cas 89717-64-6, 4-Bromo-3-nitro pyrazole | Articles data

Articles about 89717-64-6Total 8 be found

Article title
Article abstract
Author
Journal number and time
Download

N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT
N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.
-
Page/Page column 32

(2021/04/10)

AZETIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention relates to an azetidine derivative for use as a Janus kinase (JAK) inhibitor, a drug composition comprising same, a preparation method therefor, and a use thereof in the treatment of JAK-related diseases comprising, for example, infl
-
Paragraph 0327; 0328

(2018/08/29)

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7
A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cytochrome P450 inhibition driven drug-drug interaction concerns to deliver the desired balance of preclinical in vitro properties. Concerns over nonmetabolic routes of clearance, variable clearance in preclinical species, and subsequent low confidence human pharmacokinetic predictions led to the decision to conduct a human microdose study to determine clinical pharmacokinetics. The design strategies and results from preclinical PK and clinical human microdose PK data are described leading to the discovery of the first subtype selective NaV1.7 inhibitor clinical candidate PF-05089771 (34) which binds to a site in the voltage sensing domain.
Swain, Nigel. A.,Batchelor, Dave,Beaudoin, Serge,Bechle, Bruce M.,Bradley, Paul A.,Brown, Alan D.,Brown, Bruce,Butcher, Ken J.,Butt, Richard P.,Chapman, Mark L.,Denton, Stephen,Ellis, David,Galan, Sebastien R. G.,Gaulier, Steven M.,Greener, Ben S.,De Groot, Marcel J.,Glossop, Mel S.,Gurrell, Ian K.,Hannam, Jo,Johnson, Matthew S.,Lin, Zhixin,Markworth, Christopher J.,Marron, Brian E.,Millan, David S.,Nakagawa, Shoko,Pike, Andy,Printzenhoff, David,Rawson, David J.,Ransley, Sarah J.,Reister, Steven M.,Sasaki, Kosuke,Storer, R. Ian,Stupple, Paul A.,West, Christopher W.
supporting information
p. 7029 - 7042
(2017/09/07)

Benzyl-1H-pyrazole and benzyl-1H-pyrazole derivatives, and preparation method and application thereof
The invention belongs to the field of chemical medicine, and particularly relates to benzyl-1H-pyrazole and benzyl-1H-pyrazole derivatives, and a preparation method and application thereof. The structure of the benzyl-1H-pyrazole and benzyl-1H-pyrazole de
-
Paragraph 0057; 0058; 0059; 0060; 0061; 0062; 0063; 0064

(2016/10/09)

Design, Synthesis, and Biological Evaluation of 1-Benzyl-1H-pyrazole Derivatives as Receptor Interacting Protein 1 Kinase Inhibitors
Receptor interacting protein 1 (RIP1) kinase plays an important role in necroptosis, and inhibitors of the RIP1 kinase are thought to have a potential therapeutic value in the treatment of diseases related to necrosis. Herein, we report the structural optimization of a RIP1 kinase inhibitor, 1-(2,4-dichlorobenzyl)-3-nitro-1H-pyrazole (1a). A number of 1-benzyl-1H-pyrazole derivatives were synthesized and structure-activity relationship (SAR) analysis led to the discovery of a potent compound, 4b, which showed a Kd value of 0.078 μm against the RIP1 kinase and an EC50 value of 0.160 μm in a cell necroptosis inhibitory assay. Compound 4b also displayed considerable ability to protect the pancreas in an l-arginine-induced pancreatitis mouse model.
Zou, Chan,Xiong, Yu,Huang, Lu-Yi,Song, Chun-Li,Wu, Xiao-Ai,Li, Lin-Li,Yang, Sheng-Yong
p. 569 - 574
(2016/03/19)

NITROGENOUS FUSED?RING COMPOUND HAVING PYRAZOLYL GROUP AS SUBSTITUENT AND MEDICINAL COMPOSITION THEREOF
The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R4)n as substituent groups; Y represents a C3-8 cycloalkyl group, C4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R4)n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C2-6 alkenyl group, (14) C1-6 alkoxy group, (15) C1-6 alkylhydroxyamino group, (16) halogenated C1-6 alkyl group, (17) halogenated C2-6 alkenyl group, (18) (i) C3-7cycloalkyl group, (ii) C3-7cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M1-M2-M3, R1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C1-6 alkyl group, (7) C2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C2-6 alkenyl group, or (9) formula -L1-L2-L3, and R2 represents a hydrogen atom or a protecting group; and R3 represents a hydrogen atom, halogen atom, cyano group, amino group, C1-4 alkyl group or halogenated C1-4 alkyl group.
-
Page 195; 196

(2008/06/13)

Nitropyrazoles 5. Synthesis of substituted 3-nitropyrazoles from 3-amino-4-cyanopyrazole
A preparative method of synthesis of 3-nitro-4-cyanopyrazole (1) from the available 3-amino-4-cyanopyrazole was developed.Chemical conversions of 1 were studied, and 3-nitro-4-R-pyrazoles (R = CO2H, CONH2, NHCO2Me, NH2, Br, NO2), as well as 3,5-dinitro-4-methoxycarbonylaminopyrazole were obtained starting from 1.
Vinogradov, V. M.,Cherkasova, T. I.,Dalinger, I. L.,Shevelev, S. A.
p. 1552 - 1554
(2007/10/02)

Cyclic Meso-ionic Compounds. Part 21. The Examination of Nitro-derivatives of Meso-ionic Heterocycles as Potential Pharmaceuticals
The synthesis of nitro-substituted meso-ionic compounds has been examined in an attempt to obtain analogues of the biologically active heterocycles (1)-(3).The synthesis of the compounds (4) and (5) has been achieved but their instability precluded biological evaluation.The synthesis of the type-B meso-ionic heterocycle (6) was not successfully completed, but unusual nucleophilic displacement reactions of the pyrazole (13) -> (16) + (17) and the pyrazolium salt (14) -> (15) are reported.
Newton, Christopher G.,Ollis, W. David,Podmore, Michael L.,Wright, Derek E.
p. 63 - 67
(2007/10/02)