Abstract: .alpha.-Substituted amines and .alpha.-substituted-.alpha.-amino acids are described which are useful in inhibiting the growth of protozoa in animals.
Abstract: A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.
Abstract: Substituted tetrahydroimidazo[2,1-a]phthalazine compounds such as 6-methylamino-7,8,9,10-tetrahydroimidazo[2,1-a]phthalazine are prepared by reacting a 6-halo-7,8,9,10-tetrahydroimidazo[1,2-a]phthalazine with an appropriate amine. The compounds are useful as bronchodilators.
Type:
Grant
Filed:
July 12, 1982
Date of Patent:
July 5, 1983
Assignee:
The Dow Chemical Company
Inventors:
Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
Abstract: Substituted tetrahydropyridazino[1,6-a]benzimidazole compounds such as 2-methylamino-6,7,8,9-tetrahydropyridazino[1,6-a]benzimidazole are prepared by reacting a 2-halo-6,7,8,9-tetrahydropyridazino[1,6-a]benzimidazole with an appropriate amine. The compounds are useful as bronchodilators.
Type:
Grant
Filed:
July 12, 1982
Date of Patent:
July 5, 1983
Assignee:
The Dow Chemical Company
Inventors:
Catherine A. Alexander, Robert J. Cregge, Norton P. Peet
Abstract: N-(1,3-dithiolan-2-ylidene)-4-alkylanilines having a hydroxy, alkoxy or alkanoyloxy substituent on the alkyl group are useful as anti-inflammatory agents, as analgesic agents and as antiasthmatic agents. The compounds involved can be prepared by the reaction of an appropriate 4-alkylaniline with a methyl(1,3-dithiolan-2-ylidene)sulfonium salt or with carbon disulfide and ethylene dibromide in the presence of a base.
Abstract: Novel halomethyl derivatives of amino acids of the following general structure ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH.sub.2 --, F.sub.3 C--, ClCH.sub.2 -- or Cl.sub.2 CH--; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.11 R.sub.12 wherein each of R.sub.11 and R.sub.12 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms, ##STR2## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR3## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.3 and R.sub.
Abstract: The present invention refers to a new process for preparing N-2,3,4,5-substituted-1H-pyrrol-1-yl)-6-substituted amino-3-pyridazineamine, known as antihypertensive agents. The process is characterized in that a suitable 3,6-dihalogenopyridazine is reacted with hydrazine hydrate or other hydrazine derivatives of formula NH.sub.2 NHR, the obtained compound is reacted with a suitable dicarbonyl compound yielding first an alcandione-bis-[6-halogen-3-pyridazininyl]hydrazone, and then a 6-halogen-3-pyrrolylpyridazineamine derivative which is in turn reacted with an amine to yield the desired compounds.
Abstract: 1-[(2-Mercaptocycloalkyl)carbonyl]-L-proline derivatives of the formula ##STR1## wherein R, R.sup.1, and R.sup.2, each independently, represent hydrogen or a (C.sub.1 -C.sub.4)alkyl radical, n represents the integer 1, 2, 3, 4, or 5, and, in each of the n (CR'.sub.2) groups, R' represents hydrogen or (C.sub.1 -C.sub.4)alkyl, are described as well as the process for their manufacture, the intermediates for their synthesis and their use as antihypertensive agents.
Abstract: 1,3-Dihydro-2H-imidazol-2-ones having 5-acyl and 4-(substituted amino)methyl substituents, are useful as cardiotonics, antihypertensives and antithrombotic agents. The compounds are obtained by the reaction of an appropriate amine with a substituted 4-bromomethyl-1,3-dihydro-2H-imidazol-2-one.
Type:
Grant
Filed:
May 4, 1981
Date of Patent:
April 26, 1983
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Richard A. Schnettler, Richard C. Dage
Abstract: Beta-monofluoromethyl beta-alanine, beta-difluoromethyl beta-alanine and pharmaceutically acceptable esters and amides derived from the acid group, amides derived from the amine group, and salts thereof are novel compounds which inhibit .gamma.-aminobutyric acid transaminase (GABA-T).
Type:
Grant
Filed:
July 21, 1980
Date of Patent:
March 1, 1983
Assignee:
Merrell Toraude et Compagnie
Inventors:
Philippe Bey, Michael Jung, Fritz Gerhart
Abstract: 2,3-Dihydro-2-oxo-1H-imidazole-4-carboxylic acid derivatives having a (substituted amino)methyl substituent at the 5-position, are useful as cardiotonics, antihypertensives and antithrombotic agents. The compounds are obtained by the reaction of an appropriate amine with a 5-(bromomethyl)-2,3-dihydro-2-oxo-1H-imidazole-4-carboxylic acid ester or amide.
Type:
Grant
Filed:
May 4, 1981
Date of Patent:
February 1, 1983
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Richard A. Schnettler, Richard C. Dage
Abstract: 4-Alkanoylimidazol-2-ones of the following general structure which are useful as cardiotonics in the treatment of cardiac failure ##STR1## wherein Q and T are each an oxygen atom or a divalent sulfur atom; R is hydrogen, lower alkyl, lower alkylcarbonyl or benzoyl; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is a lower aliphatic hydrocarbon radical, phenyl alkylene or heterocyclo alkylene; and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
November 4, 1981
Date of Patent:
January 4, 1983
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Richard A. Schnettler, Richard C. Dage
Abstract: Compounds of the formula ##STR1## wherein R is H or C.sub.1-5 straight or branched chain alkyl; R.sub.1 is H, C.sub.1-10 straight or branched chain alkyl, allyl or phenyl; and R.sub.2 is phenyl or phenyl substituted with F, Cl, C.sub.1-5 straight or branched chain alkyl, di-F, di-Cl or di-Br; and the pharmaceutically acceptable acid addition salts thereof; are useful as muscle relaxants, anticonvulsants and analgesics.
Type:
Grant
Filed:
July 27, 1981
Date of Patent:
November 9, 1982
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, John M. Kane, Francis P. Miller
Abstract: 2-Amino-3-(3'-hydroxyphenyl)-3-butenoic acid or 2-amino-3-(3',4'-dihydroxyphenyl)-3-butenoic acid can be used to treat depression either alone or in combination with an extracerebrally acting AADC inhibitor.
Abstract: 2-Amino-2-fluoromethyl-3-(substituted)phenyl propionic acids and derivatives thereof are coadministered with dopamine for the treatment of schizophrenia, mania, tardive dyskinesia, anxiety, or depression.
Abstract: This invention relates to acylated furanyl acrylic acids, salts, esters and amides, to acylated thienyl acrylic acids, salts, esters and amides, and to their use as hypolipidemic agents, and to the processes for producing said compounds.
Abstract: There is described a method for treating benign prostatic hypertrophy comprising the administration of 2,5-di-amino-2-(mono-,di-, or trifluoromethyl)pentanoic acid or derivative thereof.