Category: 870997-85-6

Ladduwahetty, Tammy; Lee, Matthew R.; Maillard, Michel C.; Cachope, Roger; Todd, Daniel; Barnes, Michael; Beaumont, Vahri; Chauhan, Alka; Gallati, Caroline; Haughan, Alan F.; Kempf, Georg; Luckhurst, Christopher A.; Matthews, Kim; McAllister, George; Mitchell, Philip; Patel, Hiral; Rose, Mark; Saville-Stones, Elizabeth; Steinbacher, Stefan; Stott, Andrew J.; Thatcher, Emma; Tierney, Jason; Urbonas, Liudvikas; Munoz-Sanjuan, Ignacio; Dominguez, Celia published the artcile< Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease>, Quality Control of 870997-85-6, the main research area is piperazine analog preparation Rho kinase inhibitor SAR docking pharmacokinetics.

The Rho kinase (ROCK) pathway is implicated in the pathogenesis of several conditions, including neurol. diseases. In Huntington’s disease (HD), ROCK is implicated in mutant huntingtin (HTT) aggregation and neurotoxicity, and members of the ROCK pathway are increased in HD mouse models and patients. To validate this mode of action as a potential treatment for HD, a potent, selective, central nervous system (CNS)-penetrant ROCK inhibitor was sought. Identifying a compound that could be dosed orally in mice with selectivity against other AGC kinases, including protein kinase G (PKG), whose inhibition could potentially activate the ROCK pathway, was paramount for the program. The optimization of published ligands to identify a novel series of ROCK inhibitors based on a piperazine core was demonstrated. Morphing of the early series developed inhouse by scaffold hopping enabled the identification of a compound exhibiting high potency and desired selectivity and demonstrating a robust pharmacodynamic (PD) effect by the inhibition of ROCK-mediated substrate (MYPT1) phosphorylation after oral dosing.

Journal of Medicinal Chemistry published new progress about Molecular docking. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Quality Control of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Yue; Jiang, Zhensheng; Li, Zhihong; Gu, Jing; You, Qidong; Zhang, Xiaojin published the artcile< Click Chemistry-Based Discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia>, Synthetic Route of 870997-85-6, the main research area is preparation hydroxytriazolyl picolinoyl glycine derivative HIF PHD2 inhibitor anemia.

As a gene associated with anemia, the erythropoiesis gene is physiol. expressed under hypoxia regulated by †hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chem. to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the Hb of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.

Journal of Medicinal Chemistry published new progress about Anemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Synthetic Route of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Yue; Jiang, Zhensheng; Li, Zhihong; Gu, Jing; You, Qidong; Zhang, Xiaojin published the artcile< Click Chemistry-Based Discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia>, Synthetic Route of 870997-85-6, the main research area is preparation hydroxytriazolyl picolinoyl glycine derivative HIF PHD2 inhibitor anemia.

As a gene associated with anemia, the erythropoiesis gene is physiol. expressed under hypoxia regulated by †hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chem. to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the Hb of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.

Journal of Medicinal Chemistry published new progress about Anemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Synthetic Route of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Van der Plas, Steven E.; Kelgtermans, Hans; Mammoliti, Oscar; Menet, Christel; Tricarico, Giovanni; De Blieck, Ann; Joannesse, Caroline; De Munck, Tom; Lambin, Dominique; Cowart, Marlon; Dropsit, Sebastien; Martina, Sebastien L. X.; Gees, Maarten; Wesse, Anne-Sophie; Conrath, Katja; Andrews, Martin published the artcile< Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis>, Formula: C6H5BrN2O2, the main research area is preparation GLPG2451 analog CFTR potentiator cystic fibrosis structure.

Cystic fibrosis (CF) is a life-threatening recessive genetic disease caused by mutations in the gene encoding for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Lumacaftor, it has been shown that administration of one or more small mols. can partially restore the CFTR function. Correctors are small mols. that enhance the amount of CFTR on the cell surface, while potentiators improve the gating function of the CFTR channel. Herein, the discovery and optimization of a novel potentiator series are described. Scaffold hopping, focusing on retaining the different intramol. contacts, was crucial in the whole discovery process to identify a novel series devoid of genotoxic liabilities. From this series, the clin. candidate GLPG2451 was selected based on its pharmacokinetic properties, allowing QD dosing and based on its low CYP induction potential.

Journal of Medicinal Chemistry published new progress about CFTR (cystic fibrosis transmembrane conductance regulator) Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Formula: C6H5BrN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rasina, Dace; Stakanovs, Georgijs; Kanepe-Lapsa, Iveta; Bobrovs, Raitis; Jaudzems, Kristaps; Jirgensons, Aigars published the artcile< Synthesis of 2-aminopyridopyrimidinones and their plasmepsin I, II, IV inhibition potency>, Reference of 870997-85-6, the main research area is aminopyridopyrimidinone preparation antimalarial SAR.

2-Aminoquinazolin-4(3H)-one-based inhibitors, 2-aminopyrido[2,3-d]-, -[3,2-d]-, and -[4,3-d]pyrimidin-4(3H)-ones beared subpocket-specific substituents at position 7 were prepared and tested for their Plm I, II, IV inhibition potency. The position of the nitrogen atom in 2-aminopyridopyrimidinones played significant role in the inhibitory potency against Plms. Pyrido[2,3-d]pyrimidin-4(3H)-one derivatives showed poor inhibitory potency against Plms I, II, IV irresp. of the substituent at position 7. However, pyrido[4,3-d]pyrimidin-4(3H)-ones and pyrido[3,2-d]pyrimidin-4(3H)-ones were more appropriate scaffolds for Plm inhibitor development. Particularly, 2-amino-7-[4-(3-phenylpropyl)phenyl]-3-[(tetrahydrofuran-2-yl)methyl]pyrido[3,2-d]pyrimidin-4(3H)-one showed very high potency against Plm IV subtype and high selectivity against human aspartic protease, cathepsin D.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about Antimalarials. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Reference of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Josa-Cullere, Laia; Cogswell, Thomas J.; Georgiou, Irene; Jay-Smith, Morgan; Jackson, Thomas R.; Bataille, Carole J. R.; Davies, Stephen G.; Vyas, Paresh; Milne, Thomas A.; Wynne, Graham M.; Russell, Angela J. published the artcile< Identification and Preliminary Structure-Activity Relationship Studies of 1,5-Dihydrobenzo[e][1,4]oxazepin-2(3H)-ones That Induce Differentiation of Acute Myeloid Leukemia Cells In Vitro>, Name: 3-Amino-5-bromopyridine-2-carboxylic Acid, the main research area is dihydrobenzooxazepinone preparation SAR acute myeloid leukemia pharmacokinetic; CD11b; acute myeloid leukemia; benzooxazepinones; differentiation; phenotypic screen.

A series of 1,5-dihydrobenzo[e][1,4]oxazepin-2(3H)-one hit compounds e.g. I was identified and synthesized. Herein, we report the hit validation in vitro, structure-activity relationship (SAR) studies and the pharmacokinetic profiles for selected compounds

Molecules published new progress about Acute myeloid leukemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Name: 3-Amino-5-bromopyridine-2-carboxylic Acid.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Takrouri, Khuloud; Cooper, Harold D.; Spaulding, Adnrew; Zucchi, Paula; Koleva, Bilyana; Cleary, Dillon C.; Tear, Westley; Beuning, Penny J.; Hirsch, Elizabeth B.; Aggen, James B. published the artcile< Progress against Escherichia coli with the Oxazolidinone Class of Antibacterials: Test Case for a General Approach To Improving Whole-Cell Gram-Negative Activity>, COA of Formula: C6H5BrN2O2, the main research area is Escherichia oxazolidinone antibacterial gram neg permeation; Gram-negative; efflux pump; outer membrane permeability; oxazolidinones; porins.

Novel antibacterials with activity against the Gram-neg. bacteria associated with nosocomial infections, including Escherichia coli and other Enterobacteriaceae, are urgently needed due to the increasing prevalence of multidrug-resistant strains. A major obstacle that has stalled progress on nearly all small-mol. classes with potential for activity against these species has been achieving sufficient whole-cell activity, a difficult challenge due to the formidable outer membrane and efflux barriers intrinsic to these species. Using a set of compound design principles derived from available information relating physicochem. properties to Gram-neg. entry or activity, we synthesized and evaluated a focused library of oxazolidinone analogs, a currently narrow spectrum class of antibacterials active only against Gram-pos. bacteria. In this series, we have explored the effectiveness for improving Gram-neg. activity by identifying and combining beneficial structural modifications in the C-ring region. We have found polar and/or charge-carrying modifications that, when combined in hybrid C-ring analogs, appear to largely overcome the efflux and/or permeability barriers, resulting in improved Gram-neg. activity. In particular, those analogs least effected by efflux and the permeation barrier had significant zwitterionic character.

ACS Infectious Diseases published new progress about Antibiotics. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, COA of Formula: C6H5BrN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 870997-85-6, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 870997-85-6, name is 3-Amino-5-bromopyridine-2-carboxylic Acid. This compound has unique chemical properties. The synthetic route is as follows.

Example B5, Step 2. A solution of the starting material (e.g., 7-methoxy-2-oxa-6- azaspiro[3.4]oct-6-ene, 1 equiv) and 3-amino-5-bromopicolinic acid (1.5 equiv) in toluene (0.02 M) was refluxed under nitrogen atmosphere until the reaction was complete. After concentration, the residue was purified by silica gel chromatography to give the desired product (e.g., 6′-bromo-l’H-spiro[oxetane-3,2′-pyrrolo[2,l- 6]quinazolin]-9′(3’H)-one).

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 870997-85-6, 3-Amino-5-bromopyridine-2-carboxylic Acid.

Reference:
Patent; HEFFERNAN, Michele, L., R.; HARDY, Larry, Wendell; WU, Frank, Xinhe; SARASWAT, Lakshmi, D.; SPEAR, Kerry, L.; WO2012/170845; (2012); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 870997-85-6, name is 3-Amino-5-bromopyridine-2-carboxylic Acid, the common compound, a new synthetic route is introduced below. Quality Control of 3-Amino-5-bromopyridine-2-carboxylic Acid

To a 100 mL round bottom flask, 3-amino-5-bromo-pyridine-2-carboxylic acid (1 g, 0.0046 mol) and urea (27.8 g, 0.4629 mol) were added. The reaction mixture was stirred at 200 C. for 2.5 hours. The reaction mixture was cooled, water was added and the mixture was stirred to provide a precipitate. The precipitate was filtered and dried to provide the title compound (1 g, 91%). This material was taken to the next step without further purification.

The synthetic route of 870997-85-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Endo Pharmaceuticals Inc.; Smith, Roger Astbury; Venkatesan, Aranapakam; Bejugam, Mallesham; Hoshalli, Subramanya; Nanduri, Srinivas; US2014/38952; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 870997-85-6, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.870997-85-6, name is 3-Amino-5-bromopyridine-2-carboxylic Acid, molecular formula is C6H5BrN2O2, molecular weight is 217.0201, as common compound, the synthetic route is as follows.

Step 1: 3-Amino-5-(4-trifluoromethoxy-phenylsulfanyl)-pyridine-2-carboxylic acid: [00273] A solution of 3-amino-5-bromo-pyridine-2-carboxylic acid (Int 1, 3.26 g, 15 mmol), 4- trifluoromethoxy-benzenethiol (CAS: 169685-29-4, 3.5 g, 18 mmol) and DBU (2.22 mL, 15 mmol) was prepared in DMA (15 mL). This mixture was heated at 140 C for 45 minutes in a microwave reactor. Next, the mixture was diluted with a mixture of 1% AcOH in water. A suspension was obtained that was subsequently filtered. This collected solid was washed with a 101 ABV12212USO1 1% AcOH/water mixture followed by washing with petroleum ether. After drying in a vacuum oven, the titled compound was obtained

The chemical industry reduces the impact on the environment during synthesis 870997-85-6, I believe this compound will play a more active role in future production and life.

Reference:
Patent; ABBVIE S.A.R.L.; GALAPAGOS NV; ALTENBACH, Robert, J.; COWART, Marlon, D.; DE MUNCK, Tom, Roger Lisette; DROPSIT MONTOVERT, Sebastien Jean, Jacques Cedric; GFESSER, Gregory, A.; KELGTERMANS, Hans; MARTINA, Sebastien, Laurent Xavier; VAN DER PLAS, Steven, Emiel; WANG, Xueqing; (300 pag.)WO2016/193812; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem