Plural Ring Oxygens In The Hetero Ring Patents (Class 514/463)
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Patent number: 6346533Abstract: The particle diameter of itraconazole, insoluble drug, is reduced and crystallinity thereof is changed from crystalline into amorphous, increasing water solubility and a dissolution rate thereof. The improved itraconazole is applied to an oral adminstration drug.Type: GrantFiled: December 14, 1999Date of Patent: February 12, 2002Assignee: Dong-A Pharmaceutical Co., Ltd.Inventors: Bong-Jin Cha, Jun-Gyo Oh, Su-Eon Kim
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Publication number: 20020016361Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: ApplicationFiled: June 1, 2001Publication date: February 7, 2002Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
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Patent number: 6344485Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.Type: GrantFiled: June 18, 1999Date of Patent: February 5, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Patent number: 6323236Abstract: Impulse Control Disorders (ICD's) are characterized by harmful behaviors performed in response to irresistible impulses. The essential feature of an ICD is the failure to resist an impulse, drive, or temptation and to perform an act that is harmful to the person or to others. The present invention comprises methods for the treatment or prevention of ICD's using a class of sulfamates of the following formula: wherein X is CH2 or oxygen, and R1, R2, R3, R4 and R5 are as herein defined. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention are also disclosed.Type: GrantFiled: February 18, 2000Date of Patent: November 27, 2001Assignee: University of CincinnatiInventor: Susan McElroy
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Patent number: 6323238Abstract: The present invention relates to novel benzopyranyl guanidine derivatives of the formula 1, process for preparation therof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis. Wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification.Type: GrantFiled: October 20, 2000Date of Patent: November 27, 2001Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Sung-Eun Yoo, Kyu Yang Yi, Sun Kyung Lee, Nak-Jeong Kim, Jee Hee Suh, Young Sook Park, Sun Kyung Hwang, Hwa Sup Shin, Byung Ho Lee, Ho Won Seo, Hong Lim, Sun-Ok Kim, In Sun Cho, Miae Namgoong, Dongsoo Jang
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Publication number: 20010023257Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising themType: ApplicationFiled: December 12, 2000Publication date: September 20, 2001Inventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6284793Abstract: A process for preventing the transfer of harmful organisms of zooplankton including the epifauna thereof and of phytoplankton including its resting stages, which are taken up with the ballast water of ships and transferred to another locality on discharge. The organisms are substantially destroyed by the addition of an agent containing a water-soluble percarboxylic acid with 1 to 6 carbon atoms, particularly an aqueous solution containing peracetic acid and/or performic acid and hydrogen peroxide, in a quantity of 0.1 to 200 mg of percarboxylic acid per liter of ballast water and allowing it to react before discharge. In a preferred embodiment, cyanide is also added to the ballast water.Type: GrantFiled: December 6, 1999Date of Patent: September 4, 2001Assignee: Degussa-Huls AGInventors: Rainer Fuchs, Michael Huss, Peter Werle
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Patent number: 6284789Abstract: The present invention is directed to tetrahydronaphthalene derivatives of &agr;-conindendrin, &bgr;-conindendrin, sikkimotoxin, and podophyllotoxin having at least one methyleneoxy bridge wherein the oxygen atom extends to the benzhydrylic carbon atom.Type: GrantFiled: September 2, 1999Date of Patent: September 4, 2001Assignee: The Research Foundation of State University of New YorkInventors: Robert T. LaLonde, Frank D. Ramdayal, Mianji Zhang
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Patent number: 6281198Abstract: Compound of formula (I): wherein: R represents: a group of formula (i): wherein X, Y and W are as defined in the description, or a group of formula (ii): —A—G (ii) wherein: A represents a single bond or an optionally substituted alkylene chain, G represents a group selected from hydrogen, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, —OR2, —O—T1—NR3R4, —O—T1—NR2—T′1—NR3R4, —NR3R4, —NR2—T1—NR3R4, —NR2—T1—OR5, —NR2—T1—CO2R6, —NR2—T1—C(O)R6, —C(O)—NR3R4, —C(O)—NR2—T2, —O—C(O)T2, —O—C(S)—T2, —NR2—C(O)—T2, —NR2—C(S)—T2, —O—C(O)—O—T2, —O—C(O)—NR2—T2, —O—C(S)—O—T2, —O—C(S)—NR2—T2, —NR2—C(O)—O—T2,Type: GrantFiled: October 26, 2000Date of Patent: August 28, 2001Assignee: Adir et CompagnieInventors: Claude Monneret, Emmanuel Bertounesque, Philippe Meresse, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6274570Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.Type: GrantFiled: December 22, 1998Date of Patent: August 14, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Manfred Vogt, William Baettig
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Publication number: 20010012854Abstract: The present invention relates to methods for the use of specified inhibitors of multicatalytic protease (MCP) for use as inducers of programmed cell death (i.e., apoptosis) in tumor cells, and more particularly as anti-tumor agents. The present invention provides methods for inducing apoptosis in transformed cells, inhibiting proliferation of transformed cells, and inhibiting the growth of tumors using the MCP inhibitors.Type: ApplicationFiled: December 15, 1998Publication date: August 9, 2001Inventors: ROBERT SIMAN, JITESH P. JANI, RONALD H. GOLDFARB, QING PING DOU
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Patent number: 6262083Abstract: The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects.Type: GrantFiled: May 5, 2000Date of Patent: July 17, 2001Assignee: Choongwae Pharma CorporationInventors: Sung-Hwan Moon, Hea-Jin Choi, Su-Jin Lee, Jea-Uk Chung, Jong-Ryul Ha, Kyoung-June Lee, Se-Woong Oh, Kwang-Won Jeong
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Patent number: 6207673Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.Type: GrantFiled: March 12, 1997Date of Patent: March 27, 2001Assignees: The University of North Carolina at Chapel Hill, Yale UniversityInventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Xin Guo, Kenneth F. Bastow, Hui-Kang Wang
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Patent number: 6201014Abstract: A pharmaceutical composition for the treatment of irritable bowel syndrome, diarrhoea, constipation, abdominal pain and/or bloating or abdominal distension, the composition including a carrier vehicle and a vanilloid compound. The carrier vehicle enables the vanilloid compound to be released in the lower gastrointestinal tract. The vanilloid compound has the effect of desensitizing nerves in the lower gastrointestinal tract, thereby leading to symptomatic relief. Preferred vanilloid compounds are capsaicin and resiniferatoxin.Type: GrantFiled: December 7, 1999Date of Patent: March 13, 2001Assignee: Reckitt & Colman Products LimitedInventor: Fiona Kate Gardiner
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Patent number: 6201017Abstract: An ectoparasite-controlling agent for animals comprising 0.1 to 20% by weight of the neonocotinoid compounds defined in the specification and 10 to 95% by weight of a glycol or glycol monoalkyl ether has an excellent effectiveness by the application methods such as spot-on and pour-on application.Type: GrantFiled: September 21, 1999Date of Patent: March 13, 2001Assignee: Sumitomo Chemical Co., Ltd.Inventors: Satoshi Sembo, Mitsuyasu Makita
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Patent number: 6187819Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.Type: GrantFiled: June 10, 1996Date of Patent: February 13, 2001Assignee: The Trustees of Columbia University in the City of New YorkInventors: Paul B. Fisher, Jorge A. Leon
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Patent number: 6114364Abstract: The present invention relates to a compound represented by the following general formula (1) ##STR1## (wherein X represents O, S, SO, SO.sub.2, or NH, Y is a substituted or unsubstituted hydrocarbon residue containing 1 through 6 carbon atoms and having an overall molecular weight of not less than 15 and not more than 400, and the hydrocarbon residue, when the residue is ring, may contain one or two hetero-atoms in the ring, and Z is a carboxyl group, a group derived therefrom or an aliphatic hydrocarbon residue having from 1 to 4 carbon atoms which may be substituted or unsabstituted) or a pharmacologically acceptable salt thereof (excluding (1R,2S)-2-[(2R)-(2-acetyl-amino-2-carboxyethyl)thiomethyl]-3-oxo-1-cyclope ntane-carboxylic acid (cystacyclin)), a method for production thereof and a medicinal use thereof. The compound of the present invention is useful as a neuron differentiation accelerator.Type: GrantFiled: October 5, 1998Date of Patent: September 5, 2000Assignee: Nippon Kayaku Co., Ltd.Inventors: Seiichi Saito, Tomio Morino, Kuniko Masuda
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Patent number: 6069174Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.Type: GrantFiled: December 7, 1998Date of Patent: May 30, 2000Assignee: The Trustees of Columbia University in the City of New YorkInventors: Paul B. Fisher, Jorge A. Leon
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Patent number: 6066645Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.Type: GrantFiled: January 6, 1999Date of Patent: May 23, 2000Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 6022895Abstract: Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.Type: GrantFiled: March 11, 1998Date of Patent: February 8, 2000Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Wolfgang Werner Alfred Strassburger, Helmut Heinrich Buschmann, Werner Englberger, Elmar Josef Friderichs
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Patent number: 6011174Abstract: The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.Type: GrantFiled: August 4, 1998Date of Patent: January 4, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5990158Abstract: New therapeutic agents of carboxylic acid derivatives are disclosed, which are represented by the compounds of the following formula (I) or its pharmaceutically acceptable salts, ##STR1## These compounds are useful as a matrix metalloproteinases (MMPs) inhibitors.Type: GrantFiled: November 3, 1997Date of Patent: November 23, 1999Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Atsushi Noda, Yoshinori Kobayashi
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Patent number: 5948817Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.Type: GrantFiled: March 4, 1998Date of Patent: September 7, 1999Assignee: Bristol-Myers Squibb CompanyInventors: James Epperson, Graham Johnson, Daniel J. Keavy, Katherine S. Takaki
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5834507Abstract: Antineoplastic cyclolignan derivatives are of formula (I): ##STR1## in which Ar is a 3,4,5-trialkoxyphenyl or 4-hydroxy-3,5-dialkoxyphenyl; X is an oxygen, sulphur or nitrogen atom, a methine group .dbd.CH-- or an alkylmethine group .dbd.C(alkyl)--; Y is a hydrogen atom or an alkyl, alkenyl, (poly)haloalkyl, aryl, hydroxy, alkoxy, amino, monoalkylamino, dialkylamino, (poly)haloalkylamino, arylamino, acyl or acetamido group, or the group Y is absent; Z is an alkyl, hydroxyalkyl, acyl, carboxy, alkoxycarbonyl or aryloxycarbonyl group; and the dotted lines indicate one double bond located at position .DELTA..sup.7-8 or .DELTA..sup.8-8'.Type: GrantFiled: December 10, 1997Date of Patent: November 10, 1998Assignee: Universidad de SalamancaInventors: Marina Gordaliza, Maria Angeles Castro, Arturo San Feliciano, Jose Maria Miguel del Corral, Maria Luisa Lopez, Dolores G. Gravalos
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Patent number: 5753707Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.Type: GrantFiled: September 6, 1996Date of Patent: May 19, 1998Assignee: Kao CorporationInventors: Masahide Hoshino, Hiroshi Kusuoku, Tadashi Hase, Atsuko Otsuka, Ichiro Tokimitsu, Akira Yamamuro, Yoshiya Sugai, Koji Yoshino, Youichi Arai, Shinichi Meguro
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Patent number: 5747529Abstract: Antineoplastic cyclolignan derivatives are of formula (I): ##STR1## in which Ar is a 3,4,5-trialkoxyphenyl or 4-hydroxy-3,5-dialkoxyphenyl; X is an oxygen, sulphur or nitrogen atom, a methine group .dbd.CH-- or an alkylmethine group .dbd.C(alkyl)--; Y is a hydrogen atom or an alkyl, alkenyl, (poly)haloalkyl, aryl, hydroxy, alkoxy, amino, monoalkylamino, dialkylamino, (poly)haloalkylamino, arylamino, acyl or acetamido group, or the group Y is absent; Z is an alkyl, hydroxyalkyl, acyl, carboxy, alkoxycarbonyl or aryloxycarbonyl group; and the dotted lines indicate one double bond located at position .DELTA..sup.7-8 or .DELTA..sup.8-8'.Type: GrantFiled: November 13, 1995Date of Patent: May 5, 1998Assignee: Universidad de SalamancaInventors: Marina Gordaliza, Maria Angeles Castro, Arturo San Feliciano, Jose Maria Migel del Corral, Maria Luisa Lopez, Dolores G. Gravalos
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Patent number: 5723498Abstract: A composition which is capable of releasing acrolein and is easy to handle contains (i) an acetal of acrolein with a C.sub.1-6 alcohol with 1 to 4 hydroxyl groups and (ii) an acid soluble therein and chemically compatible with a pK.sub.s value of less than 4 and (iii) is anhydrous. A preferred composition contains 2-vinyl-1,3-dioxolane as acetal, anhydrous oxalic acid, fumaric acid or maleic acid or a mixture of mono- and di(C.sub.1 - to C.sub.3 -)alkyl phosphate as acid and, in addition, a non-ionic surfactant. The acrolein is released at the site of use upon contact with for example water for the purpose of combatting microbial, vegetable and animal pests.Type: GrantFiled: September 13, 1995Date of Patent: March 3, 1998Assignee: Degussa AktiengellschaftInventors: Peter Werle, Martin Trageser, Oswald Helmling, Harold Jakob
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Patent number: 5708018Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.Type: GrantFiled: February 2, 1996Date of Patent: January 13, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Susanne R. Haadsma-Svensson, Bengt R. Andersson, Clas A. Sonesson, Chiu-Hong Lin, R. Nicholas Waters, Kjell A. I. Svensson, Per A. E. Carlsson, Lars O. Hansson, N. Peter Stjernlof
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Patent number: 5700448Abstract: The present invention relates to the use of persistent free radicals, in particular persistent free radicals having a carbon-based .pi.-bonded electronic system available for delocalization of the unpaired electrons as image enhancing agents in magnetic resonance imaging (MRI), in particular electron spin resonance enhanced magnetic resonance imaging (ESREMRI). The invention also relates to contrast media containing such radicals and to the use of such radicals and their non-radical precursors in the manufacture of MRI and ESREMRI contrast media.Type: GrantFiled: April 3, 1995Date of Patent: December 23, 1997Assignee: Nycomed Imaging ASInventors: Klaes Golman, Sven Andersson, Frode Rise, Lars-Goran Wistrand, Hakan Wikstrom
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Patent number: 5696158Abstract: A pediculicidal composition is provided which is effective against both adult lice and lice eggs and additionally exhibits a strong repellent effect on adult lice. The active ingredient is piperonal which is generally used in solution at a concentration of at least 3%. An additional component of the composition is a film-forming material which is capable of holding the piperonal in contact with the host for at least two hours.Type: GrantFiled: June 6, 1995Date of Patent: December 9, 1997Assignee: Unicliffe LimitedInventor: William John Oliver
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Patent number: 5681964Abstract: Prodrugs containing an active drug molecule linked to a polyethylene glycol group, and a method of use thereof are described. Exemplary soluble ester prodrugs contain naproxen, triamcinolone acetonide, gancyclovir, taxol, cyclosporin, dideoxyinosine, trihydroxy steroids, and flurbiprofen molecules linked to polyethylene glycol (PEG) groups. Pharmaceutical compositions containing these prodrugs, and a method of using these esters for treating disease states or symptoms are also described.Type: GrantFiled: October 5, 1994Date of Patent: October 28, 1997Assignee: University of Kentucky Research FoundationInventors: Paul Ashton, Thomas J. Smith, Peter G. Glavinos, John D. Conklin, Jr., Peter A. Crooks, Robert M. Riggs, Tadeusz Cynkowski, Grazyna Cynkowska
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Patent number: 5681860Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.Type: GrantFiled: September 21, 1993Date of Patent: October 28, 1997Assignee: The Trustees of Columbia University in the City of New YorkInventors: Paul B. Fisher, Jorge A. Leon
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5658904Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: June 6, 1995Date of Patent: August 19, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5654328Abstract: There are provided compositions for, and a method of, treating malignancies which comprise effective amounts of a novel combined therapy comprising a platinum compound and a tellurium or selenium compound, e.g., ammonium trichloro (dioxoethylene-O,O-tellurate), and administering the respective compounds simultaneously or separately.Type: GrantFiled: December 15, 1994Date of Patent: August 5, 1997Inventors: Benjamin Sredni, Michael Albeck
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Patent number: 5618835Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: April 8, 1997Assignee: The Procter & Gamble CompanyInventors: Laurence I. Wu, John M. Janusz
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Patent number: 5610179Abstract: A method of treating or preventing babesiosis is described which is based on the administration of a tellurium compound. The preferred tellurium compound is ammonium trichloro (O,O'-dioxoethylene tellurate).Type: GrantFiled: December 15, 1994Date of Patent: March 11, 1997Inventors: Benjamin Sredni, Michael Albeck
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Patent number: 5594027Abstract: The invention is antiobesity/antidiabetic/beta-3 agonists of the formula ##STR1## wherein the substituents R.sub.o, R.sub.1, R.sub.4, R.sub.4 ', R.sub.5, R.sub.6 or n are as defined in the specification.Type: GrantFiled: May 5, 1995Date of Patent: January 14, 1997Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Gary H. Birnberg, Gary E. Walker, Minu D. Dutia, Jonathan D. Bloom
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Patent number: 5578638Abstract: This invention relates to a method of treating glaucoma or reducing intraocular pressure in a patient in need of such treatment which is based on the topical administration to the eye of a mammal or the systemic administration of a compound of the formula: ##STR1## wherein E', W', and the R groups are defined in the disclosure.Type: GrantFiled: November 5, 1993Date of Patent: November 26, 1996Assignee: American Cyanamid CompanyInventors: Romulus K. Brazzell, Bernard Dubnick
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Leukotriene-B.sub.4 antagonists, process for their production and their use as pharmaceutical agents
Patent number: 5559134Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.Type: GrantFiled: March 23, 1995Date of Patent: September 24, 1996Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen -
Patent number: 5541223Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.Type: GrantFiled: October 28, 1993Date of Patent: July 30, 1996Assignees: Yale University, The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yung-Chi Cheng
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Patent number: 5534499Abstract: The present invention provides novel lipophilic drug derivatives which are capable of being formulated in liposomes or micelles. These drug derivatives are known therapeutic agents which are covalently attached to a fatty acid chain of a phospholipid, glyceride, ceramide or 1,2-diacyloxypropane-3-amine. The linkage between the therapeutic agent and the lipid is one which can be cleaved in vivo, allowing the therapeutic agent to be separated from the micellar or liposomal formulation.Type: GrantFiled: May 19, 1994Date of Patent: July 9, 1996Assignee: The University of British ColumbiaInventor: Steve Ansell
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Patent number: 5510376Abstract: The invention is antiobesity/antidiabetic/beta-3 agonists of the formula ##STR1## wherein the substituents R.sub.o, R.sub.1, R.sub.4, R.sub.4 ', R.sub.5, R.sub.6 or n are as defined in the specification.Type: GrantFiled: May 27, 1994Date of Patent: April 23, 1996Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Gary H. Birnberg, Gary E. Walker, Minu D. Dutia, Jonathan D. Bloom
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Patent number: 5506243Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.Type: GrantFiled: April 28, 1994Date of Patent: April 9, 1996Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
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Patent number: 5498629Abstract: A compound of the general formula I: ##STR1## is disclosed as a potent anticonvulsant drug. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: November 10, 1994Date of Patent: March 12, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Michael J. Costenzo, Bruce E. Maryanoff, David F. McComsey, Samuel O. Nortey
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Patent number: 5496852Abstract: A pediculicidal composition is provided which is effective against both adult lice and lice eggs and additionally exhibits a strong repellent effect on adult lice. The active ingredient is piperonal which is generally used in solution at a concentration of a least 3%. An additional component of the composition is a film-forming material which is capable of holding the piperonal in contact with the host for least two hours.Type: GrantFiled: June 8, 1994Date of Patent: March 5, 1996Assignee: Charwell Consumer Products, Ltd.Inventor: William J. Oliver
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Patent number: 5492935Abstract: Therapeutic as well as preventive measures to improve cosmetic conditions and to alleviate the symptoms of dermatologic disorders with retinal and its derivatives is disclosed. Cosmetic conditions and dermatologic disorders in humans and domestic animals in which retinal and its derivatives may be useful include age spots, wrinkles, warts, eczema, seborrheic keratoses, acne, oily skin, psoriasis, dandruff, xerosis, inflammatory and pruritic skin, disturbed keratinization, skin changes associated with aging and possibly viral infections. Retinal and its derivatives include their stereoisomers, for example, all-trans, 13-cis, 11-cis, 9-cis, 7-cis, 11,13-cis and 9,13-cis vitamin A aldehydes, their hydrate, hemiacetal and acetal forms, and their adduct compounds. Compositions containing retinal or its derivative may be administered systemically such as orally, or topically to the affected areas of the skin.Type: GrantFiled: October 5, 1994Date of Patent: February 20, 1996Inventors: Ruey J. Yu, Eugene J. Van Scott