7251-09-4Relevant academic research and scientific papers
Preparation method of lenvatinib
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, (2020/05/01)
The invention discloses a preparation method of lenvatinib, which comprises the following steps: by using 4-nitro-2-chlorobenzonitrile as an initial raw material, introducing nitro into molecules forelectron withdrawing, thereby greatly lowering the elect
A [...] synthetic method
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Paragraph 0043; 0044; 0045; 0053; 0054; 0062; 0063, (2019/05/22)
The invention provides a method of synthesizing [...]. First of all the invention to 4 - cyano - 3 - hydroxy aniline as the starting material, by dimethyl carbonate methylation, after third acid in the oximation reaction at room temperature, the conditions in the PPA shut-ring forms the 6 - cyano - 7 - methoxy - 4 - quinolinone, in thionyl chloride formed under the action of the 6 - cyano - 7 - methoxy - 4 - [...], under acidic conditions [...] cyano hydrolysis synthesis of one of the intermediates 6 - formamido - 7 - methoxy - 4 - chloroquinolin. Then the 4 - hydroxy - 2 chloroaniline with cyanogen bromide at low temperature 4 - hydroxy - 2 - chloro cyaniding amine, the 4 - hydroxy - 2 - chloro cyaniding amine with bearing-displacement generating Reeth reaction synthesis [...] another key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea. Finally the two intermediate 6 - formamido - 7 - methoxy - 4 - chloroquinolin and 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea in the alkaline environment for carrying out the alkylation reaction [...]. This scheme has mild reaction conditions, no highly toxic reagent, environmental protection and the like.
CONDENSED HETEROCYCLIC COMPOUND
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Paragraph 0484; 0485, (2014/08/06)
The present invention provides a fused heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I'): wherein each symbol is as defined in the specification, provided that 2-(2-((4-cyanophenyl)amino)-2-oxoethoxy)-N-(9-ethyl-9H-carbazol-3-yl)acetamide and N-(4-cyanophenyl)-N'-(9-ethyl-9H-carbazol-3-yl)-3-methylpentanediamide are excluded, or a salt thereof.
Synthesis of prenyl- and geranyl-substituted carbazole alkaloids by DIBAL-H promoted reductive pyran ring opening of dialkylpyrano[3,2-a]carbazoles
Hesse, Ronny,Kataeva, Olga,Schmidt, Arndt W.,Knoelker, Hans-Joachim
supporting information, p. 9504 - 9509 (2014/08/18)
The DIBAL-H promoted reductive pyran ring opening of dialkylpyrano[3,2-a] carbazoles provides a direct access to a broad range of prenyl- and geranyl-substituted carbazoles. Formation of a pyran ring followed by reductive ring opening represents a new met
Development of 2-thioxoquinazoline-4-one derivatives as dual and selective inhibitors of dynamin-related protein 1 (Drp1) and puromycin-sensitive aminopeptidase (PSA)
Numadate, Akiyoshi,Mita, Yusuke,Matsumoto, Yotaro,Fujii, Shinya,Hashimoto, Yuichi
, p. 979 - 988 (2015/02/19)
An established inhibitor ot dynamin-related protein 1 (Drp1), 3-(2,4-dichloro-5-methoxyphenyl)- 2- thioxoquinazoline-4-one (mdivi-1), was recently reported also to show potent puromycin-sensitive aminopeptidase (PSA)-inhibitory activity. Herein, we report structural development of mdivi-1 derivatives and structure-activity relationship (SAR) analysis of the synthesized compounds, as well as the structurally related PSA-specific inhibitor 3-(2,6-diethylphenyl)quinazoline-2,4-dione (PAQ-22), with the aim of identifying key structural features for inhibitory activity in order to develop selective inhibitors of Drpl, which is a potential target for treatment of Huntington's disease. Among the synthesized compounds, 3-(4-chloro3methoxyphenyl)-2-thioxoquinazoline-4-one 10g) exhibited more potent Drpl-inhibitory activity than mdivi-1 with high selectivity for Drpl over PSA.
OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Page/Page column 22, (2012/11/13)
Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Page/Page column 17; 36-37, (2011/07/07)
Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.
Cyclic amine compounds
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Page/Page column 22, (2009/03/07)
The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhance
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor
Winters, Michael P.,Crysler, Carl,Subasinghe, Nalin,Ryan, Declan,Leong, Lynette,Zhao, Shuyuan,Donatelli, Robert,Yurkow, Edward,Mazzulla, Marie,Boczon, Lisa,Manthey, Carl L.,Molloy, Christopher,Raymond, Holly,Murray, Lynne,McAlonan, Laura,Tomczuk, Bruce
, p. 1926 - 1930 (2008/12/22)
A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats.
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators
Hamann, Lawrence G.,Manfredi, Mark C.,Sun, Chongqing,Krystek Jr., Stanley R.,Huang, Yanting,Bi, Yingzhi,Augeri, David J.,Wang, Tammy,Zou, Yan,Betebenner, David. A.,Fura, Aberra,Seethala, Ramakrishna,Golla, Rajasree,Kuhns, Joyce E.,Lupisella, John A.,Darienzo, Celia J.,Custer, Laura L.,Price, Jennifer L.,Johnson, James M.,Biller, Scott A.,Zahler, Robert,Ostrowski, Jacek
, p. 1860 - 1864 (2008/02/04)
Pharmacokinetic studies in cynomolgus monkeys with a novel prototype selective androgen receptor modulator revealed trace amounts of an aniline fragment released through hydrolytic metabolism. This aniline fragment was determined to be mutagenic in an Ames assay. Subsequent concurrent optimization for target activity and avoidance of mutagenicity led to the identification of a pharmacologically superior clinical candidate without mutagenic potential.
