Discovery of 6-Methylpyridazin-3-amine

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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

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Reference:
Pyridazine – Wikipedia,
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

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On reacting the 3-aminopyridazines 1a,d,e with dimethyl acetylenedicarboxylate (DMAD), the pyrimido[1,2-b]pyridazin-2(2H)-ones 2e-g, whereas starting from 1f, the 4(4H)-ones 5a and 3b,d were prepared. In the 2(2H)-one series, the reactions of 2b with various amino compounds resulted in various types of products. The reaction of N-methylaminopyridazines 1g,h with DMAD led to the endo-N-substituted derivatives 8a,b, whereas 1h with diethyl ethoxymethylenemalonate (DEM) gave the exo-N-substituted compound 1k. The constitution of the compounds was proved by spectroscopic and chemical evidences.

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The present invention concerns 1-(6-memberedazo-heterocyclic)-2,5-dihydro-1H-pyrrol-2-one compounds of the following formula (1) or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: the pharmaceutical composition thereof and their therapeutic use as inhibitors of Hepatitis C virus.

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Use of automated synthesis led to the discovery of several 6-membered nitrogen heterocycles as replacements for the N-isoxazolyl substituent present in the 1-naphthalenesulfonamide endothelin-A (ETA) antagonist 5- (dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide (BMS 182874). In each of these heterocycles, a small substituent such as halogen para to the position of attachment to the sulfonamide nitrogen atom was found to be advantageous for ETA receptor affinity. Of these heterocycles, 2- pyrazines offered the greatest scope for improving receptor affinity. Optimization of the substituents at the 3- and 5-positions in the pyrazine ring led to potent, ET(A)-selective compounds such as 5-(dimethylamino)-N- (5-chloro-3-methoxy-2-pyrazinyl)-1-naphthalenesulfonamide (7m, ET(A) pIC50 8.1). When dosed orally at 10 mg/kg to conscious, normotensive rats infused with big ET-1, compounds such as 7m showed significant inhibition of the pressor response with a duration of effect lasting for the 5-h course of the experiment.

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The present invention provides compounds of Formula I: wherein Y, AA, W, R3, R2, R4, R5, R6, R7, X1, X2, X3, X4 and X5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug or esters or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

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Discovery of 6-Methylpyridazin-3-amine

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18591-82-7, Name is 6-Methylpyridazin-3-amine, belongs to pyridazine compound, is a common compound. name: 6-Methylpyridazin-3-amineIn an article, once mentioned the new application about 18591-82-7.

The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc. , or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.

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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3 -dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

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The invention concerns pharmaceutically useful N-heterocyclyl sulphonamide derivatives, their pharmaceutically acceptable salts, processes for their manufacture, their use for antagonising one or more actions of endothelin in a human or other warm-blooded animal, their use in methods of treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role.

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The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

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