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Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same.

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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A series of new phosphoramidates and phosphonates were synthesized in single step by reacting diethyl phosphorochloridate with various bioactive amines. The newly synthesized compounds 3a-j were tested for antibacterial activity against Gram-positive and Gram-negative bacteria. All the title compounds exhibited good activity. Amongst all the tested compounds, 3b (diethyl(4-(6-fluorobenzo(d)isoxazol-3-yl)piperidin-1-yl)phosphonate), 3c (diethyl 4, 6-difluorobenzo(d)thiazole-2-ylphosphoramidate) and 3d (diethyl 5-nitro-1H-indazol-1-yl- phosphonate) displayed promising antimicrobial activity against Pseudomonas aeruginosa and Trichoderma viride due to the presence of electron with drawing fluoro and nitro groups respectively.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, ?NH?, or a direct bond; Y is ?NH? or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT6 receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT6 antagonists. The synthesis and detailed SAR of this class of compounds are reported.

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Abstract: A series of ten novel hydrazide?hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promising cytotoxicity specifically on some of the tested cell lines with IC50 values ranging between 1.93 and 25.6 muM. Further, one compound was identified as a promising drug lead which showed promising cytotoxicity with IC50 value of 1.93 muM towards MCF-7 breast cancer cell line as compared to the standard drug doxorubicin (IC50 value 0.98 muM). While, all these new compounds showed no cytotoxicity on the normal human embryonic kidney cell line, HEK-293. Graphical abstract: [Figure not available: see fulltext.]

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The invention includes a granular composition comprising the active ingredient (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-y1)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The synthesis of chloroaminoindazoles by the reduction of the nitro group of indazoles using stannous chloride in alcoholic acid solution is reported. Using catalytic hydrogenation with palladium the expected reduction to amino-indazoles occur.{A figure is presented}. Indazole Nitro Reduction Chlorination Aminochloroindazole Heterocycle.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI