Patents Examined by Mary C. Vaughn
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Patent number: 4150033Abstract: 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: GrantFiled: December 6, 1976Date of Patent: April 17, 1979Assignee: Dainippon Pharmaceutical Co., Ltd.Inventor: Tsunehiro Kitagawa
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Patent number: 4133812Abstract: 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: GrantFiled: April 25, 1977Date of Patent: January 9, 1979Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Csaba Szaantay, Jaanos Rohaaly, Istvaan Jelinek
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Patent number: 4127573Abstract: 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: GrantFiled: September 5, 1973Date of Patent: November 28, 1978Assignee: Burroughs Wellcome Co.Inventor: John H. Gorvin
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Patent number: 4126620Abstract: 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: GrantFiled: February 25, 1977Date of Patent: November 21, 1978Assignee: Sterling Drug Inc.Inventors: Malcolm R. Bell, Rudolf Oesterlin
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Patent number: 4125530Abstract: 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: GrantFiled: February 2, 1977Date of Patent: November 14, 1978Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Frederick C. Novello
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Patent number: 4125537Abstract: 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: GrantFiled: February 7, 1977Date of Patent: November 14, 1978Assignee: McNeil Laboratories, IncorporatedInventor: Richard J. Carmosin
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Patent number: 4123547Abstract: 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: GrantFiled: September 15, 1977Date of Patent: October 31, 1978Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, Edward Walton
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Patent number: 4123544Abstract: 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: GrantFiled: March 2, 1977Date of Patent: October 31, 1978Assignee: Merrell Toraude S. A.Inventors: Henri Kornowski, Bernard Roques, Robert Oberlin, Andre Jondet
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Patent number: 4120965Abstract: 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: GrantFiled: May 19, 1977Date of Patent: October 17, 1978Assignee: Sandoz Ltd.Inventors: Gerhard Bormann, Richard Berthold
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Patent number: 4120960Abstract: 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: GrantFiled: August 1, 1977Date of Patent: October 17, 1978Assignee: The Boots Company LimitedInventors: Norman W. Bristow, Peter E. Macey, Kenneth J. Nichol, Malcolm F. Sim
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Patent number: 4119726Abstract: 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: GrantFiled: May 13, 1977Date of Patent: October 10, 1978Assignee: Beecham Group LimitedInventor: Gordon Wootton
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Patent number: 4119639Abstract: 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: GrantFiled: June 27, 1977Date of Patent: October 10, 1978Assignee: McNeil Laboratories, IncorporatedInventor: John Robert Carson
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Patent number: 4118397Abstract: 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: GrantFiled: December 6, 1976Date of Patent: October 3, 1978Assignee: Hoechst AktiengesellschaftInventors: Dieter Bormann, Wulf Merkel, Roman Muschaweck
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Patent number: 4118394Abstract: 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: GrantFiled: August 8, 1977Date of Patent: October 3, 1978Assignee: Ayerst, McKenna & Harrison LimitedInventors: Christopher A. Demerson, Leslie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
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Patent number: 4118395Abstract: 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: GrantFiled: June 20, 1977Date of Patent: October 3, 1978Inventor: Werner J. Frantsits
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Patent number: 4112087Abstract: 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: GrantFiled: November 4, 1976Date of Patent: September 5, 1978Assignee: Syntex (U.S.A.) Inc.Inventor: Philip J. Beeby
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Patent number: 4107187Abstract: 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: GrantFiled: January 19, 1977Date of Patent: August 15, 1978Assignee: American Hoechst CorporationInventors: Richard C. Effland, Larry Davis, Wolfgang Schaub
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Patent number: 4101552Abstract: 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: GrantFiled: April 23, 1976Date of Patent: July 18, 1978Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Erzsebet Mago nee Karacsony, Jozsef Borsi, Laszlo Tardos, Ildiko Kiraly, Sandor Elek, Istvan Elekes
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Patent number: 4100171Abstract: 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: GrantFiled: August 6, 1976Date of Patent: July 11, 1978Assignee: Hoffmann-La Roche Inc.Inventors: John Westley, Chao-Min Liu
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Patent number: 4088773Abstract: Acylamino pyrrole compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.Type: GrantFiled: June 1, 1976Date of Patent: May 9, 1978Assignee: Lilly Industries LimitedInventors: Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann