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5596012 Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
PATENT ABSTRACTS
sublingual administration, or administration of a recombinant DNA molecule which expresses a DNA segment that encodes the matrix metalloproteinase inhibitor of this invention.
5595904 FAMILY OF MAP2 PROTEIN KINASES Boulton Teri G; Cobb Melanie H; Yancopoulos George D; Nye Steve; Panayotatos Niko Irving, TX, UNITED STATES Assigned to Board of Regents Univ of Texas; Regeneron Pharmaceuticals Inc The present invention relates to a newly identified family of protein serine/threonine kinases which phosphorylate microtub,de-associated protein 2 (MAP2). It is based, in part, on the cloning and characterization of novel MAP2 kinases designated extraceUular signal-regulated kinase 1, 2, and 3 (ERK1, ERK2, ERK3) which are expressed in the central nervous system, and on the identification of another ERK family member, ERK4, with antisera. The present invention provides for recombinant nucleic acid molecules and proteins representing members of the MAP2 ldnase family, and also for microorganisms, transgenic animals, and cell lines comprising recombinant MAP2 Idnase molecules. In additional embodiments of the invention, the present invention provides for methods for assaying cellular factor activity, including, but not limited to, nerve growth factor activity, in which the activation of MAP2 kinase serves as an indicator of cellular factor activity. These methods
521
may be extremely useful in screening compounds for the presence of a desired cellular factor activity. In specific embodiments, compounds which may be useful in the treatment of Alzheimefs disease, peripheral neuropathies, and diabetes may be identified using the methods of the invention.
5596012 SACCHARIN DERIVATIVES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS AND COMPOSITIONS AND METHOD OF USE THEREOF Dunlap Richard P; Boaz Neil W; Mura Albert J; Hlasta Dennis J; Desai Ranjit C; Subramanyam Chakrapani; Latimer Lee H; Lodge Eric P Penfield, NY, UNITED STATES Assigned to Sterling Winthrop Inc Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula (*See Patent for Chemical Structure*) wherein: L is -O-, -S-, -SO-or -SO2-; m and n are each independently 0 or 1; R1 is halo, lower-alkanoyl, l-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is -O- and n is 1, cycloheptatrienon-2-yl or, when L is -Sand n is 1, cyano or Iower-aikoxythiocarbonyl or, when L is -SO2- and n is 1, iower-alkyi or trifluoromethyl; R2 is hydrogen, lower-alkoxycarbceyL phenyl or phenylthio; and R3 and R4 are each hydrogea or various substituents and p r ~ for preparation and pharmaceutical compositions and method of use thereof are disclosed.
sublingual administration, or administration of a recombinant DNA molecule which expresses a DNA segment that encodes the matrix metalloproteinase inhibitor of this invention.
5595904 FAMILY OF MAP2 PROTEIN KINASES Boulton Teri G; Cobb Melanie H; Yancopoulos George D; Nye Steve; Panayotatos Niko Irving, TX, UNITED STATES Assigned to Board of Regents Univ of Texas; Regeneron Pharmaceuticals Inc The present invention relates to a newly identified family of protein serine/threonine kinases which phosphorylate microtub,de-associated protein 2 (MAP2). It is based, in part, on the cloning and characterization of novel MAP2 kinases designated extraceUular signal-regulated kinase 1, 2, and 3 (ERK1, ERK2, ERK3) which are expressed in the central nervous system, and on the identification of another ERK family member, ERK4, with antisera. The present invention provides for recombinant nucleic acid molecules and proteins representing members of the MAP2 ldnase family, and also for microorganisms, transgenic animals, and cell lines comprising recombinant MAP2 Idnase molecules. In additional embodiments of the invention, the present invention provides for methods for assaying cellular factor activity, including, but not limited to, nerve growth factor activity, in which the activation of MAP2 kinase serves as an indicator of cellular factor activity. These methods
521
may be extremely useful in screening compounds for the presence of a desired cellular factor activity. In specific embodiments, compounds which may be useful in the treatment of Alzheimefs disease, peripheral neuropathies, and diabetes may be identified using the methods of the invention.
5596012 SACCHARIN DERIVATIVES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS AND COMPOSITIONS AND METHOD OF USE THEREOF Dunlap Richard P; Boaz Neil W; Mura Albert J; Hlasta Dennis J; Desai Ranjit C; Subramanyam Chakrapani; Latimer Lee H; Lodge Eric P Penfield, NY, UNITED STATES Assigned to Sterling Winthrop Inc Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula (*See Patent for Chemical Structure*) wherein: L is -O-, -S-, -SO-or -SO2-; m and n are each independently 0 or 1; R1 is halo, lower-alkanoyl, l-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is -O- and n is 1, cycloheptatrienon-2-yl or, when L is -Sand n is 1, cyano or Iower-aikoxythiocarbonyl or, when L is -SO2- and n is 1, iower-alkyi or trifluoromethyl; R2 is hydrogen, lower-alkoxycarbceyL phenyl or phenylthio; and R3 and R4 are each hydrogea or various substituents and p r ~ for preparation and pharmaceutical compositions and method of use thereof are disclosed.