25083-80-1Relevant academic research and scientific papers
Indanones as high-potency reversible inhibitors of monoamine oxidase
Mostert, Samantha,Petzer, Anél,Petzer, Jacobus P.
, p. 862 - 873 (2015)
Recent reports document that α-tetralone (3,4-dihydro-2H-naphthalen-1-one) is an appropriate scaffold for the design of high-potency monoamine oxidase (MAO) inhibitors. Based on the structural similarity between α-tetralone and 1-indanone, the present stu
Adenosine A2AR/A1R Antagonists Enabling Additional H3R Antagonism for the Treatment of Parkinson’s Disease
Hagenow, Stefanie,Affini, Anna,Pioli, Elsa Y.,Hinz, Sonja,Zhao, Yan,Porras, Gregory,Namasivayam, Vigneshwaran,Müller, Christa E.,Lin, Jian-Sheng,Bezard, Erwan,Stark, Holger
, p. 8246 - 8262 (2021)
Adenosine A1/A2Areceptors (A1R/A2AR) represent targets in nondopaminergic treatment of motor disorders such as Parkinson’s disease (PD). As an innovative strategy, multitargeting ligands (MTLs) were developed to achieve comprehensive PD therapies simultaneously addressing comorbid symptoms such as sleep disruption. Recognizing the wake-promoting capacity of histamine H3receptor (H3R) antagonists in combination with the “caffeine-like effects” of A1R/A2AR antagonists, we designed A1R/A2AR/H3R MTLs, where a piperidino-/pyrrolidino(propyloxy)phenyl H3R pharmacophore was introduced with overlap into an adenosine antagonist arylindenopyrimidine core. These MTLs showed distinct receptor binding profiles with overall nanomolar H3R affinities (Kii(A1R) = 11.5 nM,Ki(A2AR) = 7.25 nM) and 12( ST-1992,Ki(A1R) = 11.2 nM,Ki(A2AR) = 4.01 nM) were evaluatedin vivo.l-DOPA-induced dyskinesia was improved after administration of compound 4(1 mg kg-1, i.p. rats). Compound 12(2 mg kg-1, p.o. mice) increased wakefulness representing novel pharmacological tools for PD therapy.
FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Paragraph 0181-0184, (2021/02/16)
Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
Condensed tricyclic compounds as RAF kinase inhibitors
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Paragraph 0313; 0314; 0315; 0316; 0317; 0318, (2016/10/07)
The invention provides certain condensed tricyclic compounds as well as salt, compositions and application methods thereof.
CONDENSED TRICYCLIC COMPOUNDS AS Raf KINASE INHIBITORS
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Paragraph 0121; 0122, (2017/01/05)
PROBLEM TO BE SOLVED: To provide specific tricyclic compounds that can be useful for inhibiting Raf kinase and for treating disorders mediated by Raf kinase. SOLUTION: A compound is represented by the general formula 1 in the figure. (Q is C or N; W is C or N; X is CH2 or O; Y is NR12, O or S; Z is O, S, NR13, CO, SO, SO2 or CR13R14; R1 to R6 are each independently hydrogen, halogen, haloalkyl, alkyl or the like.) SELECTED DRAWING: None COPYRIGHT: (C)2017,JPO&INPIT
FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Paragraph 0216-0218, (2015/02/25)
Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
SUBSTITUTED HETEROCYCLIC DERIVATIVES AS GPR AGONISTS AND USES THEREOF
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Page/Page column 136; 137, (2015/03/16)
The present invention generally relates to substituted heterocyclic derivatives (the compounds of Formula (I)), processes for their preparation, pharmaceutical compositions containing said compounds, their use as G-protein coupled receptor (GPR) agonists, particularly as GPR40 agonists and methods of using these compounds in the treatment of GPR40 mediated diseases or conditions such as Type 2 diabetes, obesity, dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS
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Page/Page column 34-35, (2013/07/19)
Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
Discovery and optimization of potent GPR40 full agonists containing tricyclic spirocycles
Wang, Yingcai,Liu, Jiwen,Dransfield, Paul J.,Zhu, Liusheng,Wang, Zhongyu,Du, Xiaohui,Jiao, Xianyun,Su, Yongli,Li, An-Rong,Brown, Sean P.,Kasparian, Annie,Vimolratana, Marc,Yu, Ming,Pattaropong, Vatee,Houze, Jonathan B.,Swaminath, Gayathri,Tran, Thanhvien,Nguyen, Khanh,Guo, Qi,Zhang, Jane,Zhuang, Run,Li, Frank,Miao, Lynn,Bartberger, Michael D.,Correll, Tiffany L.,Chow, David,Wong, Simon,Luo, Jian,Lin, Daniel C.-H.,Medina, Julio C.
supporting information, p. 551 - 555 (2013/07/25)
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to its unique mechanism leading to little risk of hypoglycemia. We recently reported the discovery of AM-1638 (2), a potent full agonist of GPR40. In this repor
CONFORMATIONALLY CONSTRAINED CARBOXYLIC ACID DERIVATIVES USEFUL FOR TREATING METABOLIC DISORDERS
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Page/Page column 265; 279, (2009/10/22)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
