Category: 1256359-96-2

Bremer, Paul T.; Xue, Song; Janda, Kim D. published an article in 2016, the title of the article was Picolinic acids as β-exosite inhibitors of botulinum neurotoxin A light chain.Application of 1256359-96-2 And the article contains the following content:

In developing small-mol. inhibitors of botulinum neurotoxin serotype A light chain (BoNT/A LC), substituted picolinic acids were identified. Extensive investigation into the SAR of the picolinic acid scaffold revealed 5-(1-butyl-4-chloro-1H-indol-2-yl)picolinic acid (I), which possessed low micromolar activity against BoNT/A. Kinetic and docking studies demonstrated binding of I to the β-exosite: a largely unexplored site on the LC that holds therapeutic relevance for botulism treatment. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to picolinate beta exosite inhibitor botulinum neurotoxin a light chain, Toxicology: Toxins and Venoms and other aspects.Application of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 15, 2019, Liu, Hong; Dai, Xing; He, Shuwen; Brockunier, Linda; Marcantonio, Karen; Ludmerer, Steven W.; Li, Fangbiao; Feng, Kung-I.; Nargund, Ravi P.; Palani, Anandan published an article.HPLC of Formula: 1256359-96-2 The title of the article was Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase. And the article contained the following:

Hepatitis C virus (HCV) NS5B polymerase is a prime target for the development of direct-acting antiviral drugs for the treatment of chronic HCV infection. Several novel and potent HCV NS5B non-nucleoside inhibitors with unique tetracyclic benzofuran-based structures were prepared and evaluated. Similar to clin. developmental compound MK-8876, N-linked (compounds 1 and 2) and C-linked (compounds 3 and 4) tetracyclic structures maintained broad spectrum anti-replicon potency profiles and demonstrated moderate to excellent oral bioavailability and pharmacokinetic parameters across the three preclin. animal species. To better understand the importance of tetracyclic structures related to pan genotypic potency profiles especially against clin. relevant GT1a variants, the teracycles with different ring size were prepared and in vitro evaluations suggested compounds with six number ring have better overall potency profiles. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).HPLC of Formula: 1256359-96-2

The Article related to tetracyclic benzofuran hepatitis virus ns5b polymerase mk8876, hepatitis c virus, mk-8876, ns5b polymerase, non-nucleoside inhibitors (nni), tetracyclic structure, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.HPLC of Formula: 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 31, 2014, Liu, Hong; Dai, Xing; Palani, Anandan; He, Shuwen; Nargund, Ravi; Xiao, Dong; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases. And the patent contained the following:

Title compounds I [X = pyridinone, pyrimidinone, pyridazone, etc.; B = (un)substituted 5- to 6-membered monocyclic ring, 9- to 10-membered bicyclic ring or C(O)NHCR5R6; A = fluorophenyl; D = absent or NR3SO2R4; R2 = alkyl; R3 = alkyl; R4 = alkyl; R5 = H, alkyl, or hydroxyalkyl; R6 = H or R5 and R6 together with the carbon to which they are attached form cyclopropyl], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by Suzuki reaction of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonylamino)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide with 5-bromo-1-methylpyridin-2(1H)-one followed by bromination and Suzuki reaction with 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-lH-indole. Compounds of the invention were tested for their inhibitory activity using HCV replicon system, e.g., II showed IC50 value of 3.616 nM for genotypes 1a and 3.885 nM for genotype 1b. The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to benzofuran preparation hcv viral disease, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Application of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 31, 2014, Liu, Hong; Dai, Xing; Palani, Anandan; He, Shuwen; Nargund, Ravi; Xiao, Dong; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Synthetic Route of 1256359-96-2 The title of the patent was Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases. And the patent contained the following:

Title compounds I [X = pyridinone, pyrimidinone, pyridazone, etc.; B = (un)substituted 5- to 6-membered monocyclic ring, 9- to 10-membered bicyclic ring or C(O)NHCR5R6; A = fluorophenyl; D = absent or NR3SO2R4; R2 = alkyl; R3 = alkyl; R4 = alkyl; R5 = H, alkyl, or hydroxyalkyl; R6 = H or R5 and R6 together with the carbon to which they are attached form cyclopropyl], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by Suzuki reaction of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonylamino)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide with 5-bromo-1-methylpyridin-2(1H)-one followed by bromination and Suzuki reaction with 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-lH-indole. Compounds of the invention were tested for their inhibitory activity using HCV replicon system, e.g., II showed IC50 value of 3.616 nM for genotypes 1a and 3.885 nM for genotype 1b. The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Synthetic Route of 1256359-96-2

The Article related to benzofuran preparation hcv viral disease, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Synthetic Route of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Electric Literature of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Electric Literature of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Brockunier, Linda L.; Nargund, Ravi; Marcantonio, Karen; Zorn, Nicolas; Xiao, Dong; Peng, Xuanjia; Li, Peng; Guo, Tao published a patent.Related Products of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl and aromatic ring system; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; E is absent and CR5R9; F is (CH)0-2 and (CH2)0-2; Z is N and CRa; Z1, Z2 and Z3 are independently CH and H, wherein 1 or 2 of Z1 – Z2 are N; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, OH, halo, etc.; R9 is H; R5R9 taken together to form C3-6 cycloalkyl; R6 is H, OH, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form oxo; R8 is H, halo and OH and derivatives; R10 is H and C1-6 alkyl; Ra is H, halo and CN; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 3.784 nM to 4.674 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Related Products of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Related Products of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Brockunier, Linda L.; Nargund, Ravi; Marcantonio, Karen; Zorn, Nicolas; Xiao, Dong; Peng, Xuanjia; Li, Peng; Guo, Tao published a patent.Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl and aromatic ring system; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; E is absent and CR5R9; F is (CH)0-2 and (CH2)0-2; Z is N and CRa; Z1, Z2 and Z3 are independently CH and H, wherein 1 or 2 of Z1 – Z2 are N; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, OH, halo, etc.; R9 is H; R5R9 taken together to form C3-6 cycloalkyl; R6 is H, OH, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form oxo; R8 is H, halo and OH and derivatives; R10 is H and C1-6 alkyl; Ra is H, halo and CN; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 3.784 nM to 4.674 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles