Patents Examined by Natalia Harkaway
  • Patent number: 4221804
    Abstract: Hypertension can be treated using compounds having the formula ##STR1## or a basic salt thereof, wherein R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR2## wherein R.sub.5 is alkyl or aryl;R.sub.2 is hydrogen or alkyl;R.sub.3 is aryl;R.sub.4 is hydrogen, alkyl or arylalkyl andn is 0, 1 or 2.
    Type: Grant
    Filed: September 27, 1979
    Date of Patent: September 9, 1980
    Inventor: George C. Rovnyak
  • Patent number: 4220792
    Abstract: Anti-diabetic agents of the formula: ##STR1## wherein R is CHO or COOR.sub.1, where R.sub.1 is hydrogen or C.sub.1-6 alkyl,R.sub.o is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, bromo, chloro, fluoro, trifluoromethyl, nitro or ##STR2## where R.sub.2 is hydrogen or C.sub.1-4 alkyl, andn is 0 or 1,and the non-toxic, pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 25, 1979
    Date of Patent: September 2, 1980
    Assignee: Sandoz, Inc.
    Inventors: Paul L. Anderson, Nicholas A. Paolella
  • Patent number: 4217454
    Abstract: Process for the stereoselective reduction of certain amino-substituted indoles and amino-substituted indole-containing structures to trans-dihydroindoles comprising the sequential steps of (1) reacting a strong acid addition salt of such an indole with a borohydride in an appropriate solvent in the absence of acid, and (2) acidifying the step (1) reaction product by which it is reduced and hydrolyzed to form the corresponding trans-dihydroindole. Many dihydroindoles so produced, for example, the trans-2-(adamantylemethyl)-=2,3,4,4a,5,9b-hexahydro-5-phenyl-1H-pyrido[4,3 -b]indole, are useful as pharmaceutical materials, such as tranquilizers.
    Type: Grant
    Filed: July 26, 1978
    Date of Patent: August 12, 1980
    Assignee: Endo Laboratories, Inc.
    Inventor: Joel G. Berger
  • Patent number: 4216313
    Abstract: Certain thiazolinyl or thiazinyl ketobenzimidazole compounds and derivatives thereof are useful as antiviral agents.
    Type: Grant
    Filed: January 12, 1979
    Date of Patent: August 5, 1980
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Paget, James W. Chamberlin, James W. Wikel
  • Patent number: 4215132
    Abstract: N,N-dimethyl-O-(3-substituted-pyrazol-5-yl)-carbamic acid esters of the formula ##STR1## in which R is hydrogen or optionally substituted alkyl,R.sup.1 is alkyl, andn is 1 or 2,which possess arthropodicidal properties.
    Type: Grant
    Filed: April 18, 1979
    Date of Patent: July 29, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Hans-Jochem Riebel, Rolf Schroder, Ingeborg Hammann, Bernhard Homeyer
  • Patent number: 4215217
    Abstract: A process for preparing 4-(oxy, thio or amino)methylimidazole compounds via displacement of the trisubstituted phosphonium group from 4-(trisubstituted phosphonium)-methylimidazole compounds is disclosed.
    Type: Grant
    Filed: June 14, 1978
    Date of Patent: July 29, 1980
    Assignee: SK&F Lab Co.
    Inventors: Joseph J. Lewis, Robert L. Webb
  • Patent number: 4215126
    Abstract: The compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N"-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitroeth ylene.
    Type: Grant
    Filed: February 21, 1979
    Date of Patent: July 29, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Patent number: 4215125
    Abstract: The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. A compound of this invention is N,N'-bis-[2-(2-pyridylmethylthioethyl]-N"-cyanoguanidine.
    Type: Grant
    Filed: January 22, 1979
    Date of Patent: July 29, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Patent number: 4213992
    Abstract: New carbamates, a process for their manufacture by reaction of salts of pyrazolinediones with a carbamyl halide, and pesticides containing these new carbamates as active ingredients.The new carbamates may be used as insecticides and acaricides. They have an excellent action on sucking insects, especially aphids.
    Type: Grant
    Filed: July 20, 1978
    Date of Patent: July 22, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Heinrich Adolphi, Annegrit Baumann, Rolf Huber, Karl Kiehs, Franz Merger
  • Patent number: 4214090
    Abstract: Fungicidal 4- and 5-pyrazolecarboxamides of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is the group --CONHR.sup.5 in which R.sup.5 is phenyl optionally substituted with one, two or three substituents independently chosen from the group consisting of alkyl, alkoxy, halogen, trifluoromethyl, nitro and cyano; R.sup.3 is chosen from the group consisting of hydrogen, alkyl, hydroxyalkyl, phenyl and --CH.sub.2 COOR.sup.6 wherein R.sup.6 is alkyl; R.sup.4 and R.sup.1 or R.sup.2, whichever is not --CONHR.sup.5, are independently chosen from the group consisting of hydrogen, halogen, and alkyl; R.sup.2 and R.sup.4 are not both hydrogen when R.sup.1 is --CONHR.sup.5 ; R.sup.1 and R.sup.3 are not both hydrogen when R.sup.2 is --CONHR.sup.5 ; and R.sup.2, R.sup.3 and R.sup.4 are not each methyl when R.sup.1 is --CONHR.sup.5 and R.sup.5 is phenyl.
    Type: Grant
    Filed: October 13, 1978
    Date of Patent: July 22, 1980
    Assignee: Commonwealth Scientific and Industrial Research Organization
    Inventor: John L. Huppatz
  • Patent number: 4213993
    Abstract: New heterocyclylcarboxylic acid derivatives which are acylated in the nucleus, especially benz-acyl-benzimidazole-2-carboxylic acid derivatives of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etherified or esterified hydroxymethyl group, R.sub.1 is an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R.sub.2 is hydrogen or an aliphatic radical and Ph is a 1,2-phenylene group containing the radical R.sub.1 --C(.dbd.O)--, with the proviso that R.sub.1 contains at least 2 carbon atoms if Ph is otherwise unsubstituted, R.sub.2 is ethyl and R is acetoxymethyl, and salts of such compounds having salt-forming properties, are useful as anti-allergic agents.
    Type: Grant
    Filed: November 20, 1978
    Date of Patent: July 22, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
  • Patent number: 4212877
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms, or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is a heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.
    Type: Grant
    Filed: January 17, 1979
    Date of Patent: July 15, 1980
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Herbert Koppe, Anton Mentrup, Ernst-Otto Renth, Kurt Schromm, Wolfgang Hoefke, Gojko Muacevic
  • Patent number: 4212875
    Abstract: Bisamidines carrying one unsaturated nitrogen heterocycle-containing substituent, representative of which is 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methyl-g uanidino]octane, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: May 2, 1978
    Date of Patent: July 15, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Peter D. Miles
  • Patent number: 4211876
    Abstract: 3-Pyrazolidinone carboxamides such as N(tertamyl)7[3-oxo-1(3-hydroxy-n-octyl)pyrazolidin-2-yl]-heptanamide exhibit prostaglandin antagonist activity.
    Type: Grant
    Filed: June 13, 1979
    Date of Patent: July 8, 1980
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Richard M. Scribner
  • Patent number: 4211786
    Abstract: Hypertension can be treated using compounds having the formula or a basic salt thereof, whereinR.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR1## wherein R.sub.5 is alkyl or aryl;R.sub.2 is hydrogen or alkyl;R.sub.3 is aryl;R.sub.4 is hydrogen, alkyl or arylalkyl andn is 0, 1 or 2.
    Type: Grant
    Filed: March 8, 1979
    Date of Patent: July 8, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Patent number: 4209630
    Abstract: A series of spiro-hydantoin compounds has been prepared by condensing the appropriate carbonyl ring compound, such as the corresponding 1-indanone, 1-tetralone, 4-chromanone, thiochroman-4-one, 7,8-dihydroquinolin-5(6H)-one, 6,7-dihydropyrindin-5(5H)-one, thiondane-3-one-1,1-dioxide and 4-oxoisothiochroman-2,2-dioxide, respectively, with potassium cyanide and ammonium carbonate. The resulting hydantoin derivatives are found to be useful in preventing or alleviating chronic diabetic complications. Preferred member compounds include spiro-[imidazolidine-4,1'-indan]-2,5-dione, 6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6-chloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,7-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,8-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6'-fluoro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione and 6',7'-dichloro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione.
    Type: Grant
    Filed: July 10, 1978
    Date of Patent: June 24, 1980
    Assignee: Pfizer Inc.
    Inventor: Reinhard Sarges
  • Patent number: 4207326
    Abstract: Quaternary N-alkyl pyrazole derivatives and their method of preparation are described. The pyrazole derivatives are useful as antimicrobial agents.
    Type: Grant
    Filed: May 21, 1979
    Date of Patent: June 10, 1980
    Assignee: Cilag-Chemie A.G.
    Inventors: Carl Richter, Georg Feth
  • Patent number: 4207325
    Abstract: Pyrazoles of the formula ##STR1## whereinR is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, cycloalkyl, cycloalkenyl, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl; are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.
    Type: Grant
    Filed: January 17, 1978
    Date of Patent: June 10, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Eike Moller, Karl-August Meng, deceased, Egbert Wehinger, Harald Horstmann, Friedel Seuter
  • Patent number: 4207327
    Abstract: N-(4-Pyrazolidinyl)benzamides having the formula ##STR1## and their amino precursors are disclosed wherein R is lower alkyl, lower cycloalkyl or phenyllower-alkyl; R.sup.1 is lower alkyl, lower cycloalkyl, or phenyllower-alkyl; R.sup.2 is hydrogen, lower alkyl or phenyl; R.sup.3 is hydroxy, cyano, nitro, amino, fluoro, chloro, bromo, trifluoromethyl, lower alkyl, lower alkoxy, sulfamoyl or actamido, R.sup.3 can be the same radical or different radicals; n is an integer from zero to three inclusive, and pharmaceutically acceptable acid addition salts thereof. The compounds have anti-emetic and gastric emptying properties.
    Type: Grant
    Filed: May 22, 1979
    Date of Patent: June 10, 1980
    Assignee: A. H. Robins Company, Inc.
    Inventors: Carl D. Lunsford, Albert D. Cale, Jr.
  • Patent number: 4207322
    Abstract: There are produced 6-aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-(1,4)-diazepines of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen atom, an alkyl mercapto group having 1 to 6 carbon atoms,R.sub.2 is hydrogen, an alkyl group with 1 to 6 carbon atoms,R.sub.3 is hydrogen or a halogen or a halogen atomthe structural part A-B is the group --CH.sub.2 .dbd.NH--and Y-Z is the group >C.dbd.N--, >C.dbd.N(.fwdarw.O), and Y-Z is the group >C.dbd.N--, their optical isomers and their pharmaceutically acceptable salts. The compounds have anticonvulsive properties.
    Type: Grant
    Filed: July 20, 1978
    Date of Patent: June 10, 1980
    Assignee: Deutsche Gold- und Silber-Scheideanstalt vormals Roessler
    Inventors: Walter von Bebenburg, Norbert Schulmeyer, Vladimir Jakovlev