835621-07-3

Basic information

• Product Name: Regorafenib (Hydrochloride)
• Synonyms: BAY73-4506 hydrochloride;4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride;Regafenib HCL;Regafenib hydrochloride;2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, monohydrochloride;4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride (1:1);4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydr;Regorafenib (Hydrochloride)
• CAS NO: 835621-07-3
• Molecular Formula: C₂₁H₁₅ClF₄N₄O₃*ClH
• Molecular Weight: 519.2763528
• EINECS: 1592732-453-0
• Mol File: 835621-07-3.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Regorafenib (Hydrochloride)(CAS DataBase Reference)
• NIST Chemistry Reference: Regorafenib (Hydrochloride)(835621-07-3)
• EPA Substance Registry System: Regorafenib (Hydrochloride)(835621-07-3)

Safety Data

• Hazardous Substances Data: 835621-07-3(Hazardous Substances Data)

Upstream product

• 757251-39-1 4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide 
• 394-41-2 3-fluoro-4-nitrophenol 
• 399-95-1 4-amino-3-fluorophenol 
• 755037-03-7 regorafenib 

Relevant articles and documents

Preparation process of agomelatin intermediate

The invention belongs to the field of medicine synthesis and particularly relates to a preparation process of a regorafenib intermediate. The structure of the regorafenib intermediate is shown in formula (I), 4-methyl-2-pentanone and 4-amino-3-fluorophenol are condensed to obtain a compound in formula (II), N-methyl-4-chloro-2pyridine carboxamide is added to be condensed with the compound in formula (II), and the regorafenib intermediate is obtained. The preparation process of the regorafenib intermediate simple to operate and easy to monitor, has yield up to 90% or above and high efficiency and is applicable to mass industrial production of regorafenib. The prepared regorafenib intermediate has low impurity content, significantly shortens impurity removal purification time and lays a solid foundation for following regorafenib synthesis.

SYNTHETIC METABOLITES OF FLUORO SUBSTITUTED OMEGA-CARBOXYARYL DIPHENYL UREA FOR THE TREATMENT AND PREVENTION DISEASES AND CONDITIONS

Synthetic metabolites of compounds of Formula (I); salts thereof, prodrugs thereof, pharmaceutical compositions containing such synthetic metabolites, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3. Described are M2, M3, M4, and M5 synthetic metabolites of compounds of formula I, wherein the structures of said compound of formula I and said M2, M3, M4, and M5 synthetic metabolites are:

TREATMENT OF CANCERS HAVING RESISTANCE TO CHEMOTHERAPEUTIC AGENTS

The present invention provides compositions and methods for treating cancer with DAST, 4{4-[3-(4-chloro-3-trifluoromethyl phenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide of the formula I, including all polymorphs, hydrates, pharmaceutically acceptable salts, metabolites, prodrugs, solvates or combinations thereof. Any cancer can be treated, including cancers that have acquired resistance to another therapeutic agent, such as kinase inhibitors. DAST can also be used to treat cancers which have become refractory to other chemotherapeutic agents.

TREATMENT OF CANCERS WITH ACQUIRED RESISTANCE TO KIT INHIBITORS

The present invention provides compositions and methods for treating cancers which have acquired resistance to a KIT inhibitor by administering effective amounts of DAST.

Pharmaceutical compositions for the treatment of hyper-proliferative disorders

This invention relates to novel pharmaceutical compositions comprising a solid dispersion of the compound of Formula I below, to processes for preparing these novel pharmaceutical compositions and to their use for treating hyper-proliferative disorders, such as cancer, either as a sole agent or in combination with other therapies. Formula I is as follows:

FLUORO SUBSTITUTED OMEGA-CARBOXYARYL DIPHENYL UREA FOR THE TREATMENT AND PREVENTION OF DISEASES AND CONDITIONS

A compound of Formula (I): (I) salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3.