Oxygen Bonded Directly To Sulfur (e.g., Sulfoxides, Etc.) Patents (Class 514/708)
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Patent number: 5672627Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 9, 1996Date of Patent: September 30, 1997Assignee: G.D. Searle & Co.Inventors: Horng-Chih Huang, David R. Reitz
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Patent number: 5622994Abstract: Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Many different disorders can be treated using these compounds, including diseases or disorders of the central and peripheral nervous systems, and disorders arising from ischemia, infection, inflammation, oxidation from exposure to radiation or cytotoxic compounds, as well as due to naturally occurring processes such as aging.Type: GrantFiled: March 15, 1994Date of Patent: April 22, 1997Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventors: John M. Carney, Robert A. Floyd
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Patent number: 5589510Abstract: A method for inhibiting retroviral infection in a subject comprising administering to said subject a therapeutically effective amount of a naphthalenesulfonic acid compound or a pharmaceutically acceptable salt thereof, as herein defined.Type: GrantFiled: May 15, 1995Date of Patent: December 31, 1996Assignee: Fuji Immunopharmaceuticals Corp.Inventors: Mitsunori Ono, Yumiko Wada, Yaming Wu, Hiroshi Kitaguchi, Yumiko Jimbo, Ryoichi Nemori, Stephen Gillies, Kin-Ming Lo
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Patent number: 5508305Abstract: 2,4-disulfonyl .alpha.-phenyl-tert-butyl nitrone and its pharmaceutically acceptable salts are disclosed. These materials are useful as pharmaceutical agents for oral or parenteral, e.g. intravenous administration to patients suffering from acute central nervous system oxidation as occurs in a stroke or from gradual central nervous system oxidation which can exhibit itself as progressive central nervous system function loss. The materials are also used to ameliorate the side effects of oxidative-damage causing antineoplastic disease treatments.Type: GrantFiled: June 6, 1995Date of Patent: April 16, 1996Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventor: John M. Carney
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Patent number: 5488075Abstract: The present invention relates to a contraceptive for use by a male. The contraceptive consists of a copolymer of styrene maleic anhydride which is prepared by the step of irradiation at a dose of 0.2 to 0.24 megarad for every 40 gms. of the copolymer. The contraceptive consists of an injectable fluid of said copolymer and pure dimethyl sulphoxide.Type: GrantFiled: September 20, 1994Date of Patent: January 30, 1996Inventor: Sujoy K. Guha
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Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5312842Abstract: The present invention relates to cyclopentane heptenylsulfinylalkyl and heptanylsulfinylalkyl-2-aliphatic or arylaliphatic derivatives. In particular, heptenylsulfinylmethyl and heptanylsulfinylmethyl 2-aliphatic or arylaliphatic derivatives, substituted at the 3 and/or 5 position of the cyclopentane ring with radicals selected from the group consisting of hydroxy, alkylcarboxy and mixtures thereof, are disclosed. These compounds are useful as ocular hypotensives.Type: GrantFiled: October 30, 1992Date of Patent: May 17, 1994Assignee: Allergan, Inc.Inventor: Ming Fai Chan
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Patent number: 5290791Abstract: The present invention relates to a fungicidal composition intended for the protection of the multiplication products of cultivated plants, containing:(a) 2-(4-chlorobenzylidene)-5,5-dimethyl-1-(1H-1,2,4-triazol-1-ylmethyl)-1-cyc lopentanol;(b) one or more fungicides suitable for the protection of the said multiplication products, optionally one or more insecticides,(c), an agriculturally acceptable inert vehicle and an agriculturally acceptable surfactant.The invention also relates to a method for protecting the multiplication products of plants against fungal diseases using these compositions.Type: GrantFiled: June 13, 1991Date of Patent: March 1, 1994Assignee: Rhone-Poulenc Secteur AgrochimieInventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
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Patent number: 5214070Abstract: The invention concerns a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms.The invention also concerns processes for the manufacture of a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cycloalkane. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: August 21, 1991Date of Patent: May 25, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Thomas G. C. Bird, Philip N. Edwards
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Patent number: 5214069Abstract: The invention concerns a compound of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; wherein R.sup.2 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; and whereinR.sup.3 is hydroxy-(1-4C)alkyl, mercapto-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, (3-4C)alkenyloxy-(1-4C)alkyl, (3-4C)alkynyloxy-(1-4C)alkyl, (1-4C)alkoxy-(2-4C)alkoxy-(1-4C)alkyl, (1-4C)alkylthio-(1-4C)alkyl, (1-4C)alkylsulphinyl-(1-4C)alkyl, (1-4C)alkylsulphonyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, (2-4C)alkanoyl-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl or cyano-(1-4C)alkyl; or R.sup.Type: GrantFiled: January 23, 1992Date of Patent: May 25, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventor: Jean-Marc M. M. Girodeau
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Patent number: 5188663Abstract: An aquatic antifouling composition comprising (A) at least one 4-isothiazolin-3-one compound represented by the general formula: ##STR1## where X.sub.1 and X.sub.2 respectively represent a hydrogen atom or a halogen atom, and (B) at least one insoluble dithiocarbamic acid derivatives possessing a dithiocarbamyl group ##STR2## selected from the group consisting of divalent and higher heavy metal (zinc, manganese, copper, iron, and nickel) salts of ethylenebisdithiocarbamic acid, linear or branched propylenebisdithiocarbamic acid, linear or branched butylenebisdithiocarbamic acid, N-substituted ethylenebisdithiocarbamic acid, N,N'-substituted ethylenebisdithiocarbamic acid, N-substituted propylenebisdithiocarbamic acid, N,N'-substituted propylene-bisdithiocarbamic acid, N-substituted butylenebisdithiocarbamic acid, and N,N'-substituted butylenebisdithiocarbamic acid.Type: GrantFiled: September 16, 1991Date of Patent: February 23, 1993Assignee: Rohm and Haas CompanyInventors: Hirotake Ikari, Teruyoshi Takahashi
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Patent number: 5183814Abstract: The invention relates to a therapeutic product comprising an oestrogen and a pure antioestrogen for simultaneous, sequential or separate use in selective oestrogen therapy of perimenopausal or postmenopausal conditions; to a process for the manufacture of said product and to a pharmaceutical composition containing said product. The invention also relates to a pharmaceutical composition comprising an oestrogen and a pure antioestrogen and to a process for the manufacture of said composition.Type: GrantFiled: June 6, 1989Date of Patent: February 2, 1993Assignee: Imperial Chemical Industries PLCInventor: Michael Dukes
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Patent number: 5132118Abstract: A method and composition for the preventive and curative treatment of exercise-induced pulmonary hemorrhage in animals. The method comprises administration to the animal of a mixture of urea, alkaline potassium salts and magnesium salts. The composition comprises a mixture of urea, alkaline potassium salts, and magnesium salts, and if required, a pharmaceutically acceptable carrier.Type: GrantFiled: November 29, 1990Date of Patent: July 21, 1992Inventor: John A. Mills
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Patent number: 5125967Abstract: A composition comprises an isothiazolinone or an isothiazolothione and a substituted urea or a halogen-containing aromatic alkyl sulphoxide or sulphone. The isothiazolinone derivative can be 1,2-benzisothiazolin-3-one. The substituted urea may be 3-(3,4-dichlorophenyl)-1-1-dimethylurea. The sulphoxide or sulphone may be a sulphone derivative such as di-iodomethyl-4-methylphenyl sulphone. A useful composition comprises 1,2-benzisothiazolin-3-one and the specified urea or sulphone derivative. The composition may include other materials including other compounds having anti-microbial properties.Type: GrantFiled: March 29, 1990Date of Patent: June 30, 1992Assignee: Imperial Chemical Industries PLCInventors: Fraser F. Morpeth, Malcolm Greenhalgh
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Patent number: 5091180Abstract: The present invention is directed to the in vivo use of compounds which prevent the generation of, effectively scavenge, or detoxify a reactive oxygen metabolite that mediates a toxic effect of rhabdomyolysis and myoglobinuria. The compounds of the invention can be used to prevent or reduce rhabdomyolysis-induced renal damage, and include but are not limited to free radical scavengers, iron chelators, oxidizable compounds, enzymes which metabolize reactive oxygen metabolites or their precursors, and biosynthetic precursors thereof.Type: GrantFiled: November 30, 1990Date of Patent: February 25, 1992Assignee: Administrators of the Tulane Educational FundInventors: Patrick D. Walker, Sudhir V. Shah
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Patent number: 5087637Abstract: Diarylacetylenes of the formula I ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.2 and R.sup.3 are each hydrogen or, when R.sup.1 is hydrogen, together form a --C(CH.sub.3).sub.2 --B--C(CH.sub.3).sub.2 -- group (where B is --CH.sub.2 Ch.sub.2 -- or --CH(CH.sub.3)--) or --OC(Ch.sub.3) (Z)CH.sub.2 CH.sub.2 -- group (where Z is C.sub.1 -C.sub.2 -alkyl) or R.sup.2 is C.sub.1 -C.sub.3 -alkoxy and R.sup.3 is C.sub.1 -C.sub.10 -alkyl or, when R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are each alkyl as defined above, R.sup.4 is C.sub.1 -C.sub.6 -alkyl and n is 0, 1 or 2, are prepared as described and used as active compounds in drugs and cosmetics.Type: GrantFiled: August 1, 1990Date of Patent: February 11, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5084478Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkylwherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: April 14, 1989Date of Patent: January 28, 1992Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, Howard Tucker
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Patent number: 5061733Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinklin, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents --S(O)R, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower-alkyl, lower-alkoxy, hydroxy, mono-lower-alkyl amino or di-lower-alkylaminoand pharmaceutically acceptable salts thereof.Type: GrantFiled: May 8, 1990Date of Patent: October 29, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Graeme F. Bryce, Stanley S. Shapiro
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Patent number: 5053547Abstract: A compound of formula (I) ##STR1## its isomers and its salts in which --R.sub.1, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, halogen, C.sub.1 -C.sub.8 -acyloxy or hydroxyl;--R' is hydrogen or C.sub.1 -C.sub.6 -alkyl;--R" is either a polyene chain or a benzene ring are useful in cosmetics and in the treatment of various dermatological and other complaints.Type: GrantFiled: November 14, 1989Date of Patent: October 1, 1991Assignee: L'OrealInventors: Gerard Lang, Jean Maignan, Serge Restle, Braham Shroot
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Patent number: 5039664Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.Type: GrantFiled: March 8, 1989Date of Patent: August 13, 1991Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, William H. Parsons, William J. Greenlee, Prasun K. Chakravarty
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Patent number: 5037807Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.Type: GrantFiled: March 8, 1989Date of Patent: August 6, 1991Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, William J. Greenlee, William H. Parsons, Prasun K. Chakravarty
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Patent number: 5032613Abstract: A solution of DMSO and a body reactive agent (such as citric acid) is provided, and is typically topically applied to the body.Type: GrantFiled: February 5, 1990Date of Patent: July 16, 1991Assignees: W. Keith R. Watson, William W. HaefligerInventor: W. Keith R. Watson
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Patent number: 4978687Abstract: A method of treating an infection attributable to a retrovirus comprises the step of administering to the patient at effective amount of a compound of formula (I):(R).sub.2 S(O).sub.n (I)wherein R is methyl or ethyl and n is 1 or 2.Type: GrantFiled: August 14, 1989Date of Patent: December 18, 1990Assignee: Rhoderton Corporation N.V.Inventor: Josep M. V. I. Pascuchi
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Patent number: 4975271Abstract: A muscosal delivery system is provided for use in treating periodontal disease. The system is composed of a chemotherapeutic agent dissolved in a skin-penetration enhancer. The solution of chemotherapeutic agent and skin-penetration enhancer is placed into the periodontal pocket where the agent is transported into the surrounding gingival tissue by means of the penetration enhancer.Type: GrantFiled: December 19, 1988Date of Patent: December 4, 1990Assignee: Vipont Pharmaceutical, Inc.Inventors: Richard L. Dunn, Kenneth C. Godowski, Ronald J. Harkrader, George L. Southard
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Patent number: 4973605Abstract: Methylsulfonylmethane is effective to relieve pain and nocturnal cramps and to reduce stress-induced deaths in ainmals.Type: GrantFiled: July 26, 1989Date of Patent: November 27, 1990Inventor: Robert J. Herschler
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Patent number: 4945094Abstract: The present invention relates to a combination for use in improving the condition of skin and/or mucosa, especially gastro-intestinal mucosa which combination comprises procaine and a physiologically acceptable, organic, in vivo sulphydryl group releasing agent.Application of a combination of the invention to skin and/or mucosa can improve the condition thereof in a number of ways including increasing its resistance to non-mechanical injury and to degeneration and increasing regeneration as for example in wound healing and skin graft taking.Type: GrantFiled: February 1, 1988Date of Patent: July 31, 1990Inventor: Aws S. M. Salim
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Patent number: 4940707Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle, attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.Type: GrantFiled: February 14, 1989Date of Patent: July 10, 1990Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 4931474Abstract: An ether derivative compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, chloro, methyl or (C.sub.1 -C.sub.3)-alkoxy, R.sup.2 is (C.sub.1 -C.sub.6)-alkyl, R.sup.3 is hydrogen, chloro, bromo, fluoro, --CF.sub.3, nitro, (C.sub.1 -C.sub.4)-alkyl, methoxy, phenoxy or (C.sub.1 -C.sub.3)-alkylthio, R.sup.4 is hydrogen, chloro or methyl, Y is oxygen, sulfur, sulfinyl, sulfonyl, or imino, x is 0, 1 or 2, y is 0 or 1, a is 0 or 1, b is an integer of 0 to 6, c is 0 or 1, d is 0, 1 or 2, e is 0 or 1, except that all of a, b and c are zero.Type: GrantFiled: July 27, 1987Date of Patent: June 5, 1990Assignee: Nippon Kayaku Kabushiki KaishaInventors: Shoichi Kato, Tatsumi Hayaoka
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Patent number: 4898884Abstract: A solution of DMSO and a body reactive agent (such as citric acid) is provided, and is typically topically applied to the body.Type: GrantFiled: February 16, 1986Date of Patent: February 6, 1990Assignees: Kenneth R. Watson, William W. HaefligerInventor: W. Keith R. Watson
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Patent number: 4877899Abstract: Sulfur-substituted alkenyl compounds, synthesis thereof, intermediates therefor, and the use of the compounds to control pests.Type: GrantFiled: November 23, 1983Date of Patent: October 31, 1989Assignee: Sandoz Ltd.Inventors: Robert L. Carney, Thomas L. Brown
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Patent number: 4855293Abstract: The use is described of both (i) a systemic non-steroidal anti-inflammatory drug and (ii) a compound of formula (1) ##STR1## wherein n is 1 or 2;m is 2-5 and X is cis or trans --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; or m is 1-4 and X is --CH.dbd.C.dbd.CH--;R.sup.1 is phenyl, substituted phenyl or naphthyl;Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl in the therapy or prophylaxis of inflammatory conditions and for analgesia in humans.Pharmaceutical compositions containing both (i) and (ii) are also described.Type: GrantFiled: October 21, 1987Date of Patent: August 8, 1989Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Duncan B. Judd
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Patent number: 4855294Abstract: A composition and method for reducing the skin irritation properties of a transdermal drug/enhancer composition which comprises incorporating into said composition, either prior to or at the time of application the skin, an effective amount of glycerin. When incorporated into the drug/enhancer composition prior to application to the skin the glycerin content will be between about 0.1 and 70 wt. %, preferably between about 1.0 and 50 wt. % and most preferably between about 5.0 and 20 wt. % of the composition.Type: GrantFiled: September 6, 1988Date of Patent: August 8, 1989Assignee: TheraTech, Inc.Inventors: Dinesh C. Patel, Charles D. Ebert
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Patent number: 4851442Abstract: A solution of lidocaine hydrochloride, dimethyl sulfoxide and citric acid or citric acid monohydrate is prepared, for topical application to an animal or human.Type: GrantFiled: May 2, 1988Date of Patent: July 25, 1989Assignees: W. Keith R. Watson, William W. HaefligerInventor: W. Keith R. Watson
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Patent number: 4847255Abstract: The use is described of compounds of formula ##STR1## in which n is 1 or 2;m is 2-5 and X is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; or m is 1-4 and X is --CH.dbd.CH.dbd.CH--;R.sup.1 is phenyl, substituted phenyl or naphthyl;Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl, in the therapy or prophylaxis of atherosclerosis and other disorders associated with abnormal levels of blood lipids and serum cholesterol.Type: GrantFiled: October 21, 1987Date of Patent: July 11, 1989Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Duncan B. Judd, Malcolm Johnson, Peter Strong
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Patent number: 4847369Abstract: Compounds are described of formula (1) ##STR1## wherein m is 1 to 4;n is zero, 1 or 2;p is 1 to 4;Z is a group CO.sub.2 R.sup.1 where R.sup.1 is(a) a hydrogen atom or an alkyl, phenalkyl or 2-naphthyl group;(b) phenyl or substituted phenyl;(c) --CH.sub.2 COR.sup.5 where R.sup.5 is phenyl substituted phenyl or 2-naphthyl;or Z is --CH.sub.2 OH, --CHO or CONHR.sup.9 [where R.sup.9 is a hydrogen atom or alkyl, aryl, --COR.sup.10 (where R.sup.10 is a hydrogen atom or an alkyl or aryl group) Or --SO.sub.2 R.sup.11 (where R.sup.11 is an alkyl or aryl group)];Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl.These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.Type: GrantFiled: October 21, 1987Date of Patent: July 11, 1989Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Duncan B. Judd, James D. Meadows
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Patent number: 4847305Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.Type: GrantFiled: May 23, 1988Date of Patent: July 11, 1989Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 4845129Abstract: The invention discloses certain diaryl substituted cyclopentane and cyclopentene derivatives useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated broncho-constriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lug injury.Type: GrantFiled: March 14, 1988Date of Patent: July 4, 1989Assignee: Sandoz Pharm. Corp.Inventors: Robert C. Anderson, William J. Houlihan, Howard C. Smith, Edwin B. Villhauer
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Patent number: 4845119Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent of each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substitutent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl;wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --; andwherein R.sup.9 is alkyl or up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: February 18, 1986Date of Patent: July 4, 1989Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, Howard Tucker
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Patent number: 4835191Abstract: Compositions of hydroquinone and an aliphatic sulfoxide of the formula ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, substituted alkyl, alkenyl, or hetero groups, along with appropriate pharmaceutical diluents, excipients, and/or adjuvants are disclosed. The preferred aliphatic sulfoxide is dimethyl sulfoxide, and the sulfoxide content can range between about 1 and 99 weight percent, preferably between about 25 and 90 weight percent. The hydroquinone content ranges between about 1 and 10 weight percent, preferably between about 1.5 and 5 weight percent.Also disclosed are various methods for preventing, eliminating, or substantially reducing post-inflammatory hyperpigmentation by applying these compositions to hyperpigmented tissue of hyman or animal subjects as often as necessry to remedy or alleviate the hyperpigmentation.Type: GrantFiled: September 1, 1987Date of Patent: May 30, 1989Inventor: Ken P. Biegeleisen
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Patent number: 4835190Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.Type: GrantFiled: June 5, 1987Date of Patent: May 30, 1989Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 4833164Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 19, 1986Date of Patent: May 23, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4831194Abstract: The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in which p1 R and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms,R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s),and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient.Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.Type: GrantFiled: July 23, 1987Date of Patent: May 16, 1989Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Janos Kreidl, Peter Turcsanyi, Zsuzsanna Aracs nee Trischler, Bela Stefko, Judit Meszaros nee Brill, Ida Deutsch nee Juhasz, Jeno Szilbereky, Eva Csizer, Szilard Vezer, Erik Bogsch, Jozsef Bakos, Laszlo Szotyori, Balint Heil
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Patent number: 4808625Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a phenanthrene or substituted phenanthrene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five-or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 28, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4801444Abstract: A medicinal preparation for individual prevention of venereal diseases and treatment of urogenital trichomoniasis comprises an efficient quantity of an active principle which is essentially a synergistic mixture of para-nitro-alpha-chlorocinnamic aldehyde of the formula: ##STR1## dimethylsulphoxide and a pharmaceutical excipient. Polyethyleneglycol having a molecular mass of 400 is recommended to be used as the pharmaceutical excipient.A method for treatment of urogenital trichomoniasis consists in application of the medicinal preparation in question to the mucosa of human genitalia in a dose of 1.5 to 10 ml twice a day for 5 to 7 days.Type: GrantFiled: March 3, 1988Date of Patent: January 31, 1989Assignee: Poltavsky Meditsinsky Stomatologichesky InstitutInventor: Vladimir G. Kravchenko
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Patent number: 4751240Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: June 14, 1988Assignee: Imperial Chemical Industries PLCInventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
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Patent number: 4747845Abstract: A synthetic resin matrix system for the delayed and extended duration delivery of drugs to humans and animals is disclosed consisting of a polymer, such as poly(2-hydroxyethylmethacrylate), referred to as PHEMA, an organic solvent, such as polyethylene glycol (PEG), and a hydrogen binding plasticizer, such as dimethylsulfoxide (DMSO). The plasticizer regulates the set-up time of the synthetic resin so that the more plasticizer present, the shorter the set-up time. The plasticizer also has a direct shortening effect upon the cure time and also profoundly influences many of the physical characteristics of the resultant synthetic resin matrix system. A variety of drugs can be embodied in the fabricated matrix system and administered to the patient (or animal) by different modes of application, including but not limited to oral, topical, rectal, subcutaneous implant, or organ-specific implant such as in the conjunctival sac of the eye.Type: GrantFiled: January 3, 1986Date of Patent: May 31, 1988Assignee: Enquay Pharmaceutical AssociatesInventor: Bernard Korol
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Patent number: 4732912Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: April 27, 1984Date of Patent: March 22, 1988Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4731359Abstract: The time during which a drug is pharmacologically active is prolonged by coating the drug with at least one chemical derivative of the drug having minor relative pharmacological activity.Type: GrantFiled: February 6, 1984Date of Patent: March 15, 1988Assignee: University of Southern CaliforniaInventor: James Swarbrick
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Patent number: 4686235Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.Type: GrantFiled: August 12, 1985Date of Patent: August 11, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Norman P. Jensen, Milton L. Hammond, Robert A. Zambias, John McDonald, Kathleen M. Rupprecht
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Patent number: 4665092Abstract: Alkenes of the formula (I) and epoxides (II) used to make them are useful as anti-inflammatory and antiallergic pharmaceuticals: ##STR1## wherein R.sup.1 =H or CH.sub.3 ; R.sup.2 =phenyl, substituted phenyl, benzyl or a cysteinyl moiety; R.sup.4 and R.sup.5 =alkyl; n=O or 1; and R.sup.3 is as described.Type: GrantFiled: October 3, 1985Date of Patent: May 12, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Michael P. Ferro, Michael P. Wachter