1780-32-1Relevant academic research and scientific papers
Indole pyrimidine compound as well as synthesis method and application thereof
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Paragraph 0062-0064, (2021/07/21)
The invention discloses an indole pyrimidine compound, the structural formula of which is as shown in formula (I): wherein L is selected from any one of H, OH, halogen, alkoxy, halogenated alkyl, alkyl, aryl and pyridine, Q is O, S or NH, X is NH or -CONH, n is a natural number, R is N(CH3)2 or T is selected from at least one of H, OH, halogen, alkoxy, halogenated alkyl, alkyl, aryl and pyridine. The indole pyrimidine compound provided by the invention can effectively inhibit adipocyte differentiation, and has a better lipid-lowering effect.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0503, (2017/11/17)
The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 253, (2017/05/02)
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
MONO AND BICYCLIC RING BORONIC ACID, ESTER AND SALT COMPOUNDS AS INHIBITORS OF P97 COMPLEX
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Page/Page column 414, (2016/12/26)
Monocyclic or bicyclic ring boronic acid or ester compounds having an arylalkyi amine substituent at the 4 position and a substituted 5:6 bicyclic group at the 2 position of the mono or bicyclic ring boronic acid or ester as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the mono or bicyclic boronic acid or ester compounds are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with the Valosin containing protein and p97 bioactivity such as cancer. Formula (I).
POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 140-141, (2016/04/26)
Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
DIAMINOPYRIMIDINES USEFUL AS INHIBITORS OF THE HUMAN RESPIRATORY SYNCYTIAL VIRUS (RSV)
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, (2013/08/28)
This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
Synthesis, crystal structure, and in vitro biological evaluation of C-6 pyrimidine derivatives: New lead structures for monitoring gene expression in vivo
Martic, Miljen,Pernot, Lucile,Westermaier, Yvonne,Perozzo, Remo,Kraljevic, Tatjana Gazivoda,Kristafor, Svjetlana,Raic-Malic, Silvana,Scapozza, Leonardo,Ametamey, Simon
experimental part, p. 293 - 315 (2012/02/03)
Novel C-6 substituted pyrimidine derivatives are good substrates of herpes simplex virus type 1 thymidine kinase (HSV1-TK). Enzyme kinetic experiments showed that our lead compound, N-methyl DHBT (N-methyl-6-(1,3-dihydroxyisobutyl) thymine; N-Me DHBT), is
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
Zhang, Zhiyuan,Wallace, Michael B.,Feng, Jun,Stafford, Jeffrey A.,Skene, Robert J.,Shi, Lihong,Lee, Bumsup,Aertgeerts, Kathleen,Jennings, Andy,Xu, Rongda,Kassel, Daniel B.,Kaldor, Stephen W.,Navre, Marc,Webb, David R.,Gwaltney, Stephen L.
scheme or table, p. 510 - 524 (2011/03/20)
The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.
Methoxymethyl (MOM) group nitrogen protection of pyrimidines bearing C-6 acyclic side-chains
Kraljevic, Tatjana Gazivoda,Petrovic, Martina,Kristafor, Svjetlana,Makuc, Damjan,Plavec, Janez,Ross, Tobias L.,Ametamey, Simon M.,Raic-Malic, Silvana
scheme or table, p. 5113 - 5129 (2011/08/06)
Novel N-methoxymethylated (MOM) pyrimidine (4-13) and pyrimidine-2,4- diones (15-17) nucleoside mimetics in which an isobutyl side-chain is attached at the C-6 position of the pyrimidine moiety were synthesized. Synthetic methods via O-persilylated or N-a
Syntheses and antitumor evaluation of C(6)-isobutyl- and C(6)-isobutenyl-substituted pyrimidines, and dihydropyrrolo[1,2-c]pyrimidine-1, 3-diones
Kristafor, Svjetlana,Kraljevic, Tatjana Gazivoda,Ametamey, Simon M.,Cetina, Mario,Ratkaj, Ivana,Hacek, Romana Tandara,Pavelic, Sandra Kraljevic,Raic-Malic, Silvana
scheme or table, p. 1455 - 1469 (2011/11/05)
A growing body of evidence supports that pyrimidine derivatives, in which the sugar residues have been replaced by acyclic side chains, might be developed as promising anticancer agents that interfere with tumor cell proliferation, survival, and metastati
