147808-42-2Relevant academic research and scientific papers
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a ]quinoxalines
Wagner, Sally,Scheunemann, Matthias,Dipper, Karolin,Egerland, Ute,Hoefgen, Norbert,Steinbach, J?rg,Brust, Peter
, p. 97 - 108 (2016)
Herein we report the synthesis of fluorinated inhibitors of phosphodiesterase 10A (PDE10A) which can be used potentially as lead structure for the development of a 18F-labeled PDE10A imaging agent for positron emission tomography. The use of or
Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
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Page/Page column 51; 52, (2017/01/09)
The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, a
NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 0421-0422, (2015/07/27)
The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, a
BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 00237, (2015/08/06)
The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I),
Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: Structure-based design and in vivo reduction of amyloid β-peptides
Rueeger, Heinrich,Lueoend, Rainer,Rogel, Olivier,Rondeau, Jean-Michel,M?bitz, Henrik,MacHauer, Rainer,Jacobson, Laura,Staufenbiel, Matthias,Desrayaud, Sandrine,Neumann, Ulf
experimental part, p. 3364 - 3386 (2012/06/01)
Structure-based design of a series of cyclic hydroxyethylamine BACE1 inhibitors allowed the rational incorporation of prime- and nonprime-side fragments to a central core template without any amide functionality. The core scaffold selection and the structure-activity relationship development were supported by molecular modeling studies and by X-ray analysis of BACE1 complexes with various ligands to expedite the optimization of the series. The direct extension from P1-aryl- and heteroaryl moieties into the S3 binding pocket allowed the enhancement of potency and selectivity over cathepsin D. Restraining the design and synthesis of compounds to a physicochemical property space consistent with central nervous system drugs led to inhibitors with improved blood-brain barrier permeability. Guided by structure-based optimization, we were able to obtain highly potent compounds such as 60p with enzymatic and cellular IC50 values of 2 and 50 nM, respectively, and with >200-fold selectivity over cathepsin D. Pharmacodynamic studies in APP51/16 transgenic mice at oral doses of 180 μmol/kg demonstrated significant reduction of brain Aβ levels.
TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 75, (2012/10/07)
The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.
TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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Page/Page column 94, (2012/10/07)
The present invention discloses tetracyclic xanthene derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b, and R2 are as defined herein. The present invention also discloses compositions comprising at least one tetracyclic xanthene derivative, and methods of using the tetracyclic xanthene derivatives for treating or preventing HCV infection in a patient.
NOVEL BICYCLIC HETEROCYCLIC COMPOUND
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Page/Page column 75, (2011/11/07)
The present invention aims to provide a drug for the treatment or prophylaxis of pathology in general in which SNS is involved, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like. The present inventi
BENZO[d]OXAZOLES AND BENZO[d]THIAZOLES AS KINASE INHIBITORS
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Page/Page column 96, (2010/04/06)
Novel benzo[d]oxazole and/or benzo[d]thiazole compounds, pharmaceutical compositions containing the benzo[d]oxazole and/or benzo[d]thiazole compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the benzo[d]oxazole and/o
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors
Yin, Yan,Lin, Li,Ruiz, Claudia,Cameron, Michael D.,Pocas, Jennifer,Grant, Wayne,Schroeter, Thomas,Chen, Weimin,Duckett, Derek,Schuerer, Stephan,LoGrasso, Philip,Feng, Yangbo
scheme or table, p. 6686 - 6690 (2010/06/14)
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.
