205448-64-2

Usage

Uses

Used in Pharmaceutical Industry:
4-[(2,2-Dimethyl-4,6-dioxo-[1,3]dioxan-5-ylidenemethyl)-amino]-2-methoxy-benzoic acid methyl ester is used as a potential pharmaceutical compound for its unique structural features. The presence of the benzene ring, methoxy group, and carboxylic acid group may allow for interactions with biological targets, while the dioxane ring and methyl ester group could provide additional functionality and stability. Further research is needed to explore its specific properties and therapeutic applications.
Used in Chemical Synthesis:
4-[(2,2-Dimethyl-4,6-dioxo-[1,3]dioxan-5-ylidenemethyl)-amino]-2-methoxy-benzoic acid methyl ester can be used as a building block or intermediate in the synthesis of other complex organic molecules. Its unique structure, including the dioxane ring and dimethyl substitution, may enable the formation of novel compounds with specific properties and applications in various industries.
Used in Material Science:
4-[(2,2-Dimethyl-4,6-dioxo-[1,3]dioxan-5-ylidenemethyl)-amino]-2-methoxy-benzoic acid methyl ester may also find applications in material science, where its structural features could contribute to the development of new materials with unique properties. For example, the presence of the benzene ring and dioxane ring may allow for the formation of polymers or other materials with specific mechanical, thermal, or electrical properties.

Upstream product

• 15568-85-1 5-methoxymethylene-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 27492-84-8 Methyl 4-amino-2-methoxybenzoate 
• 2033-24-1 cycl-isopropylidene malonate 
• 122-51-0 orthoformic acid triethyl ester 
• 65-49-6 4-Aminosalicylic acid 
• 149-73-5 trimethyl orthoformate 

Downstream Products

• 417716-92-8 lenvatinib 
• 417722-93-1 4?(4?amino?3?chlorophenoxy)?7?methoxyquinoline?6?carboxamide 
• 417721-34-7 7-Methoxy-4-oxo-1,4-dihydroquinoline-6-carboxylic acid 

Relevant academic research and scientific papers

MULTI-SUBSTITUTED PYRIDONE DERIVATIVES AND MEDICAL USE THEREOF

The present invention relates to multi-substituted pyridone derivatives and therapeutic use thereof. In particular, the present invention relates to a compound of formula (I), a preparation method therefor, a pharmaceutical composition comprising the same, as well as use thereof as a tyrosine kinase inhibitor, in particular, use thereof in treating a disease associated with tyrosine kinase activity. Each substituent in the formula (I) is defined as in the specification.

NOVEL POLYMORPHS OF 4-[3-CHLORO-4-(N'-CYCLOPROPYL UREIDO)PHENOXY]-7-METHOXYQUINOLINE-6-CARBOXAMIDE, ITS SALTS AND PROCESS FOR THE PREPARATION THEREOF

The present invention relates to novel polymorphs of 4-[3-chloro-4-(N'- cyclopropyl ureido) phenoxy]-7- methoxyquinoline- 6- carboxamide methanesulfonate represented by following structural formula-1a and process for preparation thereof. Further, the pres

Method for synthesizing lenvatinib

The invention belongs to the field of chemical pharmacy, and specifically relates to a method for synthesizing lenvatinib. The method comprises the following steps: step 1, taking 4-aminosalicylic acid as a raw material, and preparing 4-chloro-7-methoxyquinoline-6-formamide through methylation, condensation with meldrum's acid, high-temperature cyclization, chlorination and ammoniation; step 2, taking 3-chloro-4-aminophenol as a raw material, and reacting with phenyl chloroformate and cyclopropylamine to obtain 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea; and step 3, enabling the 4-chloro-7-methoxyquinoline-6-formamide prepared in step 1 to react with the 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea prepared in step 2 under action of potassium tert-butoxide to obtain the lenvatinib. The invention provides a brand-new route for synthesising the lenvatinib. The used reagent is cheap and is easily available, is simple in operation, has a yield higher than that of other methods, and is easy for industrial production.

COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS

Disclosed herein are compounds of Formula I'. Compounds of Formula I' inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer 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.

TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluation

A series of naphthyl-based compounds were synthesized as potential inhibitors of vascular endothelial growth factor (VEGF) receptors. Investigations of structure-activity relationships led to the identification of a series of naphthamides that are potent inhibitors of the VEGF receptor tyrosine kinase family. Numerous analogues demonstrated low nanomolar inhibition of VEGF-dependent human umbilical vein endothelial cell (HUVEC) proliferation, and of these several compounds possessed favorable pharmacokinetic (PK) profiles. In particular, compound 48 demonstrated significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice. A full account of the preparation, structure-activity relationships, pharmacokinetic properties, and pharmacology of analogues within this series is presented.

Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors

We have previously shown N-arylnaphthamides can be potent inhibitors of vascular endothelial growth factor receptors (VEGFRs). N-Alkyl and N-unsubstituted naphthamides were prepared and found to yield nanomolar inhibitors of VEGFR-2 (KDR) with an improved selectivity profile against a panel of tyrosine and serine/threonine kinases. The inhibitory activity of this series was retained at the cellular level. Naphthamides 3, 20, and 22 exhibited good pharmacokinetics following oral dosing and showed potent inhibition of VEGF-induced angiogenesis in the rat corneal model. Once-daily oral administration of 22 for 14 days led to 85% inhibition of established HT29 colon cancer and Calu-6 lung cancer xenografts at doses of 10 and 20 mg/kg, respectively.

COMPOUND HAVING TGF-BETA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention provides compounds of formula (I) or compounds of formula (II) and pharmaceutically acceptable salts or solvates thereof. An objective of the present invention is to provide compounds having TGF2 inhibitory activity.

Quinoline derivatives inhibiting the effect of growth factors such as VEGF

Compounds of the formula (I): wherein: R2represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0 to 5; Z represents —O—, —NH—, —S— or —CH2—; G1represents phenyl or a 5-10 membered heteroaromatic cyclic or bicyclic group; Y1, Y2, Y3and Y4each independently represents carbon or nitrogen; R1represents fluoro or hydrogen; m is an integer from 1 to 3; R3represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, —NR4R5(wherein R4and R5, can each be hydrogen or C1-3alkyl), or a group R6—X1— wherein X1represents —CH2— or a heteroatom linker group and R6is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R6is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals such as humans, processes for the preparation of such derivatives, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Quinoline derivatives as tyrosine kinase inhibitors

The invention concerns quinoline derivatives of formula (I) wherein n is 0-3 and each R4, which may be the same or different, is a substituent such as halogeno, hydroxy, amino, nitro, trifluoromethyl, trifluoromethoxy, cyano or (1-6C)alkyl, or