Abstract: 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, a class of compounds possessing anti-allergic properties for use in the treatment of allergic conditions, such as asthma prepared by etherifying an alkanoylphenol with an aminoalkyl halide, converting the ether formed to a salt of Mannich base by reacting it with a salt of a secondary amine in the presence of formaldehyde or paraformaldehyde and treating the Mannich salt with a weak base to deaminate the same and form the final product.
Abstract: Dichloroamino acid derivatives other than .alpha.-dichloroamino acids are prepared from chlorination of corresponding amino acids, and are found to be potent germicidal and fungicidal agents.
Abstract: Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C.sub.1 -C.sub.4 alkyl; n is 0 or 1; R.sub.1 and R.sub.2 are each selected from a variety of unsubstituted or substituted hydrocarbon radicals, or are combined so that --NR.sub.1 R.sub.2 represents the residue of a saturated or unsaturated heterocyclic compound containing one secondary nitrogen atom; and R.sub.3 is H or one of a variety of other substituents. Salts and N-oxides of compounds of formula (I) and the corresponding diacyloxy derivatives of known bio-affecting carboxylic acids HOOC-R'-COOH are disclosed also.
Abstract: Improved yields of Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids have been achieved from processes based on modifications performed on a pyrrole carboxylic ester rather than on a pyrrole-.alpha.-oxoacetate.
Type:
Grant
Filed:
December 11, 1981
Date of Patent:
April 19, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Bruce E. Witzel, Paul E. Finke, Debra L. Allison
Abstract: 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones of the formula: ##STR1## are inhibitors of glycolic acid oxidase useful in treating or preventing calcium oxalate kidney or bladder stones.
Type:
Grant
Filed:
June 1, 1981
Date of Patent:
April 12, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
Abstract: Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.
Abstract: Zomepirac and its analogs have been prepared from a 5-aroyl-3-hydroxycarbonyl-4-substituted pyrrole-2-acetic acid via acidic decarboxylation.
Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.
Type:
Grant
Filed:
July 25, 1980
Date of Patent:
October 19, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Tsung-Ying Shen, Howard Jones, Conrad P. Dorn
Abstract: Novel amino derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctenes, methods for their preparation, and their use as effective analgesic agents is described.
Abstract: The invention relates to 1-[4-(4-sulfanilyl)phenyl] urea and derivatives thereof in pharmaceutical compositions and in methods of treating rheumatoid arthritis and immune complex diseases such as dermatitis herpetiformis.
Type:
Grant
Filed:
February 29, 1980
Date of Patent:
July 6, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Norman P. Jensen, David P. Jacobus, Howard Jones
Abstract: 2-Substituted-aminopropene and propanenitriles of the formula: ##STR1## are effective antimicrobial agents (compounds of Formula II.), and potent anti-inflammatory agents of decreased acute toxicity (compounds of Formula I.).
Type:
Grant
Filed:
December 26, 1979
Date of Patent:
June 15, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
Abstract: Novel substituted-benzyl derivatives of 11-endo-amino-5,6,7,8,9,10-hexahydro-2-hydroxy (or methoxy)-6,9-methanobenzocyclooctene (or nonene) of the formula: ##STR1## are centrally-acting analgesics effective in the relief of pain.
Abstract: Novel N-(substituted) derivatives of 2,5-ethano-8-hydroxy (or methoxy)-1,2,3,4,5,6-hexahydro-3 (or 4)-benzazocine of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
Abstract: Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.
Abstract: A method of preparing 2,4-difluoroaniline by reacting 2,4,5-trichloronitrobenzene with a fluorinating agent to form 2,4-difluoro-5-chloronitrobenzene which is then hydrogenated with hydrogen in the presence of a catalyst to form 2,4-difluoroaniline.
Type:
Grant
Filed:
October 31, 1977
Date of Patent:
October 13, 1981
Assignee:
Merck & Co., Inc.
Inventors:
Roger J. Tull, Leonard M. Weinstock, Ichiro Shinkai