Patents Examined by Norma S. Milestone
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Patent number: 4822885Abstract: Certain substituted cyclopentanone ethylene ketal compounds, and ketones and amides derived therefrom are useful synthetic intermediates for compounds of pharmaceutical interest. A synthetic process for using the intermediates is also described.Type: GrantFiled: May 3, 1988Date of Patent: April 18, 1989Assignee: Minnesota Mining and Manufacturing CompanyInventor: Elden H. Banitt
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Patent number: 4816591Abstract: 6,11-Dihydrodibenz[b,e]oxepin-acetic acids and derivatives having the general formula ##STR1## are prepared by multi-steps sequences. X is C.dbd.O, CHCl, CHBr, CH.sub.2 or CHOR.sup.4 ; Y is alkyl or alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; n is 0, 1, 2 or 3; Z is COOR.sup.5, CH.sub.2 OR.sup.5, CONR.sub.2.sup.5 or CONHOR.sup.5 ; and R.sup.1 -R.sup.5 are hydrogen or alkyl of 1 to 4 carbon atoms.These compounds and the physiologically tolerable salts thereof are useful as antiinflammatory and analgesic agents.Type: GrantFiled: November 5, 1979Date of Patent: March 28, 1989Assignee: American Hoechst CorporationInventors: Grover C. Helsley, Arthur R. McFadden, David Hoffman
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Patent number: 4803289Abstract: Compounds of formula ##STR1## in which R represents hydrogen, formyl or an alkanoyl group of two to twenty-five carbon atoms and R' represents an alkyl group of one to thirty-five carbon atoms are of value as mosquito attractants, mosquitoes being attracted to a location where they and/or their eggs or larvae are then destroyed.Type: GrantFiled: June 8, 1983Date of Patent: February 7, 1989Assignee: National Research Development Corp.Inventors: Brian R. Laurence, John A. Pickett
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Patent number: 4795752Abstract: Novel amide derivatives are disclosed. As examples of said amide derivatives are mentioned 1-[2-[5-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2,4-pentadienoyl]-aminoethyl ]-4-benzhydroxypiperidine, 1-[2-[3-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2-propenoyl]aminoethyl]-4-be nzhydroxypiperidine, 1-[3-[5-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2,4-pentadienoyl]aminopropyl ]-4-benzhydrylpiperazine and the like. These amide derivatives are useful as antiallergic agents.Type: GrantFiled: December 8, 1986Date of Patent: January 3, 1989Assignee: Terumo Kabushiki KaishaInventors: Shin Hattori, Makoto Takai, Kazuhiro Omori, Shinji Ozawa, Toshio Wakabayashi
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Patent number: 4792613Abstract: Novel polyfluorinated cyclic carbonates of the formula ##STR1## in which R.sub.F is an unbranched or branched perfluoroalkyl radical having 1 to 18 carbon atoms, an unbranched or branched .omega.-hydro- or .omega.-haloperfluoroalkyl radical having 1 to 18 carbon atoms, or a cycloperfluoroalkyl radical having 4 to 6 carbon atoms, are described. They are prepared by reacting a polyfluorinated halohydrin of the formula R.sub.F --CH.sub.2 --CH(Hal)--CH.sub.2 OH, in which R.sub.f has the meaning mentioned and Hal represents a halogen, with carbonate or hydrogen carbonate compounds in the presence of an aprotic solvent. The novel compounds, which are generally solid and crystalline at room temperature, represent, in particular, good waterproofing and oil-proofing agents for textiles.Type: GrantFiled: July 2, 1987Date of Patent: December 20, 1988Assignee: Hoechst AktiengesellschaftInventor: Klaus Raab
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Patent number: 4791134Abstract: The invention relates to milbemycin derivatives of formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic radical or is a pyridyl ring or a heterocyclic oxygen-containing 5- or 6-membered ring, all of which may also be bound through oxygen, and R.sub.2 is methyl, ethyl or isopropyl. These compounds are suitable for controlling arthropode species such as injurious insects or endo- or ectoparasites of animals and are employed in the form of compositions. The compounds can also be used as intermediates for obtaining further milbemycin derivatives.Type: GrantFiled: June 4, 1985Date of Patent: December 13, 1988Assignee: Ciba-Geigy CorporationInventor: Urs Burckhardt
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Patent number: 4789749Abstract: Analogs of the marine natural product manoalide are useful in treating mammals, including humans, in need of a drug having analgesic/anti-inflammatory, immunosuppressive, and/or antiproliferative activity.Type: GrantFiled: February 19, 1986Date of Patent: December 6, 1988Assignee: The Regents of the University of CaliforniaInventors: Robert S. Jacobs, D. John Faulkner
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Patent number: 4789684Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of a microorganism identified as MA-5920. This novel microorganism is formed by the protoplast fusion of strains of Streptomyces avermitilis and Streptomyces hygroscopicus. The structure of the novel compounds isolated from the microorganism is presented based upon analytical studies. The compounds are highly potent antiparasitic, insecticidal, and anthelmintic agents. Compositions for such uses are also disclosed.Type: GrantFiled: May 2, 1985Date of Patent: December 6, 1988Assignee: Merck & Co., Inc.Inventor: Robert T. Goegelman
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Patent number: 4788304Abstract: There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals which comprises administering to a mammal so afflicted an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfony., halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms;X is ##STR2## A is --CH.sub.2 --,--O-- or --S--; m is 0-8;n is 0-7, with the proviso that m+n.ltoreq.Type: GrantFiled: December 7, 1987Date of Patent: November 29, 1988Assignee: American Home Products CorporationInventors: Lisa A. Marshall, Kurt E. Steiner, Guy A. Schiehser
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Patent number: 4788306Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms; ##STR2## A is --CH.sub.2 --, --O-- or --S--; m is 1-8;n is 0-7, with the proviso that m+n.ltoreq.8;or a pharmacologically acceptable salt thereof, and their use as fatty acid oxidation inhibitors possessing a significantly reduced potential for impairment of normal cardiac function, and having particular utility in the treatment of glucose and fatty acid metabolism disorders, such as diabetes.Type: GrantFiled: August 21, 1987Date of Patent: November 29, 1988Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Donald P. Strike
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Patent number: 4785123Abstract: A process for producing an alkylene oxide or mixture of alkylene oxides by a reaction which comprises reacting an alkane, an alkylene, or mixture thereof with an oxygen-containing gas in the presence of at least one molten nitrate salt.Type: GrantFiled: November 12, 1986Date of Patent: November 15, 1988Assignee: Olin CorporationInventor: B. Timothy Pennington
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Patent number: 4783452Abstract: Coordination compounds of platinum(II) with 4,5-bis(aminomethyl)-1,3-dioxolane, intended for use in the treatment of cancer. The compounds may exist as monomers or as linear or cyclic polymers.Type: GrantFiled: October 20, 1986Date of Patent: November 8, 1988Assignee: Johnson Matthey Public Limited CompanyInventors: Alan H. Haines, Christopher Morley
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4782167Abstract: A process is disclosed for preparing butyrolactones, butanediols, and mixtures thereof comprising hydrogenating a hydrogenatable precursor in the presence of an aqueous reaction medium and a catalyst comprising palladium or combinations thereof with rhenium and at least one support selected from the oxides of titanium, zirconium, and hafnium.Type: GrantFiled: January 23, 1987Date of Patent: November 1, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Velliyur N. M. Rao
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Patent number: 4782084Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R.sup.1 is hydrogen are disclosed.Type: GrantFiled: June 29, 1987Date of Patent: November 1, 1988Assignee: Merck & Co., Inc.Inventors: Kamlesh P. Vyas, Hanumath P. Kari
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Patent number: 4778902Abstract: A method of purifying L-ascorbic acid which comprises: bringing an acidic aqueous solution of L-ascorbic acid which contains a cationic surfactant into contact with active carbon activated by chemicals.The method is in particular useful for removing a cationic surfactant from a reaction mixture of diacetone-2-keto-L-gulonic acid or 2-keto-L-gulonic acid with a mineral acid in the presence of an inert solvent and a cationic surfactant, to produce L-ascorbic acid.Type: GrantFiled: July 1, 1986Date of Patent: October 18, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshitaka Fujiwara, Tetsuji Kaizu, Masami Shinohara
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Patent number: 4778809Abstract: The invention relates to ecto- and endoparasitic milbemycins of formula I ##STR1## wherein R is methyl, ethyl, isopropyl or sec-butyl;R.sub.1 is hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl;R.sub.2 is one of the groups ##STR2## in which formulaeis a value from 2 to 6;X is oxygen or sulfur;R.sub.3 is halogen; andR.sub.4 is hydrogen, C.sub.1 -C.sub.12 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy or C.sub.2 -C.sub.6 alkenyloxy; or C.sub.1 -C.sub.18 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy, hydroxy and/or COOG, G being hydrogen, an alkali metal cation or an alkaline earth metal cation; or R.sub.4 is C.sub.3 -C.sub.7 cycloalkyl which is unsubstituted or substituted by halogen and/or C.sub.1 -C.sub.4 alkyl;C.sub.2 -C.sub.18 alkenyl which is unsubstituted or substituted by halogen;C.sub.2 -C.sub.18 alkynyl which is unsubstituted or substituted by halogen;phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, nitro, cyano and/or C.sub.Type: GrantFiled: August 13, 1986Date of Patent: October 18, 1988Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Elmar Sturm
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Patent number: 4777274Abstract: A process for the preparation of isosorbide-2-mononitrate (I) ##STR1## from isosorbide-2,5-dinitrate (II) ##STR2## The isosorbide-2,5-dinitrate (II) is treated, in a reaction medium consisting of an aqueous organic solvent, with salts of metals of low oxidation state.Isosorbide-2-mononitrate (I) is obtained with high selectivity.Type: GrantFiled: November 7, 1986Date of Patent: October 11, 1988Assignee: Consiglio Nazionale Delle Ricerche - Dinamite SpaInventors: Ottorino De Lucchi, Fabiola Filipuzzi, Giorgio Modena, Ettore Camera
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Patent number: 4777270Abstract: A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.Type: GrantFiled: September 4, 1986Date of Patent: October 11, 1988Assignee: Pfizer Inc.Inventor: Frank J. Urban
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Patent number: 4777267Abstract: A 1,3-dioxol-2-one derivative represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent independently a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, a carboxyl group, salts of the carboxyl group, a sulfo group and salts of the sulfo group, and a process for producing the 1,3-dioxol-2-one derivative. The compound is useful for measuring the activity of arylesterase.Type: GrantFiled: December 5, 1986Date of Patent: October 11, 1988Assignee: Kanebo Ltd.Inventors: Hiroshi Tanaka, Mikiya Kitamura, Fumio Sakamoto, Masahiro Taguchi, Mikio Sotomura