1012058-78-4Relevant articles and documents
Preparation method and application of sorafenib photoaffinity probe molecule based on halogen intermediate
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Paragraph 0025; 0028, (2021/07/09)
The invention discloses a preparation method and application of a sorafenib photoaffinity probe molecule based on a halogen intermediate, and relates to the technical field of biological medicines. The preparation method of the sorafenib photoaffinity pro
Preparation method and application of probe molecule containing photoaffinity group diazirine
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Paragraph 0022; 0038-0039, (2021/07/24)
The invention discloses a preparation method and application of a probe molecule containing a photoaffinity group diazirine, relates to the technical field of biological medicines, and solves the problems that a large fluorescent molecule needs to be connected to a drug molecule and the photocrosslinking activity of the probe molecule is weak in the existing target confirmation technology. 2-(3-(-3-butyne-1-yl)-3H-bis(aziridin-3-yl) ethyl-1-amine is used as a linker, drug molecules react to obtain an intermediate product with monocarboxylic acid, and the linker and the intermediate product with monocarboxylic acid are condensed to obtain the photoaffinity probe molecule. According to the arrangement, the preparation method of the photoaffinity probe molecule is relatively simple, the linker contains the photoaffinity group diaziridine, the photocrosslinking activity of diaziridine is relatively high, and meanwhile, the feasibility of a photoaffinity labeling technology in the aspect of confirming a small molecule target is also verified.
PREPARATION AND USE OF MOLECULAR SITE TARGETED AND ACTIVATED KINASE INHIBITOR
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Paragraph 0068; 0071, (2019/12/12)
Disclosed are molecularly targeted and activated kinase inhibitors and use thereof. Specifically, a compound represented by the following formula A or a pharmaceutically acceptable salt thereof, wherein X is a polar and a non-polar uncharged amino acid such as alanine, proline or threonine; A is alanine; N is asparagine; PABC is -NH-phenyl-CH2-O-; and Z is a drug molecule; wherein the lactobionic acid residue, XAN and PABC are linked to each other by an amide bond; PABC is bonded to Z by an ester group, i.e., -OC(O)-. ????????Lacto-XAN-PABC-Z?????(Formula A)
Photoaffinity probe molecule based on VEGFR-2 inhibitor (sorafenib) and preparation method thereof
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Paragraph 0045; 0048, (2019/03/28)
The invention relates to a photoaffinity probe molecule based on a VEGFR-2 inhibitor (sorafenib) and a preparation method thereof. The amido bond of the sorafenib is hydrolyzed under the NaOH (sodiumhydroxide) alkaline condition, so as to obtain an interm
RAF-DEGRADING CONJUGATE COMPOUNDS
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Paragraph 0209; 0216, (2018/11/22)
The present disclosure provides, inter alia, RAF-Degrading Conjugate Compounds that are useful in the treatment of cancer and other RAF related diseases. Also provided are, pharmaceutical compositions, methods of treatment, and kits comprising a RAF- Degrading Conjugate Compound.
METHOD AND PROCESS FOR PREPARATION AND PRODUCTION OF DEUTERATED OMEGA-DIPHENYLUREA
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, (2013/03/26)
Methods and processes for preparation and production of deuterated ω-diphenylurea are disclosed. Especially, a kind of deuterated ω-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenye-N′-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.
Oximide derivatives and their therapeutical application
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Page/Page column 47, (2009/01/23)
The present invention relates to a compound represented as the following Formula (I) and a pharmaceutical composition thereof wherein all substituents are as defined in the specification; and also relates to a method for treating or lessening the severity
RAF KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 25, (2008/12/08)
The present invention relates to Raf kinase inhibitors containing zinc-binding and their use in the treatment of Raf related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.