R-c(=x)-n-x-c Containing (e.g., Hydroxamic Acid Ester, Etc.) (r Is C Or H And X Is Chalcogen) Patents (Class 514/507)
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Patent number: 5330981Abstract: This application describes 3-arylalkyl esters of 4,5-dihydro-9,10-dioxo-2-anthracenecarboxylic acid and a process for making them. Also described is a method of using the compounds in the treatment of arthritis.Type: GrantFiled: December 30, 1992Date of Patent: July 19, 1994Assignee: Istituto Gentili S.p.A.Inventors: Sergio Rosini, Maurizio Mian
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Patent number: 5326787Abstract: Compounds of the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation or metabolically cleavable group, R is alkyl, cycloalkyl, or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl alkonyl, or carbocyclic aryl, Y is alkylene, alkenylene, or cyclopropyl, and A is optionally substituted cycloalkyl or cycloalkylene are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: August 25, 1993Date of Patent: July 5, 1994Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Jimmie L. Moore, Karen E. Rodriques
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Patent number: 5254731Abstract: Substituted 3,4-dihydronaphthalenes of the formula I ##STR1## wherein R.sup.1 is a methyl or an amino group, R.sup.2 represents a hydrogen atom or a methyl group, and R.sup.3 is a linear or branched chain alkyl residue having 1 to 4 carbon atoms, an allyl or a crotyl group or a cyclopentyl group are disclosed which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of disorders attributable to the action of leucotrienes. The dihydronaphthalenes may be prepared by reacting a compound of formula II ##STR2## with hydroxylamine or a salt thereof to form the corresponding oxime, reducing the oxime to a hydroxylamine of formula III ##STR3## and introducing a --CO--R.sup.1 group.Type: GrantFiled: July 10, 1992Date of Patent: October 19, 1993Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Werner Vollenberg, Johannes Schneider
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Patent number: 5187197Abstract: Novel substituted phenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or is C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl; each of R.sub.2 and R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl; each of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; each R.sub.6 is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 C.sub.4 haloalkoxy or a --CH.dbd.CH, --CH.sub.2 or --CH.sub.2 bridge in the 2,3-or 3,4-position; n is 0, 1 or 2; Z is --NH--CS--NH--, --N.dbd.C(SR.sub.7) --NH--or --N.dbd.C.dbd.N--, and R.sub.7 is C.sub.1 -C.sub.10 alkyl or C.sub.3 -C.sub.Type: GrantFiled: August 20, 1990Date of Patent: February 16, 1993Assignee: Ciba-Geigy CorporationInventor: Josef Ehrenfreund
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Patent number: 5185368Abstract: Compounds of the formula ##STR1## in which R is alkyl having up to 4 carbon atoms, n has an average value of at least 9, X is a radical of the formula --C(.dbd.O)--(NH--SO.sub.2).sub.m -- in which m is 0 or 1 and, if m is 1, the carbonyl group may be bonded to the oxygen atom or to the nitrogen atom, and each of the radicals A.sub.1, A.sub.2 and A.sub.3, independently of the others, is hydrogen or an acyl radical, and salts of salt-forming compounds of formula I, as well as metal complexes of compounds of formula I, in which A.sub.1, A.sub.2 and A.sub.3, are hydrogen can be used as metal chelators and as auxiliaries in diagnosis.Type: GrantFiled: July 20, 1988Date of Patent: February 9, 1993Assignee: Ciba-Geigy CorporationInventors: Heinrich Peter, Theophile Moerker
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Patent number: 5155110Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: September 26, 1988Date of Patent: October 13, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5155127Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: January 18, 1990Date of Patent: October 13, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5137914Abstract: Sulfonylamino substituted bicyclyl hydroxamic acid derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy or halogen; X is alkylene or alkenylene: Y is methylene or oxygen; and n is 0, 1, or 2, or the pharmaceutically acceptable salt thereof. These compounds have an advanced antagonistic activity to thromboxane A.sub.2 (TXA.sub.2)-receptor and are useful for the treatment of thrombosis, vasoconstriction, or bronchoconstriction, and the like disease which are induced by TXA.sub.2.Type: GrantFiled: March 15, 1991Date of Patent: August 11, 1992Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Takaharu Matsuura, Kazuhiro Shirahase
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Patent number: 5130119Abstract: Fluorosubstituted benzene derivatives of Formula I ##STR1## wherein Y, R.sup.2, R.sup.3 and R.sup.4 are defined herein, are NMR diagnostic agents.Type: GrantFiled: October 6, 1989Date of Patent: July 14, 1992Assignee: Schering AktiengesellschaftInventors: Peter Blaszkiewicz, Ulrich Niedballa, Heinz Gries, Hans Bauer, Hanns-Joachim Weinmann
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Patent number: 5047421Abstract: Compounds are described of the general formula: ##STR1## wherein: R.sub.1 is acyl of the formula --C(.dbd.O)--R.sub.5 ; R.sub.2, R.sub.3, and R.sub.4 are each selected from the group consisting of hydrogen and acyl of the formula:--C(.dbd.O)--R.sub.5wherein R.sub.5 is selected from the group consisting of alkyls, substituted alkyls, alkenyls, substituted alkenyls, cycloalkyls, substituted cycloalkyls, arylalkylenes, substituted arylalkylenes, alkylenecycloalkyls, alkylene substituted cycloalkyls, alkynyls substituted alkynyls, aryls and substituted aryls, wherein R.sub.2, R.sub.3 and R.sub.4 are selected such that at least one of R.sub.2, R.sub.3 and R.sub.4 is an acyl.When R.sub.2, R.sub.3 and R.sub.4 include one or more acyls that are not identical to the acyl of R.sub.1, these compounds of formula I are novel compounds. The invention also includes processes to produce the compounds of formula I.Compounds of formula I complex and/or chelate tissue tri-valent ions, especially iron (Fe.sup.Type: GrantFiled: July 31, 1987Date of Patent: September 10, 1991Assignee: Oral-DInventor: Donald E. Green
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4999377Abstract: 2-(2-Hydroxy-3-phenoxypropylamino)ethylphenoxyacetamide compounds are disclosed as useful in the treatment of obesity and related conditions. Processes for their preparation are described, as are novel intermediates and pharmaceutical compositions containing them.Type: GrantFiled: January 19, 1989Date of Patent: March 12, 1991Assignee: Imperial Chemical Industries PLCInventors: Peter W. R. Caulkett, Michael J. Cooper, Murdoch Eakin, Geraint Jones
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Patent number: 4977188Abstract: Novel hydroxamic acid and derivatives of formula (I)Ar--(L--Ar').sub.q --(X).sub.k --(Y).sub.p --Q (I)are disclosed. Also described are their preparation, compositions containing them and their use.Type: GrantFiled: December 11, 1989Date of Patent: December 11, 1990Assignee: Burroughs Wellcome Co.Inventors: Geoffrey Kneen, William P. Jackson, Peter J. Islip, Peter J. Wates
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Patent number: 4935443Abstract: Disclosed are compounds having the formula: ##STR1## wherein: R.sub.1 is hydrogen, analkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group;R.sub.2 is an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group, an alkyl group having 1 to 6 carbon atoms which contains an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups having 1 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.These compounds increase the sensitivity of hypoxic cancer cells to radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: June 26, 1989Date of Patent: June 19, 1990Assignee: Merck & Co., Inc.Inventor: Walfred S. Saari
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Patent number: 4933329Abstract: Novel bis-S-alkylbenzene derivatives capable of inhibiting lipoxygenase, inparticular, 5-lipoxygenase are disclosed. It is expected that the compounds, which are hardly metabolized in vivo, are highly useful in the treatment and/or prevention of various diseases, including allergic diseases such as asthma, inflammation, myocardial infarction, nephritis, scabies and gout.Type: GrantFiled: December 6, 1988Date of Patent: June 12, 1990Assignee: Green Cross CorporationInventors: Youichiro Naito, Yasunari Yamaura, Masanori Sugiura, Chikara Fukaya, Kazumasa Yokoyama
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Patent number: 4923896Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: February 9, 1989Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4906667Abstract: Phenyl hydroxamic acids are disclosed having the general formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is NR, oxygen, sulfur, ##STR2## or a single bond, and Y is NR, oxygen, sulfur, ##STR3## or a single bond, where R can be hydrogen or lower alkyl, g can be 1 or 2, and with the proviso that at least one of X and Y is other than a single bond; Z is aryl, aralkyl or cycloalkyl; R.sub.1 is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl or aryl; R.sub.2 is hydrogen, lower alkyl, aroyl or acyl; m is 0 to 4 carbon atoms; and, n is 0 to 4 carbon atoms further providing that if one of X or Y is oxygen, the other of X or Y must be oxygen and further that when X and Y are oxygen Z cannot be aralalkyl.These new compounds have been found to be inhibitors or arachidonic acid 5-lipoxygenase and are therefore useful as antiallergy agents and antipsoriatics.Type: GrantFiled: May 23, 1988Date of Patent: March 6, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Ravi K. Varma, Eric M. Gordon, Martin F. Haslanger
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Patent number: 4782085Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; andZ is ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.Type: GrantFiled: July 27, 1987Date of Patent: November 1, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Ravi K. Varma, Eric M. Gordon
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Patent number: 4752615Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4728670Abstract: Biphenyl hydroxamic acids are provided having the structure ##STR1## wherein m is 1 to 7, X is S, O or NH, R is H, lower alkyl, aryl, aralkyl or cycloalkyl and R.sup.1 is H, lower alkyl, aryl, aralkyl, cycloalkyl, alkanoyl or aroyl.These compounds are inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.Type: GrantFiled: June 4, 1986Date of Patent: March 1, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Martin F. Haslanger, Ravi K. Varma, Eric M. Gordon
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Patent number: 4711900Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; and ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.Type: GrantFiled: July 23, 1986Date of Patent: December 8, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Ravi K. Varma, Eric M. Gordon
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Patent number: 4703110Abstract: The application discloses certain benzoic acid compounds, the same being more adequately described as benzoic acid derivatives having a para substituent which is a substituted phenyl radical attached to the benzoic acid in the para position by any one of a variety of linking groups, representative compounds being p-(3,4-diisopropylphenylcarbamoyl) benzoic acid and p-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylcarbamoyl)benzoic acid, pharmaceutical compositions thereof, method of treating therewith, method of diagnosis therewith, and method for the preparation thereof. The compounds and compositions are useful for diagnosis of leukemia types, the treatment of dermatological disorders, and as differentiation-inducing agents for neoplastic cells.Type: GrantFiled: July 8, 1985Date of Patent: October 27, 1987Assignee: Koichi ShudoInventor: Koichi Shudo
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Patent number: 4681894Abstract: The synthesis of amido substituted naphthalenes and their intermediates is described. The intermediates and amido substituted naphthalenes are useful as anti-inflammatory agents.Type: GrantFiled: September 26, 1986Date of Patent: July 21, 1987Assignee: Ortho Pharmaceutical CorporationInventors: William V. Murray, Michael P. Wachter
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Patent number: 4613616Abstract: The present invention relates to polymeric iron chelators based upon hydroxamic acids having the general formula: ##STR1## wherein R is hydrogen or lower alkyl. The present compound is useful for the treatment of iron overload disorders particularly arising from iron poisoning and the disease .beta.-thalassemia otherwise known as Cooley's Anemia. The polymeric hydroxamic acids of the present invention exhibit high selectivity for iron, good water solubility for both the chelator and its iron complex, low toxicity and, most significantly, increased bioactivity, i.e., the ability to remove iron in vivo.Type: GrantFiled: July 20, 1984Date of Patent: September 23, 1986Assignee: Research CorporationInventors: Anthony Winston, D. V. P. R. Varaprasad
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Patent number: 4588748Abstract: Benzylidene derivatives of the formula: ##STR1## wherein n is 3, R represents an amino or hydroxy radical, or a group --OM in which M is an alkali metal, X.sub.1 and X.sub.2 are both Cl, and X.sub.3 is hydrogen are new compounds possessing useful pharmacological properties; they are, more particularly, useful in the treatment of various diseases of the central nervous system.Type: GrantFiled: September 25, 1984Date of Patent: May 13, 1986Assignee: SynthelaboInventor: Jean-Pierre Kaplan
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Patent number: 4584315Abstract: The present invention relates to novel methods of use for known pharmacological anti-allergenic agents including disodiumchromoglycate (DSCG) and related compounds thereof, including generally bis chromones, benzopyrans, oxamic acids and salts or esters of each, preferably lodoxamide, its THAM salt and ethyl ester. All are subsequently included in the term biologues. The methods are for the treatment of pathological cardiovascular ischemic states in animals, particularly humans. Additionally, novel compositions incuding the biologues of the present invention in combination with known vasodilators and feed stuffs are also disclosed.Type: GrantFiled: December 13, 1983Date of Patent: April 22, 1986Assignee: The Upjohn CompanyInventor: Norman B. Marshall