Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen, loweralkyl, aminomethyl or halo, R.sub.1 is hydroxy or NHX where X is H, loweralkyl, phenyl, substituted phenyl, acetyl, benzyl and substituted benzyl, and Y is hydrogen, loweralkyl or halo and may be the same or different, and pharmaceutically acceptable salts thereof.The compounds are effective as diuretic agents.
Type:
Grant
Filed:
October 9, 1981
Date of Patent:
February 1, 1983
Assignee:
Abbott Laboratories
Inventors:
Jacob J. Plattner, Andre G. Pernet, Anthony K. Fung
Abstract: The present invention provides a deoxyribonucleic acid (DNA) segment related to a human plasminogen activator gene. The segment is inserted into a plasmid vector which in turn can be incorporated into a bacterium or other microorganism. The bacterium can then be cultured to produce a plasminogen activator protein having properties of human urokinase.
Type:
Grant
Filed:
April 3, 1980
Date of Patent:
January 25, 1983
Assignee:
Abbott Laboratories
Inventors:
Paul P. Hung, Shaw-Guang Lee, Ranajit Roychoudhury, Barry J. Ratzkin, W. Jurgen Schrenk, Michael C. Chen
Abstract: 2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
Type:
Grant
Filed:
May 22, 1981
Date of Patent:
November 23, 1982
Assignee:
Abbott Laboratories
Inventors:
John S. Tadanier, Jerry R. Martin, Paulette Collum
Abstract: 2-Deoxyfortimicin, A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
Type:
Grant
Filed:
May 22, 1981
Date of Patent:
November 23, 1982
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Collum
Abstract: 2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
Type:
Grant
Filed:
May 22, 1981
Date of Patent:
November 23, 1982
Assignee:
Abbott Laboratories
Inventors:
John S. Tadanier, Jerry R. Martin, Paulette Collum
Abstract: A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl; and R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-lower-alkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, amino hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N-N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, hydroxy-substituted aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N, N-diloweralkylaminoacyl, hydroxysubstituted-N-loweralkylaminoacyl and hydroxy-substituted-N, N-diloweralkylaminoacyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.
Type:
Grant
Filed:
October 28, 1980
Date of Patent:
July 20, 1982
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Johnson
Abstract: 4-N-Lysyl-2'-N-des-.beta.-lysyl antibiotic AX-127B-1 and the pharmaceutically acceptable salts thereof. The compounds are useful as intermediates in the preparation of 3-O-demethyl 4-N-lysyl-2'-N-des-.beta.-lysyl antibiotic AX-127B-1 and as a broad spectrum antibacterial agents.
Abstract: 2'-N-Des-.beta.-lysyl antibiotic AX-127B-1 and the 4-N-acyl and alkyl derivatives thereof. The compounds are useful as intermediates in the preparation of 3-O-demethyl antibiotic AX-127B-1 and its derivatives. 2'-N-des-.beta.-lysyl antibiotic AX-127B-1 is also useful as a broad spectrum antibacterial agent.
Abstract: 4',5'-Dihydro-antibiotic AX-127B-1, 2'-N-des-.beta.-lysyl-4',5'-dihydro-antibiotic AX-127B-1, the 4-N-acyl and alkyl derivatives thereof and their pharmaceutically acceptable salts. The compounds are useful as antibiotics and as intermediates for preparing the corresponding 3-O-demethyl derivatives of antibiotic AX-127B-1.
Abstract: Described is a method of obtaining complete copying of the entire length of single stranded ribonucleic acid (RNA) into its complementary deoxyribonucleic acid (cDNA) by reverse transcription using binding protein. The method can be used in recombinant DNA research to copy total messenger RNA into DNA.
Abstract: What is described is 2-epi-fortimicin A, 2-epi-fortimicin B or a 2-epi-fortimicin B derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxy; R.sub.3 is methyl or hydrogen; and R.sub.4 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoalkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl of the formula ##STR2## wherein R.sub.5 is loweralkyl, aminoacyl, diaminoacyl, hydroxyacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue other than those defined above and the pharmaceutically acceptable salts thereof useful in the treatment of infections.
Type:
Grant
Filed:
September 26, 1979
Date of Patent:
May 25, 1982
Assignee:
Abbott Laboratories
Inventors:
John S. Tadanier, Robert Hallas, Jerry R. Martin
Abstract: An improved process for producing 3-O-demethylfortimicins and other O-methyl-containing aminoglycoside antibiotics comprising the steps of reacting the fortimicin to be 3-O-demethylated with a borontrihalide and recovering the 3-O-demethylfortimicin from the reaction mixture. 3-O-Demethylfortimicin derivatives which can be prepared by this process include compounds represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are hydrogen or methyl with the limitation that one of either R.sub.1 or R.sub.2 must be hydrogen; R.sub.3 is hydrogen or methyl; R.sub.4 and R.sub.11 are the same or different members of the group consisting of hydrogen, acyl, aminoacyl, diaminoacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, loweralkyl, aminoloweralkyl, diaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, N-loweralkylaminohydroxyloweralkyl and N,N-diloweralkylaminohydroxyloweralkyl; R.sub.5 and R.sub.
Abstract: Described is a structurally modified urokinase which is biologically active over an extended time period in comparison to native urokinase. The extended activity permits the administration of lower doses of urokinase when it is used in the treatment of thromboembolic diseases. Methods of appropriately modifying the structure of urokinase are described.
Type:
Grant
Filed:
May 5, 1980
Date of Patent:
April 20, 1982
Assignee:
Abbott Laboratories
Inventors:
William H. Holleman, Shaw-Guang Lee, Paul P. Hung
Abstract: Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,R.sub.2 is hydrogen, halo, haloloweralkyl, loweralkyl, loweralkoxy, loweralkylthio or ##STR3## wherein R.sub.5 and R.sub.6 are previously defined, R.sub.3 is hydroxy, alkoxy, branched alkoxy, adamantyloxy, morpholino, amino or amino substituted by loweralkyl or alkylene of 4 or 5 carbon atoms,R.sub.4 is hydrogen or loweralkyl, andX.sub.1 and X.sub.2 are hydrogen, loweralkyl, halo or when substituted on adjacent carbon atoms of the benzene ring form a 1,3-butadienylene linkage, Y is oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents in increasing urinary excretion.
Abstract: A new fortimicin antibiotic, 2-deoxyfortimicin B, intermediates useful in the preparation of the compound, methods of making and using the compound and compositions containing 2-deoxyfortimicin B.
Type:
Grant
Filed:
April 27, 1980
Date of Patent:
March 9, 1982
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Collum
Abstract: An elastometer for measuring the mechanical strength of biological gels such as blood or fibrin clots. Thus this device may be used for accessing anticoagulant and fibrinolitic activities, particularly with respect to drug evaluation. The instrument can also be used to study abnormalities in the blood clotting process, i.e. for clinical diagnosis purposes.
Abstract: A new fortimicin antibiotic, 2-deoxyfortimicin B, intermediates useful in the preparation of the compound, methods of making and using the compound and compositions containing 2-deoxyfortimicin B.
Type:
Grant
Filed:
April 27, 1979
Date of Patent:
March 2, 1982
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Collum
Abstract: Fortimicin AN is coproduced with fortimicin A, fortimicin B and a number of other minor factors in the fermentation of Micromonospora olivoasterospora ATCC Nos. 21819,31009 or 31010. Structurally, fortimicin AN is 1-N-glycyl-3-O-demethylfortimicin B. The compound is useful as an intermediate for 3-O-demethylfortimicin B which is readily obtained by hydrolysis of fortimicin AN in base.
Abstract: A method of reducing intra-ocular pressure in mammalian patients comprising administering to a glaucoma patient a therapeutically effective amount of a compound of the formula ##STR1## wherein, in the C ring, X is CH.sub.2, S, ##STR2## or NR.sub.4 where R.sub.4 is H, loweralkyl, loweralkenyl, loweralkynyl or loweralkanoyl; n is an integer of 0 to 3; m is an integer of 0 to 3, or the C ring is a quinuclidine ring ##STR3## each R.sub.1 is loweralkyl, and when taken together, the substituents R.sub.1 R.sub.1 form oxygen; R.sub.2 is a C.sub.1 -C.sub.20 straight or branched chain alkyl, cycloalkyl, or ##STR4## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms, and each R.sub.5, R.sub.6 and R.sub.7 are the same or different members of the group consisting of H, halo or loweralkyl; R.sub.3 is H or ##STR5## wherein Y' is a straight or branched chain alkylene group having 1 to 8 carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.