6319-40-0Relevant academic research and scientific papers
Synthesis of multifunctional metal-organic frameworks and tuning the functionalities with pendant ligands
Prasad, Thazhe Kootteri,Suh, Myunghyun Paik
supporting information, p. 15034 - 15040 (2020/11/11)
A series of multifunctional metal-organic frameworks (MOFs), SNU-170-SNU-176, has been synthesized using ligands, in which various functional pendants such as -NH2, -SMe, -OMe, -OEt, -OPr, and -OBu are attached to the phenyl ring of 4-(2-carboxyvinyl)benz
BENZAMIDE OR BENZAMINE COMPOUNDS USEFUL AS ANTICANCER AGENTS FOR THE TREATMENT OF HUMAN CANCERS
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Paragraph 0730; 0731; 0732, (2017/01/26)
The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not
Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8
Larson, Peter,Kucaba, Tamara A.,Xiong, Zhengming,Olin, Michael,Griffith, Thomas S.,Ferguson, David M.
supporting information, p. 1148 - 1152 (2017/11/15)
A series of N1-modified imidazoquinolines were synthesized and screened for Toll-like receptors (TLR) 7 and 8 activities to identify recognition elements that confer high affinity binding and selectivity. These receptors are key targets in the development of immunomodulatory agents that signal the NF-κB mediated transcription of pro-inflammatory chemokines and cytokines. Results are presented showing both TLR7/8 activations are highly correlated to N1-substitution, with TLR8 selectivity achieved through inclusion of an ethyl-, propyl-, or butylamino group at this position. While the structure-activity relationship analysis indicates TLR7 activity is less sensitive to N1-modification, extension of the aminoalkyl chain length to pentyl and p-methylbenzyl elicited high affinity TLR7 binding. Cytokine profiles are also reported that show the pure TLR8 agonist [4-amino-2-butyl-1-(2-aminoethyl)-7-methoxycarbonyl-1H-imidazo[4,5-c]quinoline] induces higher levels of IL-1β, IL-12, and IFNγ when compared with TLR7 selective or mixed TLR7/8 agonists. The results are consistent with previous work suggesting TLR8 agonists are Th1 polarizing and may help promote cell-mediated immunity.
Elongated and substituted triazine-based tricarboxylic acid linkers for MOFs
Klinkebiel, Arne,Beyer, Ole,Malawko, Barbara,Lüning, Ulrich
supporting information, p. 2267 - 2273 (2016/11/17)
New triazine-based tricarboxylic acid linkers were prepared as elongated relatives of triazinetribenzoic acid (TATB). Additionally, functional groups (NO2, NH2, OMe, OH) were introduced for potential post-synthetic modification (PSM) of MOFs. Functionalized tris(4-bromoaryl)triazine "cores" (3a,3b) were obtained by unsymmetric trimerization mixing one equivalent of an acid chloride (OMe or NO2 substituted) with two equivalents of an unsubstituted nitrile. Triple Suzuki coupling of the cores 3 with suitable phenyl- and biphenylboronic acid derivatives provided elongated tricarboxylic acid linkers as carboxylic acids 17 and 20 or their esters 16 and 19. Reduction of the nitro group and cleavage of the methoxy group gave the respective amino and hydroxy-substituted triazine linkers.
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 74, (2016/10/31)
The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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Page/Page column 56, (2015/12/08)
The present invention is directed to substituted five membered heteroaryl benzamide compounds compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 104, (2015/12/30)
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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Page/Page column 46, (2016/03/04)
The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula(I) which are tropomyosin-related kinase(Trk)family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF)receptor TrkA.
Combined muta- and semisynthesis: A powerful synthetic hybrid approach to access target specific antitumor agents based on ansamitocin P3
Taft, Florian,Harmrolfs, Kirsten,Nickeleit, Irinia,Heutling, Anja,Kiene, Miriam,Malek, Nisar,Sasse, Florenz,Kirschning, Andreas
supporting information; experimental part, p. 880 - 886 (2012/03/26)
Access of four new tumor specific folic acid/ansamitocin conjugates is reported that relies on a synthetic strategy based on the combination of mutasynthesis and semisynthesis. Two bromo-ansamitocin derivatives were prepared by mutasynthesis or by a modif
COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS
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Page/Page column 32, (2009/01/20)
The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
