Abstract: A novel crystal modification of the compound 2,4-diamino-6-hydroxymethylpteridine hydrobromide and a process for its preparation and its use for preparing methotrexate. The novel crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide is distinguished in particular by the fact that only one equivalent of the brominating agent triphenylphosphine dibromide is needed for brominating the 6-hydroxymethyl group. No reaction with the amino groups in the 2 and 4 positions takes place. This facilitates the reaction to give 2,4-diamino-6-pteridinyl derivatives such as methotrexate.
Abstract: A method is described for the production of 6,12-dihydro-6-hydroxy-cannabidiol which is obtained by the reaction of olivetol and cis-p-menth-2-ene-1,8,-diol and the reaction thereof to yield trans-delta-9-tetrahydrocannabinol.
Abstract: A pharmaceutical preparation for parenteral administration of a drug consisting of a solvent system containing:(a) 0 to 65% by weight of .alpha.-tetrahydrofurfuryl-.omega.-hydroxy-polyloxyethylene;(b) 10 to 100% by weight polyethylene glycol with a mean molecular weight of 200 to 600; and(c) 0 to 35% by weight of waterThe sum of components (a) and (b) amounting to at least 65% by weight, and one or more therapeutically active compounds of the formula ##STR1## wherein R.sub.1 denotes a phenyl radical optionally substituted with 1 to 3 substituents independently selected from the group consisting of F, Cl, Br, I, CF.sub.3, C.sub.1 to C.sub.4 alkyl, and C.sub.1 to C.sub.4 alkoxy, or 5-chloro-pyrid-2-yl; X denotes OH, F, Cl or Br; R.sub.2 is H, CH.sub.3 or F; and R.sub.3 is H or F.
Abstract: Oxime ethers of 2,6-dioxabicyclo[3.3.0]octanones of the formula I ##STR1## have pharmacological activity and are especially applicable as drugs for the prophylaxis and therapy of cardiac and circulatory diseases.
Abstract: Isohexide nucleosides of the formula I ##STR1## in which R and B have the meaning given in the description, processes for their preparation and their use as medicaments, in particular as cytostatics, virustatics and immunostimulants.
Abstract: Dianhydrohexites of the formula ##STR1## wherein R.sup.1 is hydrogen or benzyl, R.sub.2 is alkyl or omega-theophyllin-7-yl-alkyl, and R.sup.1 and R.sub.2 together with the nitrogen atom to which they are attached form a bicyclic group and R.sup.3 is hydrogen, acyl, pyridylcarbonyl, nitro or a hydroxylamino group, are formed by an analogous method and used as pharmaceuticals in the treatment of heart and circulatory diseases.
Abstract: Stable aqueous solutions of piroxicam suitable for pharmaceutical use are disclosed. These solutions all contain piroxicam in conjunction with a sub-stoichiometric amount of D-(-)-N-methylglucamine and have proplyene glycol, ethanol and water as the solvent, with the pH of said solutions being in the range of from about pH 8 to about pH 9. These particular pharmaceutical compositions possess excellent chemical stability properties and are especially suitable for parenteral administration.
Abstract: The present invention relates to new acyl derivatives of 1,4:3,6-dianhydrohexitols, processes for their preparation and drugs containing the same. The new compounds have a cardiovascular effect and can be used as antihypertensive agents, as peripheral and central vasodilators and as coronary therapeutic agents.
Abstract: A process for the preparation of isosorbide-2-nitrate of the formula ##STR1## comprising contacting isosorbide with a carboxylic acid anhydride in the presence of a metal salt; esterifying the resultant isosorbide-5-acylate with nitric acid; and converting the resultant isosorbide-5-acylate-2-nitrate to isosorbide-2-nitrate by treatment with an alkyl alcohol in the presence of an alkali metal alcoholate.
Type:
Grant
Filed:
May 24, 1982
Date of Patent:
November 22, 1983
Assignee:
Heinrich Mack Nachf. Chem.-Pharmazeutische Fabrik
Abstract: This invention relates to a process for the production of isosorbide-5-nitrate comprising(a) subjecting an acylation mixture of isosorbide containing varying proportions of isosorbide, isosorbide-2-acylate, isosorbide-5-acylate and/or isosorbide-2,5-diacylate, or pure isosorbide-5-acylate or an equimolar mixture of isosorbide-2,5-diacylate and isosorbide to a transacylation reaction in the presence of a catalyst and removing the isosorbide-2-acylate present from the reaction mixture by fractional distillation;(b) optionally subjecting the separated isosorbide-2-acylate to a further purification step;(c) esterifying the obtained isosorbide-2-acylate with nitric acid; and(d) partially hydrolyzing the obtained isosorbide-2-acylate-5-nitrate.
Abstract: Vincamine saccharinate, a novel derivative of vincamine, and pharmaceutical compositions containing vincamine saccharinate are disclosed. The solubility of vincamine saccharinate in glycerol-ethanol mixtures and the superior taste characteristics of vincamine saccharinate allow the preparation of preferred pharmaceutical compositions in solution form which are suitable for oral administration, especially in the form of drops.