Patents Examined by Mary C. Vaughn
  • Patent number: 4150033
    Abstract: A novel maleimidobenzoic acid N-hydroxysuccinimide ester of the formula: ##STR1## which is suitable as a binding agent for binding an enzyme and an antigen to give an enzyme-labeled antigen of the formula: ##STR2## wherein X and Y are different and are each an enzyme or an antigen, and an enzyme immuno assay using the enzyme-labeled antigen (II) and further a kit for the enzyme immuno assay which contains the enzyme-labeled antigen (II).
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: April 17, 1979
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventor: Tsunehiro Kitagawa
  • Patent number: 4133812
    Abstract: Compounds are prepared with anti-amoeba activity of the following formula: ##STR1## wherein R.sup.1 equals R.sup.2 and each is lower alkyl and R.sup.3 and R.sup.4 are each lower alkyl, with the proviso that R.sup.1 and R.sup.2 are not methyl and R.sup.3 and R.sup.4 are not both ethyl.
    Type: Grant
    Filed: April 25, 1977
    Date of Patent: January 9, 1979
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Csaba Szaantay, Jaanos Rohaaly, Istvaan Jelinek
  • Patent number: 4127573
    Abstract: Acridone and xanthone compounds substituted by at least one tetrazolyl group in one ring, and further substituted in the other ring, optionally for the acridones have antiallergic activity.
    Type: Grant
    Filed: September 5, 1973
    Date of Patent: November 28, 1978
    Assignee: Burroughs Wellcome Co.
    Inventor: John H. Gorvin
  • Patent number: 4126620
    Abstract: 2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as antisecretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.
    Type: Grant
    Filed: February 25, 1977
    Date of Patent: November 21, 1978
    Assignee: Sterling Drug Inc.
    Inventors: Malcolm R. Bell, Rudolf Oesterlin
  • Patent number: 4125530
    Abstract: 4(5)-Trifluoromethylimidazoles having optional substituents in the 1 and 2 positions are provided. The novel 4(5)-trifluoromethylimidazoles are prepared by reacting a 1,1-dihalo-3,3,3-trifluoroacetone compound with an appropriate carboxaldehyde and ammonia. The 4(5)-trifluoromethylimidazoles are useful as anti-gout and anti-hyperuricemic agents.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: November 14, 1978
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Frederick C. Novello
  • Patent number: 4125537
    Abstract: Loweralkyl 1-loweralkyl-pyrrole-2-glyoxylates are reduced by the base-catalyzed action of hydrogen sulfide under pressure of at least 30 p.s.i. to loweralkyl 1-loweralkyl-pyrrole-2-acetates.
    Type: Grant
    Filed: February 7, 1977
    Date of Patent: November 14, 1978
    Assignee: McNeil Laboratories, Incorporated
    Inventor: Richard J. Carmosin
  • Patent number: 4123547
    Abstract: Thienamycin sulfoxide (I, n=1), Thienamycin sulfone (I, n=2), and their pharmaceutically acceptable salts are disclosed to be useful as antibiotics: ##STR1## Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: September 15, 1977
    Date of Patent: October 31, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Edward Walton
  • Patent number: 4123544
    Abstract: This invention relates to acetylsalicylic acid derivatives of the formula ##STR1## wherein R is H or OH, which have good analgesic, anti-inflammatory, and antipyretic activity and are, at the same time, free of ulcerogenic activity when administered orally.
    Type: Grant
    Filed: March 2, 1977
    Date of Patent: October 31, 1978
    Assignee: Merrell Toraude S. A.
    Inventors: Henri Kornowski, Bernard Roques, Robert Oberlin, Andre Jondet
  • Patent number: 4120965
    Abstract: This invention provides new compounds of formula I, ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 5 carbon atoms,R.sub.2 is a group ##STR2## wherein N IS A WHOLE NUMBER FROM 0 TO 3,R.sub.5 and R.sub.6, independently, are hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen of atomic number from 9 to 35, or together are 3,4-methylenedioxy,R.sub.7 is hydrogen, or when both R.sub.5 and R.sub.6 are alkoxy of 1 to 4 carbon atoms also may be alkoxy of 1 to 4 carbon atoms,R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or halogen of atomic number from 9 to 35, andR.sub.4 is hydrogen or alkoxy of 1 to 4 carbon atoms,Useful as sleep-promoting agents, and anti-aggressive agents.
    Type: Grant
    Filed: May 19, 1977
    Date of Patent: October 17, 1978
    Assignee: Sandoz Ltd.
    Inventors: Gerhard Bormann, Richard Berthold
  • Patent number: 4120960
    Abstract: Therapeutic activity, and in particular the ability to induce diuresis or saluresis, has been discovered in 4-hydroxy- or 4-mercapto-2-aryl-1,2-dihydrophthalazine-1-acetic acids, the tautomers of these namely 4-oxo or thio-2-aryl-1,2-tetrahydrophthalazine-1-acetic acids, and in the ester and alcohol derivatives of the acids, and in the acyl derivatives of the 4-hydroxy or mercapto compounds and in the 3-alkyl derivatives of the 4-oxo or thio compounds. Therapeutic compositions and methods using the compounds are described, as also are novel compounds.
    Type: Grant
    Filed: August 1, 1977
    Date of Patent: October 17, 1978
    Assignee: The Boots Company Limited
    Inventors: Norman W. Bristow, Peter E. Macey, Kenneth J. Nichol, Malcolm F. Sim
  • Patent number: 4119726
    Abstract: Compounds of formula (I): ##STR1## wherein: M IS 0 OR 1;n is 4 to 8;X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected;R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group inWhich the R.sub.1 moiety contains 1 to 12 carbon atoms;R.sub.3 is hydroxy or protected hydroxy;R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups, or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent C.sub.5-8 cycloalkyl;R.sub.5 is hydrogen, C.sub.1-4 alkyl or phenyl; and salts thereof; have useful pharmacological properties including anti-gastric secretion, bronchodilator and platelet aggregation inhibition activities.
    Type: Grant
    Filed: May 13, 1977
    Date of Patent: October 10, 1978
    Assignee: Beecham Group Limited
    Inventor: Gordon Wootton
  • Patent number: 4119639
    Abstract: The interaction of a 2-aryldithiolanium cation with an appropriate pyrrole-2-acetic acid derivative to give a 5-[2-aryl-2-(1,3-dithiolanyl)]pyrrole-2-acetic acid derivative which is then converted to the corresponding 5-aroylpyrrole-2-acetic acid derivative.
    Type: Grant
    Filed: June 27, 1977
    Date of Patent: October 10, 1978
    Assignee: McNeil Laboratories, Incorporated
    Inventor: John Robert Carson
  • Patent number: 4118397
    Abstract: A process is disclosed for preparing 5-sulfamoylbenzoic acid derivatives substituted in 4-position by various substituents and in 3-position by a cyclic amino group and having sali-diuretic properties. Novel intermediate compounds are also disclosed.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: October 3, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Dieter Bormann, Wulf Merkel, Roman Muschaweck
  • Patent number: 4118394
    Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indone nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives having the amino(lower)alkyl radical only at position 9 possess two substituents at position 1 and may be optionally substituted at position 3, 4, 5, 6, 7, and 8. The derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7 and 8.
    Type: Grant
    Filed: August 8, 1977
    Date of Patent: October 3, 1978
    Assignee: Ayerst, McKenna & Harrison Limited
    Inventors: Christopher A. Demerson, Leslie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
  • Patent number: 4118395
    Abstract: A method for the production of indolyl lactones of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, or an alkoxy group having 1 to 4 C atoms and R.sub.3 is hydrogen, characterized in the manner that one reacts a 2-hydroxymethylindole of the formula ##STR2## wherein R.sub.1 has the above named meaning and R.sub.2 is an alkanoyl group or a phenyl alkanoyl group, with an .alpha.-diazoester of the formula ##STR3## wherein R.sub.3 has the above named meaning and R.sub.4 is an alkyl group having 1 to 4 C atoms and a, benzyl group, to a 3-indolyl acetic acid ester of the formula ##STR4## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the above named meanings, saponifies the thus obtained 3-indolyl acetic acid ester of the formula (IV) to the 3-indolyl acetic acid of the formula ##STR5## wherein R.sub.1 and R.sub.3 have the above named meaning, and the latter is dehydrated to indolyl lactone with the formula (I).
    Type: Grant
    Filed: June 20, 1977
    Date of Patent: October 3, 1978
    Inventor: Werner J. Frantsits
  • Patent number: 4112087
    Abstract: Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, .beta.-haloethyl, allyl, propargyl, cyclopentyl or benzyl; R.sup.1 is hydrogen or an .alpha.-substituted acetamido group; R.sup.2 is hydrogen or a protecting group; and the pharmaceutically acceptable salts thereof. The 7.beta.-amino compounds are useful as intermediates for the 7.beta.-(.alpha.-substituted acetamido) compounds which are useful as antibacterials against a wide variety of gram positive and gram negative bacteria.
    Type: Grant
    Filed: November 4, 1976
    Date of Patent: September 5, 1978
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Philip J. Beeby
  • Patent number: 4107187
    Abstract: Novel aminoalkylpyrrolobenzoxazalkanes, physiologically tolerable acid addition salts thereof, method of preparing same and novel intermediates in the preparation thereof are described. These compounds are useful as analgesic agents and tranquilizers.
    Type: Grant
    Filed: January 19, 1977
    Date of Patent: August 15, 1978
    Assignee: American Hoechst Corporation
    Inventors: Richard C. Effland, Larry Davis, Wolfgang Schaub
  • Patent number: 4101552
    Abstract: 9,10-Dihydrolysergic acid-(3'-/pyrrolid-2"-on-1'-yl/-propyl)-amide, 1-methyl-9,10-dihydrolysergic acid-(thiazoline-2'-yl)-amide and lysergic acid-(3'-allyloxy-2'-oxy-propyl)-amide and their pharmaceutically acceptable acid addition salts possess antihypertensive and antiserotonin effect and exert an action on the central nervous system.
    Type: Grant
    Filed: April 23, 1976
    Date of Patent: July 18, 1978
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Erzsebet Mago nee Karacsony, Jozsef Borsi, Laszlo Tardos, Ildiko Kiraly, Sandor Elek, Istvan Elekes
  • Patent number: 4100171
    Abstract: The invention relates to a new and useful antibiotic substance which is of the formula ##STR1## and to processes for its production and recovery. The antibiotic which exhibits ionophoric properties, is classified as a polyether group antibiotic. The antibiotic of formula I is effective in inhibiting the growth of gram positive bacteria and exhibits utility as an antihypertensive agent and as a compound to improve ruminant feed utilization. The antibiotic of Formula I is prepared by cultivating a strain of Streptomyces sp. X-14547 in an aqueous carbohydrate solution containing nitrogenous nutrients and mineral salts and thereafter isolating the antibiotic from the fermentation broth.
    Type: Grant
    Filed: August 6, 1976
    Date of Patent: July 11, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John Westley, Chao-Min Liu
  • Patent number: 4088773
    Abstract: Acylamino pyrrole compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: May 9, 1978
    Assignee: Lilly Industries Limited
    Inventors: Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann