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)
  • Patent number: 5330981
    Abstract: 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: Grant
    Filed: December 30, 1992
    Date of Patent: July 19, 1994
    Assignee: Istituto Gentili S.p.A.
    Inventors: Sergio Rosini, Maurizio Mian
  • Patent number: 5326787
    Abstract: 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: Grant
    Filed: August 25, 1993
    Date of Patent: July 5, 1994
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Jimmie L. Moore, Karen E. Rodriques
  • Patent number: 5254731
    Abstract: 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: Grant
    Filed: July 10, 1992
    Date of Patent: October 19, 1993
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Werner Vollenberg, Johannes Schneider
  • Patent number: 5187197
    Abstract: 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: Grant
    Filed: August 20, 1990
    Date of Patent: February 16, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Josef Ehrenfreund
  • Patent number: 5185368
    Abstract: 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: Grant
    Filed: July 20, 1988
    Date of Patent: February 9, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Heinrich Peter, Theophile Moerker
  • Patent number: 5155110
    Abstract: 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: Grant
    Filed: September 26, 1988
    Date of Patent: October 13, 1992
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Daniel L. Flynn
  • Patent number: 5155127
    Abstract: 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: Grant
    Filed: January 18, 1990
    Date of Patent: October 13, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5137914
    Abstract: 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: Grant
    Filed: March 15, 1991
    Date of Patent: August 11, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Takaharu Matsuura, Kazuhiro Shirahase
  • Patent number: 5130119
    Abstract: 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: Grant
    Filed: October 6, 1989
    Date of Patent: July 14, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Blaszkiewicz, Ulrich Niedballa, Heinz Gries, Hans Bauer, Hanns-Joachim Weinmann
  • Patent number: 5047421
    Abstract: 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: Grant
    Filed: July 31, 1987
    Date of Patent: September 10, 1991
    Assignee: Oral-D
    Inventor: Donald E. Green
  • Patent number: 5010104
    Abstract: 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: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 4999377
    Abstract: 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: Grant
    Filed: January 19, 1989
    Date of Patent: March 12, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter W. R. Caulkett, Michael J. Cooper, Murdoch Eakin, Geraint Jones
  • Patent number: 4977188
    Abstract: 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: Grant
    Filed: December 11, 1989
    Date of Patent: December 11, 1990
    Assignee: Burroughs Wellcome Co.
    Inventors: Geoffrey Kneen, William P. Jackson, Peter J. Islip, Peter J. Wates
  • Patent number: 4935443
    Abstract: 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: Grant
    Filed: June 26, 1989
    Date of Patent: June 19, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Patent number: 4933329
    Abstract: 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: Grant
    Filed: December 6, 1988
    Date of Patent: June 12, 1990
    Assignee: Green Cross Corporation
    Inventors: Youichiro Naito, Yasunari Yamaura, Masanori Sugiura, Chikara Fukaya, Kazumasa Yokoyama
  • Patent number: 4923896
    Abstract: 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: Grant
    Filed: February 9, 1989
    Date of Patent: May 8, 1990
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4906667
    Abstract: 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: Grant
    Filed: May 23, 1988
    Date of Patent: March 6, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon, Martin F. Haslanger
  • Patent number: 4782085
    Abstract: 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: Grant
    Filed: July 27, 1987
    Date of Patent: November 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon
  • Patent number: 4752615
    Abstract: 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: Grant
    Filed: November 13, 1986
    Date of Patent: June 21, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
  • Patent number: 4728670
    Abstract: 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: Grant
    Filed: June 4, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Martin F. Haslanger, Ravi K. Varma, Eric M. Gordon
  • Patent number: 4711900
    Abstract: 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: Grant
    Filed: July 23, 1986
    Date of Patent: December 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon
  • Patent number: 4703110
    Abstract: 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: Grant
    Filed: July 8, 1985
    Date of Patent: October 27, 1987
    Assignee: Koichi Shudo
    Inventor: Koichi Shudo
  • Patent number: 4681894
    Abstract: The synthesis of amido substituted naphthalenes and their intermediates is described. The intermediates and amido substituted naphthalenes are useful as anti-inflammatory agents.
    Type: Grant
    Filed: September 26, 1986
    Date of Patent: July 21, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: William V. Murray, Michael P. Wachter
  • Patent number: 4613616
    Abstract: 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: Grant
    Filed: July 20, 1984
    Date of Patent: September 23, 1986
    Assignee: Research Corporation
    Inventors: Anthony Winston, D. V. P. R. Varaprasad
  • Patent number: 4588748
    Abstract: 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: Grant
    Filed: September 25, 1984
    Date of Patent: May 13, 1986
    Assignee: Synthelabo
    Inventor: Jean-Pierre Kaplan
  • Patent number: 4584315
    Abstract: 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: Grant
    Filed: December 13, 1983
    Date of Patent: April 22, 1986
    Assignee: The Upjohn Company
    Inventor: Norman B. Marshall