78920-21-5Relevant articles and documents
Histone deacetylase inhibitor taking pyridazinone as mother nucleus structure, and preparation method and applications thereof
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Paragraph 0398; 0400; 0402, (2019/02/10)
The invention discloses a histone deacetylase inhibitor taking pyridazinone as a mother nucleus structure, and a preparation method and applications thereof. The structure of the inhibitor is shown asa formula I; and the compound shown as the formula I has good histone deacetylase inhibitory activity and anti-tumor cell proliferation effects, and can be used for treating cancers. The structure ofthe inhibitor is shown as the formula I.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR SALT THEREOF
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Paragraph 1529; 1530; 1531, (2015/11/30)
A compound represented by Formula [1] (in the formula, Z1 represents N, CH, or the like; X1 represents NH or the like; R1 represents a heteroaryl group or the like; each of R2, R3, and R4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R5 represents a heteroaryl group or the like) or salt thereof.
SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 60, (2010/10/20)
The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic beta cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
A new pyridazine series of GABAA α5 ligands
Van Niel, Monique B.,Wilson, Kevin,Adkins, Charles H.,Atack, John R.,Castro, José L.,Clarke, Dawn E.,Fletcher, Stephen,Gerhard, Ute,Mackey, Mark M.,Malpas, Sallie,Maubach, Karen,Newman, Robert,O'Connor, Desmond,Pillai, Gopalan V.,Simpson, Peter B.,Thomas, Steven R.,MacLeod, Angus M.
, p. 6004 - 6011 (2007/10/03)
Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse ago
Pyridazine derivatives. Part 39: Reactivity of 5-iodopyridazin-3(2H)-ones in palladium-catalysed reactions
Coelho, Alberto,Sotelo, Eddy,Novoa, Héctor,Peeters, Oswald M.,Blaton, Norbert,Ravi?a, Enrique
, p. 12177 - 12189 (2007/10/03)
In the search for novel antiplatelet agents, convenient and efficient methods for the preparation of 2,5-disubstituted pyridazin-3(2H)-ones are reported that utilise palladium-catalysed cross-coupling reactions. A post-coupling base-promoted isomerisation
PYRIDAZINES - 61. UNEXPECTED REACTION BEHAVIOR OF PYRIDAZINECARBONITRILE DERIVATIVES TOWARDS PHENYLMAGNESIUM CHLORIDE
Haider, Norbert,Heinisch, Gottfried,Moshuber, Joeran
, p. 8573 - 8578 (2007/10/02)
Reactions of 4-cyano-3(2H)-pyridazonone (1) and tetrazolopyridazine-8-carbonitrile (4) with phenylmagnesium chloride were found to be governed by formal replacement of the nitrile function to afford the phenyl-substituted pyridazine derivatives 3 a
Synthesis and Structure-Activity Relationships of Series of Aminopyridazine Derivatives of γ-Aminobutyric Acid Acting as Selective GABA-A Antagonists
Wermuth, Camille-Georges,Bourguignon, Jean-Jacques,Schlewer, Gilbert,Gies, Jean-Pierre,Schoenfelder, Angele,et al.
, p. 239 - 249 (2007/10/02)
We have recently shown that an aryloaminopyridazine derivarive of GABA, SR 95103 , is a selective and competitive GABA-A receptor antagonist.In order to further explore the structural requirements for GABA receptor affinity, we synthesized a series of 38 compounds by attaching various pyridazinic structures to GABA or GABA-like side chains.Most of the compounds displaced GABA from rat brain membranes.All the active compounds antagonized the GABA-elicited enhancement of diazepam binding, strongly suggesting that all these compounds are GABA-A receptor antagonists.None of the compounds that displaced GABA from rat brain membranes interacted with other GABA recognition sites (GABA-B receptor, GABA uptake binding site, glutamate decarboxylase, GABA-transaminase).They did not interact with the Cl- ionophore associated with the GABA-A receptor and did not interact with the benzodiazepine, strychnine, and glutamate binding sites.Thus these compounds appear to be specific GABA-A receptor antagonists.In terms of structure-activity, it can be concluded that a GABA moiety bearing a positive charge is necessary for optimal GABA-A receptor recognition.Additional binding sites are tolerated only if they are part of a charge-delocalized amidinic or guanidinic system.If this delocalization is achieved by linking a butyric acid moiety to the N(2) nitrogen of a 3-aminopyridazine, GABA-antagonistic character is produced.The highest potency (ca.250 times bicuculline) was observed when an aromatic ? system, bearing electron-donating substituents, was present on the 6-position of the pyridazine ring.
PREPARATION AND SOME REACTIONS OF 4- AND 5-ARYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONES
Breukelman, Stephen P.,Meakins, G. Denis
, p. 1627 - 1636 (2007/10/02)
Efficient preparations of 4- and 5-phenyl-4,5-dihydropyridazin-3(2H)-ones have been developed, the main reactions of these compounds have been studied, and the synthetic routes have been used to give analogues with substituents in the phenyl rings.In the best synthesis of the 4-phenyldihyropyridazinone (72 percent overall yield) the product was obtained from phenylacetic acid by three simple stages.This approach was applied in preparations of the 2- and 4-hydroxyphenyl compounds and, in conjunction with a recent method for amine protection, the 4-aminophenyl analogue.A four stage synthesis starting from benzaldehyde gave the 5-phenyldihydropyridazinone in 47 percent overall yield; hydroxybenzaldehydes were similarly converted into 5-(allyloxyphenyl)dihydropyridazinones.Oxidation to phenylpyridazinones occured more readily with the 4- and 5-phenyldihydropyridazinones than with the 6-phenyl isomer.The 4- and 5-dihydropyridazinones were smoothly reduced to tetrahydropyridazinones by hydrogenation over platinum but were uneffected by palladium in the presence of hydrazine or cyclohexene.
Lactone Chemistry. Synthesis of β-Substituted, γ-Functionalized Butanolides and Butenolides and Succinaldehydic Acids from Glyoxylic Acid
Bourguignon, J. J.,Wermuth, C. G.
, p. 4889 - 4894 (2007/10/02)
The Mannich-type aminoalkylation reaction of enolizable aldehydes with morpholine and glyoxylic acid instead of formaldehyde was investigated: in basic and neutral media were obtained α,γ-dimorpholinobutanolides 2 and α-morpholino-γ-hydroxybutanolides 1, respectively.In acidic medium the spontaneous elimination of the α-morpholino group afforded the γ-hydroxybutenolide 8.The reaction pathways were suggested from the isolation and characterization of some intermediates of the Mannich reaction.These lactone structures constitute versatile synthetic intermediates for the preparation of β-substituted succinaldehydic acids 15 and 5-substituted 3-(2H)-pyridazinones 13 and 14.
