Patents Represented by Attorney Steven R. Crowley
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Patent number: 5342981Abstract: The present invention relates to intermediates useful in a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.2a is hydrogen or loweralkyl, R.sub.2b is hydrogen, loweralkyl, cycloalkyl or phenyl and R.sub.1 is cycloalkyl, cycloalkylalkyl, phenyl or benzyl. These intermediates are compounds of the formula: ##STR2## wherein P.sub.2 is an O-protecting group, P.sub.3 is an N-protecting group and R.sub.1, R.sub.2a and R.sub.2b are defined as above.Type: GrantFiled: February 10, 1993Date of Patent: August 30, 1994Assignee: Abbott LaboratoriesInventors: Daniel J. Plata, Anthony K. L. Fung, Howard E. Morton, Robert Leanna, William R. Baker, John K. Pratt
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Patent number: 5340802Abstract: Peptide analog type-B CCK receptor ligands or pharmaceutically-acceptable salts thereof, which are useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and for the treatment of shock, respiratory and cardiocirculatory insufficiencies.Type: GrantFiled: January 29, 1993Date of Patent: August 23, 1994Assignee: Abbott LaboratoriesInventors: Kazumi Shiosaki, Alex M. Nadzan, David S. Garvey, Youe-Kong Shue, Mark S. Brodie, Mark W. Holladay, John Y.-L. Chung, Michael D. Tufano, Paul D. May
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Patent number: 5338726Abstract: Compounds are disclosed which inhibit endothelin converting enzyme. These compounds are useful for treating hypertension, congestive heart failure, myocardial infarction, reperfusion injury, coronary angina, cerebral vasospasm, acute renal failure, non-steroidal antiinflammatory drug induced gastric ulceration, cyclosporin induced nephrotoxicity, endotoxin-induced toxicity, asthma and atherosclerosis.Type: GrantFiled: September 29, 1992Date of Patent: August 16, 1994Assignee: Abbott LaboratoriesInventors: Kazumi Shiosaki, Andrew S. Tasker, Terry J. Opgenorth
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Patent number: 5332742Abstract: A renin inhibiting compound of the formula: ##STR1## wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-l-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, 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 isobutyl 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; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.Type: GrantFiled: November 3, 1993Date of Patent: July 26, 1994Assignee: Abbott LaboratoriesInventor: Saul H. Rosenberg
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Patent number: 5326776Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.Type: GrantFiled: February 24, 1993Date of Patent: July 5, 1994Assignee: Abbott LaboratoriesInventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Kenneth P. Spina, Thomas W. von Geldern, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
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Patent number: 5310740Abstract: A renin inhibiting compound 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, 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 isobutyl 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; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.Type: GrantFiled: June 19, 1992Date of Patent: May 10, 1994Assignee: Abbott LaboratoriesInventors: Saul H. Rosenberg, Jon F. Denissen
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Patent number: 5284849Abstract: A renin inhibiting compound 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, 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 isobutyl 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; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.Type: GrantFiled: August 14, 1992Date of Patent: February 8, 1994Assignee: Abbott LaboratoriesInventors: Saul H. Rosenberg, Jon F. Denissen
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Patent number: 5284954Abstract: The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: ##STR1## or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.Type: GrantFiled: September 30, 1992Date of Patent: February 8, 1994Assignee: Abbott LaboratoriesInventors: Steven J. Wittenberger, Bikshandar A. Narayanan, Anthony R. Haight, David Scarpetti
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Patent number: 5275950Abstract: Intermediates and a process for their preparation are disclosed which are useful for the preparation of a renin inhibiting compound of the formula: ##STR1## wherein R is a nitrogen-containing heterocycle which is bonded via a nitrogen atom to the sulfonyl group, R.sub.6 is hydrogen, alkoxy, halogen or loweralkyl, R.sub.7 is loweralkyl having 2 to 7 carbon atoms, and R.sub.8 is loweralkyl, cycloalkyl, or aryl or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: February 10, 1993Date of Patent: January 4, 1994Assignee: Abbott LaboratoriesInventors: Daniel A. Dickman, Bruce W. Horrom, Chi-Nung W. Hsiao, M. Robert Leanna, Hormoz Mazdiyasni, Howard E. Morton, Thomas M. Zydowsky, William R. Baker, Stephen L. Condon
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Patent number: 5276031Abstract: 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.Type: GrantFiled: October 26, 1992Date of Patent: January 4, 1994Assignee: Abbott LaboratoriesInventor: Hollis D. Kleinert
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Patent number: 5270302Abstract: Selective and potent Type-A CCK receptor agonists of formula (I):X--Y--Z--Q (I)or a pharmaceutically acceptable salt thereof, wherein,X is selected from ##STR1## Y is selected from ##STR2## Z is ##STR3## and Q is ##STR4## or pharmaceutically-acceptable salts thereof, useful in the treatment of gastrointestinal disorders (including gallbladder disorders), central nervous system disorders, insulin-related disorders and pain, as well as in appetite regulation.Type: GrantFiled: June 17, 1991Date of Patent: December 14, 1993Assignee: Abbott LaboratoriesInventors: Kazumi Shiosaki, Alex M. Nadzan, Hana Kopecka, Youe-Kong Shue, Mark W. Holladay, Chun W. Lin, Hugh N. Nellans
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Patent number: 5268182Abstract: 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.Type: GrantFiled: August 14, 1992Date of Patent: December 7, 1993Assignee: Abbott LaboratoriesInventors: Dale R. Brinker, Enrique D. Eveline
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Patent number: 5268374Abstract: The present invention relates to renin inhibiting compounds of the formula: ##STR1##Type: GrantFiled: May 22, 1991Date of Patent: December 7, 1993Assignee: Abbott LaboratoriesInventors: Anthony K. L. Fung, William R. Baker, Yoek-Lin Armiger, Saul H. Rosenberg, Biswanath De, Jacob J. Plattner, Steven A. Boyd, Dale J. Kempf, Hing L. Sham, Hollis D. Kleinert, Robert A. Mantei
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Patent number: 5268476Abstract: 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.Type: GrantFiled: July 6, 1992Date of Patent: December 7, 1993Assignee: Abbott LaboratoriesInventor: Thomas M. Zydowsky
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Patent number: 5258362Abstract: A renin inhibiting compound of the formula: ##STR1## wherein R.sub.0 is a mimic of the Phe-His dipeptide sequence of angiotensinogen which preceeds the renin cleavage site;R.sub.4 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.5 is hydrogen, loweralkyl, hydroxyalkyl, loweralkenyl or formyl;R.sub.6 is --OH or --NH.sub.2 ; andD is ##STR2## wherein R.sub.7 is hydrogen or loweralkyl and R.sub.8 is hydrogen, loweralkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, cycloalkylalkyl, loweralkenyl, alkynyl, aryl, arylalkyl, heterocyclic or heterocyclicalkyl; or R.sub.7 and R.sub.8 taken together --(CH.sub.2).sub.n -- wherein n is 3-6; and R.sub.9 is loweralkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: May 13, 1992Date of Patent: November 2, 1993Assignee: Abbott LaboratoriesInventor: Saul H. Rosenberg
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Patent number: 5256677Abstract: 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: GrantFiled: June 19, 1992Date of Patent: October 26, 1993Assignee: Abbott LaboratoriesInventors: Hing L. Sham, Daniel W. Norbeck, Dale J. Kempf, Chen Zhao
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Patent number: 5250548Abstract: Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Abbott LaboratoriesInventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
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Patent number: 5244910Abstract: A renin inhibiting compound of the formula: ##STR1## wherein X is O NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-(methoxymethoxy)piperidin-1 -yl)carbonyl-2- phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopropylhexanamid e.Type: GrantFiled: July 31, 1991Date of Patent: September 14, 1993Assignee: Abbott LaboratoriesInventors: William R. Baker, Steven A. Boyd, Anthony K. L. Fung, Herman H. Stein, Jon F. Denissen, Charles W. Hutchins
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Patent number: 5229518Abstract: The present invention relates to intermediates useful in the process for the preparation of a compound of the formula: ##STR1## wherein R.sub.2a is hydrogen or loweralkyl, R.sub.2b is hydrogen, loweralkyl, cycloalkyl or phenyl and R.sub.1 is loweralkyl, cycloalky, cycloalkylalkyl, phenyl or benzyl. These intermediates are compounds of the formula: ##STR2## wherein R.sub.1, R.sub.2a and R.sub.2b are defined as above.Type: GrantFiled: November 20, 1991Date of Patent: July 20, 1993Assignee: Abbott LaboratoriesInventors: Daniel J. Plata, Anthony K. L. Fung, Howard E. Morton, M. Robert Leanna, William R. Baker, John K. Pratt
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Patent number: 5214129Abstract: 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.sub.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, loweralkenyl, 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: GrantFiled: November 18, 1991Date of Patent: May 25, 1993Assignee: Abbott LaboratoriesInventors: Jay R. Luly, Jacob J. Plattner, Dale J. Kempf