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IMIDAZOTHIADIAZOLE AND IMIDAZOPYRIDAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPT-OR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION

The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W,Y, R0, R2, R4, Ra, Rb, X 1, X 2, X 3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are in-hibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N224 – PubChem

 

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An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury

Death associated protein kinase (DAPK) is a calcium and calmodulin regulated enzyme that functions early in eukaryotic programmed cell death, or apoptosis. To validate DAPK as a potential drug discovery target for acute brain injury, the first small molecule DAPK inhibitor was synthesized and tested in vivo. A single injection of the aminopyridazine-based inhibitor administered 6 h after injury attenuated brain tissue or neuronal biomarker loss measured, respectively, 1 week and 3 days later. Because aminopyridazine is a privileged structure in neuropharmacology, we determined the high-resolution crystal structure of a binary complex between the kinase domain and a molecular fragment of the DAPK inhibitor. The co-crystal structure describes a structural basis for interaction and provides a firm foundation for structure-assisted design of lead compounds with appropriate molecular properties for future drug development.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N243 – PubChem

 

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TYK2 INHIBITORS AND USES THEREOF

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£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N214 – PubChem

 

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IMIDAZOPYRIDAZINES AS AKT KINASE INHIBITORS

Imidazopyridazines of formula (I) a process for their production and the use thereof

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N202 – PubChem

 

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QUINUCLIDINE DERIVATIVES AS MUSCARINIC M3 RECEPTOR ANTAGONISTS

The invention provides named compounds of formula (I), wherein R4 is a N- sustituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for’ the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N212 – PubChem

 

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THERAPEUTICALLY ACTIVE STEROIDAL DERIVATIVES

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof (I) wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17beta-HSD1 and in treatment or prevention of steroid hormone de- pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17beta-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore mentioned compounds or pharmaceutically acceptable salts thereof.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N219 – PubChem

 

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Electrochemical Synthesis of Imidazo-Fused N-Heteroaromatic Compounds through a C?N Bond-Forming Radical Cascade

We have developed a unified strategy for preparing a variety of imidazo-fused N-heteroaromatic compounds through regiospecific electrochemical (3+2) annulation reaction of heteroarylamines with tethered internal alkynes. The electrosynthesis employs a novel tetraarylhydrazine as the catalyst, has a broad substrate scope, and obviates the need for transition-metal catalysts and oxidizing reagents.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N236 – PubChem