20197-76-6

Upstream product

• 52791-03-4 7-nitro-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid methyl ester 
• 2150-43-8 3,4-dihydroxybenzoic acid methyl ester 
• 99-50-3 3,4-Dihydroxybenzoic acid 
• 20197-75-5 2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid methyl ester 
• 4442-54-0 2,3-dihydro-1,4-benzodioxin-6-carboxylic acid 

Downstream Products

• 99358-09-5 7-amino-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxylic acid 
• 52791-04-5 3,4,7,8-tetrahydro[1,4]dioxino[2,3-g]quinazolin-4-one 

Relevant academic research and scientific papers

BENZOXAZINONE COMPOUNDS AS KLK5/7 DUAL INHIBITORS

The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): whe

As the PI3K/mTOR inhibitor tricyclic compound, its preparation and use

The invention discloses a tricyclic compound as a PI3K/mTOR inhibitor. The tricyclic compound is a compound with the general formula (I) in the specification, wherein Ar is selected from aryl or heteroaryl; X, Y and Z are independently selected from O, CR2R3 and NR4 respectively; Q is selected from O, CR2R3 and NR4 or does not exists; R1 represents C1-C6 alkyl; n is selected from integers from 0 to 4; when n is more than or equal to 2, two R1 and a morpholine cycle can be combined into a combined cycle, a bridge cycle or a spiral cycle; R2 and R3 are selected from hydrogen and C1-C6 alkyl; R4 is selected from hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, heterocyclic radical, acyl and sulfonyl. The invention further discloses a perpetration method of the compound with the general formula (I) as well as a pharmaceutical composition and application of the compound with the general formula (I).

METHODS AND COMPOUNDS FOR ANTIMICROBIAL INTERVENTION

The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and t

SUBSTITUTED 3-CYANOQUINOLINES AS PROTEIN TYROSINE KINASES INHIBITORS

This invention provides compounds of formula (1) wherein R1, G1, G2, R4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof, which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

4-anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors

The synthesis and SAR of a series of 4-anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor (EGF-R) kinase are described. Condensation of 3,4-dialkoxyanilines with ethyl (ethoxymethylene)cyanoacetate followed by thermal cyclization gave, regiospecifically, 6,7-dialkoxy-4-oxo-1,4-dihydroquinoline-3-carbonitriles. Chlorination (POCl3) followed by the reaction with substituted anilines furnished the 4-anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of EGF-R kinase. An alternate synthesis of these compounds starts with a methyl 3,4-dialkoxybenzoate. Nitration followed by reduction (Fe, NH4Cl, MeOH-H2O) gave a methyl 2-amino-4,5-dialkoxybenzoate. Amidine formation using DMF-acetal followed by cyclization using LiCH2CN furnished a 6,7-dialkoxy-4-oxo-1,4-dihydroquinoline-3-carbonitrile, which was transformed as before. Compounds containing acid, ester, amide, carbinol, and aldehyde groups at the 3-position of the quinoline ring were also prepared for comparison, as were several 1-anilino-6,7-dimethoxyisoquinoline-4-carbonitriles. The compounds were evaluated for their ability to inhibit the autophosphorylation of the catalytic domain of EGF-R. The SAR of these inhibitors with respect to the nature of the 6,7-alkoxy groups, the aniline substituents, and the substituent at the 3-position was studied. The compounds were further evaluated for their ability to inhibit the growth of cell lines that overexpress EGF-R or HER-2. It was found that 4-anilinoquinoline-3-carbonitriles are effective inhibitors of EGF-R kinase with activity comparable to the 4-anilinoquinazoline-based inhibitors. A new homology model of EGF-R kinase was constructed based on the X-ray structures of Hck and FGF receptor-1 kinase. The model suggests that with the quinazoline-based inhibitors, the N3 atom is hydrogen-bonded to a water molecule which, in turn, interacts with Thr 830. It is proposed that the quinoline-3-carbonitriles bind in a similar manner where the water molecule is displaced by the cyano group which interacts with the same Thr residue.

Bi-4-[1-(quinazolinyl-4)piperidyls] and bis{4-[1-(quinazolinyl-4)piperidyl]alkanes}

Disclosed are bi-4-[1-(quinazolinyl-4)piperidyls] and bis{4-[1-(quinazolinyl-4)piperidyl]alkanes}, e.g. 1,3-bis{4-[1-(6,7-dimethylquinazolinyl-4)piperidyl]propane}, having pharmacological activity in animals and useful for example, as anti-obesity and anti-diabetic agents. Said compounds may be prepared by reacting a 4-haloquinazoline with bi-4-piperidyl or a bis(piperidyl-4)alkane.

N,N-Bis(4-Quinazolinyl)alkanediamines

Disclosed are N,N'-Bis(4-Quinazolinyl)alkanediamines, e.g., N,N'-Bis(7-chloro-4-quinazolinyl)-1,9-nonanediamine, having pharmacological activity in animals and useful for example, as anti-obesity agents. Said compounds may be prepared by reacting a 4-haloquinazoline with an alkanediamine.