cas 14628-57-0, 4-CHLORO-5-METHOXY-2-METHYL-2,3-DIHYDROPYRIDAZIN-3-ONE

Articles about 14628-57-0Total 12 be found

SULFONAMIDE DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
PROBLEM TO BE SOLVED: To provide novel compounds having excellent α4 integrin inhibitory action. SOLUTION: The invention relates to sulfonamide derivatives represented by the general formula (I) in the figure, or pharmaceutically acceptable salts thereof, or prodrugs thereof. (In the formula, a, b, c, d, D, E, R11, B, e, f, g, h and W are as defined herein.) SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0063

(2016/10/08)

IMIDAZOLES
The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
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Page/Page column 11

(2011/02/18)

DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS
The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trif luoromethyl, halogen such as F, C1, -when n=m=1, W represents CH then Y represents oxygen, -U represents: ? either - (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, ? or -(C=O)NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, - R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enyzme inhibitors for the treatment of obesitz, tzpe-2 diabetes and lipid disorders.
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Page/Page column 48; 49

(2011/02/24)

IMIDAZOLE DERIVATIVES AS MGLUR5 ANTAGONISTS
The present invention relates to imidazole derivatives of the general formula (I) wherein R1 signifies halogen, lower alkyl or lower alkoxy; R2 signifies lower alkyl, lower hydro xyalkyl or lower alkoxyalkyl; R3 signifies hydrogen, lower alkyl, lower hydroxyalkyl or alkoxyalkyl; Q signifies either -N= or -CH=; R4 is a group of formula IIa or lIb (formula IIa and IIb) wherein X, Y and Z independently are -CH= or -N=, and whereby only one of X or Y can be a nitrogen atom; R5 and R6 independently are hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, -(CH2)m-(CO)O-lower alkyl, -(CH2)m-S(O)2-lower alkyl, -(CH2)m-C(O)-NR'R" and where m = 0-3 and R' and R'' are independently hydrogen or lower alkyl; as well as to pharmaceutically acceptable salts thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
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Page/Page column 23

(2011/02/24)

Methyl carbonium ion migration during the reaction of 4-chloro-5-methoxyl- 3(2H)-pyridazinone with trifluoroethylation agents
To synthesize 4-chloro-5-methoxy-2-(β-trifluoroethyl)-3(2H)- pyridazinone (4), the reactions of 4-chloro-5-methoxy-3(2H)-pyridazinone (5) with RCH2CF3 (R = I, TsO, MsO, TfO) in different solvents were studied. It was found that methyl group migration took place during this reaction. An oxonium salt 9 was suggested as the active intermediate for the formation of the byproduct 4-chloro-5-methoxy-2-methyl-3(2H)-pyridazinone (7) and4-chloro-2-methyl-5-(β-trifluoroethoxy)-3(2)-pyridazinone(8).
Li, Qin,Lin, Guichun,Liu, Li,Yang, Zhenjun,Zhang, Li-He
scheme or table
p. 777 - 784
(2009/05/26)

Synthesis of alkyl or aryl pyridazinyl ethers
This paper presents the synthesis of some alkyl or aryl pyridazinyl ethers from 2-alkyl-4-halo-5-hydroxy-and 2-alkyl-4,5-dichloropyridazin-3(2H)-ones or 3,6-dichloropyridazine. Reaction of 2-alkyl-4-halo-5-hydroxypyridazin-3(2H)-ones 1 with 1,2-dibromoeth
Chung, Hyun-A.,Kim, Jeum-Jong,Kim, Ho-Kyun,Kweon, Deok-Heon,Cho, Su-Dong,Lee, Sang-Gyeong,Yoon, Yong-Jin
p. 639 - 646
(2007/10/03)

Pyridazine derivatives. XXIV. Efficient N-methylation of diversely substituted 3(2H)-pyridazinones using N,N-dimethylformamide dimethylacetal
A series of diversely substituted 3(2H)-pyridazinones were efficiently N-methylated at position 2 by treatment with N,N-dimethylformamide dimethylacetal in DMF.
Sotelo, Eddy,Ravina, Enrique
p. 1675 - 1680
(2007/10/03)

Synthesis of new pyridazino[4,5-c]isoquinolinones by Suzuki cross-coupling reaction
Suzuki cross-coupling reaction of 2-alkyl(methyl and benzyl)-5-chloro-4-methoxy- and 2-alkyl(methyl and benzyl)-4-chloro-5-methoxypyridazin-3(2H)-ones with 2-formylphenylboronic acid afforded the corresponding biaryl products which were cyclized with ammonia to yield hitherto undescribed pyridazino[4,5-c]isoquinolinones. Removal of the N-benzyl protective group in position 2 yielded the unsubstituted tricyclic pyridazinones.
Riedl, Zsuzsanna,Maes, Bert U.W,Monsieurs, Katrien,Lemière, Guy L.F,Mátyus, Péter,Hajós, Gy?rgy
p. 5645 - 5650
(2007/10/03)

Dehalogenation of 1-Methyl-5-halo-4-substituted-pyridazin-6-ones
In order to confirm the regiochemistry for the functionalization of 1-(1,1-dibromo-2-oxopropyl)-4,5-dihalopyridazin-6-ones, the dehalogenation of 1-methyl-5-halo-4-substituted-pyridazin-6-ones using Pd/C and hydrogen was carried out. The results of the title reaction are reported.
Kweon, Deok-Heon,Kang, Young-Jin,Chung, Hyun-A.,Yoon, Yong-Jin
p. 819 - 826
(2007/10/03)

Concurrent Alkylation-Methoxylation of 4,5-Dihalopyridazin-6-ones and Synthesis of 5-Halo-4-hydroxypyridazin-6-ones
1-Alkyl-5-halo-4-methoxypyridazin-6-ones were synthesized from 1-alkyl-4,5-dihalopyridazin-6-ones by the concurrent alkylation-methoxylation. 1-Alkyl-5-halo-4-hydroxypyridazin-6-ones were also prepared.
Cho, Su-Dong,Choi, Woo-Yong,Yoon, Yong-Jin
p. 1579 - 1582
(2007/10/03)

5-amino-6-pyridazone derivatives, their preparation and herbicidal mixtures containing these derivatives
5-Amino-6-pyridazones of the general formulae Ia and Ib STR1 where R1 is C1 -C4 -alkyl which may carry up to three halogen atoms, R2 is C1 -C4 -alkyl or C3 -C6 -alkeny
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(2008/06/13)

Pyridazines with Heteroatom Substituents in Position 3 and 5, Part 1: 5-Hydroxy-3(2H)-pyridazinone and Its Derivatives
The synthesis of the title compound 7 was achieved starting with mucochloric acid via the pyridazinones 1,2 and 6.The electrolytic ionisation constants for 7 were found to be 4.81 (+/-0.03) and -0.3 (+/-0.3).Crystal structure analyses were performed for 7 and its "fixed" derivatives 6 and 9. - Keywords.Synthesis of 5-methoxy- and 5-hydroxy-3(2H)-pyridazinones; pKa Values of 5-hydroxy-3(2H)-pyridazinone; Crystal structure of 3(2H)-pyridazinones.
Wagner, Ulrike Gabriella,Kratky, Christoph,Kappe, Thomas
p. 329 - 342
(2007/10/02)