cas 455280-00-9, 5-BROMOBENZO[D]ISOXAZOL-3-YLAMINE

Articles about 455280-00-9Total 9 be found

BENZENE FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
The present disclosure provides a benzene fused heterocyclic compound of Formula (I): wherein (A) is a single or double bond; n is 0 or 1; X is -CH2-, O, NR1, or S; A is -C(Ra1)(Ra2)(Ra3) or -N(R
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Paragraph 0280; 0352-0354

(2019/06/17)

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models
We report on a novel series of aryl sulfonamides that act as nanomolar potent, isoform-selective inhibitors of the human sodium channel hNaV1.7. The optimization of these inhibitors is described. We aimed to improve potency against hNaV1.7 while minimizing off-target safety concerns and generated compound 3. This agent displayed significant analgesic effects in rodent models of acute and inflammatory pain and demonstrated that binding to the voltage sensor domain 4 site of NaV1.7 leads to an analgesic effect in vivo. Our findings corroborate the importance of hNaV1.7 as a drug target for the treatment of pain.
Focken, Thilo,Liu, Shifeng,Chahal, Navjot,Dauphinais, Maxim,Grimwood, Michael E.,Chowdhury, Sultan,Hemeon, Ivan,Bichler, Paul,Bogucki, David,Waldbrook, Matthew,Bankar, Girish,Sojo, Luis E.,Young, Clint,Lin, Sophia,Shuart, Noah,Kwan, Rainbow,Pang, Jodie,Chang, Jae H.,Safina, Brian S.,Sutherlin, Daniel P.,Johnson,Dehnhardt, Christoph M.,Mansour, Tarek S.,Oballa, Renata M.,Cohen, Charles J.,Robinette, C. Lee
p. 277 - 282
(2016/03/22)

COMBINATION OF KINASE INHIBITORS AND USES THEREOF
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
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Paragraph 00502

(2014/10/04)

COMBINATION PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
The present invention provides for methods and pharmaceutical compositions for treating proliferative disorders. In one aspect, the method comprises administration of two cell-cycle suppressors having a synergistic effect. In another aspect, two cell-cycle suppressors having a synergistic effect are provided in a pharmaceutical composition.
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Paragraph 0485

(2014/12/09)

Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach
DRAK2 emerged as a promising drug target for the treatment of autoimmune diseases and to prevent graft rejection after organ transplantation. Screening of a compound library in a DRAK2 binding assay led to the identification of an isothiazolo[5,4-b]pyridine derivative as a novel ligand for DRAK2, displaying a Kdvalue of 1.6 μM. Subsequent medicinal chemistry work led to the discovery of a thieno[2,3-b]pyridine derivative with strong DRAK2 binding affinity (Kd= 9 nM). Moreover, this compound also behaves as a functional inhibitor of DRAK2 enzymatic activity, displaying an IC50value of 0.82 μM, although lacking selectivity, when tested against DRAK1. This paper describes for the first time functionally active dual DRAK1 and DRAK2 inhibitors that can be used as starting point for the synthesis of chemical tool compounds to study DRAK1 and DRAK2 biology, or they can be considered as hit compounds for hit-to-lead optimization campaigns in drug discovery programs.
Gao, Ling-Jie,Kovackova, Sona,?ála, Michal,Ramadori, Anna Teresa,De Jonghe, Steven,Herdewijn, Piet
p. 7624 - 7643
(2015/01/08)

HEPATITIS C VIRUS INHIBITORS
This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
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Page/Page column 57-58

(2010/12/26)

BENZOXAZOLE KINASE INHIBITORS AND METHODS OF USE
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
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Page/Page column 134

(2010/05/14)

BENZO(D)ISOXAZOL-3-YL-AMINE COMPOUNDS AND THEIR USE AS VANILLOID RECEPTOR LIGANDS
The substituted benzo(d)isoxazol-3-yl-amine compounds of general formula (I) are suitable for treating pains and have an excellent affinity to vanilloid receptor subtype 1 (VR1/TRPV1 receptor) and are therefore especially useful in the prophylaxis and/or
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Page/Page column 60-61

(2008/06/13)