Výsledky vyhledávání - "Rombouts FJR"

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Akademický článek

Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.

Autor: Demin S; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Peschiulli A; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Velter AI; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Vos A; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., De Boeck B; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Miller B; Janssen Research & Development LLC, 1400 McKean Road (Welsh Road), Spring House, Pennsylvania 19477, United States., Rombouts FJR; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Reuillon T; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Lento W; Janssen Research & Development LLC, 1400 McKean Road (Welsh Road), Spring House, Pennsylvania 19477, United States., Blanco MD; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Jouffroy M; Chemical Process R&D, Discovery Process Research, Janssen Pharmaceutica N.V., Beerse B-2340, Belgium., Steyvers H; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Bekkers M; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Altrocchi C; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Pietrak B; Janssen Research & Development LLC, 1400 McKean Road (Welsh Road), Spring House, Pennsylvania 19477, United States., Koo SJ; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium., Szewczuk L; Janssen Research & Development LLC, 1400 McKean Road (Welsh Road), Spring House, Pennsylvania 19477, United States., Attar R; Janssen Research & Development LLC, 1400 McKean Road (Welsh Road), Spring House, Pennsylvania 19477, United States., Philippar U; Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse B-2340, Belgium.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2023 Jul 03; Vol. 14 (7), pp. 955-961. Date of Electronic Publication: 2023 Jul 03 (Print Publication: 2023).

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Vybrat výsledek číslo 2 2

Akademický článek

Discovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein-Protein Interaction Modulator with the Potential of Treating Hematological Malignancies.

Autor: Romanov-Michailidis F; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Hsiao CC; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Urner LM; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Jerhaoui S; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Surkyn M; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Miller B; Janssen Research & Development LLC, 1400 McKean Road, Spring House, Pennsylvania 19477, United States., Vos A; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Dominguez Blanco M; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Bueters R; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Vinken P; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Bekkers M; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Walker D; Janssen Research & Development LLC, 1400 McKean Road, Spring House, Pennsylvania 19477, United States., Pietrak B; Janssen Research & Development LLC, 1400 McKean Road, Spring House, Pennsylvania 19477, United States., Eyckmans W; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Dores-Sousa JL; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Joo Koo S; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Lento W; Janssen Research & Development LLC, 1400 McKean Road, Spring House, Pennsylvania 19477, United States., Bauser M; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Philippar U; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium., Rombouts FJR; Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 May 11; Vol. 66 (9), pp. 6122-6148. Date of Electronic Publication: 2023 Apr 28.

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Vybrat výsledek číslo 3 3

Akademický článek

Modulating physicochemical properties of tetrahydropyridine-2-amine BACE1 inhibitors with electron-withdrawing groups: A systematic study.

Autor: Rombouts FJR; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium. Electronic address: frombout@its.jnj.com., Hsiao CC; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Bache S; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., De Cleyn M; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Heckmann P; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Leenaerts J; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Martinéz-Lamenca C; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Van Brandt S; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Peschiulli A; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Vos A; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium., Gijsen HJM; Janssen Research & Development, Turnhoutseweg 30, B-2340, Beerse, Belgium.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2022 Jan 15; Vol. 228, pp. 114028. Date of Electronic Publication: 2021 Dec 01.

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Vybrat výsledek číslo 4 4

Akademický článek

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.

Autor: Peschiulli A; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Oehlrich D; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Van Gool M; Discovery Chemistry, Discovery Sciences, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain., Austin N; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Van Brandt S; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Surkyn M; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., De Cleyn M; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Vos A; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Tresadern G; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Rombouts FJR; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Macdonald GJ; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Moechars D; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium., Trabanco AA; Discovery Chemistry, Discovery Sciences, Janssen Research & Development, Janssen-Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain., Gijsen HJM; Discovery Chemistry, Discovery Sciences, DMPK, Discovery Sciences, and Neuroscience Biology, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2021 Dec 01; Vol. 13 (1), pp. 76-83. Date of Electronic Publication: 2021 Dec 01 (Print Publication: 2022).

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Vybrat výsledek číslo 5 5

Akademický článek

Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.

Autor: Ueno T; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Matsuoka E; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Asada N; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Yamamoto S; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Kanegawa N; Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Ito M; Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Ito H; Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Moechars D; Neuroscience, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Rombouts FJR; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Gijsen HJM; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Kusakabe KI; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Oct 14; Vol. 64 (19), pp. 14165-14174. Date of Electronic Publication: 2021 Sep 23.

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Vybrat výsledek číslo 6 6

Akademický článek

JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.

Autor: Rombouts FJR; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Kusakabe KI; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Alexander R; Janssen Research & Development, Welsh & McKean Roads, Spring House, Pennsylvania 19477, United States., Austin N; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Borghys H; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., De Cleyn M; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Dhuyvetter D; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Gijsen HJM; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Hrupka B; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Jacobs T; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Jerhaoui S; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Lammens L; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Leclercq L; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Tsubone K; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Ueno T; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Morimoto K; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Einaru S; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Sumiyoshi H; Shionogi Pharmaceutical Research Center, Ltd., 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Van den Bergh A; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Vos A; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Surkyn M; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Teisman A; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium., Moechars D; Janssen Research & Development, Janssen Pharmaceutica N. V., Turnhoutseweg 30, Beerse B-2340, Belgium.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Oct 14; Vol. 64 (19), pp. 14175-14191. Date of Electronic Publication: 2021 Sep 23.

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Vybrat výsledek číslo 7 7

Fragment Binding to beta-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches

Autor: Rombouts, FJR, Alexander, R, Cleiren, E, De Groot, A, Carpentier, M, Dijkmans, J, Fierens, K, Masure, S, Moechars, D, Palomino-Schatzlein, M, Pineda-Lucena, A, Trabanco, AA, Van Glabbeek, D, Vos, A, Tresadern, G

Publikováno v: Acs Omega
r-CIPF: Repositorio Institucional Producción Científica del Centro de Investigación Principe Felipe (CIPF)
Centro de Investigación Principe Felipe (CIPF)
r-CIPF. Repositorio Institucional Producción Científica del Centro de Investigación Principe Felipe (CIPF)
instname
r-IIS La Fe. Repositorio Institucional de Producción Científica del Instituto de Investigación Sanitaria La Fe

An approach to identify beta-secretase 1 (BACE1) fragment binders that do not interact with the catalytic aspartate dyad is presented. A ThermoFluor (thermal shift) and a fluorescence resonance energy transfer enzymatic screen on the soluble domain o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::28843c2cb087ea2e2c8990bfa690bfe3
https://fundanet.cipf.es/Publicaciones/ProdCientif/PublicacionFrw.aspx?id=1360

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Vybrat výsledek číslo 8 8

Akademický článek

Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2.

Autor: Fujimoto K; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Yoshida S; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Tadano G; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Asada N; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Fuchino K; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Suzuki S; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Matsuoka E; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Yamamoto T; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Yamamoto S; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Ando S; Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Kanegawa N; Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Tonomura Y; Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Ito H; Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan., Moechars D; Neuroscience, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Rombouts FJR; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Gijsen HJM; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Kusakabe KI; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Mar 25; Vol. 64 (6), pp. 3075-3085. Date of Electronic Publication: 2021 Mar 15.

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Vybrat výsledek číslo 9 9

Akademický článek

Clinical evaluation of [ ¹⁸ F] JNJ-64326067, a novel candidate PET tracer for the detection of tau pathology in Alzheimer's disease.

Autor: Schmidt ME; Janssen Research & Development, Janssen Pharmaceutica NV, Beerse, Belgium. mschmid4@its.jnj.com., Janssens L; Janssen Research & Development, Janssen Pharmaceutica NV, Beerse, Belgium., Moechars D; Janssen Research & Development, Janssen Pharmaceutica NV, Beerse, Belgium., Rombouts FJR; Janssen Research & Development, Janssen Pharmaceutica NV, Beerse, Belgium., Timmers M; Janssen Research & Development, Janssen Pharmaceutica NV, Beerse, Belgium., Barret O; Invicro, a Konica Minolta company, New Haven, CT, USA.; Laboratory of Neurodegenerative Diseases, Molecular Imaging Research Center, French Atomic Energy Commission, Fontenay-aux-roses, France., Constantinescu CC; Invicro, a Konica Minolta company, New Haven, CT, USA., Madonia J; Invicro, a Konica Minolta company, New Haven, CT, USA.; Biohaven Pharmaceuticals, New Haven, Connecticut, USA., Russell DS; Invicro, a Konica Minolta company, New Haven, CT, USA., Sandiego CM; Invicro, a Konica Minolta company, New Haven, CT, USA., Kolb H; Janssen Research & Development, La Jolla, CA, USA.

Publikováno v: European journal of nuclear medicine and molecular imaging [Eur J Nucl Med Mol Imaging] 2020 Dec; Vol. 47 (13), pp. 3176-3185. Date of Electronic Publication: 2020 Jun 13.

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Vybrat výsledek číslo 10 10

Correction to Discovery of N -(4-[ ¹⁸ F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer.