223404-63-5Relevant articles and documents
Quinoline derivative, and preparation method and uses thereof
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Paragraph 0262; 0264-0265, (2018/11/04)
The invention relates to a quinoline derivative, and a composition including the derivative, and also relates to a preparation method of the derivative, and uses of the derivative in the prevention ortreatment of harmful fungi and the killing of pests.
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs)
Lu, Yanli,Mao, Fei,Li, Xiaokang,Zheng, Xinyu,Wang, Manjiong,Xu, Qing,Zhu, Jin,Li, Jian
supporting information, p. 5099 - 5119 (2017/06/28)
Stem cell factor receptor (c-KIT) and platelet derived growth factor receptor alpha (PDGFRα) kinases play an important role in gastrointestinal stromal tumors (GISTs). Here, we have discovered an c-KIT/PDGFRα dual inhibitor, compound 31, with single-digit nanomolar potency against c-KIT and PDGFRα. Compared to Imatinib (1), 31 showed better antiproliferative efficacy against various TEL-c-KIT/PDGFRα-BaF3 isogenic cells, including three 1-resistant BaF3 cell lines, as well as against GIST-T1 and GIST-882 cell lines. Furthermore, compound 31 showed a good KinomeScan selectivity (468 kinases) (S score (1) = 0.01 at 1 μM concentration), good metabolic stability in liver microsomes, and no hERG inhibitory activity. It was worth noting that 31 inhibited GIST-T1 tumor growth (TGI = 81.5%) and even the BaF3-TEL-cKIT-T670I tumor progression (TGI = 41.9%, 1-resistant GISTs) at a dosage of 100 mg/kg/day without exhibiting apparent toxicity.
COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
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Page/Page column 94, (2015/03/28)
The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
MORPHOLINYLANILINOQUINAZO- LINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS
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Page/Page column 36, (2008/06/13)
Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses, wherein R1, R2, R3 and R4 are as defined in the claims.
Dye compositions and methods of dyeing keratin fibers
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, (2008/06/13)
The dye composition has a pH of 3 to 12 and contains water, alcohols and/or mixtures thereof as a solvent; from 0.01 to 10 percent by weight of at least one dye compound of formula (I), wherein R1 represents hydrogen or a methyl group and Y is an amino group of the formula —NHR2, and R2 is either a cyclopropyl group, a methoxyethyl group or a methoxypropyl group; OR wherein R1 represents hydrogen or a linear or branched alkyl group with 1 to 4 carbon atoms and Y represents a heterocyclic ring of formula (II): wherein X is a nitrogen atom or an oxygen atom and m is 1, 2 or 3 and n is 0 or 1; and from 0.5 to 30 percent by weight of at least one anionic, cationic, amphoteric and nonionic and/or zwitterionic surface-active substances and/or from 0.1 to 25 percent by weight of at least one thickener and/or from 0.1 to 5 percent by weight of at least one care material. A method of dyeing fibers using the composition is also described.
Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 2.1) Relationship between lipophilicity and antibacterial activity in 5-thiocarbonyl oxazolidinones
Tokuyama,Takahashi,Tomita,Tsubouchi,Yoshida,Iwasaki,Kado,Okezaki,Nagata
, p. 353 - 360 (2007/10/03)
5-Thiourea and 5-dithiocarbamate oxazolidinones were synthesized as a continuation of research on 5-thiocarbonyl oxazolidinone antibacterial agents considering the hydrophobic parameters of the molecule. The structure-activity relationship (SAR) study revealed that the antibacterial activity on 5-thiocarbonyl oxazolidinones was significantly affected by the lipophilicity, especially the calculated log P value and the balance between 5-hydrophilic (or hydrophobic) substituent and hydrophobic (or hydrophilic) substituents on the benzene ring. Some of 5-thiocarbonyl oxazolidinones were found to have good in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).