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Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2979 – PubChem

 

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The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2980 – PubChem

 

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Design, synthesis, and structure-activity relationships of a novel series of 5-alkylidenepyridazin-3(2H)-ones with a non-cAMP-based antiplatelet activity

5-Alkylidenepyridazin-3-ones with four points of diversity (R2, R6, X, Y) have been synthesized and evaluated as platelet aggregation inhibitors. Several derivatives eliciting antiplatelet activity in the low micromolar range (e.g., 14e, 14k, 14p, 14v, IC50 ? 1 mu M) were identified. Structure-activity relationships studies on these compounds revealed the key molecular determinants of this new family of antiplatelet agents: (a) two ester groups in the alkoxy moieties; (b) lipophilic substituents at the N2 position of the pyridazin-3-one. The preliminary results of a pharmacological study aimed at determining the mechanism of action of a set of representative compounds revealed that, unlike other pyridazinones, the documented antiplatelet effect is not a consequence of a PDE-III inhibitory activity.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2986 – PubChem

 

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PYRIDAZINONE DERIVATIVES AS PHOSHOINOSITIDE 3-KINASES INHIBITORS

Compounds of formula (I) described herein inhibit phosphoinositide 3-kinases (PI3K) and useful for the treatment of disorders associated with PI3K enzymes.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2976 – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 825633-94-1, name is 5-Iodo-2,3-dihydropyridazin-3-one, introducing its new discovery. name: 5-Iodo-2,3-dihydropyridazin-3-one

INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N2981 – PubChem

 

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SERINE/THREONINE KINASE INHIBITORS

Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N2978 – PubChem

 

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Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists

A novel series of 4-pyridazin-3-one and 5-pyridazin-3-one analogues were designed and synthesized as H3R antagonists. Structure-activity relationship revealed the 5-pyridazin-3-ones 8a and S-methyl 8b had excellent human and rat H3R affinities, and acceptable pharmacokinetic properties. In vivo evaluation of 8a showed potent activity in the rat dipsogenia model and robust wake-promoting activity in the rat EEG/EMG model.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2985 – PubChem

 

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PYRIDIZINONE DERIVATIVES

The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2982 – PubChem

 

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AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS

MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N, E is C or N, Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N, D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10′ -, -C-C-, or 1,2-cyclopropyl; X is O, S or NR 11, R 1 , R 2 , and R 3 are ,independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12, G is O, S or -NR 15, D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14′ , -CN, -CONR 14 R 14′ , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14′ , -NR 14 CO 2 R 14′ , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14′ , SOR 12 , SO 2 R 12 , NR 14 COR 14′ , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10′ , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14′ are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14′ together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N2972 – PubChem

 

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Pyridazine derivatives. Part 39: Reactivity of 5-iodopyridazin-3(2H)-ones in palladium-catalysed reactions

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 has been observed during Sonogashira alkynylation of 5-iodopyridazin-3(2H)-ones (3) with 1-phenyl-2-propyn-1-ol. Variable amounts of phthalazinones were isolated as by-products during the Heck alkenylation of 3. The usefulness of the hydroxymethyl fragment as a protecting group during the synthesis of 5-substituted pyridazin-3(2H)-ones has been validated. Graphical Abstract

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N2987 – PubChem