Abstract: Compounds having the structure ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, alkanoyloxy, alkoxy, alkylthio, alkyl or trifluoromethyl; R.sub.2 is hydrogen, alkyl or alkenyl; R.sub.3 is hydrogen, halogen or alkyl; R.sub.4 is formyloxy or alkanoyloxy; m is 1 or 2; and n is 0, 1 or 2; have useful physiological activity.
Abstract: New benzoylpiperidylalkylindoles and related compounds possessing tranquilizing, anti-hypertensive and analgesic properties and a process for the preparation thereof are described.
Type:
Grant
Filed:
March 4, 1976
Date of Patent:
September 6, 1977
Assignee:
American Hoechst Corporation
Inventors:
Grover C. Helsley, Joseph T. Strupczewski, Beth Ann Gardner
Abstract: .beta.-[Benzo(b)thienyl-3] propionic acid derivatives in the form of their amino esters (and salts thereof) are prepared. These compounds have spasmolytic, vasodilatatric, antiserotanic and local anaesthetic activity.
Type:
Grant
Filed:
January 22, 1976
Date of Patent:
July 12, 1977
Assignee:
Innothera
Inventors:
Max Fernand Robba, Denise Jeanne Claude Duval
Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial water where bacterial control is desired.
Type:
Grant
Filed:
July 2, 1976
Date of Patent:
July 5, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: This invention provides new compounds of formula I, ##STR1## wherein R.sub.1 is hydrogen, halogen of atomic number from 9 to 35, or alkyl or alkoxy of 1 to 4 carbon atoms,R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms,R.sub.3 is hydrogen, chlorine, or alkyl of 1 to 4 carbon atoms,Either A and B are each hydrogen or together a single bond, andn is a whole number from 3 to 7, useful as salidiuretics.
Abstract: This invention provides new compounds of formula I, ##STR1## wherein N IS A WHOLE NUMBER FROM 1 TO 3,R.sub.1 is hydrogen, or halogen of atomic number from 9 to 35,Each of the two radicals R.sub.2 are the same, and each is hydrogen or alkyl of 1 to 4 carbon atoms,Each of the two radicals R.sub.3 are the same, and each is hydrogen or alkyl of 1 to 4 carbon atoms, andX is carbonyl or methylene,Useful as anti-arrhythmics.
Abstract: A process is disclosed for the interconversion of alkaloids of the heteroyohimbane group, more particularly of tetrahydroalstonine into raubasine, having the formulae ##STR1## according to which the asymmetry center at C-20 is inverted by several steps involving changes of the ring E structure.
Abstract: N-disubstituted aminoethyl esters of 11-methoxy-raubasinic acid of the formula : ##STR1## in which R is an alkyl group containing up to 4 carbon atoms or the two R groups, together with the nitrogen atom to which they are attached, form a morpholinyl, piperidinyl, piperazinyl or pyrrolidinyl group, and their physiologically acceptable acid addition salts. The process for the preparation of an N-disubstituted aminoethyl ester of 11-methoxy-raubasinic acid of the formula specified hereinabove, which comprises esterifying 11-methoxy-raubasinic acid with a substituted aminoethyl halide of the formula: ##STR2## in which X is a halogen atom and R has the meaning specified in claim 1.
Abstract: This invention encompasses novel 2-azabicyclo[2.2.2]-octan-2-yl-diphenyl-alkanones and related compounds. These compounds are useful as anti-diarrheal agents.
Abstract: 2-Naphthyl-lower-alkylamines, useful as anti-inflammatory agents, are prepared by reaction of a 2-naphthyl-lower-alkanoyl halide with an amine and reduction of the resulting 2-naphthyl-lower-alkanoylamine with a reagent effective to reduce an amide to an amine.
Abstract: Derivatives of spiro-(4,5)-decane, are prepared from an N-substituted-4-piperidone according to a modification of the Reformatsky reaction. The N-substituted-4-piperidone is reacted in an appropriate solvent or solvent mixture with an alpha halogen ester in the presence of activated zinc. The obtained beta-hydroxy ester is reacted with an excess of hydrazine, the resultant compound being a beta hydroxy hydrazide. The latter is subjected to a Curtius transposition with nitrous acid in excess.
Abstract: 2H(1)Benzothiopyrano[4,3,2-cd]indazole N-oxides, 2H(1)benzopyrano[4,3,2-cd]indazole N-oxides and acid addition salts thereof are disclosed. These compounds can be produced by oxidation of the corresponding amines with oxidizing agents capable of forming an N-oxide derivative. The compounds are parasiticidal agents useful in the treatment of schistosome infections.
Abstract: .alpha.,.alpha.-Diaryl-.beta.-(tert-amino)-propanols having the general formula: ##STR1## wherein R', R" and R.sup.1 to R.sup.10 represent certain specific substituent groups, exhibit a diuretic and saluretic activity.Pharmaceutical composition containing at least one compound of the general Formula II together with a pharmaceutically acceptable diluent or carrier. The pharmaceutical compositions may be in a form suitable for oral or parenteral administration.
Abstract: This invention provides new compounds of formula I, ##STR1## wherein R.sub.1 is hydrogen, alkyl or 1 to 4 carbon atoms, fluorine, chlorine or bromine,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkylalkyl of 4 to 10 carbon atoms, alkenyl or alkinyl of 3 to 6 carbon atoms, the multiple bond thereof being other than adjacent to the nitrogen atom of the tricyclic ring system, oxoalkyl of 2 to 5 carbon atoms, the oxygen atom thereof being separated by at least two carbon atoms from the nitrogen atom of the tricyclic ring system, or phenylalkyl of 7 to 10 carbon atoms,R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,And R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms,Useful as antidepressants.
Abstract: This invention provides new compounds of formula I, ##STR1## wherein R.sub.1 is hydrogen, halogen of an atomic number of from 9 to 35, or alkyl of 1 to 4 carbon atoms,R.sub.2 is alkyl of 1 to 4 carbon atoms,R.sub.4 is alkyl of 1 to 4 carbon atoms, and eitherI.R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms, andA and B together form a bond, orIi.R.sub.3 is hydrogen, andA and B are both hydrogen,Useful as LH inhibitors and antidepressants.
Abstract: A process for the preparation of acylamido derivatives by reaction of a compound of the formula Z - N = C = O, wherein Z is an optionally substituted alkyl-, aryl- (preferably phenyl or naphthyl) or cycloalkyl or optionally substituted heterocyclic, preferably a penicillanic acid or a cephalosporanic acid nucleus, having carboxyl groups and an optionally present hydroxy group protected, with a carboxylic acid of the formula ##STR1## wherein Z.sup.1 is an optionally substituted hydrocarbon group, in the presence of a catalyst selected from the group consisting of substituted pyridines and their N-oxides, optionally substituted imidazoles or their N-oxides, optionally substituted benzimidazoles or their N-oxides, and optionally substituted imidazo [1,2-.alpha.] pyridines or their N-oxides.
Type:
Grant
Filed:
November 3, 1971
Date of Patent:
May 17, 1977
Assignee:
Gist-Brocades N.V.
Inventors:
Peter Wolfgang Henniger, Antoon Van Harrewijn
Abstract: The N-oxide of 10,11-dihydro-3-carboxycyproheptadine is disclosed to have pharmaceutical utility as an appetite stimulant and as an anthihistaminic agent. Also disclosed are processes for the preparation of such compound; pharmaceutical compositions comprising such compound; and methods of treatment comprising administering such compound and compositions.
Abstract: Novel 10-aryl-1,2,3,4-tetrahydropyrazino(1,2-.alpha.)indole and derivatives and intermediates for their preparation are described, the products having anticonvulsant and central nervous system depressant activity.
Abstract: 4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are substituted or unsubstituted in the 1-position of the piperidine nucleus, such as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolylpiperidines, and their substantially non-toxic, pharmaceutically-acceptable acid addition salts, are highly effective central nervous system (CNS) stimulants which are superior to known amphetamine-type stimulants. A novel and highly advantageous process of making such 4,4-diarylpiperidine compounds comprises reacting a 4-aryl-4-hydroxypiperidine compound which may be substituted in its 3-position by an aroyl group, with an aromatic hydrocarbon, in particular with benzene, in the presence of a Friedel-Crafts-type catalyst.