Chalcogen Bonded Directly To Ring Sulfur By Nonionic Bonding Patents (Class 514/446)
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Patent number: 5270301Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.Type: GrantFiled: May 7, 1990Date of Patent: December 14, 1993Assignee: ICI Americas Inc.Inventor: Donald J. Wolanin
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Patent number: 5216002Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.Type: GrantFiled: December 7, 1990Date of Patent: June 1, 1993Assignee: Eli Lilly and CompanyInventors: Jaswant S. Gidda, Jill A. Panetta, Michael L. Phillips
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Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5032609Abstract: The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 16, 1988Date of Patent: July 16, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
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Patent number: 4990505Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein the substituents are defined in the specification, and physiologically acceptable salts and solvates thereof.The compounds of formula (I) have a selective stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: April 18, 1989Date of Patent: February 5, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4959385Abstract: This invention relates to thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl, Y represents an ethylene or methylene radical or a valency bond, and n represents 0 or 1, bioprecursors thereof and pharmaceutically acceptable salts thereof which possess useful pharmacological properties, processes for their preparation and compositions containing them.Type: GrantFiled: January 19, 1989Date of Patent: September 25, 1990Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. Walsh, Jean-Claude Aloup
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Patent number: 4933369Abstract: The present invention relates to new compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R.sup.1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R.sup.2 wherein R.sup.2 is lower alkyl, alkenyl, alkoxy, or aralkyl; n is an integer of from 2-4; m is an integer of from 0-4; A is S(O).sub.x wherein x is an integer of from 0-2; and Ar is phenyl or thienyl. These compounds are useful as analgesics.Type: GrantFiled: September 30, 1988Date of Patent: June 12, 1990Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Donald W. Hansen, Jr., Gilbert W. Adelstein
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Patent number: 4880828Abstract: A new class of 2-(tetrahydro-2-theinyl)phenyl esters of phosphorothioic acid is disclosed. This class of compounds is an effective pesticide and finds particular application as an insecticide. A class of pesticidal compositions employing these compounds in combination with a carrier therefor is also set forth.Type: GrantFiled: January 29, 1988Date of Patent: November 14, 1989Assignees: Uniroyal Chemical, Inc., Uniroyal Chemical Ltd./LteeInventors: Anupama Mishra, Richard C. Moore
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Patent number: 4873350Abstract: The present invention relates to new diselenobis-benzoic acid amides of primary and secondary amines of the general formula (I): ##STR1## and processes for the treatment of diseases in humans caused by a cell injury.Type: GrantFiled: October 3, 1988Date of Patent: October 10, 1989Assignee: A Nattermann & CIE GmbHInventors: Andre Welter, Harmut Fischer, Leon Christiaens, Albrecht Wendel, Eugen Etschenberg, Norbert Dereu, Peter Kuhl, Eric Graf
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Patent number: 4861766Abstract: An antimicrobial composition containing, as a mixture of active ingredients, (A) at least one complex of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a substituted or unsubstituted monovalent hydrocarbyl group, R.sup.2 and R.sup.3 are each independently a hydrogen atom or a halogen atom, M is a metal or ammonium cation, X is a complex-forming anion, a is 1 or 2 and b is an integer which is such that the anion X satisfies the valence of the cation M, and (B) 3,3,4,4-tetrachlorotetrahydrothiophene 1,1-dioxide effectively inhibits the growth of microbes in, for example, industrial water systems for pulp and paper.Type: GrantFiled: December 19, 1986Date of Patent: August 29, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Mitsui, Shigeru Kurose, Hiroshi Saimoto
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Novel class of acyl-derivatives of carnitine, process for preparing same and therapeutic use thereof
Patent number: 4859698Abstract: A novel class of acyl-derivatives of carnitine is disclosed wherein the acyl radical is either the radical of unsaturated organic acids (typically, acrylic acid) or the radical of saturated organic acids substituted with tert-alkyl, cycloalkyl, cycloalkenyl, alkoxyl, heterocyclic and carboalkoxylradicals, or with aldehyde or hydroxy groups. These acyl-derivatives of carnitine are useful therapeutical agents in the treatment of cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias.Type: GrantFiled: May 31, 1988Date of Patent: August 22, 1989Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Claudio Cavazza, Paolo De Witt, Maria O. Tinti -
Patent number: 4847288Abstract: The present invention relates to compounds which are allenyl amines, more specifically, .beta.-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a noval reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.Type: GrantFiled: February 8, 1988Date of Patent: July 11, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Thomas M. Bargar, Charlotte L. Barney, Donald P. Matthews, Robert J. Broersma
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Patent number: 4546110Abstract: Compounds which are .beta.-farnesene derivatives obtainable as a Diels-Adler adduct of .beta.-farnesene and a dienophile or by a modification of such an adduct in a manner as defined herein are of value in pest control, particularly in the control of aphids.Type: GrantFiled: January 20, 1983Date of Patent: October 8, 1985Assignee: National Research Development CorporationInventors: Glenn W. Dawson, David C. Griffiths, John A. Pickett