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Items: 16

1.

(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase.

Rageot D, Bohnacker T, Keles E, McPhail JA, Hoffmann RM, Melone A, Borsari C, Sriramaratnam R, Sele AM, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Burke JE, Wymann MP.

J Med Chem. 2019 Jul 11;62(13):6241-6261. doi: 10.1021/acs.jmedchem.9b00525. Epub 2019 Jun 20.

PMID:
31244112
2.

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.

Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Löscher W, Burke J, Fabbro D, Wymann MP.

J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14.

PMID:
30359003
3.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP.

J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1.

4.

6-Alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds.

Röver S, Andjelkovic M, Bénardeau A, Chaput E, Guba W, Hebeisen P, Mohr S, Nettekoven M, Obst U, Richter WF, Ullmer C, Waldmeier P, Wright MB.

J Med Chem. 2013 Dec 27;56(24):9874-96. doi: 10.1021/jm4010708. Epub 2013 Nov 20.

PMID:
24175572
5.

Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase.

Hebeisen P, Haap W, Kuhn B, Mohr P, Wessel HP, Zutter U, Kirchner S, Ruf A, Benz J, Joseph C, Alvarez-Sánchez R, Gubler M, Schott B, Benardeau A, Tozzo E, Kitas E.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3237-42. doi: 10.1016/j.bmcl.2011.04.044. Epub 2011 Apr 20.

PMID:
21550236
6.

A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.

Angehrn P, Goetschi E, Gmuender H, Hebeisen P, Hennig M, Kuhn B, Luebbers T, Reindl P, Ricklin F, Schmitt-Hoffmann A.

J Med Chem. 2011 Apr 14;54(7):2207-24. doi: 10.1021/jm1014023. Epub 2011 Mar 9.

PMID:
21388139
7.

Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes.

Byrne SJ, Fletcher AJ, Hebeisen P, Willis MC.

Org Biomol Chem. 2010 Feb 21;8(4):758-60. doi: 10.1039/b923186b. Epub 2009 Dec 21.

PMID:
20135030
8.

Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.

Kitas E, Mohr P, Kuhn B, Hebeisen P, Wessel HP, Haap W, Ruf A, Benz J, Joseph C, Huber W, Sanchez RA, Paehler A, Benardeau A, Gubler M, Schott B, Tozzo E.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):594-9. doi: 10.1016/j.bmcl.2009.11.093. Epub 2009 Nov 22.

PMID:
19969452
9.

Allosteric FBPase inhibitors gain 10(5) times in potency when simultaneously binding two neighboring AMP sites.

Hebeisen P, Kuhn B, Kohler P, Gubler M, Huber W, Kitas E, Schott B, Benz J, Joseph C, Ruf A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4708-12. doi: 10.1016/j.bmcl.2008.06.103. Epub 2008 Jul 5.

PMID:
18650089
10.

Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.

Richter HG, Adams DR, Benardeau A, Bickerdike MJ, Bentley JM, Blench TJ, Cliffe IA, Dourish C, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Monck NJ, Plancher JM, Roever S, Roffey JR, Taylor S, Vickers SP.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1207-11. Epub 2005 Dec 19.

PMID:
16361098
11.

Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.

Röver S, Adams DR, Bénardeau A, Bentley JM, Bickerdike MJ, Bourson A, Cliffe IA, Coassolo P, Davidson JE, Dourish CT, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Muller M, Porter RH, Richter H, Taylor S, Vickers SP.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3604-8.

PMID:
15975787
12.

New antibacterial agents derived from the DNA gyrase inhibitor cyclothialidine.

Angehrn P, Buchmann S, Funk C, Goetschi E, Gmuender H, Hebeisen P, Kostrewa D, Link H, Luebbers T, Masciadri R, Nielsen J, Reindl P, Ricklin F, Schmitt-Hoffmann A, Theil FP.

J Med Chem. 2004 Mar 11;47(6):1487-513.

PMID:
14998336
13.

New anti-MRSA and anti-VRE carbapenems; synthesis and structure-activity relationships of 1beta-methyl-2-(thiazol-2-ylthio)carbapenems.

Sunagawa M, Itoh M, Kubota K, Sasaki A, Ueda Y, Angehrn P, Bourson A, Goetschi E, Hebeisen P, Then RL.

J Antibiot (Tokyo). 2002 Aug;55(8):722-57.

14.

In vitro and in vivo properties of Ro 63-9141, a novel broad-spectrum cephalosporin with activity against methicillin-resistant staphylococci.

Hebeisen P, Heinze-Krauss I, Angehrn P, Hohl P, Page MG, Then RL.

Antimicrob Agents Chemother. 2001 Mar;45(3):825-36.

15.

Synthesis and structure-activity relationship of (lactamylvinyl)cephalosporins exhibiting activity against staphylococci, pneumococci, and enterococci.

Heinze-Krauss I, Angehrn P, Guerry P, Hebeisen P, Hubschwerlen C, Kompis I, Page MG, Richter HG, Runtz V, Stalder H, Weiss U, Wei CC.

J Med Chem. 1996 Apr 26;39(9):1864-71.

PMID:
8627610
16.

Cyclothialidine and its congeners: a new class of DNA gyrase inhibitors.

Goetschi E, Angehrn P, Gmuender H, Hebeisen P, Link H, Masciadri R, Nielsen J.

Pharmacol Ther. 1993 Nov;60(2):367-80. Review.

PMID:
8022866

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