Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).
Abstract: A process is described for preparing budesonide which comprises the steps of: a) preparing an aqueous hydrochloric acid solution; b) reacting 16?-hydroxyprednisolone and butyraldehyde within the solution prepared in step a), in an inert atmosphere; c) quenching the reaction of step b) with water. The process of the invention enables the ratio between the A and B epimers of budesonide to be controlled.
Abstract: This invention relates to new 19-nor-17?-pregna-1,3,5(10)-trien-17?-ols with a 21,16?-lactone ring with a long-chain substituent in 11?-position of general formula II in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
October 10, 2006
Assignee:
Schering Aktiengesellschaft
Inventors:
Gerd Mueller, Jens Hoffmann, Karl-Heinrich Fritzemeier, Alexander Hillisch
Abstract: This invention relates to new 19-nor-17?-pregna-1,3,5(10)-trien-17?-ols with a 21,16?-lactone ring with a long-chain substituent in 11?-position of general formula II in which R11 is a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
October 18, 2005
Assignee:
Schering Aktiengesellschaft
Inventors:
Alexander Hillisch, Walter Elger, Rolf Bohlmann, Jens Hoffmann
Abstract: Compounds of the androstane series are described having the formula (I) and solvates thereof in which R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or C.sub.1-6 alkyl; R.sub.3 and R.sub.4 are the same or different and each represents hydrogen or halogen; and ##STR1## represents a single or a double bond. Compounds of formula (I) and their solvates are useful as anti-inflammatory or anti-allergic agents.
Type:
Grant
Filed:
June 24, 1998
Date of Patent:
September 5, 2000
Assignee:
Glaxo Group Limited
Inventors:
Keith Biggadike, Panayiotis Alexandrou Procopiou