Abstract: The present invention relates to a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, lower alkenyl, lower alkynyl, cycloalkyl and cycloalkylalkyl; R.sub.2 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, halogen and loweralkoxy; R.sub.3 is selected from hydrogen, loweralkyl, and halogen; R* and R** are independently selected from loweralkyl and P.sub.1 is hydrogen or an nitrogen-protecting group; or an acid addition salt thereof.
Type:
Grant
Filed:
January 10, 1992
Date of Patent:
May 11, 1993
Assignee:
Abbott Laboratories
Inventors:
Howard E. Morton, Biswanath De, Daniel J. Kerkman
Abstract: The present invention relates to the use of renin inhibitors and to renin inhibitor compositions for prevention, treatment, inhibition or reversal of renal dysfunction or disease, especially renal failure.
Abstract: A pharmaceutical composition comprising a solution of a tenin inhibitor of the formula: ##STR1## wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, p-methoxybenzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --;R.sub.4 is loweralkyl or cyclopropyl;R.sub.5 is hydrogen or loweralkyl; andX is CH.sub.2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof in a pharmaceutically acceptable solvent, said solution being encapsulated in a soft elastic gelatin capsule.
Type:
Grant
Filed:
July 29, 1991
Date of Patent:
January 12, 1993
Assignee:
Abbott Laboratories
Inventors:
Kevin G. Garren, Madhu K. Vadnere, John J. Wieland, Mary J. Leveque
Abstract: A sustained-release coating composition is described that contains an ethylcellulose and/or a methacrylic methylester together with a plasticizer and a detackifying agent. Sized drug granules are coated with this composition and then mixed with a polymeric composition containing at least one viscosity agent and formed into drug dosage units for the administration and sustained release of the drug in a patient. The sustained-release drug dosage units described produce a continuous, slow release of the drug at a therapeutically effective dosage level when administered to a patient.
Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.
Type:
Grant
Filed:
April 18, 1991
Date of Patent:
November 17, 1992
Assignee:
Abbott Laboratories
Inventors:
Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
Abstract: A novel process for the preparation of .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids is disclosed. These .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids are useful as intermediates for the preparation of enzyme inhibitors (for example, renin inhibitors) and other peptides or amino acid derivatives or analogs.
Abstract: Compounds are disclosed which are retroviral protease inhibitors. Also disclosed are methods of using the compounds and compositions for inhibiting a retroviral protease and for treating an HIV infection.
Type:
Grant
Filed:
March 27, 1991
Date of Patent:
September 29, 1992
Assignee:
Abbott Laboratories
Inventors:
Hing L. Sham, Daniel W. Norbeck, Dale J. Kempf, Chen Zhao
Abstract: A retroviral protease inhibiting compound of the formulaA--X--Bor a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group; A is(1) substituted amino,(2) substituted carbonyl,(3) functionalized imino,(4) functionalized alkyl,(5) functionalized acyl,(6) functionalized heterocyclic or(7) functionalized (heterocyclic)alkyl; and B is(1) substituted carbonyl independently defined as herein,(2) substituted amino independently defined as herein,(3) functionalized imino independently defined as herein,(4) functionalized alkyl independently defined as herein,(5) functionalized acyl independently defined as herein,(6) functionalized heterocyclic independently defined as herein or(7) functionalized (heterocyclic)alkyl independently defined as herein.
Type:
Grant
Filed:
May 9, 1990
Date of Patent:
August 25, 1992
Assignee:
Abbott Laboratories
Inventors:
Dale J. Kempe, Daniel W. Norbeck, John W. Erickson
Abstract: The present invention relates to novel LHRH analogs. The LHRH analogs include "pseudo" hexapeptide, heptapeptide, octapeptide and nonapeptide analogs of LHRH, wherein all or some of the amino acids, 1, 2 and 3 have been eliminated and the remaining (2-9), (2-10), (3-9), (3-10), (4-9) or (4-10) peptide is linked to various carboxylic acids which take the place of amino acids 1, 2 or 3 in LHRH.
Type:
Grant
Filed:
July 10, 1990
Date of Patent:
August 18, 1992
Assignee:
Tap Pharmaceuticals, Inc.
Inventors:
Fortuna Haviv, Jonathan Greer, Christopher A. Palabrica, Timothy D. Fitzpatrick
Abstract: The present invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R.sub.2 is lower alkoxy; or R.sub.1 and R.sub.2 together form a methylenedioxy or ethylenedioxy ring; R.sub.3 and R.sub.4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R.sub.7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and ##STR2## where R.sub.13 and R.sub.14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy.The compounds of the present invention selectively inhibit .alpha..sub.2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
Type:
Grant
Filed:
January 25, 1990
Date of Patent:
July 7, 1992
Assignee:
Abbott Laboratories
Inventors:
John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.
Type:
Grant
Filed:
August 23, 1990
Date of Patent:
July 7, 1992
Assignee:
Abbott Laboratories
Inventors:
Alex M. Nadzan, James F. Kerwin, Chun W. Lin
Abstract: Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R.sub.1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;R.sub.2 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.3 is --OH or --NH.sub.2 ;R.sub.4 is(a) --CH(OH)--R.sub.5 wherein R.sub.5 is loweralkyl, cycloalkyl or cycloalkylalkyl or(b) --CH.sub.2 CH(R.sub.6)C(O)NHR.sub.7 wherein R.sub.6 is loweralkyl and R.sub.7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andA is ##STR2## wherein R.sub.8 is arylalkyl, B is --C(O) or --S(O).sub.2 -- and R.sub.9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R.sub.10 is arylalkyl and R.sub.11 is (a) --C(O)R.sub.12 wherein R.sub.12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O).sub.2 --R.sub.
Type:
Grant
Filed:
June 13, 1991
Date of Patent:
June 9, 1992
Assignee:
Abbott Laboratories
Inventors:
Robert C. Goldman, William R. Baker, Hwan-Soo Jae, Biswanath De, Thomas M. Zydowsky, Edwin de Lara
Abstract: The present invention relates to novel "pseudo" nonapeptide and decapeptide derivatives of LHRH. More particularly the present invention relates to derivatives of LHRH wherein the nitrogen atom of at least one of the amide bonds has been alkylated.
Abstract: A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are useful in the production of these carboxylic acids.
Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sup.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl; phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl; lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.
Type:
Grant
Filed:
June 10, 1991
Date of Patent:
February 25, 1992
Assignee:
Abbott Laboratories
Inventors:
Jay R. Luly, Jacob J. Plattner, Dale J. Kempf
Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.
Type:
Grant
Filed:
March 26, 1990
Date of Patent:
February 4, 1992
Assignee:
Abbott Laboratories
Inventors:
John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
Abstract: Compositions and methods for treating bacterial infections are disclosed. Compositions of a quinolone carboxylic acid or a pharmaceutically acceptable salt or metal ion-acid complex thereof and a polymeric additive that reduces vein irritation upon infusion are described and utilized as antibacterial agents. The compositions of the present invention are parenterally administered to a patient.
Type:
Grant
Filed:
January 5, 1990
Date of Patent:
January 28, 1992
Assignee:
Abbott Laboratories
Inventors:
Martin H. Yunker, Jacqueline E. Briskin, David L. Schwinke