26905-03-3Relevant academic research and scientific papers
Nitrogen-containing heterocycle derivatives and applications thereof
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Paragraph 0238-0240, (2018/03/24)
The invention discloses nitrogen-containing heterocycle derivatives and applications thereof, relates to compounds of a general formula (V), a preparing method thereof and applications of the compounds in medicines, and more particularly relates to compound derivatives of compounds shown as the general formula (V), a preparing method thereof and uses of the derivatives in medicines preventing andtreating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty degeneration of liver, diabetes mellitus type 2, hyperglycemia, obesity or insulin resistance and metabolic syndrome and resisting antitumor, with the derivatives being adopted as therapeutic agents. The compounds disclosed by the invention can also reduce total cholesterol, LDL-cholesterol and triglyceride, can increase liver LDL receptor expression, and inhibit PCSK9 expression.
Imidazole derivatives, its pharmaceutical composition and use thereof
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Paragraph 0586-0588, (2017/02/24)
Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
TANK-BINDING KINASE INHIBITOR COMPOUNDS
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Paragraph 0390, (2016/05/02)
Compounds having the following formula (I) and methods of their use and preparation are disclosed:
INHIBITORS OF ACK1/TNK2 TYROSINE KINASE
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Page/Page column 98, (2015/02/25)
Described are cancer therapies and anti-cancer compounds. In particular, disclosed are ihibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specifc example, compound having Formula I through IV are disclosed.
7-HYDROXY-INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
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Paragraph 00208, (2014/02/16)
The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments.
Synthesis and evaluation of cyclohexane carboxylic acid head group containing isoxazole and thiazole analogs as DGAT1 inhibitors
Kandre, Shivaji,Bhagat, Pundlik Rambhau,Kumar Reddy, M. Mahesh,Dalal, Roda,Dixit, Amol,Deshmukh, Nitin J.,Anthony, Jessy,Bose, Julie,Anupindi, Raghuram,Sharma, Rajiv,Gupte, Amol
, p. 203 - 215 (2014/05/06)
Diacylglycerol acyltransferase 1 (DGAT1) is known to play an important catalytic role in the final step of triglyceride biosynthesis. High fat diet fed DGAT1 knockout mice were resistant to weight gain and exhibited increased insulin and leptin sensitivity thereby indicating a plausible role for DGAT1 inhibitors in the treatment of obesity. 4-Phenylpiperidine-1-carbonyl cyclohexanecarboxylic acid (compound 6, DGAT1 IC50 = 57 nM) has been lately reported as a potent DGAT1 inhibitor. In our search for newer scaffolds possessing potent DGAT1 activity we undertook a systematic diversification of compound 6 to identify a 4-(5-phenylthiazole-2-carboxamido)cyclohexanecarboxylic acid scaffold. Further linker optimization of this scaffold identified compound 9e (DGAT1 IC50 = 14.8 nM) as a potent DGAT1 inhibitor. Coupled with its in vitro potency, compound 9e also exhibited 112 percent plasma triglyceride reduction at a 3 mpk dose in an oral fat tolerance test (FTT) when studied in Swiss mice.
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases
Zificsak, Craig A.,Gingrich, Diane E.,Breslin, Henry J.,Dunn, Derek D.,Milkiewicz, Karen L.,Theroff, Jay P.,Thieu, Tho V.,Underiner, Ted L.,Weinberg, Linda R.,Aimone, Lisa D.,Albom, Mark S.,Mason, Jennifer L.,Saville, Lisa,Husten, Jean,Angeles, Thelma S.,Finn, James P.,Jan, Mahfuza,O'Kane, Teresa M.,Dobrzanski, Pawel,Dorsey, Bruce D.
scheme or table, p. 133 - 137 (2012/02/15)
The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression.
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl- piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase
Guagnano, Vito,Furet, Pascal,Spanka, Carsten,Bordas, Vincent,Le Douget, Micka?l,Stamm, Christelle,Brueggen, Josef,Jensen, Michael R.,Schnell, Christian,Schmid, Herbert,Wartmann, Markus,Berghausen, Joerg,Drueckes, Peter,Zimmerlin, Alfred,Bussiere, Dirksen,Murray, Jeremy,Graus Porta, Diana
supporting information; experimental part, p. 7066 - 7083 (2011/12/04)
A novel series of N-aryl-N′-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine kinases 1, 2, and 3 by rationally designing the substitution pattern of the aryl ring. On the b
BISAMLDE DERIVATIVES AND USE THEREOF AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 159-160, (2008/12/05)
A compound of formula I, or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus,
THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
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Page/Page column 27, (2008/06/13)
To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].
