220000-86-2Relevant academic research and scientific papers
PREPARATION AND USE OF MOLECULAR SITE TARGETED AND ACTIVATED KINASE INHIBITOR
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Paragraph 0081-0082, (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)
PREPARATION METHOD OF FLUORO-SUBSTITUTED DEUTERATED DIPHENYLUREA
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, (2013/03/26)
A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-2-(N-(methyl-d3))picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.
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.
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors
Hwang, Sung Hee,Wecksler, Aaron T.,Zhang, Guodong,Morisseau, Christophe,Nguyen, Long V.,Fu, Samuel H.,Hammock, Bruce D.
, p. 3732 - 3737 (2013/07/27)
To reduce the pro-angiogenic effects of sEH inhibition, a structure-activity relationship (SAR) study was performed by incorporating structural features of the anti-angiogenic multi-kinase inhibitor sorafenib into soluble epoxide hydrolase (sEH) inhibitors. The structural modifications of this series of molecules enabled the altering of selectivity towards the pro-angiogenic kinases C-RAF and vascular endothelial growth factor receptor-2 (VEGFR-2), while retaining their sEH inhibition. As a result, sEH inhibitors with greater potency against C-RAF and VEGFR-2 were obtained. Compound 4 (t-CUPM) possesses inhibition potency higher than sorafenib towards sEH but similar against C-RAF and VEGFR-2. Compound 7 (t-CUCB) selectively inhibits sEH, while inhibiting HUVEC cell proliferation, a potential anti-angiogenic property, without liver cancer cell cytotoxicity. The data presented suggest a potential rational approach to control the angiogenic responses stemming from sEH inhibition.
SORAFENIB DERIVATIVES AS sEH INHIBITORS
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, (2012/09/10)
The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease
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Page/Page column 98, (2010/06/22)
The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
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Page/Page column 65, (2010/05/14)
Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.
Oximide derivatives and their therapeutical application
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Page/Page column 46-47, (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
Bicyclic heterocycles as kinase inhibitors
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Page/Page column 17, (2008/06/13)
The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula I or II,
Substituted benzazoles and methods of their use as inhibitors of Raf kinase
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Page 88, (2008/06/13)
New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
