104612-36-4Relevant articles and documents
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ
Liu, Linyi,Li, Xinyu,Cheng, Yu,Wang, Lianjian,Yang, Huizhu,Li, Jiurong,He, Siying,shuangjie Wu,Yin, Qianqian,Xiang, Hua
, p. 304 - 316 (2019)
BTK and PI3Kδ play crucial roles in the progression of leukemia, and studies confirmed that the dual inhibition against BTK and PI3Kδ could provide superior anticancer agents to single targeted therapies. Herein, a new series of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives were optimized based on a BTK/PI3Kδ inhibitor 2 designed by our group. Biological studies clarified that compound 6f exhibited the most potent inhibitory activity (BTK: IC50 = 74 nM; PI3Kδ: IC50 = 170 nM) and better selectivity than 2. Moreover, 6f significantly inhibited the proliferation of Raji and Ramos cells with IC50 values of 2.1 μM and 2.65 μM respectively by blocking BTK and PI3K signaling pathways. In brief, 6f possessed of the potency for further optimization as an anti-leukemic drug by inhibiting BTK and PI3Kδ kinase.
Development of a pilot-plant process for a nevirapine analogue HIV NNRT inhibitor
Busacca, Carl A.,Cerreta, Mike,Dong, Yong,Eriksson, Magnus C.,Farina, Vittorio,Feng, XuWu,Kim, Ji-Young,Lorenz, Jon C.,Sarvestani, Max,Simpson, Robert,Varsolona, Rieh,Vitous, Jana,Campbell, Scot J.,Davis, Mark S.,Jones, Paul-James,Norwood, Daniel,Qiu, Fenghe,Beaulieu, Pierre L.,Duceppe, Jean-Simon,Hache, Bruno,Brong, Jim,Chiu, Fang-Ting,Curtis, Tom,Kelley, Jason,Lo, Young S.,Powner, Tory H.
, p. 603 - 613 (2008)
The pilot-plant synthesis of nevirapine analogue 1 is described. The compound was prepared in eight steps from substituted pyridine raw materials and 4-hydroxyquinoline. The key transformation involves a novel one-pot conversion of an arylhalide to arylac
NOVEL COMPOUNDS FOR THE TREATMENT OF HEPATITIS C
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Page/Page column 31, (2016/09/26)
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Synthesis of pyridodiazepinediones by using the ugi multicomponent reaction
Van Den Bogaert, An M.,Nelissen, Jo,Ovaere, Margriet,Van Meervelt, Luc,Compernolle, Frans,De Borggraeve, Wim M.
scheme or table, p. 5397 - 5401 (2010/11/18)
Benzodiazepines show a broad spectrum of biological activities. In an ongoing effort to extend molecular diversity in this type of systems, we developed a strategy for synthesizing 3,4-dihydro-1H-pyrido[2,3-e][1,4] diazepine-2,5-dione compounds starting from 2-hydroxynicotinic acid and by using an Ugi reaction as a key step in the synthesis. We opted to use 2isocyanophenyl benzoate instead of Armstrong's convertible isocyanide in this multicomponent reaction.
HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 112, (2010/12/26)
Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors
Letavic, Michael A.,Keith, John M.,Ly, Kiev S.,Barbier, Ann J.,Boggs, Jamin D.,Wilson, Sandy J.,Lord, Brian,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 2566 - 2569 (2008/02/01)
A series of novel tetrahydronaphthyridine-based histamine H3 ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
NAPHTHYRIDINE COMPOUNDS
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Page/Page column 26, (2010/11/25)
Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
PYRIDINE N-OXIDES AS ANTIVIRAL AGENTS
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Page 17; 18, (2010/02/09)
The present invention relates to pyridinone derivatives of formula (I) wherein Z represents C2-6 alkynyl, aryl or heteroaryl, any of which groups may be optionally substituted, and R1 represents hydrogen, C1-6alkyl, C
Substituted alkylamine derivatives and methods of use
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, (2008/06/13)
Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
