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WNT PATHWAY ANTAGONISTS

The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N136 – PubChem

 

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(Chlorosulfonyl)benzenesulfonyl Fluorides – Versatile Building Blocks for Combinatorial Chemistry: Design, Synthesis and Evaluation of a Covalent Inhibitor Library

Multigram synthesis of (chlorosulfonyl)benzenesulfonyl fluorides is described. Selective modification of these building blocks at the sulfonyl chloride function under parallel synthesis conditions is achieved. It is shown that the reaction scope includes the use of (hetero)aromatic and electron-poor aliphatic amines (e.g., amino nitriles). Utility of the method is demonstrated by preparation of the sulfonyl fluoride library for potential use as covalent fragments, which is demonstrated by a combination of in silico and in vitro screening against trypsin as a model enzyme. As a result, several inhibitors were identified with activity on par with that of the known inhibitor.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N165 – PubChem

 

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Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors

Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N119 – PubChem

 

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Highly regioselective Buchwald-Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

The highly regioselective Buchwald-Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodology is robust and provides facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald-Hartwig amination at higher temperature to enable rapid exploration of the chemical space at C-4 and to provide a library of 2,4-bisaminopyridines.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N148 – PubChem

 

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NOVEL PESTICIDAL PYRAZOLE COMPOUNDS

The present invention relates to novel pyrazoles of formula (I) wherein the variables are as defined in the description, a method for controlling invertebrate pests, a method for protecting plant propagation material and/or the plants which grow there from, to plant propagation material, comprising at least one compound according to the present invention, and to an agricultural composition.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N114 – PubChem

 

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BENZO[B]FURANS AS BROMODOMAIN INHIBITORS

The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N106 – PubChem

 

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SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES

The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N109 – PubChem

 

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PYRIDAZINE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS

The present invention relates to pyridazine compounds of formulae (I) or (II) and the salts and N-oxides thereof, wherein A is a substituted or unsubstituted isoxazole or isothiazole radical; V is C(Rv) or N; W is C(Rw) or N; with the proviso that either V or W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyl and the like. The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow there- from, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N138 – PubChem

 

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TRICYCLIC HETEROARYL-SUBSTITUTED QUINOLINE AND AZAQUINOLINE COMPOUNDS AS PAR4 INHIBITORS

Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a tricyclic heteroaryl group substituted with R3a and zero to 2 R3b; and R1, R2, R3a, R3b, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N142 – PubChem

 

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On the Metalation of 4-Substituted Pyridazines

A series of new pyridazines bearing ortho-directing groups at C-4 (protected/activated amino or carboxylic acid functionalities) was prepared and their metalation with lithium 2,2,6,6-tetramethylpiperidine was studied.Reactions of the ortho-lithiated species thus obtained with aldehydes as electrophiles opens an access to 4,5-disubstituted pyridazines 3, 4, 14, and 15.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N166 – PubChem