Top Picks: new discover of 4,5-Dibromopyridazin-3(2H)-one

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A 3(2H)pyridazinone of the formula: STR1 wherein R1 is hydrogen, methyl, C3 -C6 alkenyl, C5 or C6 cycloalkyl, benzyl, phenyl, –(CH2)m CO2 R3 (wherein R3 is hydrogen or C1 -C5 alkyl, and m is an integer of from 1 to 4), –(CH2)n A (wherein A is –OH or –N(R4)2 wherein R4 is C1 -C3 alkyl, and n is an integer of from 2 to 6) or –CH2 CF3 ; R2 is chlorine or bromine; each of Y1 and Y2 which may be the same or different, is hydrogen, C1 -C5 alkyl, C2 -C8 alkenyl, halogen, –OR5 (wherein R5 is hydrogen, C1 -C8 alkyl or STR2 wherein q is an integer of from 1 to 4), –CO2 R6 (wherein R6 is hydrogen or C1 -C5 alkyl), –N(R7)2 (wherein R7 is C1 -C4 alkyl) or –SR8 (wherein R8 is C1 -C4 alkyl); and Y3 is C1 -C5 alkyl, C2 -C8 alkenyl, halogen, –OR5 (wherein R5 is as defined above), –CO2 R6 (wherein R6 is as defined above), –N(R7)2 (wherein R7 is as defined above) or –SR8 (wherein R8 is as defined above), or a pharmaceutically acceptable salt thereof.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3153 – PubChem

 

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This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the IKr channel; poor selectivity against IKr had been a liability of earlier analogs in this series.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3179 – PubChem

 

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2-Cyanopyridazin-3(2H)-ones are novel, effective, selective and electrophilic cyanating agents. A variety of amino, thiol and carbon nucleophiles are chemoselectively N-, S- or C-cyanated in excellent yield using 2-cyanopyridanzin-3(2H)-ones in water or tetrahydrofuran.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3174 – PubChem

 

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HETEROARYLPIPERIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3159 – PubChem

 

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ANTIMICROBIAL AGENTS AND SCREENING METHODS

Disclosed herein are antibacterial and antimicrobial compositions and methods of use. Also disclosed are screening assays for identification of an agent that specifically inhibits DsbB or bVKOR. Such methods are useful, for example, in identifying antibacterial and antimicrobial agents and compositions.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3145 – PubChem

 

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PYRIDAZINONES AND METHODS OF USE THEREOF

Disclosed are compounds according to Formula (A), and related tautomers and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (A).

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3166 – PubChem

 

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Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors

The p38 mitogen-activated protein kinase (MAPK) plays an important role in the production of proinflammatory cytokines, making it an attractive target for the treatment of various inflammatory diseases. A series of pyridazinopyridinone compounds were designed as novel p38 kinase inhibitors. A Structure-activity investigation identified several compounds possessing excellent potency in both enzyme and human whole blood assays. Among them, compound 31 exhibited good pharmacokinetic properties and showed excellent selectivity against other related kinases. In addition, 31 demonstrated efficacy in a collagen-induced arthritis disease model in rats.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3185 – PubChem

 

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PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein R1, R2, R3, R4, R5, W and X are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3156 – PubChem

 

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A one-pot synthesis of […] method (by machine translation)

The present invention discloses a one-pot synthesis of […] new method, the structure of formula (I) indicated by the […], having a structure of formula (III) as shown by a tri-substituted tertiary amine, added in a reaction vessel, for 20 – 130 C temperature by the trifluoro methane directly into the high temperature generated from the decomposition of carbon dioxide and hydrogen fluoride gas, and the temperature in the stirring reaction, for thin layer chromatography tracking after the reaction, cooling, of added dichloromethane dilution, for column chromatography separation to obtain the structure shown in formula (II) of the […], Wherein formula (I), (II) in the formula (III) R in theR1, R2, R3said carbon atom number is 1 – 10 alkyl, or the carbon atom number is 6 – 10 containing various substituted aryl, X chlorine atom or bromine atom. The invention not only provides a one-pot synthesis of […] new method, and the use of renewable energy sources. (by machine translation)

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3154 – PubChem

 

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PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS

Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3158 – PubChem