Patents Examined by G. Thomas Todd
  • Patent number: 4051248
    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.
    Type: Grant
    Filed: May 20, 1976
    Date of Patent: September 27, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: B. Richard Vogt, David A. Cullison
  • Patent number: 4046900
    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
  • Patent number: 4035371
    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
  • Patent number: 4033748
    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
  • Patent number: 4032640
    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.
    Type: Grant
    Filed: June 9, 1976
    Date of Patent: June 28, 1977
    Assignee: Sandoz Ltd.
    Inventor: Jean-Michel Bastian
  • Patent number: 4031226
    Abstract: Compounds of the class of N-[(1-piperidinyl)alkyl]arylcarboxamides, useful as antiemetic and psychotropic agents.
    Type: Grant
    Filed: June 21, 1976
    Date of Patent: June 21, 1977
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Willem Soudijn, Ineke VAN Wijngaarden, Paul Adriaan Jan Janssen
  • Patent number: 4031225
    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.
    Type: Grant
    Filed: June 14, 1976
    Date of Patent: June 21, 1977
    Assignee: Sandoz Ltd.
    Inventors: Jean-Michel Bastian, Richard Berthold
  • Patent number: 4029664
    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.
    Type: Grant
    Filed: July 6, 1976
    Date of Patent: June 14, 1977
    Assignee: Siphar S.A.
    Inventors: Cesare Casagrande, Giorgio Ferrari
  • Patent number: 4029659
    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.
    Type: Grant
    Filed: July 22, 1974
    Date of Patent: June 14, 1977
    Assignee: Omnium Chimique Societe Anonyme
    Inventor: Jean Alfred Alphonse Joseph Hannart
  • Patent number: 4028364
    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.
    Type: Grant
    Filed: July 6, 1976
    Date of Patent: June 7, 1977
    Assignee: G. D. Searle & Co.
    Inventor: Gilbert William Adelstein
  • Patent number: 4028366
    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.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: June 7, 1977
    Assignee: Sterling Drug Inc.
    Inventor: Bernard L. Zenitz
  • Patent number: 4028351
    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.
    Type: Grant
    Filed: February 11, 1975
    Date of Patent: June 7, 1977
    Assignee: Buskine S.A.
    Inventor: Ida Taccone
  • Patent number: 4026899
    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.
    Type: Grant
    Filed: March 26, 1976
    Date of Patent: May 31, 1977
    Assignee: Parke, Davis & Company
    Inventor: Edward Faith Elslager
  • Patent number: 4025633
    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.
    Type: Grant
    Filed: March 3, 1975
    Date of Patent: May 24, 1977
    Assignee: Firma Temmler A.G.
    Inventors: Wilhelm A. Behrendt, Bernhard Stieh
  • Patent number: 4024265
    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.
    Type: Grant
    Filed: October 20, 1975
    Date of Patent: May 17, 1977
    Assignee: Sandoz Ltd.
    Inventor: Jean-Michel Bastian
  • Patent number: 4024266
    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.
    Type: Grant
    Filed: February 20, 1976
    Date of Patent: May 17, 1977
    Assignee: Sandoz Ltd.
    Inventor: Jean-Michel Bastian
  • Patent number: 4024129
    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
  • Patent number: 4022902
    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.
    Type: Grant
    Filed: August 29, 1975
    Date of Patent: May 10, 1977
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Patent number: 4022778
    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.
    Type: Grant
    Filed: November 5, 1971
    Date of Patent: May 10, 1977
    Assignee: American Home Products Corporation
    Inventor: Meier E. Freed
  • Patent number: 4022786
    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.
    Type: Grant
    Filed: March 26, 1974
    Date of Patent: May 10, 1977
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Gerhard Hackmack, Josef Klosa