Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.
Abstract: Antibacterial activity is exhibited by .beta.-lactams having a sulfate substituent in the 1-position and an acylamino substituent in the 3-position.
Abstract: 7-Oxabicycloheptane substituted enaminone prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: A drainage bag employs a non-return valve assembly including at least one baffle positioned between the top and bottom of the bag. Each baffle extends completely across the interior of the bag and includes an upper portion which is continuously attached to one face of the bag and a lower portion which is attached to an opposite face of the bag at spaced intervals so as to form at least one opening adapted to permit liquid to flow readily from the top of the bag to the bottom of the bag while inhibiting liquid from flowing from the bottom of the bag to the top of the bag.
Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## or the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, alkanoyloxyalkyl, arylcarbonyloxyalkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl;R.sub.2 is hydrogen, hydroxy, alkoxy, aryloxy, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or halogen;R.sub.3 is hydrogen, methyl, hydroxy or halogen; andn is 0, 1 or 2.
Abstract: A pharmaceutically acceptable salt of (R)-3-(acetylamino)-3-methoxy-2-oxo-1-azetidinesulfonic acid can be prepared by culturing Chromobacterium violaceum A.T.C.C. No. 31532 at about 25.degree. C. under submerged aerobic conditions on an aqueous nutrient medium containing an assimilable carbohydrate and nitrogen source.
Type:
Grant
Filed:
November 5, 1984
Date of Patent:
July 16, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Richard B. Sykes, William L. Parker, Christopher M. Cimarusti, William H. Koster, William A. Slusarchyk
Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, mono-, di- or trifluoroalkyl, ##STR2## aryl or alkylthioalkyl, wherein R.sub.6 is alkyl or aryl and m is 1, 2, 3 or 4;R.sub.2 is ##STR3## wherein R.sub.7, R.sub.8 and R.sub.9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2;with the proviso that if R.sub.1 is alkylthioalkyl, n is 0.
Abstract: 7-Oxabicycloheptane substituted oxamide prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: 7-Oxabicycloheptane substituted oxo prostaglandin analogs are provided having the structural formula ##STR1## wherein R is hydrogen, lower alkyl, alkali metal or tris(hydroxymethyl)aminomethane, R.sup.1 and R.sup.2 may be the same or different and are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl, aryl or cycloalkyl, A is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --, m is 1 to 8, and n is 1 to 4, p is 1 to 12 and q is 0 to 5, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: 7-Oxabicycloheptane substituted thiocarbamate prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: Acyloxyketone substituted imino and amino acids of the formula ##STR1## are disclosed. These compounds are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.
Abstract: 7-Oxabicycloheptane ethers of prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: 7-Oxabicycloheptane substituted interphenylene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: Tetrahydrofuranyl substituted ethers are provided having the structural formula ##STR1## wherein A is (CH.sub.2).sub.2, CH.dbd.CH or a single bond, m is 1 to 5, B is a single bond or CH.dbd.CH, n is 1 to 4, X is O or ##STR2## wherein n' is 0, 1 or 2, R is H, lower alkyl or alkali metal and R.sup.1 is lower alkyl, arylalkyl, aryl, cycloalkyl, cycloalkylalkyl or lower alkenyl and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease and as antiinflammatory agents and analgesics.
Abstract: An insert, having a non-heat sealable surface, is affixed to a first thin film wall. The first wall is aligned with a second thin film wall, with the non-heat sealable surface of the insert facing the interior surface of the second wall. The walls are welded along their periphery to form the contour of the pouch. An adhesive-backed label is then welded to the exterior of the second wall. The insert prevents the interior surfaces of the walls from being sealed together as the adhesive-backed label is welded, simplifying the manufacturing process. The non-heat sealable surface of the insert may be composed of a low friction material to facilitate movement of solid waste within the pouch.
Abstract: A method is provided for preparing intermediates for use in preparing 7-oxabicycloheptane prostaglandin derivatives which method includes the steps of reducing (exo)hexa hydro-4,5-epoxyisobenzofuran-1,3-dione to the corresponding diol, subjecting the diol to a chloroformylation reaction to form a compound of the structure ##STR1## reacting the above with pyridine to form the cyclic carbonate reacting the cyclic carbonate with an alkanol to form the alcohol of the strucure ##STR2## tosylating the above alcohol to form the tosylate and subjecting the above tosylate to a cyanation reaction to form the cyano carbonate of the structure ##STR3## The cyano carbonate may then be reduced by, for example, reaction with diisobutyl aluminum hydride to form the hemiacetal ##STR4## which is used in preparing 7-oxabicycloheptane prostaglandin derivatives as disclosed in U.S. Pat. No. 4,143,054.New intermediates of the structures set out above, other than the hemiacetal, are also provided.
Abstract: Hydroxy substituted peptide compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Type:
Grant
Filed:
July 21, 1983
Date of Patent:
April 30, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Eric M. Gordon, Jollie D. Godfrey, Jr., Sesha I. Natarajan
Abstract: 7-Oxabicycloheptane ethers of prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: Compounds of the formula ##STR1## and X is an oxo substituted thiazine or thiazepine are disclosed. These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.
Type:
Grant
Filed:
March 1, 1984
Date of Patent:
April 23, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Harold N. Weller, III, Eric M. Gordon, Donald S. Karanewsky, Denis E. Ryono