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Selective and Combined Neurokinin Receptor Antagonists

Progress in Medicinal Chemistry, 2005, Vol.43, p.49-103

Gerspacher, Marc

2005

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16173-16203

2022

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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Cancer discovery, 2022-06, Vol.12 (6), p.1500-1517

2022

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Design and Biochemical Characterization of Peptidic Inhibitors of the Myb/p300 Interaction

Biochemistry (Easton), 2023-04, Vol.62 (7), p.1321-1329

2023

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The 7 TM G-Protein-Coupled Receptor Target Family

ChemMedChem, 2006-08, Vol.1 (8), p.760-782

2006

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16173-16203

2022

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Discovery of a novel tricyclic 4H-thiazolo[5′,4′:4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3582-3584

2015

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Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805

Molecular cancer therapeutics, 2010-07, Vol.9 (7), p.1945-1955

2010

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Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (6), p.1858-1860

2010

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Stereoselective Preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a Potent and Orally Active Dual Neurokinin NK1/NK2 Receptor Antagonist

Journal of medicinal chemistry, 2003-07, Vol.46 (16), p.3508-3513

2003

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Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3569-3574

2015

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Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3575-3581

2015

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Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.4026-4026

2022

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1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: A Novel Series of Potent Calcium-Sensing Receptor Antagonists

Journal of medicinal chemistry, 2010-03, Vol.53 (5), p.2250-2263

2010

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Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (8), p.2609-2613

2010

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Synthesis and sar of a novel, potent and structurally simple LTD4 antagonist of the quinoline class

Bioorganic & medicinal chemistry letters, 1998-04, Vol.8 (8), p.965-970

1998

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2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1724-1727

2010

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Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists)

Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.5161-5164

2010

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Novel, Potent and Selective JAK2 Inhibitors

Blood, 2009-11, Vol.114 (22), p.3777-3777

2009

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1-Alkyl-4-phenyl-6-alkoxy-1 H -quinazolin-2-ones: A Novel Series of Potent Calcium-Sensing Receptor Antagonists

Journal of medicinal chemistry, 2010-03, Vol.53 (5), p.2250-2263

2010

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The 7 TM G-protein-coupled receptor target family

ChemMedChem, 2006-08, Vol.1 (8), p.761-782

2006

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2-Amino-2-deoxyhexoses as chiral educts for hydroxylated indolizidines. Synthesis of (+)-castanospermine and (+)-6-epicastanospermine

Journal of organic chemistry, 1991-05, Vol.56 (11), p.3700-3706

1991

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Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists

Bioorganic & medicinal chemistry letters, 2004-05, Vol.14 (10), p.2451-2457

2004

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C45 und C50-Carotinoide. 6. Mitteilung. Synthese eines optisch aktiven cyclischen C20-Bausteins und von Decaprenoxanthin (= (2R, 6R, 2′R, 6′R)-2,2′-Bis(4-hydroxy-3-methylbut-2-enyl)-ϵ, ϵ-carotin)

Helvetica chimica acta, 1989-02, Vol.72 (1), p.151-157

1989

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Selective and Combined Neurokinin Receptor Antagonists

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Design and Biochemical Characterization of Peptidic Inhibitors of the Myb/p300 Interaction

The 7 TM G-Protein-Coupled Receptor Target Family

Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors

Discovery of a novel tricyclic 4H-thiazolo[5′,4′:4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805

Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing

Stereoselective Preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a Potent and Orally Active Dual Neurokinin NK1/NK2 Receptor Antagonist

Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6

1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: A Novel Series of Potent Calcium-Sensing Receptor Antagonists

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

Synthesis and sar of a novel, potent and structurally simple LTD4 antagonist of the quinoline class

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists)

Novel, Potent and Selective JAK2 Inhibitors

1-Alkyl-4-phenyl-6-alkoxy-1 H -quinazolin-2-ones: A Novel Series of Potent Calcium-Sensing Receptor Antagonists

The 7 TM G-protein-coupled receptor target family

2-Amino-2-deoxyhexoses as chiral educts for hydroxylated indolizidines. Synthesis of (+)-castanospermine and (+)-6-epicastanospermine

Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists

C45 und C50-Carotinoide. 6. Mitteilung. Synthese eines optisch aktiven cyclischen C20-Bausteins und von Decaprenoxanthin (= (2R, 6R, 2′R, 6′R)-2,2′-Bis(4-hydroxy-3-methylbut-2-enyl)-ϵ, ϵ-carotin)

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