28987-45-3Relevant academic research and scientific papers
Design and Synthesis of Highly Active Peroxisome Proliferator-Activated Receptor (PPAR) β/δ Inverse Agonists with Prolonged Cellular Activity
Toth, Philipp M.,Lieber, Sonja,Scheer, Frithjof M.,Schumann, Tim,Schober, Yvonne,Nockher, Wolfgang A.,Adhikary, Till,Müller-Brüsselbach, Sabine,Müller, Rolf,Diederich, Wibke E.
supporting information, p. 488 - 496 (2016/03/12)
Based on 3-(((4-(hexylamino)-2-methoxyphenyl)amino)sulfonyl)-2-thiophenecarboxylic acid methyl ester (ST247, compound 2), a recently described peroxisome proliferator-activated receptor (PPAR)β/δ-selective inverse agonist, we designed and synthesized a se
N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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Paragraph 0193, (2015/06/10)
Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.
N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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Paragraph 0072, (2015/07/02)
The present invention relates to a N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and to a composition containing same as an active ingredient for preventing or treating cancer. Since the compound according to the present invention has good effects in inhibiting the activities of anaplastic lymphoma kinase (ALK) and activated Cdc42-associated kinase (ACK1), the compound can have improved therapeutic effects against cancer cells having ALK fusion proteins such as EML4-ALK and NPM-ALK and is expected to be effective in preventing the recurrence of cancer. Therefore, the compound can be effectively used as a composition for preventing or treating cancer.
Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment
Park, Chi Hoon,Choe, Hyeonjeong,Jang, In-Young,Kwon, So Yeong,Latif, Muhammad,Lee, Heung Kyoung,Lee, Hyeon Ji,Yang, Eun Hye,Yun, Jeong In,Chae, Chong Hak,Cho, Sung Yun,Choi, Sang Un,Ha, Jae Du,Jung, Heejung,Kim, Hyoung Rae,Kim, Pilho,Lee, Chong Ock,Yun, Chang-Soo,Lee, Kwangho
, p. 6192 - 6196 (2013/11/06)
The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4- dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model.
HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM
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Page/Page column 50, (2010/12/29)
The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.
