113293-70-2

Usage

Chemical Properties

White to yellow solid

InChI:InChI=1/C6H3Cl2NO/c7-5-1-4(3-10)2-6(8)9-5/h1-3H

Upstream product

• 42521-08-4 2,6-dichloroisonicotinoyl chloride 
• 2591-86-8 N-Formylpiperidine 
• 2402-78-0 2,6-dichloropyridine 
• 101990-69-6 (2,6-dichloropyridin-4-yl)methanol 
• 99-11-6 citrazinic acid 
• 5398-44-7 2,6-dichloropyridine-4-carboxylic acid 
• 68-12-2 N,N-dimethyl-formamide 
• 42521-09-5 methyl 2,6-dichloroisonicotinate 
• 1604-14-4 2,6-dichloroisonicotinic acid ethyl ester 

Downstream Products

• 101990-69-6 (2,6-dichloropyridin-4-yl)methanol 
• 211183-10-7 C₂₀H₁₉N₃O₅S₂ 
• 1201675-01-5 2,6-dichloro-4-(difluoromethyl) pyridine 
• 1239363-46-2 (S)-6-chloro-N-[1-(4-fluorophenyl)ethyl]-4-(oxazol-5-yl)pyridin-2-amine 
• 1239358-92-9 (S)-N²-[1-(4-fluorophenyl)ethyl]-4-(imidazooxazole-5-yl)-N⁶-(aminopyrazine-2-yl)-2,6-diamine 
• 1390656-84-4 tert-butyl 4-(4-(7-chloro-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-3-methoxyphenyl)piperazine-1-carboxylate 
• 1390656-69-5 tert-butyl-4-(4-(7-(2,6-dichlorophenylamino)-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-3-methoxyphenyl)piperazine-1-carboxylate 
• 1390655-23-8 7-[(2,6-dichlorophenyl)amino]-5-{[2-methoxy-4-(piperazin-1-yl)phenyl]amino}pyrido[3,4-d]pyridazin-4-ol mono-trifluoroacetate 
• 1390656-76-4 tert-butyl 4-(4-(7-chloro-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-2,5-difluorophenyl)piperazine-1-carboxylate 
• 1390656-77-5 tert-butyl 4-(4-(7-(2,6-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-2,5-difluorophenyl)piperazine-1-carboxylate 
• 1390655-34-1 7-(2,6-dichlorobenzyl)-5-{[2,5-difluoro-4-(piperazin-1-yl)phenyl]amino}pyrido[3,4-d]pyridazin-4(3H)-one 
• 1390656-82-2 tert-butyl 4-(4-(7-(2-(isopropylsulfonyl)phenylamino)-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-3-methoxyphenyl)piperazine-1-carboxylate 
• 1390656-85-5 tert-butyl-4-(4-(7-(2-chlorophenylamino)-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-3-methoxyphenyl)piperazine-1-carboxylate 
• 1390655-39-6 7-[(2-chlorophenyl)amino]-5-{[2-methoxy-4-(piperazin-1-yl)phenyl]amino}pyrido[3,4-d]pyridazin-4(3H)-one 

Relevant academic research and scientific papers

Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity

To obtain a new anticancer drug, we focused on FER tyrosine kinase. Starting with high-throughput screening with our in-house chemical library, compound 1, which has a pyridine moiety, was found. Referring to their X-ray crystal structure with FES proto-oncogene tyrosine kinase, as a surrogate of FER followed by chemical modification including scaffold hopping of the pyridine template, we discovered pyrido-pyridazinone derivatives with potent FER kinase inhibitory activity. Here, we disclose the structure-activity relationship on the scaffold and representative compound 21 (DS21360717), which showed in vivo antitumor efficacy in a subcutaneous tumor model.

2 Tyrosine kinase mediated signal transduction inhibitors

Disclosed herein are compounds of Formula (), and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, X, X, X, X, X, and n are as defined herein, pharmaceutical compositions comprising same, and methods of preparation and use.

BICYCLIC INHIBITORS OF ALK

The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

PREPARATION AND USE OF MAGNESIUM AMIDES

The present application relates to mixed Mg/Li amides of the general formula R1R2N-Mg-NR3R4.zLiY (II) wherein R1, R2, R3, and R4 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together, or R3 and R4 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 and at least one of R3 and R4 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; HaIOn, wherein n = 3 or 4 and Hal is selected from Ci, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RxCO2; an alcoholate of the general formula ORx; a thiolate of the general formula SRx; RxP(O)O2; or SCORx; or SCSRx; OnSRx, wherein n = 2 or 3; or NOn, wherein n = 2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or derivatives thereof, or H; m is O or 1; and z > 1; as well as a process for the preparation of the mixed Mg/Li amides and the use of these amides, e.g. as bases.

Preparation and use of magnesium amides

The present application relates to mixed Mg/Li amides of the general formula ???????? R1R2N-MgX·zLiY?????(I), wherein R1, R2 and R3 independently are selected from substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or derivatives thereof, and, for R1 and R2 only, the silyl derivatives thereof; one of R1 and R2 may be H; or R1 and R2 together can be part of a cyclic or polymeric structure; X and Y independently are selected amongst others from the group consisting of F; Cl; Br; I; CN; SCN; NCO; and z > 0, as well as a process for the preparation of the mixed Mg/Li amides and the use of these amides, e.g. as bases.

Mixed Mg/Li amides of the type R2NMgCl·LiCl as highly efficient bases for the regioselective generation of functionalized aryl and heteroaryl magnesium compounds

(Chemical Equation Presented) Two are better than one: Mixed lithium-magnesium complexes of the type R2NMgCl·LiCl are kinetically highly active bases that convert a range of polyfunctional aromatic and heteroaromatic substrates into the corresponding magnesiated derivatives with high regioselectivity.

Electron transfer in a hydrogen-bonded assembly consisting of porphyrin-diimide

Electron-transfer reactions in an H-bonded assembly composed of a diacylaminopyridine bearing zinc porphyrin and 1,8:4,5-naphthalenetetracarboxylic diimide(Ka = 2.8 × 102 dm3 mol-1) in benzene occur with kCS = 4.1 × 1010 s-1 and kCR = 3.7 × 109 s-1, while the corresponding covalently linked model with a comparable distance and energy gap undergoes electron transfer with kCS = 9.9 × 1010 s-1 and kCR = 6.7 × 108 s-1.

Pesticidal cyclopropyl-2,4-dieneamides

The present Application discloses pesticidally active compounds of the formula (I): or a salt thereof, wherein Q is an monocyclic aromatic ring. or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each optionally substituted, or Q is a dihalovinyl group or a group R6 --C C-- where R6 is C1-4 alkyl, tri C1-4 alkylsilyl, halogen or hydrogen; Q1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C1-3 alkyl. halo, C1-3 haloalkyl, alkynyl, or cyano; R2,R3, R4 and R5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo. C1-4 alkyl or C1-4 haloalkyl; X is oxygen or sulphur; and R1 is selected from hydrogen and C1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C1-6 alkoxy. their preparation, pesticidal compositions containing them and their use against pests.

Heteroarylethanol-pyridylalkylamines for controlling animal growth

A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula STR1 in which A represents =CH-- or =N--, R0 represents hydrogen or methyl, R1 and R3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO2 -alkyl, R2 represents hydrogen, hydroxyl, alkoxy or the radical --NR5 R6, R4 represents hydrogen, C1 -C10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH7 R8, or represents the radical COR9 or the radical --O--Z--R10, Z represents C1 -C10 -alkylene, -alkenylene or alkynylene, R5 represents hydrogen or alkyl, R6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R5 and R6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring, R7 and R8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl, R9 represents hydroxyl, alkoxy or the radical --NR7 R8, R10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy, with the substituent R4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another, or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.