69722-29-8Relevant academic research and scientific papers
1,2,4-Oxadiazole ring–containing pyridylpyrazole-4-carboxamides: Synthesis and evaluation as novel insecticides of the anthranilic diamide family
Khallaf, Abdalla,Liu, Hui,Wang, Ping,Zhu, Hongjun,Zhuo, Shuping
, (2020/02/18)
Herein, we describe the preparation of pyridylpyrazole-4-carboxamides containing a 1,2,4-oxadiazole ring as novel anthranilic diamide derivatives and compare their insecticidal activities to that of chlorantraniliprole, a well-established potent insectici
Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists
Katte, Timothy A.,Reekie, Tristan A.,Werry, Eryn L.,Jorgensen, William T.,Boyd, Rochelle,Wong, Erick C.N.,Gulliver, Damien W.,Connor, Mark,Kassiou, Michael
, p. 330 - 333 (2017/06/09)
The neuropeptide oxytocin has been implicated in multiple central nervous system functions in mammalian species. Increased levels have been reported to improve trust, alleviate symptoms related to autism and social phobias, and reduce social anxiety. Hoffman-La Roche published a patent claiming to have found potent small molecule oxytocin receptor agonists, smaller than the first non-peptide oxytocin agonist reported, WAY 267,464. We selected two of the more potent compounds from the patent and, in addition, created WAY 267,464 hybrid structures and determined their oxytocin and vasopressin receptor activity. Human embryonic kidney and Chinese hamster ovary cells were used for the expression of oxytocin or vasopressin 1a receptors and activity assessed via IP1 accumulation assays and calcium FLIPR assays. The results concluded that the reported compounds in the patent and the hybrid structures have no activity at the oxytocin or vasopressin 1a receptors.
5-Amino-pyrazoles as potent and selective p38α inhibitors
Das, Jagabandhu,Moquin, Robert V.,Dyckman, Alaric J.,Li, Tianle,Pitt, Sidney,Zhang, Rosemary,Shen, Ding Ren,McIntyre, Kim W.,Gillooly, Kathleen,Doweyko, Arthur M.,Newitt, John A.,Sack, John S.,Zhang, Hongjian,Kiefer, Susan E.,Kish, Kevin,McKinnon, Murray,Barrish, Joel C.,Dodd, John H.,Schieven, Gary L.,Leftheris, Katerina
scheme or table, p. 6886 - 6889 (2011/02/22)
The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on a 5-amino-pyrazole scaffold are described. These studies led to the identification of compound 2j as a potent and selective inhibitor of p38α MAP kinase with excellent cellular potency toward the inhibition of TNFα production. Compound 2j was highly efficacious in vivo in inhibiting TNFα production in an acute murine model of TNFα production. X-ray co-crystallography of a 5-amino-pyrazole analog 2f bound to unphosphorylated p38α is also disclosed.
Pyrazolobenzotriazinone derivatives as COX inhibitors: Synthesis, biological activity, and molecular-modeling studies
Raffa, Demetrio,Migliara, Onofrio,Maggio, Benedetta,Plescia, Fabiana,Cascioferro, Stella,Cusimano, Maria Grazia,Tringali, Giuseppe,Cannizzaro, Carla,Plescia, Fulvio
experimental part, p. 631 - 638 (2011/09/15)
Pyrazolylbenzotriazinones are endowed with a structural analogy with the COX-2 selective inhibitor celecoxib. Considering that our research group has long been interested in the 3-pyrazolyl-substituted benzotriazinones as anti-inflammatory agents, six new
PYRAZOLE-I, 2, 4 -OXAD IAZOLE DERIVATIVES AS S.PHING0SINE-1-PH0SPHATE AGONISTS
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Page/Page column 45-46, (2010/08/08)
Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY
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Page/Page column 137, (2008/06/13)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
HSP INDUCTOR
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, (2008/06/13)
An agent for inducing HSP, comprising a compound represented by the formula (I): ???wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, etc.; R2 is absent, a hydrogen atom or a hydrocarbon group which maybe substituted; R3 is a heterocyclic group which may be substituted; X, Y and Z are, respectively, a hydrogen, a halogen, a nitrile, a hydrocarbon group which may be substituted, or X and Y may bind to each other to form ring A, or Y and Z may bind to each other to form ring B; bond portions indicated by a solid line and a broken line are, respectively, a single bond or a double bond, and bond portions indicated by a broken line are, respectively, a single bond or absent; ring A is a homocyclic or heterocyclic 5- to 7-membered ring which may be substituted; ring B is a homocyclic or heterocyclic 5- to 7-membered ring which may be substituted; and n is an integer of 0 or 1, or a salt thereof;
Condensed pyrazole derivatives, process for producing the same and use thereof
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, (2008/06/13)
Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.
Herbicidal pyrazolesulfonamides
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, (2008/06/13)
This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.
