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  1. Article ; Online: Ligand-Accelerated Stereoretentive Suzuki-Miyaura Coupling of Unprotected 3,3'-Dibromo-BINOL.

    Qu, Bo / Haddad, Nizar / Rodriguez, Sonia / Sieber, Joshua D / Desrosiers, Jean-Nicolas / Patel, Nitinchandra D / Zhang, Yongda / Grinberg, Nelu / Lee, Heewon / Ma, Shengli / Ries, Uwe Jörg / Yee, Nathan K / Senanayake, Chris H

    The Journal of organic chemistry

    2016  Volume 81, Issue 3, Page(s) 745–750

    Abstract: An efficient synthesis of the enantiomerically pure 3,3'-bis-arylated BINOL derivatives is accomplished through the palladium-catalyzed Suzuki-Miyaura coupling of the unprotected 3,3'-dibromo-BINOL with complete retention of enantiopurity. The active ... ...

    Abstract An efficient synthesis of the enantiomerically pure 3,3'-bis-arylated BINOL derivatives is accomplished through the palladium-catalyzed Suzuki-Miyaura coupling of the unprotected 3,3'-dibromo-BINOL with complete retention of enantiopurity. The active catalyst system Pd(OAc)2/BI-DIME has enabled mild reaction conditions at palladium loads as low as 500 ppm.
    Language English
    Publishing date 2016-02-05
    Publishing country United States
    Document type Journal Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.5b02368
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Book ; Thesis: Alkylphosphonate als neue Antitumormittel

    Ries, Uwe Jörg

    1989  

    Language Undetermined
    Size 195 S, graph. Darst, 21 cm
    Document type Book ; Thesis
    Thesis / German Habilitation thesis @Braunschweig, Techn. Univ., Diss. : 1989
    Database Former special subject collection: coastal and deep sea fishing

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  3. Book: Alkylphosphonate als neue Antitumormittel

    Ries, Uwe Jörg

    1989  

    Author's details Uwe Jörg Ries
    Size 195 S
    Document type Book
    Note Braunschweig, TU, naturwiss. Fakultät, Diss. 1989
    Database Library catalogue of the German National Library of Science and Technology (TIB), Hannover

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  4. Article: In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate.

    Wienen, Wolfgang / Stassen, Jean-Marie / Priepke, Henning / Ries, Uwe Joerg / Hauel, Norbert

    Thrombosis and haemostasis

    2007  Volume 98, Issue 1, Page(s) 155–162

    Abstract: Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug, dabigatran etexilate. This study set out to determine the molecular potency and anticoagulant efficacy of ... ...

    Abstract Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug, dabigatran etexilate. This study set out to determine the molecular potency and anticoagulant efficacy of dabigatran and its prodrug dabigatran etexilate. This was achieved through enzyme inhibition and selectivity analyses, surface plasmon resonance studies, platelet aggregation, thrombin generation and clotting assays in vitro and ex vivo. These studies demonstrated that dabigatran selectively and reversibly inhibited human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively. In vivo, dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively. These data suggest that dabigatran is a potent, selective thrombin inhibitor and an orally active anticoagulant as the prodrug, dabigatran etexilate.
    MeSH term(s) Administration, Oral ; Animals ; Anticoagulants/administration & dosage ; Anticoagulants/pharmacology ; Benzimidazoles/administration & dosage ; Benzimidazoles/pharmacology ; Blood Coagulation/drug effects ; Blood Coagulation Tests ; Dabigatran ; Dose-Response Relationship, Drug ; Hemostasis/drug effects ; Humans ; Macaca mulatta ; Pharmacokinetics ; Platelet Aggregation/drug effects ; Prodrugs/administration & dosage ; Prodrugs/pharmacology ; Pyridines/administration & dosage ; Pyridines/pharmacology ; Rats ; Thrombin/antagonists & inhibitors
    Chemical Substances Anticoagulants ; Benzimidazoles ; Prodrugs ; Pyridines ; Thrombin (EC 3.4.21.5) ; Dabigatran (I0VM4M70GC)
    Language English
    Publishing date 2007-07
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 518294-3
    ISSN 0340-6245
    ISSN 0340-6245
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats.

    Wienen, Wolfgang / Stassen, Jean-Marie / Priepke, Henning / Ries, Uwe Joerg / Hauel, Norbert

    Thrombosis and haemostasis

    2007  Volume 98, Issue 2, Page(s) 333–338

    Abstract: Dabigatran is a reversible direct, selective thrombin inhibitor, undergoing clinical development as its orally active prodrug, dabigatran etexilate. The objective of this trial was to assess the antithrombotic and anticoagulant effects of dabigatran and ... ...

    Abstract Dabigatran is a reversible direct, selective thrombin inhibitor, undergoing clinical development as its orally active prodrug, dabigatran etexilate. The objective of this trial was to assess the antithrombotic and anticoagulant effects of dabigatran and dabigatran etexilate in a rat model of venous thrombosis. In order to do this a modified Wessler model was used to assess the antithrombotic and anticoagulant effects of intravenous (i.v.) dabigatran and oral dabigatran etexilate administration. In addition, a rat tail bleeding time model was used to investigate the antihemostatic effect of dabigatran. The study demonstrated that bolus administration of dabigatran (0.01-0.1 mg/kg) reduced thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. By comparison, ED50 values for heparin (0.03-0.3 mg/kg), hirudin (0.01-0.5 mg/kg) and melagatran (0.1-0.5 mg/kg) were 0.07, 0.15 and 0.12 mg/kg, respectively. Oral administration of dabigatran etexilate (5-30 mg/kg) inhibited thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action. Following i.v. administration of dabigatran (0.1-1.0 mg/kg), a statistically significant prolongation of bleeding time was observed at doses at least 15- and 5-fold greater than ED50 and ED100 (100% of the effective dose) doses, respectively; there was no significant increase in bleeding tendency at the maximum therapeutically effective dose (0.1 mg/kg). It can be concluded that dabigatran and its oral prodrug, dabigatran etexilate, show promise in the management of thromboembolic disease.
    MeSH term(s) Animals ; Anticoagulants/administration & dosage ; Anticoagulants/pharmacology ; Benzimidazoles/administration & dosage ; Benzimidazoles/pharmacology ; Bleeding Time ; Dabigatran ; Dose-Response Relationship, Drug ; Drug Administration Routes ; Drug Evaluation, Preclinical ; Prodrugs/administration & dosage ; Prodrugs/pharmacology ; Pyridines/administration & dosage ; Pyridines/pharmacology ; Rats ; Thrombosis/drug therapy ; Thrombosis/prevention & control
    Chemical Substances Anticoagulants ; Benzimidazoles ; Prodrugs ; Pyridines ; Dabigatran (I0VM4M70GC)
    Language English
    Publishing date 2007-08
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 518294-3
    ISSN 0340-6245
    ISSN 0340-6245
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate

    Wienen, Wolfgang / Stassen, Jean-Marie / Priepke, Henning / Ries, Uwe Joerg / Hauel, Norbert

    Thrombosis and Haemostasis

    2007  Volume 97, Issue 07, Page(s) 155–162

    Abstract: Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug, dabigatran etexilate.This study set out to determine the molecular potency and anticoagulant efficacy of ... ...

    Abstract Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug, dabigatran etexilate.This study set out to determine the molecular potency and anticoagulant efficacy of dabigatran and its prodrug dabigatran etexilate.This was achieved through enzyme inhibition and selectivity analyses, surface plasmon resonance studies, platelet aggregation, thrombin generation and clotting assays in vitro and ex vivo.These studies demonstrated that dabigatran selectively and reversibly inhibited human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC 50 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC 50 0.56 μM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. In vivo, dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively. These data suggest that dabigatran is a potent, selective thrombin inhibitor and an orally active anticoagulant as the prodrug, dabigatran etexilate. Footnote: Parts of this study were presented at the XVIII Congress of the International Society on Thrombosis and Haemostasis, Paris, July 2001. Thromb Haemost 2001; 86 (Suppl): Abstracts P755, P763. Institution where work was carried out: Boehringer Ingelheim Pharma GmbH &Co KG, 88397 Biberach, Germany.
    Keywords Activated partial thromboplastin time ; dabigatran etexilate ; direct thrombin inhibitor ; ecarin clotting time ; oral anticoagulant
    Language English
    Publishing date 2007-01-01
    Publisher Schattauer GmbH
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 518294-3
    ISSN 2567-689X ; 0340-6245
    ISSN (online) 2567-689X
    ISSN 0340-6245
    DOI 10.1160/TH07-03-0183
    Database Thieme publisher's database

    Full text online

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  7. Article: Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats

    Wienen, Wolfgang / Stassen, Jean-Marie / Priepke, Henning / Ries, Uwe Joerg / Hauel, Norbert

    Thrombosis and Haemostasis

    2007  Volume 97, Issue 08, Page(s) 333–338

    Abstract: Dabigatran is a reversible direct, selective thrombin inhibitor, undergoing clinical development as its orally active prodrug, dabigatran etexilate. The objective of this trial was to assess the antithrombotic and anticoagulant effects of dabigatran and ... ...

    Abstract Dabigatran is a reversible direct, selective thrombin inhibitor, undergoing clinical development as its orally active prodrug, dabigatran etexilate. The objective of this trial was to assess the antithrombotic and anticoagulant effects of dabigatran and dabigatran etexilate in a rat model of venous thrombosis. In order to do this a modifiedWessler model was used to assess the antithrombotic and anticoagulant effects of intravenous (i.v.) dabigatran and oral dabigatran etexilate administration. In addition, a rat tail bleeding time model was used to investigate the antihemostatic effect of dabigatran.The study demonstrated that bolus administration of dabigatran (0.01–0.1 mg/kg) reduced thrombus formation dose-dependently,with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. By comparison,ED50 values for heparin (0.03–0.3 mg/kg),hirudin (0.01–0.5 mg/kg) and melagatran (0.1–0.5 mg/kg) were 0.07, 0.15 and 0.12 mg/kg, respectively. Oral administration of dabigatran etexilate (5–30 mg/kg) inhibited thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action. Following i.v. administration of dabigatran (0.1–1.0 mg/kg), a statistically significant prolongation of bleeding time was observed at doses at least 15- and 5-fold greater than ED50 and ED100 (100% of the effective dose) doses, respectively; there was no significant increase in bleeding tendency at the maximum therapeutically effective dose (0.1 mg/kg). It can be concluded that dabigatran and its oral prodrug, dabigatran etexilate, show promise in the management of thromboembolic disease.
    Keywords Activated partial thromboplastin time ; anticoagulant ; dabigatran etexilate ; direct thrombin inhibitor ; thrombosis
    Language English
    Publishing date 2007-01-01
    Publisher Schattauer GmbH
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 518294-3
    ISSN 2567-689X ; 0340-6245
    ISSN (online) 2567-689X
    ISSN 0340-6245
    DOI 10.1160/TH07-02-0113
    Database Thieme publisher's database

    Full text online

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