Patents Assigned to Merck Sharpe & Dohme
  • Patent number: 5310899
    Abstract: A process for preparing a single enantiomer of a 4-aryloxyazetidin-2-one derivative in optically pure form comprises reacting a hindered vinyl ester with chlorosulphonyl isocyanate; displacing the hindered acyloxy group with a phenolic derivative containing a protected carboxy group; deprotecting the carboxylate moiety; resolving with a chiral amine; filtering; and regenerating the desired enantiomer by acidification. A method for enriching the product obtained from the acyloxy displacement step in favour of the desired enantiomeric form, by treating with an asymmetric catalyst such as a chiral alkaloid derivative, is provided; as also is a method for racemising the unwanted antipode of the desired 4-aryloxyazetidin-2-one enantiomer. The invention further provides novel enantiomers based on the 4-aryloxyazetidin-2-one ring structure.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: May 10, 1994
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Michael S. Ashwood, Brian C. Bishop, Peter G. Houghton, Guy R. Humphrey
  • Patent number: 5302591
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## R.sup.1 is H, certain optionally substituted alkyl or C.sub.3-7 cycloalkyl;R.sup.2 represents (CH.sub.2).sub.m -tetrazolyl, (CH.sub.2).sub.m -imidazolyl, CONR.sup.6 R.sup.7, CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9, SOC.sub.1-4 alkyl, SO.sub.2 NHR.sup.10, 5-hydroxy-4-pyrone, (CH.sub.2).sub.n CO.sub.2 H, ##STR2## or a group ##STR3## wherein X is O, S or NR.sup.11 ; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.12 ;R.sup.3 represents H or C.sub.1-6 alkyl;R.sup.4 represents 2-, 3- or 4-pyridyl;R.sup.5 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists useful in therapy.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: April 12, 1994
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: S. R. Fletcher, V. G. Matassa
  • Patent number: 5208248
    Abstract: A class of indazole-substituted five-membered heteroaromatic compounds are specific agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: May 4, 1993
    Assignee: Merck Sharpe & Dohme, Ltd.
    Inventors: Raymond Baker, Mark S. Chambers, Leslie J. Street
  • Patent number: 4906761
    Abstract: This invention provides the 4-mono-anion of myo-inositol orthoformate, and describes a process for preparing this anion as well as the use of this anion in the preparation of a variety of mono- and poly-phosphate derivatives of myo-inositol.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: March 6, 1990
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventor: David C. Billington