF-MEK-ERK and PI3K-PDK1-AKT pathways, respectively. The results reported here provide robust experimental basis for the discovery and optimization of dual pathway agents for anti-lung cancer therapy.
- Yu, Zutao,Chen, Zhuo,Su, Qiongli,Ye, Shiqi,Yuan, Hongbo,Kuai, Mengni,Lv, Meng,Tu, Zhijun,Yang, Xiaoping,Liu, RangRu,Hu, Gaoyun,Li, Qianbin
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supporting information
p. 944 - 954
(2019/02/20)
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- PAN-GENOMIC INHIBITORS OF NS5A PROTEIN ENCODED BY HCV, PHARMACEUTICAL COMPOSITIONS, INTERMEDIATES FOR INHIBITOR SYNTHESIS, AND THEIR SYNTHESIS AND APPLICATION METHODS.
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Compound represented by formula 1 : or a pharmaceutically acceptable salt, a hydrate, a crystalline form, or a stereoisomer thereof, wherein: where R11 is an optionally substituted C1-C6 alkyl, an optionally substituted C3-C6 cycloalkyl, or an optionally substituted C1-C6 alkyloxy, and arrows (1-C4alkyl; R3 is an optionally substituted aryl, an optionally substituted aryloxy, an optionally substituted arylsulfanyl, an optionally substituted arylamino, or an optionally substituted nitrogen hetaryl; where R41 is an optionally substituted C1-C6 alkyl, an optionally substituted C3-C6 cycloalkyl, or an optionally substituted C1-C6 alkyloxy; X is buta-1,3-diynylene or 1,4-phenylene; arrows (— ) indicate the position of substituents attachment.
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Page/Page column 40-41; 65-66
(2017/03/21)
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- SMALL MOLECULE INHIBITORS OF DYRK1A AND USES THEREOF
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This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a benzimidazole or imidazopyridine structure which function as inhibitors of DYRK1A protein, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, glioblastoma, autoimmune diseases, inflammatory disorders (e.g., airway inflammation), and other diseases.
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Page/Page column 34-35
(2017/03/21)
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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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Page/Page column 351; 352
(2016/04/26)
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- LUMINESCENT DIAZA- MONOAZA- AND BENZIMIDAZOLE METAL CARBENE COMPLEXES FOR USE IN ELECTRONIC DEVICES SUCH AS OLEDS
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A cyclometallated Ir complex comprising one, two or three ligands of formula (I) or (I') substituted at the R5 and R7 position; an organic electronic device comprising at least one inventive cyclometallated Ir complex; alight-emitting layer comprising at least one inventive cy-clometallated Ir complex; the use of the inventive cyclometallated Ir complexin an OLED; an apparatus selected from the group consisting of stationary visual display units, mobile visual display units, illumination units, units in items of clothing, units in handbags, units in accessories, units in furniture and units in wallpaper, comprising the organic electronic device; and a process for preparing a the inventive cyclometallated Ir complex.
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Page/Page column 115; 116
(2015/02/25)
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- METAL COMPLEXES, COMPRISING CARBENE LIGANDS HAVING AN O-SUBSTITUTED NON-CYCLOMETALATED ARYL GROUP AND THEIR USE IN ORGANIC LIGHT EMITTING DIODES
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Cyclometallated Ir complex comprising three N,N diaryl substituted carbene ligands, bearing substituents in the 2 position of the non-cyclometallated aryl ring;an organic electronic device, preferably an organic light-emitting diode (OLED), comprising at least one cyclometallated Ir complexas described above, a light-emitting layer comprising said cyclometallated Ir complex preferably as emitter material, preferably in combination with at least one host material, use of said cyclometallated Ir complex in an OLED and an apparatus selected from the group consisting of stationary visual display units, mobile visualdisplay units, illumination units, units in items of clothing, units in handbags, units in accessoires, units in furniture and units in wallpaper comprising said organic electronic device, preferably said OLED, or said light-emitting layer. The present invention further relates to a process for the preparation of said cyclometallated Ir complex.
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Page/Page column 85
(2015/11/17)
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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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Page/Page column 71
(2015/02/19)
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- PRMT5 INHIBITORS AND USES THEREOF
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Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described
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Paragraph 00349
(2014/07/08)
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- Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties
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Herein we report investigations into the p38α MAP kinase activity of trisubstituted imidazoles that led to the identification of compounds possessing highly potent in vivo activity. The SAR of a novel series of imidazopyridines is demonstrated as well, resulting in compounds possessing cellular potency and enhanced in vivo activity in the rat collagen-induced arthritis model of chronic inflammation.
- Mader, Mary,de Dios, Alfonso,Shih, Chuan,Bonjouklian, Rosanne,Li, Tiechao,White, Wesley,de Uralde, Beatriz Lopez,Sanchez-Martinez, Concepcion,del Prado, Miriam,Jaramillo, Carlos,de Diego, Eugenio,Martin Cabrejas, Luisa M.,Dominguez, Carmen,Montero, Carlos,Shepherd, Timothy,Dally, Robert,Toth, John E.,Chatterjee, Arindam,Pleite, Sehila,Blanco-Urgoiti, Jaime,Perez, Leticia,Barberis, Mario,Lorite, Maria Jose,Jambrina, Enrique,Nevill Jr., C. Richard,Lee, Paul A.,Schultz, Richard C.,Wolos, Jeffrey A.,Li, Li C.,Campbell, Robert M.,Anderson, Bryan D.
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p. 179 - 183
(2008/09/18)
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