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  • Inorganic Chemistry  (132)
  • General Chemistry  (37)
  • pharmacokinetics
  • 1990-1994  (110)
  • 1975-1979  (33)
  • 1935-1939  (33)
  • 1
    Electronic Resource
    Electronic Resource
    Clinical implications of slow sulphoxidation of thioridazine in a poor metabolizer of the debrisoquine type (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 613-614 
    Details
    ISSN: 1432-1041
    Keywords: Thioridazine ; debrisoquine polymorphism ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00316110
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  • 2
    Electronic Resource
    Electronic Resource
    Über ein Oxidchlorid des Calciums: Ca4OCl6 (1991)
    Weinheim : Wiley-Blackwell
    Zeitschrift für anorganische Chemie 596 (1991), S. 89-92 
    Details
    ISSN: 0044-2313
    Keywords: Calcium oxychloride ; preparation ; crystal structure ; Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: An Oxychloride of Calcium: Ca4OCl6Ca4OCl6 (hexagonal, P63mc, Z = 2), a = 905.8(3), c = 686.3(4) pm, (R = 0.031) crystallizes as colourless needles from reducing melts (CaCl2, Ca) that contain small amounts of „oxygen“. It contains „isolated“ tetrahedral units [Ca4O] and is isotypic with e.g., Ba4OCl6, Yb4OCl6 and K6HgS4. Ca4OCl6 does not form in the dehydration process of, for example, CaCl2 · 6 H2O.
    Notes: Ca4OCl6 (hexagonal, P63mc, Z = 2, a = 905.8(3)); c = 686.3(4) pm, (R = 0,031) kristallisiert in Form farbloser Nadeln aus „reduzierenden Schmelzen“ (CaCl2, Ca), die wenig „Sauerstoff“ enthalten. Es enthält „isolierte“ tetraedrische [Ca4O]-Einheiten und ist isotyp mit z. B. Ba4OCl6, Yb4OCl6 oder K6HgS4. Ca4OCl6 entsteht nicht beim Entwässern von z. B. CaCl2 · 6 H2O.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/zaac.19915960112
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  • 3
    Electronic Resource
    Electronic Resource
    The effect of renal impairment on the pharmacokinetics of oxcarbazepine and its metabolites (1994)
    Springer
    European journal of clinical pharmacology 47 (1994), S. 161-167 
    Details
    ISSN: 1432-1041
    Keywords: Oxcarbazepine ; 10,11-dihydro-10-hydroxy-carbamazepine ; renal impairment ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract We have studied the effect of renal impairment on the pharmacokinetics of oxcarbazepine, its active monohydroxy-metabolite (which predominates in plasma), their glucuronides, and the inactive dihydroxy-metabolite after a single oral dose of oxcarbazepine (300 mg). Six subjects with normal renal function and 20 patients with various degrees of renal impairment participated. The mean areas under the plasma concentration-time curves of oxcarbazepine and its monohydroxy-metabolite were 2–2.5-times higher in patients with severe renal impairment (CLCR〈10 ml·min−1) than in healthy subjects. The apparent elimination half-life of the monohydroxy-metabolite [19 (SD 3) h] in these patients was about twice that in healthy subjects. The effect of renal impairment on the plasma concentrations of glucuronides was more marked. The renal clearances of the unconjugated monohydroxy-metabolite and its glucuronides (the main compounds recovered in urine) correlated well with creatinine clearance. The maximum target dose in patients with slight renal impairment (CLCR〉30 ml·min−1) should not be changed. In patients with moderate renal impairment (CLCR10–30 ml·min−1) it should be reduced by 50%. In patients with severe renal impairment (CLCR〈10 ml·min−1), the glucuronides of oxcarbazepine and its monohydroxy-metabolite are likely to accumulate during repeated administration, and dosage adjustment of oxcarbazepine in these patients could not be proposed from this single administration study.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00194967
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  • 4
    Electronic Resource
    Electronic Resource
    Effects of diclofenac on isradipine pharmacokinetics and platelet aggregation in volunteers (1993)
    Springer
    European journal of clinical pharmacology 44 (1993), S. 391-393 
    Details
    ISSN: 1432-1041
    Keywords: Isradipine ; Diclofenac ; pharmacokinetics ; platelet aggregation ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In this open, two-period crossover study in 18 healthy male volunteers, a single oral dose of 50 mg diclofenac was administered alone and on day 7 of multiple oral dosing of 5 mg b.i.d. isradipine to assess a possible pharmacokinetic interaction. The effect of these drugs on ex vivo platelet function was also determined. Serial blood samples were obtained over 12-hour periods on three occasions: after the single diclofenac dose; after the morning dose of isradipine on day 6 and after co-administration of both drugs on day 7 of steady-state isradipine administration. Additional samples were taken at 2 h post dose for determination of ex vivo platelet aggregation. Isradipine plasma concentrations were determined by a gas chromatographic method and diclofenac plasma concentrations by an HPLC method. The pharmacokinetic characteristics of diclofenac were unaltered during co-administration. The maximum plasma concentration of isradipine was increased 19.6% during co-administration from 5.06 to 6.05 ng·ml−1. This is not expected to be of clinical importance. Isradipine's apparent total body clearance and steady-state AUC remained unchanged. Ex vivo induced platelet aggregation was not affected by any of the treatments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00316480
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  • 5
    Electronic Resource
    Electronic Resource
    Lack of interaction between ramipril and simvastatin (1994)
    Springer
    European journal of clinical pharmacology 47 (1994), S. 373-375 
    Details
    ISSN: 1432-1041
    Keywords: ACE-inhibitors ; Simvastatin ; ramipril ; lipid lowering drugs ; drug interaction ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Twenty two healthy males participated in a randomised, placebo-controlled, double blind, cross-over study to investigate the influence of simvastatin on the pharmacokinetics of ramipril and its active metabolite (ramiprilat), and on the ACE-inhibiting effect of ramiprilat. During two study periods, each of 7 days, subjects received daily either simvastatin 20 mg at 19.00 h or placebo; ramipril (5 mg) was given on Day 5 of each of the periods. Plasma concentrations of ramipril and ramiprilat and ACE-activity were measured in sequential blood specimens, and ramipril and ramiprilat concentrations were measured in urine. Blood and urine collections for pharmacokinetic and pharmacodynamic assessment were made up to 72 h after the dose of ramipril. The mean AUC of ramipril for ramipril+placebo (R+P) and ramipril+simvastatin (R+S) was 22.2 and 21.3 ng.h.ml−, respectively; for ramiprilat the corresponding figures were 61.3 and 57.6 ng.h.ml−. The urinary excretion of ramipril+metabolites for (R+P) and (R+S) was 25.2 and 24.1% of dose. The maximum percentage inhibition of ACE-activity for (R+P) was 94.6%, and for (R+S) it was 94.1%. It is concluded that concomitant administration of simvastatin and ramipril has no clinically relevant effect on the pharmacokinetics or ACE-inhibition of the latter drug and its metabolites.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00191171
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  • 6
    Electronic Resource
    Electronic Resource
    Di- und Polyaminozucker, XXI. Synthese von Derivaten der 2,4-Diamino-2,3,4-tridesoxy-D-ribo-hexose (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 3397-3411 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Di-and Polyamino Sugars, XXI. Synthesis of Derivatives of 2,4-Diamino-2,3,4-trideoxy-D-ribo-hexoseStarting with D-glucose the title compound has been synthesized as its di-N-acetyl. -trifluoroacetyl and N,N′-bis(2,4-dinitrophenyl) derivative. The free sugar could not be obtained in a pure state.
    Notes: Die Titelverbindung wurde, ausgehend von D-Glucose, in Form ihres Di-N-acetyl-, -trifluoracetyl- und ihres N,N′-Bis(2,4-dinitrophenyl)-Derivates erhalten. Reindarstellung des freien Zuckers gelang nicht.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751081031
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  • 7
    Electronic Resource
    Electronic Resource
    Heterocyclische Siebenring-Verbindungen, XVI. Synthese gezielt 3,5-substituierter 4-Phenyl-1-benzothiepine (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 3596-3610 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Heterocyclic Seven-membered Ring Compounds, XVI. Synthesis of 3,5-Substituted 4-Phenyl-1-benzothiepins4-Phenyl-1-benzothiepins 7 and 8 are synthesized starting from their 5-methoxy-2,3-dihydro-precursor 2; using the 2,5-dihydro-intermediate 12 yields the 4-phenyl-1-benzothiepins 13 and 14. The 1-benzothiepin 17 can be obtained from the diketone 1 directly. The 3-cyano-substituted compound 22 is prepared from its 2,5-dihydro-precursor 21. Some ring-contraction and ring-cleavage reactions of the heterocyclic seven-membered ring-system are described.
    Notes: Die 5-Methoxy-2,3-dihydro-Vorstufe 2 wird in die 4-Phenyl-1-benzothiepine 7 und 8 übergeführt; aus der 2,5-Dihydro-Vorstufe 12 werden die 4-Phenyl-1-benzothiepine 13 und 14 dargestellt. Das 1-Benzothiepin 17 wird direkt aus dem Siebenring-Diketon 1 erhalten. Das 3-cyan-substituierte 1-Benzothiepin 22 erhält man aus der 2,5-Dihydro-Vorstufe 21. Es werden einige Ringverengungsbzw. Ringspaltungsreaktionen des heterocyclischen Siebenring-Systems beschrieben.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751081121
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  • 8
    Electronic Resource
    Electronic Resource
    Eine moderne Strömungsapparatur für kinetische Messungen an thermischen Umlagerungen in der Gasphase: Thermolysekinetik neuer Kleinringverbindungen (1977)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 110 (1977), S. 2545-2560 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: A Modern Flow Reactor for Kinetic Measurements of Gasphase Thermal Rearrangements: Thermolysis Kinetics of Some New Small Ring CompoundsAn apparatus with a laminar flow reactor is introduced, which serves for kinetic measurements in the gas phase using rather small amounts (5-10mg) of compounds. Test runs for the well studied vinylcyclopropane rearrangement and the retro-Diels-Alder reaction of dicyclopentadiene demonstrate the reliability of the results thus obtained.  -  The thermolytic rearrangements of the following compounds were studied with this device: diademane (1), dispiro[2.0.2.4]deca-7,9-diene (3) including the formation of o-ethylstyrene (4) and tetrahydronaphthalene 5, 3,3,4,4-tetramethyl-1,5-hexadiene (6), 1,4-bis(cyclopropylidene)butane (8), dispiro[cyclopropane-1,2′-bicyclo[2.2.0]hexane-3′,1″-cyclopropane] (10), 2,2,3,3-tetramethylbicyclo[2.2.0]hexane (11) and 2,2-dimethylbicyclo[2.2.0]hexane-3-spirocyclopropane (12). All these reactions followed first order rate laws with the following Arrhenius relationships: ln(k1) = 33.6 - 31600/RT, ln(k3) = 34.2 - 35500/RT, ln(k4) = 33.6 - 35100/RT, ln(k5) = 33.6 - 36000/RT, ln(k6) = 29.1 - 33300/RT, ln(k8) = 22.0 - 26200/RT, ln(k10) = 32.0 - 35200/RT, ln(k11) = 32.0 - 40900/RT, ln(k12) = 32.3 - 39400/RT. The kinetic isotope effects of 1.4 and 1.1 (at 175°C) for the formation of 4 and 5 respectively and the difference Ea4 - Ea5 ≈ 0.1-0.9 kcal/mol strongly favor a mechanism, by which 3 rearranges via a 1,6-diradical to yield 4 and 5 by intramolecular disproportionation and recombination, respectively.
    Notes: Für kinetische Messungen in der Gasphase wird eine Apparatur mit laminarem Strömungsreaktor vorgestellt, die mit sehr geringen Substanzmengen (5-10mg) auskommt. Testmessungen an der eingehend untersuchten Vinylcyclopropanumlagerung und der Retro-Diels-Alder-Reaktion des Dicyclopentadiens beweisen die Verläßlichkeit der gewonnenen Daten.  -  Mit der Apparatur wurden die Thermolysen von Diademan (1), Dispiro[2.0.2.4]deca-7,9-dien (3) einschließlich Bildung von o-Ethylstyrol (4) und Tetrahydronaphthalin (5), 3,3,4,4-Tetramethyl-1,5-hexadien (6), 1,4-Bis(cyclopropyliden)butan (8), Dispiro[cyclopropan-1,2′-bicyclo[2.2.0]hexan-3′,1″-cyclopropan] (10), 2,2,3,3-Tetramethylbicyclo[2.2.0]hexan (11) und 2,2-Dimethylbicyclo[2.2.0]-hexan-3-spirocyclopropan (12) untersucht. Alle Reaktionen verlaufen nach Zeitgesetzen erster Ordnung und ergeben die folgenden Arrhenius-Beziehungen: ln(k1) = 33.6 - 31600/RT, ln(k3) = 34.2 - 35500/RT, ln(k4) = 33.6 - 35100/RT, ln(k5) = 33.6 - 3600/RT, ln(k6) = 29.1 - 33300/RT, ln(k8) = 22.0 - 26200/RT, ln(k10) = 32.0 - 35200/RT, ln(k11) = 32.0 - 40900/RT, ln(k12) = 32.3 - 39400/RT. Die kinetischen Isotopieeffekte von 1.4 und 1.1 bei der Bildung von 4 bzw. 5 (gemessen bei 175°C) und die gefundene Differenz Ea4 - Ea5 ≈ 0.1-0.9 kcal/mol sprechen für einen Umlagerungsmechanismus von 3 über ein 1,6-Diradikal, das intramolekular disproportioniert und rekombiniert zu 4, bzw. 5.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19771100713
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  • 9
    Electronic Resource
    Electronic Resource
    Phosphorhaltige Kohlenhydrate, XVII: Untersuchung der Hydrierung ungesättigter Glycosylphosphonate. Anomerer Effekt und A-Wert der Dimethylphosphono-Gruppe (1978)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 111 (1978), S. 3325-3335 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Phosphorus-containing Carbohydrates, XVII: Studies on the Hydrogenation of Unsaturated Glycosylphosphonates. Anomeric Effect and A-Value of the Dimethylphosphono GroupBy hydrogenation unsaturated glycosylphosphonates of type 1 give rise to the formation of 2,3-dideoxyglycosylphosphonates 2 and 2,3,4-trideoxyglycosylphosphonates 3. Their product ratio depends on configuration and conformation of the educts 1a-f. 1H and 13H and 13C NMR data permit an assigment of the anomers of the hydrogenated glycosylphosphonates. For the one-bond coupling constant between 13C-1 and 31P the correlation 1JC, Peq 〉 1JC, Pax is valid, which exhibits a difference of 19-23 Hz. The unsaturated glycosylphosphonates show deviations from Hudson's isorotation rule. In dimethyl cis-4-methyl-1-cyclohexanephosphonate (9) the A-value of the dimethylphosphono group has been determined to 8.34 kJ/mol. The ratio of conformers in 3a leads to an anomeric effect of the dimethylphosphono group of 2.33 kJ/mol.
    Notes: Ungesättigte Glycosylphosphonate vom Typ 1 liefern bei der Hydrierung außer 2,3-Didesoxyglycosylphosphonaten 2 auch 2,3,4-Tridesoxyglycosylphosphonate 3. Das Produktverhältnis ist von Konfiguration und Konformation der Ausgangsprodukte 1a-f abhängig. 1H- und 13C-NMR-Daten erlauben eine Anomerenzuordnung der hydrierten Glycosylphosphonate. Für die 13C-31P-Direktkopplung an C-1 gilt 1JC, Peq 〉 1JC, Pax mit einer Differenz von 19-23 Hz. Die ungesättigten Glycosylphosphonate zeigen Abweichungen von der Hudsonschen Regel. Am Dimethyl-cis-4-methyl-1-cyclohexanphosphonat (9) wurde der A-Wert der Dimethylphosphono-Gruppe zu 8.34 kJ/mol bestimmt. Aus der Konformerenverteilung bei 3a ergibt sich der anomere Effekt der Dimethylphosphono-Gruppe zu 2.33 kJ/mol.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19781111006
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  • 10
    Electronic Resource
    Electronic Resource
    Darstellung, chemische Eigenschaften und thermische Umlagerung von Spiro[3.4]octa-5,7-dien (1977)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 110 (1977), S. 2561-2573 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis, Chemical Properties and Thermal Rearrangement of Spiro[3,4]octa-5,7-dieneThe synthesis of spiro[3.4]octa-5,7-diene (2) was achieved along two routes starting from spiro-[3.4]octan-5-one (5). In both cases the last step was a dehydrohalogenation of the halospiro-[3.4]octenes 8b/9b and 11, respectively, which had to be carried out at room temperature, because 2 dimerizes about as fast as cyclopentadiene. It also underwent addition of maleic anhydride and 2-chloroacryloyl chloride to yield 13 and 14a respectively. 14a could be degraded to the bicyclo[2.2.1]hept-2-en-5-on-7-spirocyclobutane (15a), which served as a precursor to the hydrocarbon 17. Above 90°C 2 isomerizes to a mixture of bicyclo[3.3.0]octadienes 18a and 18b. This reaction followed a first order kinetics in the gas phase with the Arrhenius equation ln(k) = 31.7 - 29200/RT. These kinetic parameters are interpreted in terms of a sigmatropic [1,5]-alkyl shift.
    Notes: Die Synthese von Spiro[3.4]octa-5,7-dien (2) gelingt ausgehend von Spiro[3.4]octan-5-on (5) auf zwei Wegen. Bei beiden wird in der letzten Stufe eine Dehydrohalogenierung eines Halogenspiro[3.4]octens 8b/9b bzw. 11 bei Raumtemperatur vorgenommen, weil 2 bei höheren Temperaturen ähnlich schnell dimerisiert wie 1,3-Cyclopentadien. Ebenso addiert es leicht Maleinsäureanhydrid und 2-Chloracryloylchlorid zu 13 bzw. 14a. 14a läßt sich zum Bicyclo[2.2.1]hept-2-en-5-on-7-spirocyclobutan (15a) abbauen, aus dem der Kohlenwasserstoff 17 zugänglich ist. Oberhalb von 90°C isomerisiert 2 zu einem Gemisch der Bicyclo[3.3.0]octadiene 18a und 18b. Die Kinetik dieser Reaktion in der Gasphase zeigt einen Verlauf erster Ordnung und folgt dem Arrhenius-Ansatz ln(k) = 31.7 - 29200/RT. Daraus ist für den Mechanismus auf eine konzertierte [1,5]-Alkylverschiebung zu schließen.
    Additional Material: 2 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19771100714
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