Abstract: The azepine intermediates of the formula ##STR1## wherein R.sub.6 and R.sub.7 are other than hydrogen are disclosed. These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.
Abstract: It would be desirable to have improved designs of ostomy couplings which embody a springy or resilient split ring as a locking ring.In an ostomy coupling, first and second coupling members 50, 60 are held together by a springy flexible split locking ring 70. A plurality of tabs 71 symmetrically arranged on each limb of the locking ring 70, can be withdrawn generally radially outwardly by an upward pull on the locking ring to permit separation of the two coupling members. The ring 70 is generally circular in its unstressed condition.
Type:
Grant
Filed:
April 12, 1996
Date of Patent:
November 3, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Peter L. Steer, Keith G. M. Hollands, Graham Emery Steer, Ronald A. Plass, Howard Barratt
Abstract: Thromboxane receptor antagonist activity is exhibited by compounds of the formula ##STR1## wherein: V is --(CH.sub.2).sub.m --, --O--, or ##STR2## but if V is --O--or ##STR3## R.sup.3 and R.sup.4 must complete an aromatic ring; W is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or phenylene;X is a single bond, --CH.dbd.CH--, --(CH.sub.2).sub.n --, or --O--(CH.sub.2).sub.n --; or X is branched alkylene or --O--branched alkylene wherein W is linked to Y through a chain n carbon atoms long;Y is --CO.sub.2 H, --CO.sub.2 alkyl, --CO.sub.2 alkali metal, --CH.sub.2 OH, --CONHSO.sub.2 R.sup.5, --CONHR.sup.6, or --CH.sub.2 -5-tetrazolyl;Z is O or NH;R.sup.3 and R.sup.4 are each independently hydrogen or alkyl or R.sup.3 and R.sup.4 together complete a ring optionally substituted through a ring carbon with a halo, lower alkyl, phenyl, halo (lower alkyl), halophenyl, oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
Type:
Grant
Filed:
October 7, 1991
Date of Patent:
October 27, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Raj N. Misra, Jagabandhu Das, Steven E. Hall, Wen-Ching Han, Philip M. Sher, Philip D. Stein
Abstract: Methods for the enzymatic resolution of mixtures of enantiomers, such as .beta.-lactam compounds, which may be employed as intermediates in the preparation of taxanes such as taxol, the latter useful in the pharmaceutical field.
Type:
Grant
Filed:
August 1, 1996
Date of Patent:
September 22, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ramesh N. Patel, Laszlo J. Szarka, Richard A. Partyka
Abstract: Nucleic acid sequences, particularly DNA sequences, coding for all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods utilizing these materials. The invention also concerns polypeptide molecules comprising all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, and methods for producing these polypeptide molecules. The invention additionally concerns novel methods for preventing, stabilizing or causing regression of atherosclerosis and therapeutic agents having such activity. The invention concerns further novel methods for lowering serum liquid levels and therapeutic agents having such activity.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 4, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
John R. Wetterau, II, Daru Young Sharp, Richard E. Gregg
Abstract: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
July 7, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Eric M. Gordon, Joel C. Barrish, Gregory S. Bisacchi, Chong-Qing Sun, Joseph A. Tino, Gregory D. Vite, Robert Zahler
Abstract: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
June 2, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Eric M. Gordon, Joel C. Barrish, Gregory S. Bisacchi, Chong-Oing Sun, Joseph A. Tino, Gregory D. Vite, Robert Zahler
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and are thus useful as cardiovascular agents.
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus are useful as cardiovascular agents.
Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## wherein R.sub.2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R.sub.5 is alkyl; R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
Abstract: The invention is a wound dressing prepared from alginate fibers which have good structural integrity, whereby layers are firmly joined together, e.g. by stitching or calendering at a plurality of points to produce a composite fabric.
Type:
Grant
Filed:
October 24, 1995
Date of Patent:
February 3, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
John Charles Fenton, Allison Frances Keys, Peter Michael John Mahoney
Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.
Type:
Grant
Filed:
March 7, 1995
Date of Patent:
January 6, 1998
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
William H. Koster, Joseph E. Sundeen, Henner Straub, Peter Ermann, Uwe D. Treuner, Kent Amsberry, Michael Fakes, Sailesh A. Varia
Abstract: A method of injection moulding an undercut formation on a circular body in which the formation is moulded in a series of arcuate sections alternating with spaces. According to the method, the moulding core, which produces the formation, is extracted by firstly relatively rotating the body and the core so that the body is expanded radially and then ejecting the body off the core. The method is applicable to the manufacture of closure members and coupling elements.
Abstract: An alginate fibre is provided which includes one or more medicaments incorporated into the fibre core such that the one or more medicaments can be released in a sustained manner over time and, optionally, one or more medicaments attached to the surface of the fibre whereby the one or more medicaments attached to the surface of the fibre can be released rapidly therefrom.
Type:
Grant
Filed:
November 22, 1994
Date of Patent:
November 25, 1997
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Bryan Griffiths, Pter Michael John Mahoney
Abstract: Compositions and methods for avidin immobilized on an inert support material, e.g., agarose, are disclosed. The compositions have high activity levels of avidin and may further include a bulking agent, e.g., maltose, and a protectant to maintain the stability and integrity of the avidin agarose during lyophilization and terminal sterilization processes. These compositions have applicability in any instance where avidin agarose and/or the avidin/biotin technology are useful. In particular, the present compositions are useful in an enzyme capture system to prepare fibrin monomer useful for fibrin sealants.
Type:
Grant
Filed:
November 9, 1995
Date of Patent:
November 25, 1997
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Steven James Burton, James C. Pearson, Peter A. D. Edwardson
Abstract: An enzymatic reduction method, particularly a stereoselective enzymatic reduction method, for the preparation of compounds useful as intermediates in the preparation of taxanes.
Type:
Grant
Filed:
February 1, 1995
Date of Patent:
November 11, 1997
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ramesh N. Patel, Amit Banerjee, Clyde G. McNamee, John K. Thottathil, Laszlo J. Szarka
Abstract: A method is provided for treatment of Parkinson's disease or controlling movement of a Parkinsonian patient by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, (for example, tolbutamide), or quinine.
Abstract: A container for receiving and separating blood plasma into its ingredients that has two sealingly coupled sections (1 and 2). One container section (2) and the adjacent portion of the other container section are made of solid material, and the two container sections are screwed together. The container sections (1 and 2) comprise their respective chambers (29 and 30) for receiving their respective fluid ingredients, and these chambers are interconnected through a connecting channel (31) through the abutting portions, at which the container sections (1 and 2) are screwed together. A valve seat (21, 27) is shaped at each end of the connecting channel (31) for each valve member (22, 16) for a sealing closing of the chambers (29, 30) in the separated state of the container sections (1, 2).
Abstract: A method for the production of taxanes such as taxol. The method includes inducing formation of callus cells by contacting an explant tissue with a liquid medium without complete submergence of the tissue in the medium. The callus cells formed are employed in a liquid suspension cell culture to produce one or more taxanes.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 9, 1997
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Paul M. Cino, Steven R. Schwarz, Dana L. Cazzulino
Abstract: A coupling, which may be an ostomy coupling but could be any kind of tube or pipe coupling, includes a first coupling member 10 and a second coupling member 30 which are mutually interengageable and which surround an orifice 70. The coupling also includes a resilient split ring 50 which encircles the two coupling members and has a handle member 51 which can be manipulated to cause the split ring to be deformed. This causes the radially-inwardly extending tabs 52 on the ring to be shifted between respective first positions in which the split ring is undeformed and the tabs lock the two coupling members together and respective second positions in which the split ring is deformed in such a way as to shift the tabs radially outwardly to positions where they permit separation of the two coupling members.The split ring is desirably made of a relatively rigid but springy plastics material, for example an acetal resin.