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AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS

Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the com­pounds and using the compounds for treatment of dis­eases associated with LRRK2 receptor, such as Parkin­son?s disease

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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MULTIPLE D2 A(NTA)GONISTS/H3 ANTAGONISTS FOR TREATMENT OF CNS-RELATED DISORDERS

The present invention relates to compounds compound according to Formula (III); and pharmaceutically acceptable salts, hydrates and solvates thereof. These compounds have D2receptor antagonist/(partial) agonist effects and H3antagonistic effects, pharmaceutical compositions thereof, and methods of using them for application in the prophylaxis or treatment of CNS disorders.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Cobalt-Catalyzed C(sp2)?H Methylation by using Dicumyl Peroxide as both the Methylating Reagent and Hydrogen Acceptor

The first cobalt-catalyzed direct methylation of a C(sp2)?H bond using dicumyl peroxide (DCP) as both the methylating reagent and hydrogen acceptor has been established. The reaction proceeded without the use of any additives, and was proven to be applicable to various amides bearing a 2-pyridinylisopropyl (PIP) directing group, providing an efficient access to o-methyl aryl amides with high functional-group tolerance. Preliminary mechanistic studies suggest a radical process would be involved in the catalytic process.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Quinazoline and heterocyclic compound and its preparation method and application (by machine translation)

Quinazoline and heterocyclic compound and its preparation method and application, which belongs to the field of pharmaceutical chemistry. The structural formula (I): Wherein R1 Said – H, – CH3 ; R2 Said First preparation 8, 10 – dichloro – 2, 3 – dihydro – [1, 4] dioxane [2, 3 – f] quinazoline (IX), Then R1 And R2 Substituted. The compounds of this invention can be used as a medicine for treating cancer of the phosphatidylinositol 3 – kinase (PI3K) inhibitors. (by machine translation)

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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ALDOSTERONE SYNTHASE INHIBITORS

The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3, are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Heterocyclic compounds

The invention relates to compound of general formula (I): STR1 wherein: Z represents O or CH 2n is from 0 to 4R, X and Y are as defined in the description, andA represents STR2 wherein R 1, R 2, R 6, R 7 and T” are as defined in the description,and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Palladium-Catalyzed Carboxylate-Assisted Ethoxycarboxylation of Aromatic Acids to Synthesize Monoethyl Phthalate Derivatives with Ethyl Bromodifluoroacetate

A novel and efficient approach for direct carbonation of aromatic acids with ethyl bromodifluoroacetate as the carbonyl source is reported. A broad range of substrates bearing various functional groups were tolerated, leading to monoalkyl phthalate derivatives in moderate to good yields.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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FUNCTIONALIZED BENZAMIDE DERIVATIVES AS ANTIVIRAL AGENTS AGAINST HBV INFECTION

Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, and are useful for the treatment of Hepatitis B virus (HBV) infection.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N -[3-[(Benzimidazol-2-yl)amino]propyl]amides

Malaria continues to be a major global health problem, being particularly devastating in the African population under the age of five. Artemisinin-based combination therapies (ACTs) are the first-line treatment recommended by the WHO to treat Plasmodium falciparum malaria, but clinical resistance against them has already been reported. As a consequence, novel chemotypes are urgently needed. Herein we report a novel, in vivo active, fast-acting antimalarial chemotype based on a benzimidazole core. This discovery is the result of a medicinal chemistry plan focused on improving the developability profile of an antichlamydial chemical class previously reported by our group. (Graph Presented).

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of C9H8O4

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Discovery of 2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2?,3?:3,4]benzo[1,2-d]imidazole-5-carboxamide as potent, selective and efficacious microsomal prostaglandin E2synthase-1 (mPGES-1) inhibitor

The discovery and SAR of potent, selective dioxane-fused tricyclic benz[d]imidazole derivatives as mPGES-1 inhibitor are herein described. Various amide modifications in this series afforded many potent mPGES-1 inhibitors, of which 17d proved to be suitable for further profiling in vivo. Compound 17d {2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2?,3?:3,4]benzo[1,2-d]imidazole-5-carboxamide} exhibited excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM). In rodent species, 17d strongly inhibited guinea pig mPGES-1 (IC50: 10.79 nM), but not the rat and mouse enzyme. Furthermore 17d displayed excellent in vitro selectivity over mPGES-2, cPGES, COX-enzymes (COX-1, 2), selectivity against other prostanoid synthases, favorable hERG and CEREP panel profile. Likewise, our lead 17d demonstrated good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig. Lead 17d also unveiled good efficacy in LPS-induced thermal hyperalgesia pain model with ED50of 36.7 mg/kg, respectively.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem