Abstract: Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH.sub.2).sub.m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group.These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.
Type:
Grant
Filed:
February 24, 1994
Date of Patent:
November 21, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Hans-Jugen Federsel, Thomas Ho, Sten I. Ramsby, Peter H. E. Strom
Abstract: Compounds of the formula I as well as a process for their preparation, their pharmaceutical preparations and their useH--Tyr--Tic--X (I)wherein X is--Phe--OH,--Phe--NH.sub.2,--Phe--Phe--OH,--Phe--Phe--NH.sub.2,--Trp--Phe--NH.sub.2,--Trp--Phe--OH,--Phe--Phe(p-NO.sub.2)--OH,--Trp--Phe(p-NO.sub.2)--H or--Phe--Trp--NH.sub.2.
Abstract: The present invention is directed to a process for preparing formoterol and related compounds and derivatives thereof and their pharmacologically and pharmaceutically acceptable fumarate salts and/or solvates. The present invention is also directed to certain formoterol related compounds per se.
Type:
Grant
Filed:
September 20, 1994
Date of Patent:
July 18, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Jan W. Trofast, Edib Jakupovic, Katarina L. Mansson
Abstract: The novel compounds of the formula I ##STR1## and physiologically acceptable salts thereof, wherein R.sup.1 and R.sup.2, which are different is each H alkyl containing 1-4 carbon atoms or --C(O)--R.sup.5 ;whereinR.sup.5 is alkyl containing 1-4 carbon atoms or alkoxy containing 1-4 carbon atoms and one of R.sup.1, or R.sup.2 is always selected from the group --C(O)--R.sup.5 ;R.sup.3 and R.sup.4 are the same or different and selected from ##STR2## and --CH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.3 and R.sup.4 together with the adjacent oxygen atoms atached to the pyridine ring and the carbon atoms in the pyridine ring form a ring, wherein the part constituted by R.sup.3 and R.sup.4 is --CH.sub.2 CH.sub.2 CH.sub.2 --, or --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --; as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient and the use of the compounds in medicine.
Abstract: 3-amino-5-carbamoylchromans and 8-fluoro-3-amino-5-carbamoylchromans, as well as enantiomers and salts thereof, are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
Type:
Grant
Filed:
October 28, 1993
Date of Patent:
May 30, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Eva M. Hammarberg, Lars G. Johansson, Svante B. Ross, Seth-Olov Thorberg
Abstract: A method for the manufacture of oral controlled release dosage units containing hydroxypropyl methylcellulose wherein the aqueous granulation is performed in the presence of one or more solutes, which inhibit gel formation during the granulation but allows the formation of a gel when administered orally. Also the new dosage units prepared according to the invention are included.
Abstract: A liquid containing thermoplastic unit dose container (1) which comprises a body portion (2), a neck portion (3) and an outlet opening (7) at the end of the neck portion (3) which is sealed by a non-resealable cap (4). The outside wall of the neck portion (3) comprises a thread engagement portion (8) which is located at or proximate the outermost edge of the neck portion (3) so that after removal of cap (4) thread engagement portion (8) is adapted to engage within an inwardly facing screw thread channel (14) at the end of a syringe. This enables sealing connection of the container (1) to the syringe so that liquid within container (1) may be directly transferred from the container (1) to the syringe.
Type:
Grant
Filed:
December 3, 1993
Date of Patent:
April 25, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Michael B. Kimber, Anders T. Kers, Borje Jonsson
Abstract: In this patent application we have described the construction of a novel secretion vector based on E. coli enterotoxin coding sequence. We have shown categorically that pre and pro regions of toxin gene are absolutely necessary for extra cellular secretion of the stable toxin. We have also shown with specific examples that when the nucleotide coding sequence of a heterologous peptide is fused in frame to the end of the pro region in the st gene, the resultant vector in an E. coli host secretes extracellularly correctly processed heterologous peptide. This application also includes construction of suitable vectors where this gene fusion can be achieved. Generally methods to create such fusions involving a) recombinant DNA technology and b) the use of site directed in vitro mutagenesis, have also been described. A general method of purification of heterologous peptides is also described in this application.
Type:
Grant
Filed:
June 14, 1991
Date of Patent:
March 21, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Tanjore S. Balganesh, Goutam Das, Sandhya S. Visweswariah
Abstract: The invention provides a device for mixing a pharmaceutical from a solid supply into a parenterally acceptable liquid flowing through a set for parenteral administration of the liquid to a patient, said device comprising a first compartment defining a mixing space through which the liquid flows in a define flow direction and in which the liquid mixes with the pharmaceutical in liquid solution.
Abstract: New pharmaceutical formulations comprising 5-(2-chloro-1-hydroxyethyl)-4-methylthiazole or optical isomers or a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
August 14, 1991
Date of Patent:
January 31, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Bernard R. Boar, Alan J. Cross, Alfred R. Green, Curt-Eric Hagberg
Abstract: The present invention relates to an improved method for the synthesis of omeprazole, comprising the steps of reacting 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methylthio]-1H-benzimida zole with m-chloroperoxybenzoic acid in a methylene chloride solution at a substantially constant pH of about 8.0 to 8.6; extracting the reaction mixture with aqueous NaOH; separating the aqueous phase from the organic phase; and adding an alkyl formate to the aqueous phase, resulting in crystallization of omeprazole.
Abstract: New crystalline organic salts of N,N'-diacetyl cystine with immunomodulating effect, processes for their preparation, pharmaceutical compositions containing them and methods of their pharmacological use.
Type:
Grant
Filed:
November 25, 1992
Date of Patent:
January 31, 1995
Assignee:
Aktiebolaget Astra
Inventors:
Carl-Magnus A. Andersson, Hakan S. A. M. Bergstrand, Edib Jakupovic, Bo-Goran Josefsson, Magnus L. Lindvall, Bengt O. Sarnstrand, Eric N. G. Teneberg