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Analgesic and/or opiate antagonist tripeptide amides and processes for preparation and compositions thereof

A genus of tripeptide amides and fifteen species thereof of Examples 4-18, which are useful as analgesics and/or opiate antagonists, three processes for preparation thereof, pharmaceutical compositions thereof, and the three tripeptide amide species of Examples 1-3, which are not within the genus and are useful as analgesics and/or opiate antagonists, are disclosed.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2574 – PubChem

 

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PROCESS FOR THE PREPRATION OF 7-(4,7-DIAZASPIRO[2.5]OCTAN-7-YL)-2-(2,8-DIMETHYLIMIDAZO[1,2-B]PYRIDAZIN-6-YL)PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES

The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)pyrido[l,2-a]pyrimidin-4-one derivatives useful pharmaceutically active compounds.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1031 – PubChem

 

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QUINOXALINONES AND DIHYDROQUINOXALINONES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS

Quinoxalinones and dihydroquinoxalinones having inhibitory activity on RSV replication and having the formula (I) including addition salts, and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N358 – PubChem

 

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2-Cyanopyridazin-3(2H)-ones: Effective and chemoselective electrophilic cyanating agents

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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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2329 – PubChem

 

Brief introduction of 141-30-0

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Development of new highly potent imidazo[1,2-b[pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1

Using a structure-based design approach, we have developed a new series of imidazo[1,2-b]pyridazines, targeting the calcium-dependent protein kinase-1 (CDPK1) from Toxoplasma gondii. Twenty derivatives were thus synthesized. Structure-activity relationships and docking studies confirmed the binding mode of these inhibitors within the ATP binding pocket of TgCDPK1. Two lead compounds (16a and 16f) were then identified, which were able to block TgCDPK1 enzymatic activity at low nanomolar concentrations, with a good selectivity profile against a panel of mammalian kinases. The potential of these inhibitors was confirmed in vitro on T. gondii growth, with EC50 values of 100 nM and 70 nM, respectively. These best candidates also displayed low toxicity to mammalian cells and were selected for further in vivo investigations on murine model of acute toxoplasmosis.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1822 – PubChem

 

More research is needed about 3-Phenyl-6-chloropyridazine

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A 2,3-butanedione protected chiral glycine equivalent–a new building block for the stereoselective synthesis of enantiopure N-protected alpha-amino acids.

A new chiral glycine equivalent 7 has been synthesised from glycidol using a chiral memory protocol, and its use in the synthesis of N-Z protected alpha-amino acids was demonstrated in a series of diasteroselective lithium enolate alkylation reactions and subsequent acid hydrolyses.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2614 – PubChem

 

Archives for Chemistry Experiments of 3-Chloro-6-methylpyridazine

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PYRAZOLE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS

The present invention relates to compounds of formula (I) for their use in the treatment and/or prevention of auto-immune or auto-immune related diseases, cancer, viral infections, and central nervous system diseases and disorders, by inhibiting human dehydroorate dehydrogenase (DHODH), wherein R1, R2, R3, R4 and Ar are as defined in claim 1.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N585 – PubChem

 

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6-Methyl-5-azacytidine – Synthesis, conformational properties and biological activity. A comparison of molecular conformation with 5- azacytidine

The title compound was prepared by the isocyanate procedure and the trimethylsilyl method. The measurement of 1H NMR spectrum of 6-methyl-5- azacytidine (1) revealed a preference of gamma(t) (46%) rotamer around C(5′)- C(4′) bond, a predominance of N conformation of the ribose ring (K(eq) 0.33) and a preference of syn conformation around the C-N glycosyl bond. An analogous measurement of 5-azacytidine has shown a preference of gamma+ (60%) rotamer around the C(5′)-C(4′) bond, a predominance of N conformation of the fibose ring (K(eq) 0.41) and a preference of anti conformation around the C- N glycosyl bond 6-Methyl-5-azacytidine (1) inhibits the growth of bacteria E coli to the extent of 85% at 4000 muM concentration and the growth of LoVo/L, a human colon carcinoma cell line, to the extent of 30% at 100 muM concentration but did not inhibit L1210 cells at ? 100 muM concentration 6- Methyl-5-azacytidine (1) exhibited no in vitro antiviral activity at ? 1 muM concentration.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N75 – PubChem

 

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Electric Literature of 15456-86-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.15456-86-7, Name is 4-Bromo-1,2-dihydropyridazine-3,6-dione, molecular formula is C4H3BrN2O2. In a Patent,once mentioned of 15456-86-7

TRIAZOLO-PYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS

1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl, 1-methylcyclopentyl or pyrrolidin-1-yl, are selective ligands for GABA A receptors, in particular having high affinity for the alpha2 and/or alpha3 subunit thereof, are useful in the treatment of anxiety and convulsions.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2798 – PubChem

 

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Synthesis of 3,6-Dichloro-4-(2-chloro-1,1-dimethylethyl)pyridazine

3,6-Dichloro-4-(2-chloro-1,1-dimethylethyl)pyridazine (3) is a systemic plant fungicide whose synthesis by several routes is described.Free-radical alkylations of 3,6-dichloropyridazine (1) gave either the 4-tert-butyl derivative 2 or the alcohol 3,6-dichloro-beta,beta-dimethyl-4-pyridazineethanol (24).Pyridazine (2) must be subjected to a free-radical chlorination, which resulted in other products, but alcohol 24 could be smoothly converted to 3.Alternatively, the pyridazine ring was constructed with the side chain preattached by utilizing lactone intermediates 10 or 18.The lactone 10 with hydrazine yielded the ether 11, and chlorination with ether cleavage proceeded to 3.Lactone 20 could not be transformed to 3.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1721 – PubChem