Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/100)
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Publication number: 20020045600Abstract: A topical treatment for skin irritation that uses a spray-on liquid or a rub-on lotion based papain skin treatment for relief of symptoms related to skin irritation. Papain is suspended in a water solution that is spread on the surface of the affected area. The liquid solution ensures that the active ingredient contacts the skin without missing spots as may occur when using dry or powdered skin treatments. The papain is an active ingredient extracted from papaya which relieves the skin irritation caused by sea lice, insect bites, etc. The water solution is used to suspend the papain such that it more completely contacts the affected area, and further to maintain the papain in a fresh and active state. Optionally, aloe vera is included in the solution to increase the soothing effect on the skin in combination with the papain. In another preferred embodiment, citric acid and sodium benzoate are also used to increase shelf life.Type: ApplicationFiled: July 7, 2000Publication date: April 18, 2002Inventor: Laura M. Schwarzman
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Publication number: 20020045601Abstract: An ophthalmic composition particularly in the form of eye-drops suitable for the treatment of diseases of the eye and surrounding areas. The composition contains a cyclosporin and a surfactant selected from polyoxyethylene fatty acid esters, polyoxyethylene alkylphenyl ethers and polyoxyethylene alkyl ethers, or mixtures thereof.Type: ApplicationFiled: August 27, 2001Publication date: April 18, 2002Inventors: Yoichi Kawashima, Mitsuaki Kuwano
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Publication number: 20020037879Abstract: The invention concerns monoclonal antibodies and their biological applications. These monoclonal antibodies are characterised by the fact that they recognize an epitope of a bacterium of the T. equigenitalis species.Type: ApplicationFiled: October 9, 1998Publication date: March 28, 2002Inventors: FREDERIC KLEIN, DRAGOS GRADINARU
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Publication number: 20020032176Abstract: Carcinogenesis inhibitors containing as the active ingredient carotenoids extracted from the pure-line species of paradicsom paprika (species classified as Capsicum annuum L. var. grossum), etc., such as capsanthin, its fatty acid esters, capsorubin diesters, capsanthin 3,6-epoxide, capsorubin and cucurbitaxanthine A-3′ ester. These carcinogenesis inhibitors and paradicsom paprika extracts originate in natural substances and, therefore, make it possible to provide excellent Epstein-Barr virus genome inactivating agents. Thus, they are expected as being useful in preventing carcinogenesis and, based on their effects, applicable in various fields including drugs, cosmetics and health foods.Type: ApplicationFiled: June 24, 1999Publication date: March 14, 2002Inventors: TAKASHI MAOKA, KOOICHI MOCHIDA, MUTSUO KOZUKA, HARUKUNI TOKUDA, YOSHIHIRO ITO, YOKO OKUDA
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Publication number: 20020028791Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1Type: ApplicationFiled: July 18, 2001Publication date: March 7, 2002Inventors: Robert F. Kaltenbach, George L. Trainor
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Publication number: 20020010160Abstract: A method for the treatment of obesity in a human in need of such treatment which comprises administration to the human of a therapeutically effective amount of a compound of formula I 1Type: ApplicationFiled: December 16, 1998Publication date: January 24, 2002Inventors: DAVID JOHN HEAL, HELEN CHRISTINE JACKSON
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Publication number: 20010055809Abstract: A method of preserving tissue by placing the tissue in a media containing pure perfluorocarbon is provided. Also provided is a tissue preserving media including storage media and pure perfluorocarbon. A method of making media by adding pure perfluorocarbon to the media is provided. A method of preserving tissue by oxygenating the storage media by adding pure perfluorocarbons to the media is also provided.Type: ApplicationFiled: January 29, 1999Publication date: December 27, 2001Inventor: HARPAL S. MANGAT
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Patent number: 6331532Abstract: The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR•Z− where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.Type: GrantFiled: May 25, 2000Date of Patent: December 18, 2001Assignee: University of OtagoInventors: Michael P. Murphy, Robin A. J. Smith
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Publication number: 20010046976Abstract: The invention includes antibiotic pharmaceutical compositions comprising eukaryotic histone H1 protein and methods of using eukaryotic histone H1 protein to kill or to inhibit the growth of microorganisms, including, but not limited to, human pathogenic bacteria. The invention further includes a eukaryotic histone H1-containing animal feed and methods of improving growth of an animal by supplying the feed to the animal. The invention still further includes a kit comprising a eukaryotic histone H1-containing antibiotic pharmaceutical composition and an instructional material which describes the use of the composition. In addition, the invention includes a vaccine comprising a eukaryotic histone H1 protein and a method of vaccinating an animal using the vaccine.Type: ApplicationFiled: August 11, 1999Publication date: November 29, 2001Inventors: REINER J. W. CLASS, CHRISTOPHER M. HAND
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Publication number: 20010041182Abstract: An object of the present invention is to provide a composition for enhancing the immunological effects of a vaccine for viruses, bacteria and/or infectious disease pathogens, containing a stable activity-type provitamin; a method for enhancing the immunological effects of a vaccine for viruses, bacteria and/or infectious disease pathogens by administering the composition; and a method of employing the composition. A composition for enhancing the immunological effects of a vaccine for viruses, bacteria and/or infectious disease pathogens, contains L-ascorbic acid-2-phosphate and/or &agr;-tocopheryl phosphate as a stable activity antioxidant provitamin.Type: ApplicationFiled: February 28, 2001Publication date: November 15, 2001Inventors: Shinobu Ito, Eiji Ogata
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Publication number: 20010027187Abstract: Provided are functionalized silicon compounds and methods for their synthesis and use. The functionalized silicon compounds include at least one activated silicon group and at least one derivatizable functional group. Exemplary derivatizable functional groups include hydroxyl, amino, carboxyl and thiol, as well as modified forms thereof, such as activated or protected forms. The functionalized silicon compounds may be covalently attached to surfaces to form functionalized surfaces which may be used in a wide range of different applications. In one embodiment, the silicon compounds are attached to the surface of a substrate comprising silica, such as a glass substrate, to provide a functionalized surface on the substrate, to which molecules, including polypeptides and nucleic acids, may be attached.Type: ApplicationFiled: April 11, 2001Publication date: October 4, 2001Applicant: Affymetrix, Inc.Inventors: Glenn McGall, Jonathan Eric Forman
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Publication number: 20010025035Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.Type: ApplicationFiled: December 8, 2000Publication date: September 27, 2001Applicant: University of KansasInventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
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Publication number: 20010021383Abstract: The invention includes a vaccine and sera for treatment of Mystery Swine Disease (MSD), a method for producing the vaccine, methods for diagnosis of MSD, a viral agent that will mimic “mystery swine disease” and antibodies to the viral agent useful in diagnosis and treatment of MSD. The serum contains mammalian antibodies which are effective in treating MSD.Type: ApplicationFiled: December 18, 2000Publication date: September 13, 2001Applicant: Boehringer Ingelheim Animal Health, Inc.Inventors: James E. Collins, David A. Benfield, Danny W. Chladek
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Publication number: 20010018430Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: ApplicationFiled: February 7, 2001Publication date: August 30, 2001Applicant: Tularik, Inc.Inventor: Jonathan B. Houze
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Patent number: 6277834Abstract: A medicament for reducing side effects of adrenocortical hormones comprising a phosphodiester compound of the following formula or a pharmacologically acceptable salt thereof wherein R1 and R2 are the same or different and each denotes hydrogen or methyl.Type: GrantFiled: December 11, 2000Date of Patent: August 21, 2001Assignee: Senju Pharmaceutical Co. Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Masahito Iemura
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Publication number: 20010014674Abstract: Devices and methods for enhancing the healing of wounds, especially chronic wounds (e.g., diabetic wounds), involving the use of keratinocytes and transformed cells are described. A cell-coated transplantable solid support (e.g., beads coated with keratinocytes and/or transformed cells), are placed in an enclosure. The enclosure, in turn, is placed in the wound for use as an interactive wound healing promoter.Type: ApplicationFiled: May 27, 1999Publication date: August 16, 2001Inventors: RILEY S. REES, ROBERT GILMONT, BELINDA ADAMSON
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Publication number: 20010014672Abstract: An isolated and purified outer membrane protein of a Moraxella strain, particularly M. catarrhalis, having a molecular mass of about 200 kDa, is provided. The about 200 kDa outer membrane protein as well as nucleic acid molecules encoding the same are useful in diagnostic applications and immunogenic compositions, particularly for in vivo administration to a host to confer protection against disease caused by a bacterial pathogen that produces the about 200 kDa outer membrane protein or produces a protein capable of inducing antibodies in a host specifically reactive with the about 200 kDa outer membrane protein.Type: ApplicationFiled: March 19, 1998Publication date: August 16, 2001Inventors: KEN SASAKI, ROBIN E. HARKNESS, SHEENA M. LOOSMORE, PELE CHONG, MICHEL H. KLEIN
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Publication number: 20010014673Abstract: Live Brucella vaccines and methods for preparing the live vaccines protective against brucellosis are described. The vaccines are prepared by introducing a deletion in the rfbU gene of a strain of Brucella which results in attenuation of the strain while retaining the desired immunogenicity to initiate a protective immunogenic response. Other strains with varying levels of attenuation are described.Type: ApplicationFiled: January 22, 1998Publication date: August 16, 2001Inventors: MIKELJON P. NIKOLICH, DAVID L. HOOVER, RICHARD L. WARREN, LUTHER E. LINDLER, TED L. HADFIELD, CERHARDT G. SCHURIG, STEPHEN M. BOYLE, JOHN R. MCOULSTON, NAMMALWAR SRIRANGANATHAN
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Publication number: 20010008887Abstract: The invention provides a method for the specific detection of a target pathogen in a sample. The method of the invention comprises, as a first step, incubating the sample under sufficient conditions to enrich the target pathogen population in the sample. As a second step, the target pathogen is selected by immunoselection from the sample enriched in the first step. The selection of the target pathogen is followed by amplification of a nucleic acid sequence specific to the target pathogen from the target pathogen so selected. The amplified nucleic acid sequence is then detected, the presence of the amplified nucleic acid sequence indicating the presence of the target pathogen. By following the method of the invention, a single colony-forming unit (CFU) of bacterial pathogen can be detected in a contaminated food product in 8 hours or less. The invention provides improved tools for rapid and early detection of pathogens, including E. coli O157:H7, and Salmonella strains: S. agona; S. anatum; S. enteritidis; S.Type: ApplicationFiled: May 4, 1999Publication date: July 19, 2001Inventors: PRABHAKARA V. CHOUDARY, CHRISTOPHER M. GOODING
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Patent number: 6258539Abstract: The present invention relate to methods and compositions for simultaneously analyzing multiple different polynucleotides of a polynucleotide composition comprising multiple diverse polynucleotide sequences. The subject methods and compositions may also be applied to analyze or identify single polynucleotides; however, the subject methods and compositions are particularly useful for analyzing large diverse populations of polynucleotides, e.g., cDNA libraries. Most embodiments of the invention involve hybridizing terminus probes (of known base sequence) to adapter-modified restriction fragment generated from polynucleotide for analysis, and subsequently joining the terminus probes and internal fragment probes to each other. The terminus probe hybridizes to bases of restriction endonuclease recognition site present at the terminus of a restriction fragment generated from the polynucleotide for analysis.Type: GrantFiled: April 30, 1999Date of Patent: July 10, 2001Assignee: The Perkin-Elmer CorporationInventors: Michael W. Hunkapiller, John H. Richards
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Publication number: 20010006959Abstract: An composition, method and system for identifying novel antimicrobial agents including the steps of, displaying a &bgr;-lactamase inhibitor protein on a virus, contacting the virus with a &bgr;-lactamase binding protein target, selecting for the virus that has a higher affinity for the target and testing the &bgr;-lactamase inhibitor protein for antimicrobial activity, is disclosed. The invention also includes a nucleic acid encoding a fusion protein comprising a &bgr;-lactamase inhibitor protein and an affinity carrier and the protein expressed therefrom. Mutant &bgr;-lactamase inhibitor proteins may be produced, characterized, isolated and expressed in prokaryotic cells and used as antimicrobial agents.Type: ApplicationFiled: September 25, 1998Publication date: July 5, 2001Inventors: TIMOTHY G. PALZKILL, JOSEPH PETROSINO, WANZHI HUANG
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Patent number: 6211167Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: June 14, 2000Date of Patent: April 3, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6087347Abstract: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.Type: GrantFiled: March 12, 1999Date of Patent: July 11, 2000Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Mamoru Mieda, Tomohito Fujii
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Patent number: 6083874Abstract: This invention relates to an improved composition of matter for and method of desiccating plants such as, for example, cotton. More particularly, this invention relates to an improved desiccating composition comprising a solution of endothall, an ammonium salt, a glutamine synthetase inhibitor, and optionally, a surface active agent, and a method of using the composition.Type: GrantFiled: October 9, 1998Date of Patent: July 4, 2000Assignee: Elf Atochem North America, Inc.Inventor: Nasir S. A. Malik
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Patent number: 6069139Abstract: A pharmaceutical composition is provided for prophylaxis and treatment of a retinal disease in a human comprising (a) a compound of the formula I: ##STR1## wherein R.sub.1 and R.sub.2 independently from each other denote hydrogen or methyl group, or a pharmacologically acceptable salt thereof, and (b) a pharmacologically acceptable carrier therefor. Also provided are a method for prophylaxis and treatment of a retinal disease comprising administering such a compound and a use of such a compound for preparing a pharmaceutical composition for the same purpose.Type: GrantFiled: November 17, 1997Date of Patent: May 30, 2000Assignee: Senju Pharmaceutical Company, Ltd.Inventors: Hiroshi Kuriyama, Hiroaki Naka, Mitsunori Waki
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Patent number: 6054448Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 6046181Abstract: Disclosed herein are a highly purified tocopheryl phosphate and/or a salt thereof (tocopheryl phosphates) wherein a P,P'-bistocopheryl hypophosphate and/or a salt thereof (P,P'-bistocopheryl diphoshates) is contained in a proportion of not higher than 3% by weight; a process for producing a highly purified tocopheryl phosphate and/or a salt thereof, which comprises the steps of reacting a tocopherol with an oxyphosphorus trihalide followed by treating with an acid or basic aqueous solution to thereby form tocopheryl phosphates (i) in which P,P'-bistocopheryl diphoshates (ii) formed as by-products are contained, hydrolyzing the P,P'-bistocopheryl diphoshates (ii) under acid condition, and, optionally, rendering the hydrolyzate neutral or basic under basic condition; and a method of analyzing tocopheryl phosphates, comprising analyzing a sample containing components (i) and (ii) with the use of a high-performance liquid chromatograph column packed with a gel of a polymethacrylate having, bonded thereto, long-chType: GrantFiled: June 29, 1999Date of Patent: April 4, 2000Assignee: Showa Denko K.K.Inventors: Yutaka Oonishi, Tsutomu Nozawa, Takami Ooe, Keisuke Mano, Naoaki Misu, Yohei Kurata, Shinobu Ito, Eiji Ogata
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Patent number: 6043270Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the polyacetate-, diaminobenzyl alcohol-, diacylglycerol- and bryostatin-classes.Type: GrantFiled: June 7, 1995Date of Patent: March 28, 2000Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 6022867Abstract: A vitamin E source composition for administration to animals, which comprises a tocopheryl phosphate, a salt thereof or a composition containing a tocopheryl phosphate or a salt thereof. Also, disclosed is a method of supplying vitamin E to animals which comprises administering to animals the above vitamin E source composition. The tocopheryl phosphoric acid and a salt thereof can be formed into a composition and also can contain an antioxidant or the like.Type: GrantFiled: November 28, 1997Date of Patent: February 8, 2000Assignee: Showa Denko Kabushiki KaishaInventors: Shinobu Ito, Eiji Ogata
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Patent number: 5994328Abstract: A method for inhibiting the growth of cancer cells ous tumors. The method comprises administering to a subject in need of anticancer or antitumor therapy a pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula ##STR1## where: R is(i) H, PO.sub.3.sup..dbd., alkyl of 1 to 12 carbon atoms substituted or unsubstituted, straight chain or branched, 0 to 6 double bonds, (CH.sub.2).sub.n morpholine where n=1-4, morpholinomethylphenyl, orthoaminophenyl, orthohydroxyphenyl, (CH.sub.2).sub.n COOR.sub.2 where n=1-4where R.sub.2 is H, an alkali metal salt, an alkaline earth metal salt, NH.sub.4.sup.+, N.sup.+ (R.sub.3).sub.4 where R.sub.3 is independently selected from the group consisting of H and alkyl of 1 to 4 carbon atoms, or(ii) COR.sub.1 wherein R.sub.1 is selected from the group consisting of H, (CH.sub.2).sub.n CH.sub.3, where n=0-6, (CH.sub.2).sub.n COOR.sub.2 where n=1-4 and R.sub.2 is previously defined, (CH.sub.2).sub.n N.sup.+ (R.sub.3).sub.Type: GrantFiled: January 14, 1998Date of Patent: November 30, 1999Assignee: Immune Modulation, Inc.Inventors: Emmanuel A. Ojo-Amaize, Vellalore N. Kakkanaiah, Joseph I. Okogun
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Patent number: 5985856Abstract: The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.Type: GrantFiled: December 30, 1998Date of Patent: November 16, 1999Assignee: University of KansasInventors: Valentino Stella, Jeffrey P. Krise, Jan J. Zygmunt, Ingrid Gunda Georg
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Patent number: 5981514Abstract: Disclosed herein are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein R.sub.1 is alkyl of 1-6 carbon atoms;A is alkylene having from 2-5 carbon atoms, each of which carbon atoms is substituted with R.sub.2, where each R.sub.2 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl;Y and Y.sub.1 are hydrogen or halogen; andR.sub.4 is hydrogen or --PO.sub.3 H,which compounds are water soluble and can be used for the treatment of arrhythmias.Type: GrantFiled: February 12, 1999Date of Patent: November 9, 1999Inventor: John C. Somberg
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Patent number: 5962438Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.Type: GrantFiled: October 17, 1997Date of Patent: October 5, 1999Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Michihiro Yamamoto, Akira Sasaki, Takashi Katsumata, Naomi Tsushima, Hideyuki Harada
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Patent number: 5958905Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.Type: GrantFiled: March 26, 1996Date of Patent: September 28, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Erik Joel Verner
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Patent number: 5955453Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.Type: GrantFiled: April 24, 1998Date of Patent: September 21, 1999Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Tao Jiang
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Patent number: 5952001Abstract: The present invention relates to the use of an .alpha.-tocopherol phosphate, especially in its dl or d form, or an ester thereof, of the general formula ##STR1## in which: R.sub.1 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or an .alpha.-tocopheryl radical; and R.sub.2 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as methyl or ethyl radical in particular, or an oxyethylene chain of the formula ##STR2## in which R.sub.3 and R.sub.4 independently are a hydrogen atom or a methyl radical and n is an integer greater than or equal to 1, or a salt thereof, for preparing a pharmaceutical, dermatological or cosmetic composition for the prevention or treatment of allergic manifestations such as skin allergy or bronchial asthma, or inflammatory manifestations, or for the prevention or treatment of the harmful effects of free radicals.Type: GrantFiled: May 30, 1995Date of Patent: September 14, 1999Assignee: LVMH RechercheInventors: Alain Meybeck, Frederic Bonte, Christian Marechal
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Patent number: 5919816Abstract: 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: October 17, 1997Date of Patent: July 6, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 5880111Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5861384Abstract: According to the present invention, there are provided immunosuppressive-activity potentiating compositions which comprise a phosphoric acid diester compound represented by the following formula ?I!: ##STR1## (R.sub.1 and R.sub.2 are the same or different and represent individually a hydrogen atom or methyl group) or its pharmacologically acceptable salt, and the immunosuppressive-activity potentiating compositions can suppress effectively acute rejection after transplantation.Type: GrantFiled: January 17, 1997Date of Patent: January 19, 1999Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Nobuyoshi Shimizu, Motoi Aoe, Tetsunobu Udaka, Toshiharu Tsuboi, Ken-ichi Yoshida
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Patent number: 5858995Abstract: This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.Type: GrantFiled: October 25, 1996Date of Patent: January 12, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Kawai, Hitoshi Yamazaki, Natsuko Kayakiri, Kousei Yoshihara, Takumi Yatabe, Teruo Oku
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Patent number: 5846956Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.Type: GrantFiled: July 7, 1997Date of Patent: December 8, 1998Assignee: Societe Civile BioprojetInventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil
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Patent number: 5821263Abstract: This invention provides a novel series of taxane derivatives which are characterized by the C3' nitrogen bearing one or two sulfur substituents. The new derivatives are antitumor agents useful in the treatment of such cancers as ovarian, breast, lung, gastric, colon, head and neck, melanoma and leukemia.Type: GrantFiled: July 29, 1997Date of Patent: October 13, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Paul M. Scola, Dolatrai M. Vyas
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Patent number: 5807845Abstract: The present invention provides a pharmaceutical composition for the therapy of acne vulgaris which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents hydrogen or methyl.Type: GrantFiled: July 29, 1997Date of Patent: September 15, 1998Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Sachiko Matsuura, Masahito Iemura
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Patent number: 5786344Abstract: This invention provides methods and combination formulations and kits to reduce the toxicity of camptothecin drugs, such as irinotecan (CPT-11). Disclosed are therapeutics and treatment methods employing such drugs in combination with agents that increase conjugative enzyme activity or glucuronosyltransferase activity, and agents that decrease biliary transport protein activity, such as cyclosporine A, the resultant effects of which are to decrease the significant side effects previously associated with treatment using these drugs.Type: GrantFiled: April 17, 1995Date of Patent: July 28, 1998Assignee: Arch Development CorporationInventors: Mark J. Ratain, Elora Gupta
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Patent number: 5750516Abstract: This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).Type: GrantFiled: September 30, 1996Date of Patent: May 12, 1998Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Masayuki Nakamura, Kazumi Ogata, Takahiro Sakaue, Noriko Saito, Masahito Iemura
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Patent number: 5741784Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; ....... represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## ,or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: August 30, 1996Date of Patent: April 21, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5719183Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5716985Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 23, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Maria Amparo Lago
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Patent number: 5712261Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.Type: GrantFiled: June 21, 1995Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky