Patents Examined by Robert T. Bond
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Patent number: 5919926Abstract: Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.Type: GrantFiled: January 25, 1994Date of Patent: July 6, 1999Assignee: The Regents of the University of CaliforniaInventors: William H. Fenical, Robert S. Jacobs, Paul R. Jensen
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Patent number: 5917033Abstract: The present invention pertains to a method for designing inhibitors of enzyme human immunodeficiency virus type 1 reverse transcriptase which comprises the steps of:(a) providing a three dimensional model of the receptor site in the prepolymerization complex of the p66 subunit of enzyme human immunodeficiency virus type 1 reverse transcriptase and a known nonnucleoside inhibitor;(b) locating the conserved residues in the p66 subunit which constitute the nonnucleoside inhibitor binding pocket; and(c) designing a new nonnucleoside inhibitor which possesses complementary structural features and binding forces to the residues in the p66 subunit nonnucleoside inhibitor binding pocket.Type: GrantFiled: October 31, 1995Date of Patent: June 29, 1999Assignee: University of Medicine & Dentistry of New JerseyInventors: Mukund J. Modak, Prem N. S. Yadav, Janardan S. Yadav
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Patent number: 5843941Abstract: Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated.Type: GrantFiled: September 26, 1994Date of Patent: December 1, 1998Assignees: Genentech, Inc., Board of Regents University of TexasInventors: James C. Marsters, Jr., Michael S. Brown, Craig W. Crowley, Joseph L. Goldstein, Guy L. James, Robert S. McDowell, David Oare, Thomas E. Rawson, Mark Reynolds, Todd C. Somers
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Patent number: 5831094Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.Type: GrantFiled: February 20, 1996Date of Patent: November 3, 1998Assignee: Merrell Pharamceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5801168Abstract: Antagonists at the NMDA receptor complex which are benz?b!azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.Type: GrantFiled: February 3, 1997Date of Patent: September 1, 1998Assignee: Zeneca LimitedInventors: Marc Jerome Chapdelaine, Timothy W. Davenport, Laura E. Garcia-Davenport, Paul Francis Jackson, Jeffrey A. McKinney, Charles D. McLaren
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Patent number: 5798381Abstract: Bistramide derivatives with virtually no toxic effects, of formula (I) wherein --R.sub.1, X, Y and R.sub.2 are a saturated or unsaturated hydrocarbonaceous chain having from 1 to 20 carbon atoms, substituted by at least one --OH group and/or a ketone function, including, if need be, at least one ring (a), the ring including one more unsaturations; --R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from hydrogen, alkyl or alkoxy radicals having from 1 to 4 carbon atoms, a group --COOH, --OH, --NH or --NO.sub.2, or a halogen atom. The invention also concern bistramide derivatives of formula (I) such as ethers or esters and their isomers, excluding A, B and C bistramides. Said bistramides are useful especially as drugs having a cytostatic effect, in particular as antitumour or anti-parasitic drugs.Type: GrantFiled: March 4, 1996Date of Patent: August 25, 1998Assignee: Institut Francais de Recherche Scientifique pour le Development en Cooperation (Orstom)Inventors: Jean-Francois Biard, Dominique Cortadellas, Cecile Debitus, Dominique Laurent, Cristos Roussakis, Jean-Francois Verbist
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Patent number: 5789587Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: November 6, 1996Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5786350Abstract: Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.Type: GrantFiled: January 31, 1997Date of Patent: July 28, 1998Assignee: Gruppo Lepetit S.p.A.Inventors: Emilio Occelli, Sergio Lociuro, Romeo Ciabatti, Maurizio Denaro
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Patent number: 5780623Abstract: Process to prepare .epsilon.-caprolactam starting from a liquid aqueous mixture containing an alcohol and 6-aminocaproic acid by cyclization of 6-aminocaproic acid in the aqueous mixture at an elevated temperature. The alcohol is separated from the starting aqueous mixture before performing the cyclization to such extent that the concentration of alcohol in the aqueous mixture during the cyclization is less than 1 wt. %. The advantages include reduced amounts of undesirable by-product.Type: GrantFiled: February 23, 1996Date of Patent: July 14, 1998Assignee: DSM N.V.Inventors: Rudolf P.M. Guit, Samuel L. Lane, Wim Buijs
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Patent number: 5776936Abstract: There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants.Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.Type: GrantFiled: May 19, 1994Date of Patent: July 7, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Byung H. Lee, Stephen J. Nelson
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Patent number: 5776929Abstract: A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.Type: GrantFiled: June 25, 1996Date of Patent: July 7, 1998Assignee: Shionogi & Co., Ltd.Inventors: Sanji Hagishita, Susumu Kamata, Kaoru Seno, Nobuhiro Haga, Yasunobu Ishihara
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Patent number: 5777105Abstract: Imidazolmethyloxy-substituted tricyclo-macrolide immunosuppressants are prepared by reacting a tricyclo-macrolide with an imidazolmethyl trichloroacetimidate in the presence of an acid. The invention further provides a crystalline salt of imidazolmethyloxy-substituted tricyclo-macrolide, as well as novel compounds useful in the process of the present invention.Type: GrantFiled: July 23, 1996Date of Patent: July 7, 1998Assignee: Merck & Co., Inc.Inventors: David J. Mathre, Richard F. Shuman, Paul Sohar, Zhiguo Song
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Patent number: 5773428Abstract: Compounds of formula (I): ##STR1## as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.Type: GrantFiled: February 5, 1996Date of Patent: June 30, 1998Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo Lucas Castelhano, Teng Jiam Liak, Stephen Horne, Alexander Krantz, Zhengyu Yuan, Jian Jeffrey Chen, Paul David Cannon, Hal Van Wart
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Patent number: 5770604Abstract: This invention provides novel aconitine compounds of the formula (I) or salt thereof ##STR1## wherein, R.sub.1 is a hydrogen atom or hydroxyl group; R.sub.2 is an acetyloxy group; R.sub.3 is an alkyl having 1-4 carbon atoms; and R.sub.4 is a hydrogen atom, a hydroxyl group, or an acetyloxy group; and antipyretic/analgesic/anti-inflammatory agents containing the compound as an active ingredient which are highly safe and exhibit a powerful analgsic effect and antipyretic/anti-inflammatory activities. The compound is usable alone in painful, pyretic and inflammatory illnesses but its concomitant use with morphine reinforces the analgesic effect of morphine and allows alleviation of morphine side effects through reduction in morphine dosage.Type: GrantFiled: October 6, 1995Date of Patent: June 23, 1998Assignee: Sanwa Shoyaku Kabushiki KaishaInventor: Mitsuo Murayama
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Patent number: 5756728Abstract: An improved process for preparing 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.Type: GrantFiled: December 30, 1996Date of Patent: May 26, 1998Assignee: Johnson Matthey Public Limited CompanyInventors: David Xu, Prasad Kapa, Oljan Repic, Thomas J. Blacklock
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Patent number: 5753677Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.Type: GrantFiled: June 7, 1995Date of Patent: May 19, 1998Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5750680Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.Type: GrantFiled: September 12, 1996Date of Patent: May 12, 1998Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & TechnologyInventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
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Patent number: 5750725Abstract: The present invention provides a class of compounds having the formula:Y--R--CH.sub.2 --CH.sub.2 --?O--CH.sub.2 --CH.sub.2 !.sub.n --R'--Y'wherein n is an integer from about 5 to about 200; R is carbamate, urea, or amide; R' is carbamate, urea, amide, or oxygen; Y is 4-phenylmalemimido or 3-phenylmaleimido; and Y' is 4-phenylmalemimido, 3-phenylmaleimido, methyl or hydrogen. The present invention also provides various hemoglobin compositions modified with the class of compounds of the present invention, processes for preparing these compositions, as well as pharmaceutical compositions comprising these compositions.Type: GrantFiled: September 26, 1996Date of Patent: May 12, 1998Assignee: Albert Einstein College of Medicine of Yeshiva University, a Division of YeshivaInventors: A. Seetharama Acharya, Belur N. Manjula, Paul K. Smith
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Patent number: 5750700Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof;useful for treating disorders of the central nervous system.Type: GrantFiled: June 2, 1995Date of Patent: May 12, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5741904Abstract: A method of producing .epsilon.-caprolactam from cyclohexanone in the gaseous phase using MFI catalysts on whose surface symmetrically arranged OH groups are present.Type: GrantFiled: May 6, 1996Date of Patent: April 21, 1998Assignee: Degussa AktiengesellschaftInventors: Wolfgang Hoelderich, Joerg Roeseller, Dietrich Arntz