Abstract: The invention relates to novel substituted [2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy]-alkanoic acids their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
December 23, 1985
Date of Patent:
November 25, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Adolph M. Pietruszkiewicz, Otto W. Woltersdorf, Jr.
Abstract: An improved method for the direct preparation of an enantiomer of a substituted fluorenyloxyacetic acid including the enhancement of a chiral phase transfer alkylation step in the synthesis using a non-ionic surfactant as co-catalyst. The substituted fluorenyloxyacetic acid is useful in the treatment of brain edema.
Abstract: A process for direct preparation of an enantiomer of a substituted fluorenyloxyacetic acid is disclosed. The acetic acid derivative is useful for treating brain edema.
Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
May 1, 1984
Date of Patent:
August 12, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
May 1, 1984
Date of Patent:
August 12, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
May 1, 1984
Date of Patent:
August 5, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: The invention relates to novel [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-yl)oxy]ethanimidamid es and [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidic acid hydrazides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
Type:
Grant
Filed:
September 26, 1985
Date of Patent:
August 5, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
May 1, 1984
Date of Patent:
June 24, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: A process for direct preparation of enantiomers of a substituted fluorenyloxyacetic acid is disclosed. The acetic acid derivative is useful for treating brain edema.
Abstract: The invention relates to novel substituted [(2,3-dihydro-1-oxo-1H-inden-5-yl)amino]alkanoic acids, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
Type:
Grant
Filed:
August 2, 1985
Date of Patent:
April 1, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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 for reducing intraocular pressure, for use as .alpha.- and .beta.-and adrenergic blocking agents, as antihypertensive agents and for effecting bronchodilation.
Type:
Grant
Filed:
March 25, 1982
Date of Patent:
February 4, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, John J. Baldwin, David E. McClure
Abstract: Novel amino-phenyl-thiadiazoledioxides and related compounds and processes for preparing such compounds are disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.
Type:
Grant
Filed:
June 7, 1983
Date of Patent:
January 28, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Adolph Pietruszkiewicz, William A. Bolhofer, William C. Lumma, Jr.
Abstract: Aqueous compositions containing a thickener, a hypochlorite and cyanuric acid are disclosed. They are especially useful as hydraulic fracturing fluids.
Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-diones, which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
Type:
Grant
Filed:
January 25, 1985
Date of Patent:
January 7, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Roger M. Freidinger, Ben E. Evans, George D. Hartman
Abstract: The present application is concerned with compounds useful as carriers of cytotoxic agents. More particularly it deals with derivatives of steroid compounds having a 5-androstene carbon skeleton and having an oleyl ester at the 3-position and having a 17-carbamyl alkyl substituent which linked to cytotoxic agents for delivery to cancer cells exclusively via the low-density lipoprotein (LDL) pathway.