849217-60-3

Usage

Uses

Used in Pharmaceutical Industry:
N-(4-fluorophenyl)-N-(4-hydroxyphenyl)cyclopropane-1,1-dicarboxamide is used as a therapeutic agent for treating kinase-dependent disorders. Its molecular structure allows it to modulate the activity of specific kinases, which are enzymes that play crucial roles in various cellular processes. By targeting these kinases, the compound can help regulate abnormal cell signaling and potentially treat diseases driven by kinase dysregulation.

Upstream product

• 113020-21-6 1,1-cyclopropanedicarboxylic acid monomethyl ester 
• 123-30-8 4-amino-phenol 
• 1345847-71-3 methyl 1-((4-fluorophenyl)amidomethyl)cyclopropyl-1-carboxylate 
• 6914-71-2 dimethyl 1,1-cyclopropanedicarboxylate 
• 849217-48-7 ((4-fluorophenyl)carbamoyl)cyclopropanecarboxylic acid 
• 208121-91-9 1-[(4-fluorophenyl)amido]cyclopropanecarboxylic acid 
• 371-40-4 4-fluoroaniline 
• 598-10-7 cyclopropane-1,1-dicarboxylic acid 

Downstream Products

• 849217-68-1 cabozantinib 

Relevant academic research and scientific papers

Structure-guided design and development of novel N-phenylpyrimidin-2-amine derivatives as potential c-Met inhibitors

The HGF/Met signaling pathway is over-expressed in many types of cancers and closely related to oncogenesis and metastasis. Thus, we developed novel N-phenylpyrimidin-2-amine derivatives to test their inhibitory activities towards c-Met kinase, and most o

CRYSTALLINE FORMS AND SALT FORMS OF A KINASE INHIBITOR

The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid

COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS

Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.

CRYSTALLINE SALT FORMS OF A KINASE INHIBITOR

The present invention relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid crystalline salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.

Synthesis and anti-tumor activity of [1,4] dioxino [2,3-f] quinazoline derivatives as dual inhibitors of c-Met and VEGFR-2

Both c-Met and VEGFR-2 were important targets for cancer therapies. In order to develop reversible and non-covalent c-Met and VEGFR-2 dual inhibitors, a series of [1,4]dioxino[2,3-f]quinazoline derivatives were designed and synthesized. The enzyme assay demonstrated that most target compounds had inhibition potency on both c-Met and VEGFR-2 with IC50 values in nanomolar range especially compounds 7m and 7k. Based on further cell proliferation assay in vitro, compound 7k showed significantly anti-tumor activity in vivo on a hepatocellular carcinoma (MHCC97H cells) xenograft mouse model. We docked the compound 7m with c-Met and VEGFR-2 kinases, and interpreted the SAR of these analogues. All results indicated that the target compounds were dual inhibitors of c-Met and VEGFR-2 kinases that held promising potential in cancer therapy.

PYRIDO-AZAHETERECYDIC COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.

Substituted arylamino aromatic heterocyclic compound and application of substituted arylamino aromatic heterocyclic compound as antitumor drugs

The invention discloses a substituted arylamino aromatic heterocyclic compound shown in a formula (1), pharmaceutically acceptable salts thereof, a preparation method of the substituted arylamino aromatic heterocyclic compound and application of the subst

Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors

Over expression of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as to cause therapeutic resistance. Herein a series of novel 6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepine derivatives were designed, synthesised and evaluated for their c-Met kinase inhibition. Compounds 17e, 17f, 18a, and 18b were further examined for their anti-proliferative activities against four typical cancer cell lines (PC-3, Panc-1, HepG2, and Caki-1). The promising compound 17f was identified as a multi-target receptor tyrosine kinase inhibitor, which also displayed favourable pharmacokinetic properties in rats, had an acceptable safety profile in preclinical studies, and significant anti-tumour activity in the Caki-1 tumour xenograft model.

Cabozantinib preparation method

The invention discloses a cabozantinib preparation method. The target product cabozantinib is prepared by performing five-step reaction on diethyl malonate, 4-fluoroaniline, 4-chloro-6,7-dimethoxyquinoline, 4-aminophenol, 1,2-dibromoethane and the like us

C-MET MODULATORS AND METHODS OF USE

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.