Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.3 is a readily removable carboxyl protecting group.
Type:
Grant
Filed:
March 29, 1982
Date of Patent:
November 8, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
Abstract: Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.
Abstract: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are Z-2-(2,2-dimethylcyclo-propanecarboxamido)-.omega.-pyridylthio-2-alkenoic acids (and related arylthio and heterocyclylthio analogs).
Type:
Grant
Filed:
July 23, 1981
Date of Patent:
September 27, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Louis Barash, Jeannette E. Brown, Donald W. Graham
Abstract: An aqueous suspension containing methyldopa and sucrose is disclosed. This composition is an oral dosage form for treating hypertension that is bioavailable.
Abstract: In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## there is disclosed a process for preparing III via ##STR2## wherein R is a protecting group.
Type:
Grant
Filed:
January 21, 1981
Date of Patent:
August 23, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Ronald W. Ratcliffe, Thomas N. Salzmann
Abstract: Novel substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts, certain intermediates and their preparation are disclosed. These pyridines have pharmaceutically useful properties such as .beta.-adrenergic blocking activity.
Abstract: Some derivatives of interphenylene-9-thia-11-oxo-12-azaprostanoic acid which are active renal vasodilator agents are resolved via diastereomeric camphanyl or camphorcarbonyl esters. Upon hydrolysis, the separated diastereoisomers yield optically pure enantiomers.
Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
Abstract: A pharmaceutical composition containing an interphenylene 9-thia-11-oxo-12-aza prostanoic acid type renal vasodilator and a non-steroidal anti-inflammatory agent and its use are disclosed.
Abstract: The present application discloses certain 2-substituted propoxy-3-cyano-5-hydroxypyridines. The compounds have pharmaceutical activity e.g. as antihypertensives.
Type:
Grant
Filed:
February 10, 1981
Date of Patent:
February 15, 1983
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Stanley Vickers, Alfred Steuerwald
Abstract: Heterocyclic aminoethanols of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.
Type:
Grant
Filed:
December 23, 1980
Date of Patent:
November 9, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, John J. Baldwin, David E. McClure
Abstract: Compounds of the formula Het--O--CH.sub.2 --CHOR--CH.sub.2 -NHaralkyl where Het is a 10 membered N-containing ring are disclosed. The compounds are useful as pharmaceuticals.
Abstract: Heterocyclic ethanolamines of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.