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.
Abstract: 3-O-demethylsannamycin C, 3-O-demethyl-antibiotic AX-127B-1 and their 4-N- and 2'-N-acyl and alkyl derivatives are provided. The compounds are broad spectrum antibiotics and anti-bacterial agents.
Abstract: 1-Epi-2-deoxyfortimicin B and 4-N-derivatives thereof represented by the formula: ##STR1## wherein: R.sub.1 is hydrogen or loweralkyl and R.sub.2 is selected from the group consisting of loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminoloweralkyl, acyl, aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted aminoacyl hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted-N-loweralkylaminoacyl or hydroxysubstituted N,N-diloweralkylaminoacyl with the limitation that R.sub.2 cannot be hydrogen glycyl, formylglycyl or hydantoyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.
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 hydroxysubstituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
Type:
Grant
Filed:
November 6, 1979
Date of Patent:
June 30, 1981
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Collum
Abstract: Fortimicin B-4,5-carbamates represented by the formula: ##STR1## wherein R is hydrogen or an amine-protecting group; R.sub.1 is hydrogen or an amine-protecting group; R.sub.2 is hydrogen or loweralkoxycarbonyl; and R.sub.4 is hydrogen or loweralkoxycarbonyl. The compounds are useful as intermediates in the preparation the 2-epi-fortimicins.
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:
June 16, 1981
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Collum
Abstract: A method of producing 1-epi-2-deoxyfortimicin A, key intermediates therefor and an improved process for synthesizing the key intermediate 1,2-di-epi-fortimicin A.
Abstract: A 1,2-carbamate of fortimicin B and derivatives represented by the formula: ##STR1## wherein: R is hydrogen or monocyclicaryloxycarbonyl, R.sub.1 is hydrogen or monocyclicaryloxycarbonyl; and R.sub.2 is selected from the group consisting of loweralkyl, loweralkoxycarbonyl aminoloweralkyl, hydroxyloweralkyl, hydroxy-substituted aminolowerakyl, an amino acid residue, and N-protected amino acid residue, or when R and R.sub.1 are hydrogen, R.sub.2 can also be hydrogen; and the acid addition salts thereof when R,R.sub.1 or R.sub.2 are hydrogen or an unprotected aminoacid residue.
Abstract: A fortimicin intermediate selected from the group consisting of 1,2',6'-tri-N-benzyloxycarbonylfortimicin B-4,5-carbamate and 1,2',6'-tri-N-acetylfortimicin A-4,5-carbamate. The compounds are useful as intermediates in the preparation of 2-epi-fortimicin B.
Abstract: 2',6'-Di-N-benzyloxycarbonylfortimicin B-1,2:4,5-bis-carbamate and fortimicin B-1,2:4,5-bis-carbamate and its salt are provided by the present invention. The compound is represented by the formula ##STR1## wherein each R is either hydrogen or benzyloxycarbonyl The bis-carbamate is useful as in intermediate in the preparation of fortamine bis-carbamate, which in turn is useful as an intermediate in the preparation of aminoglycoside antibiotics via glycosidation with suitably protected sugar moieties.
Abstract: The present invention provides 2-deoxy-3-O-demethyl-fortimcins A and B and the 4-N-acyl and alkyl derivatives thereof, represented by the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, acyl, aminoacyl,diaminoacyl,N-monoloweralkylaminoalkyl,N,N-diloweralkylaminoalky l, hydroxy-substituted aminoacyl,loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl and hydroxy-substituted aminoloweralkyl and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 26, 1979
Date of Patent:
February 17, 1981
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Johnson
Abstract: Disclosed are 2-deoxy-2-substituted fortimicin A and B derivatives represented by the formula ##STR1## wherein R is hydrogen glycyl, .beta.-alanyl, acetyl, or .beta.-amino lower alkyl, R.sub.1 is hydrogen, amino, azido, halo, glycylamido, .beta.-alanyl amido or 2-O-methanesulfonyl and R.sub.2 is hydrogen or halo and their pharmaceutically acceptable salts. The compounds are active antibacterial agents.
Type:
Grant
Filed:
September 26, 1979
Date of Patent:
February 10, 1981
Assignee:
Abbott Laboratories
Inventors:
Jerry R. Martin, John S. Tadanier, Paulette Johnson, Alex M. Nadzan
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.
Abstract: Described is a vehicle towing hitch designed for permanent installation on the towing vehicle and having a plurality of readily selectable tow balls. The hitch allows the user the ability to select one of any standard tow ball size by simply removing an index pin, rotating the desired tow ball to the upper vertical position, and reinstalling the index pin. In a heavy duty embodiment, a tongue which may be incorporated including a tow pin for receiving the tongue of a towed vehicle such as a trailer as well as an additional large tow ball size.
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 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.sub.9 where R.
Abstract: Derivatives of O-demethylseldomycin factor 5 represented by the following formula are provided: ##STR1## wherein: R is hydrogen or loweralkyl; R.sub.1 and R.sub.2 can be either hydrogen or hydroxy with the limitation that both R.sub.1 and R.sub.2 cannot be hydroxy; R.sub.3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, or ##STR2## with the limitation that when R.sub.1 is hydroxy, R.sub.3 cannot be hydrogen when R is hydrogen; and R.sub.4 is selected from the group consisting of loweralkyl, aminoloweralkyl, diaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, aminohydroxyloweralkyl and N-loweralkylaminohydroxyloweralkyl; and the pharmaceutically acceptable salts thereof. The compounds are potent anti-bacterial agents.
Type:
Grant
Filed:
March 29, 1979
Date of Patent:
December 16, 1980
Assignee:
Abbott Laboratories
Inventors:
Ronald E. Carney, Robert L. Devault, James B. McAlpine, Arthur C. Sinclair
Abstract: Described is a method of treating hypertensive by administering to mammalian patients compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, loweralkyl, lowercycloalkyl, aralkyl, aryl, pyridyl, isoquinolyl, phthalazinyl, or aryl substituted by one or more hydrogen, halo, loweralkyl, lowercycloalkyl, haloloweralkyl, haloloweralkyl, aminosulfonyl, nitro, hydroxy, alkoxy, carboxy, alkoxycarbonyl, cycloalkoxy carbonyl, aminocarbonyl, diloweralkylaminocarbonyl or ##STR2## wherein n is 4 or 5.R.sub.3 is hydrogen, halogen, loweralkyl or aryl, andR.sub.4 is hydrogen, acyl, amino or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
May 7, 1979
Date of Patent:
November 18, 1980
Assignee:
Abbott Laboratories
Inventors:
Martin Winn, Carl W. Nordeen, David L. Arendsen
Abstract: This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.
Type:
Grant
Filed:
January 10, 1979
Date of Patent:
November 4, 1980
Assignee:
Abbott Laboratories
Inventors:
John S. Tadanier, Jerry R. Martin, Paul Kurath