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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Journal of medicinal chemistry, 2022-02, Vol.65 (3), p.1770-1785

2022

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Efficient Synthesis of 2-Aryl-6-chloronicotinamides via PXPd2-Catalyzed Regioselective Suzuki Coupling

Organic letters, 2003-08, Vol.5 (17), p.3131-3134

2003

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Methyl-2,2-difluoro-2-(fluorosulfonyl) acetate (MDFA)/copper (I) iodide mediated and tetrabutylammonium iodide promoted trifluoromethylation of 1-aryl-4-iodo-1,2,3-triazoles

Journal of fluorine chemistry, 2020-08, Vol.236, p.109516, Article 109516

2020

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Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species

Journal of medicinal chemistry, 2020-07, Vol.63 (13), p.7226-7242

2020

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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

Journal of medicinal chemistry, 2017-02, Vol.60 (3), p.1060-1075

2017

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Macrocyclic factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2017-09, Vol.27 (17), p.4056-4060

2017

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Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

Bioorganic & medicinal chemistry letters, 2019-10, Vol.29 (19), p.126604-126604, Article 126604

2019

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Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.9915-9932

2014

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Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa

Bioorganic & medicinal chemistry letters, 2020-02, Vol.30 (4), p.126949, Article 126949

2020

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Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (16), p.3833-3839

2017

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Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (10), p.2257-2272

2016

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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (7), p.1635-1642

2015

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Novel phenylalanine derived diamides as Factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (2), p.472-478

2016

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Pyridine and pyridinone-based factor XIa inhibitors

Bioorganic & medicinal chemistry letters, 2015-02, Vol.25 (4), p.925-930

2015

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Synthesis and Characterization of 3-Arylquinazolinone and 3-Arylquinazolinethione Derivatives as Selective Estrogen Receptor Beta Modulators

Journal of medicinal chemistry, 2006-04, Vol.49 (8), p.2440-2455

2006

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Characterization of a new class of selective nonsteroidal progesterone receptor agonists

Steroids, 2004-03, Vol.69 (3), p.201-217

2004

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Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

Bioorganic & medicinal chemistry letters, 2008-05, Vol.18 (9), p.2845-2849

2008

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Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists

Bioorganic & medicinal chemistry letters, 2005-12, Vol.15 (24), p.5478-5482

2005

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Towards the Total Synthesis of Saponaceolides: Synthesis ofcis-2,4-Disubstituted 3,3-Dimethylmethylenecyclohexanes

Angewandte Chemie International Edition, 1999-12, Vol.38 (24), p.3662-3664

1999

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Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (10)

2016

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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (7)

2015

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Towards the Total Synthesis of Saponaceolides: Synthesis of cis-2,4-Disubstituted 3,3-Dimethylmethylenecyclohexanes

Angewandte Chemie International Edition, 1999-12, Vol.38 (24), p.3662-3664

1999

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Total Synthesis of (+)-Saponaceolide B

Angewandte Chemie International Edition, 1999-12, Vol.38 (24), p.3664-3666

1999

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Totalsynthese von (+)-Saponaceolid B

Angewandte Chemie, 1999-12, Vol.111 (24), p.3947-3949

1999

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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Efficient Synthesis of 2-Aryl-6-chloronicotinamides via PXPd2-Catalyzed Regioselective Suzuki Coupling

Methyl-2,2-difluoro-2-(fluorosulfonyl) acetate (MDFA)/copper (I) iodide mediated and tetrabutylammonium iodide promoted trifluoromethylation of 1-aryl-4-iodo-1,2,3-triazoles

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

Macrocyclic factor XIa inhibitors

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Novel phenylalanine derived diamides as Factor XIa inhibitors

Pyridine and pyridinone-based factor XIa inhibitors

Synthesis and Characterization of 3-Arylquinazolinone and 3-Arylquinazolinethione Derivatives as Selective Estrogen Receptor Beta Modulators

Characterization of a new class of selective nonsteroidal progesterone receptor agonists

Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists

Towards the Total Synthesis of Saponaceolides: Synthesis ofcis-2,4-Disubstituted 3,3-Dimethylmethylenecyclohexanes

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

Towards the Total Synthesis of Saponaceolides: Synthesis of cis-2,4-Disubstituted 3,3-Dimethylmethylenecyclohexanes

Total Synthesis of (+)-Saponaceolide B

Totalsynthese von (+)-Saponaceolid B

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