Nitrogen Double Bonded Directly At 2-position Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/388)
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Patent number: 6630503Abstract: A cell adhesion inhibitor of the general formula: R3—L—L′—R1 is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing and using such a cell adhesion inhibitor, as well as pharmaceutical compositions containing the same.Type: GrantFiled: August 14, 2000Date of Patent: October 7, 2003Assignee: Biogen, Inc.Inventors: Daniel Scott, Wen-Cherng Lee, Russell C. Petter, Mark Cornebise
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Patent number: 6608096Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm-blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 26, 2000Date of Patent: August 19, 2003Assignee: University of Arizona FoundationInventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
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Patent number: 6569875Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A is an aryl group or an aromatic or nonaromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1 toType: GrantFiled: June 13, 2000Date of Patent: May 27, 2003Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6569880Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: GrantFiled: February 28, 2002Date of Patent: May 27, 2003Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbæk
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Patent number: 6552059Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed. The methods comprise the step of treating the leukemia with an effective amount of a compound of the Formula I or a pharmaceutically acceptable salt or prodrug form thereof, wherein: X is hydrogen, halogen or alkyl of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl or ethyl; R is hydrogen or an alkyl group of from 1 to 8 carbon atoms, alkylcarbamyl; R2 is 4-thiazolyl or NHCOOR1; and R1 is an aliphatic hydrocarbon of less than 7 carbon atoms. A chemotherapeutic agent and/or potentiator can be used in conjunction with the compound of the Formula I.Type: GrantFiled: February 23, 2001Date of Patent: April 22, 2003Assignee: University of Arizona FoundationInventor: James Berger Camden
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Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Publication number: 20030022926Abstract: The present invention relates to a method for a sustained treatment and/or prophylaxis of neuropathic pain in mammal comprising administering by peripheral nerve injection a neuropathic pain relieving composition comprising an alpha-2-adrenergic agonist.Type: ApplicationFiled: May 7, 2002Publication date: January 30, 2003Inventor: Patricia Lavand'Homme
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Patent number: 6506783Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: wherein R is selected from the group consisting of H, carboxyl (—CO2H), hydroxyl, amino or esters (—CO2R′) wherein R′ is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH3CH2(OCH2CH2)n—or CH3CH2CH2(OCH2CH2CH2)n—or (CH3)2CH—(OCH(CH3)CH2)n—wherein n is from 1-3, the pharmaceutically acceptable salts thereof, or mixtures thereof.Type: GrantFiled: May 16, 1997Date of Patent: January 14, 2003Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6498194Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus whichType: GrantFiled: January 16, 2002Date of Patent: December 24, 2002Assignee: BASF AktiengsellschaftInventors: Henry Van Tuyl Cotter, Gunther Reichert, Ewald Sieverding, Petrus Martinus Franciscus Emanuel Jegerings
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Patent number: 6495698Abstract: Novel, binder-free compacted forms of 1,3-dihalo-5,5-dimethylhydantoins in which one halogen atom is chlorine and the other is a bromine or chlorine atom are produced and used for microbiological control in aqueous media and water.Type: GrantFiled: January 18, 2000Date of Patent: December 17, 2002Assignee: Albemarle CorporationInventor: Jonathan N. Howarth
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Patent number: 6482843Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 29, 2000Date of Patent: November 19, 2002Assignee: The Procter & Gamble CompanyInventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
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Patent number: 6479526Abstract: This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a benzimidazole derivative. The composition is also claimed. The benzimidazole derivative is selected from the group consisting of: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl, ethyl or oxychloro; R is hydrogen, alkylaminocarbonyl wherein the alkyl group has from 3 to 6 carbon atoms, or an alkyl group of from 1 to 8 carbon atoms and R2 is 4-thiazolyl, NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, prodrugs, pharmaceutically acceptable salts and mixtures thereof and a pharmaceutically acceptable carrier.Type: GrantFiled: March 26, 2002Date of Patent: November 12, 2002Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6462062Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 26, 2000Date of Patent: October 8, 2002Assignee: The Procter & Gamble CompanyInventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
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Patent number: 6423734Abstract: Methods of treating and inhibiting cancerin animals by administering a therapeutically effective amount of a pharmaceutical composition having benzimidazole of the general formula: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, oxychloro, nitro, methyl or ethyl; and R is hydrogen, or an alkyl group of from 1 to 8 carbon atoms and R2 is NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, and preferably an alkyl group of less than 7 carbon atoms and pharmaceutically acceptable derivatives alone, or in combination, or in conduction with other therapeutic agents such as other cancer inhibiting compounds, and operative combinations thereof.Type: GrantFiled: August 13, 1999Date of Patent: July 23, 2002Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6407105Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 26, 2000Date of Patent: June 18, 2002Assignee: The Procter & Gamble CompanyInventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
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Patent number: 6380232Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 26, 2000Date of Patent: April 30, 2002Assignee: The Procter & Gamble CompanyInventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
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Publication number: 20020049246Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: ApplicationFiled: December 29, 2000Publication date: April 25, 2002Applicant: NeuroSearch A/SInventors: Bo Skaaning Jensen, Soren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strobaek
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Patent number: 6365613Abstract: A fungicidal mixture comprises a.1)a phenyl benzyl ether derivative of the formula I.a, I.b or I.c, or a.2) a carbamate of the formula I.d, where X is CH and N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl and C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a salt or adduct thereof, and b) a fungicidally active compound from the class of the benzimidazoles or benzimidazole-releasing precursors (II), in a synergistically effective amount.Type: GrantFiled: November 17, 1999Date of Patent: April 2, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Hubert Sauter, Bernd Müller, Erich Birner, Joachim Leyendecker, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6365734Abstract: Cucurbituril derivatives, their preparation methods and uses.Type: GrantFiled: June 28, 2000Date of Patent: April 2, 2002Assignee: Pohang University of Science and Technology FoundationInventors: Kimoon Kim, Jaheon Kim, In-Sun Jung, Soo-Young Kim, Eunsung Lee, Jin-Koo Kang
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Patent number: 6348464Abstract: The present invention relates to pharmaceutical compositions and methods of using pyrrolecarbonylimino derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases and cancers.Type: GrantFiled: November 12, 1999Date of Patent: February 19, 2002Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Publication number: 20020010201Abstract: The invention relates to an active substance combination consisting of clonidine and pramipexole for treating Restless Leg Syndrome.Type: ApplicationFiled: October 4, 2001Publication date: January 24, 2002Inventor: Hans Michael Brecht
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Publication number: 20010053387Abstract: A pharmaceutical composition which is a solid pellet comprising an inert core, a benzimidazole in or on the core, a moisture resistant coating around the core, the moisture resistant coating comprising at least one hydrophobic material, and an enteric coating around the moisture resistant coating.Type: ApplicationFiled: July 9, 2001Publication date: December 20, 2001Inventors: Yusuf Khwaja Hamied, Vinay G. Nayak, Geena Malhotra
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Patent number: 6329355Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.Type: GrantFiled: April 19, 2000Date of Patent: December 11, 2001Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6319949Abstract: A method for preventing fungal diseases in crops which comprises the steps of: (a) applying to a crop an aqueous or a non-aqueous spray composition which includes a pesticide and a spray adjuvant including a solvent and an emulsifier, wherein the solvent is a mixture of aliphatic hydrocarbons having a distillation range of about 520 to 600° F. and an aromatic content of about 1% or less, or the solvent is a single or combination of C6-C18 fatty alcohol(s); and (b) applying chlorothalonil to the crop previously to, simultaneously with, or subsequently to the application of the aqueous spray composition, wherein phytotoxicity associated with the application of chlorothalonil is reduced or eliminated.Type: GrantFiled: November 4, 1996Date of Patent: November 20, 2001Assignee: Syngenta LimitedInventors: Jeffrey R. Schussler, Robert E. Moser, Kevin E. Crosby, John R. Washington
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Publication number: 20010027205Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed.Type: ApplicationFiled: February 23, 2001Publication date: October 4, 2001Applicant: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6271217Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.Type: GrantFiled: December 22, 1998Date of Patent: August 7, 2001Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6265427Abstract: Method of treating leukemia, inhibiting the growth or proliferation of leukemic cells or extending the life span of a animal having leukemia are disclosed. The methods comprise the step of treating the leukemia with an effective amount of a compound of the Formula I or a pharmaceutically acceptable salt or prodrug form thereof, wherein: X is hydrogen, halogen or alkyl of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl or ethyl; R is hydrogen or an alkyl group of from 1 to 8 carbon atoms, alkylcarbamyl; R2 is 4-thiazolyl or NHCOOR1; and R1 is an aliphatic hydrocarbon of less than 7 carbon atoms. A chemotherapeutic agent and/or potentiator can be used in conjunction with the compound of the Formula I.Type: GrantFiled: August 16, 1999Date of Patent: July 24, 2001Assignee: The Proctor & Gamble CompanyInventor: James Berger Camden
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Patent number: 6262093Abstract: This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a benzimidazole derivative. The composition is also claimed.Type: GrantFiled: March 9, 1999Date of Patent: July 17, 2001Assignee: The Proctor & Gamble CompanyInventor: James Berger Camden
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Patent number: 6242445Abstract: A novel benzimidazole derivative [specifically, for example, 2-ethoxy-1-[{4′-(2″-N,N-dimethylaminoethoxycarbonyl)phenyl}methyl]-1H-benzimidazole-6-carboxylic acid morpholide] represented by formula (I) and a salt thereof. The compound exhibits satisfactory curative effects for cardiac and nephric diseases, although having little action on blood-pressure.Type: GrantFiled: August 23, 2000Date of Patent: June 5, 2001Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Shigeru Suzuki, Fuyuhiko Nishijima, Hiroshi Takahashi, Mikio Sugano, Hiroshi Maruoka, Toru Yamazaki, Toshikazu Dewa, Hiroyuki Enari, Michihito Ise
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Patent number: 6211200Abstract: Invented are zinc chelated G-CSF receptor ligands, pharmaceutical compositions containing these compounds, and methods of using these compounds as agonist of the G-CSF receptor. Also invented are novel processes used in preparing these compounds. Also invented are novel G-CSF receptor binding moieties of the invented zinc chelated G-CSF receptor ligands.Type: GrantFiled: October 30, 1998Date of Patent: April 3, 2001Assignees: SmithKline Beecham Corporation, Ligand PharmaceuticalsInventors: Juan I. Luengo, Stephen G. Miller
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Patent number: 6204278Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.Type: GrantFiled: May 19, 1997Date of Patent: March 20, 2001Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
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Patent number: 6197804Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: May 16, 2000Date of Patent: March 6, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Steven Gregory Mischke
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Patent number: 6197805Abstract: This invention is directed to a broad spectrum antimicrobial composition which comprises a mixture of an iodopropynyl compound in combination with 2-(methoxycarbonylamino)benzimidazole and, where desirable, an algicide said mixture provided in an amount sufficient to protect a substrate from attack by one or more organisms. The composition can be used broadly in industrial systems and more particularly with substrates such as paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, leather, wood, preservatives, metal working fluids, drilling muds, clay slurries, glazes, optical brightness, carpet backing, pigments and as a preservative for other aqueous and wet state products, and the like.Type: GrantFiled: May 27, 1999Date of Patent: March 6, 2001Assignee: Troy Technology Corporation, Inc.Inventor: Roger Errol Smith
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Patent number: 6194447Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: GrantFiled: July 2, 1999Date of Patent: February 27, 2001Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbæk
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Patent number: 6194396Abstract: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.Type: GrantFiled: October 22, 1999Date of Patent: February 27, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 6153634Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: December 15, 1999Date of Patent: November 28, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
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Patent number: 6143747Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 26, 1998Date of Patent: November 7, 2000Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 6127422Abstract: A method of inhibiting an envelope virus selected from the group consisting of influenza bovine diarrheal, hepatitis C and tick borne encephalitis virus that udergoes hemagglutinin-mediated fusion with a host cell is disclosed which comprises administering to a virus-infected cell, a cell susceptible of infection or a mammal in need thereof, an effective amount of a compound as defined by Formula I in the specification.Type: GrantFiled: January 6, 1999Date of Patent: October 3, 2000Assignee: Eli Lilly and CompanyInventors: Joseph M. Colacino, William J. Hornback, Scott C. Mauldin, John E. Munroe, Joseph C. Tang
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Patent number: 6114327Abstract: The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such as polioviruses, coxsackieviruses of the A and B groups, or echo virus, cardioviruses such as encephalomyocarditis (EMC), apthoviruses such as foot and mouth disease virus, and flaviviruses such as hepatitis C virus and bovine viral diarrhea virus.Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.Type: GrantFiled: October 22, 1999Date of Patent: September 5, 2000Assignee: Eli Lilly and CompanyInventors: Steven Eugene Dunlap, Louis Nickolaus Jungheim, Mark Joseph Tebbe, Gilbert Thomas Voy, John Arnold Werner
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Patent number: 6083961Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.Type: GrantFiled: February 3, 1997Date of Patent: July 4, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 6077862Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: ##STR1## wherein R is selected from the group consisting of H, carboxyl (--CO.sub.2 H), hydroxyl, amino or esters (--CO.sub.2 R') wherein R' is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH.sub.3 CH.sub.2 (OCH.sub.2 CH.sub.2).sub.n --or CH.sub.3 CH.sub.2 CH.sub.2 (OCH.sub.2 CH.sub.2 CH.sub.2).sub.n --or (CH.sub.3).sub.2 CH--(OCH(CH.sub.3)CH.sub.2).sub.n -- wherein n is from 1-3, the pharmaceutically acceptable salts thereof, or mixtures thereof.Type: GrantFiled: March 1, 1999Date of Patent: June 20, 2000Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6071941Abstract: A method for the protection of trees of the families Musaceae or Plantanginaceae from destructive pests whereby the trees to be protected share a common root system.Type: GrantFiled: October 6, 1999Date of Patent: June 6, 2000Assignee: Rhone-Poulenc AgroInventors: Jorge Cepeda, Juan Bocanegra
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Patent number: 6063795Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: G.D. Searle & CompanyInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5981551Abstract: Described herein are substituted 2,5-Diimino-3a,6a-diaryl-1,2,3,3a,4,5,6,6a-octahydroimidazo[4,5-d]imidazol es of formula (I), wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined therein, pharmaceutical compositions containing these compounds, methods of using these compounds as G-CSF Mimetics, and processes used in preparing these compounds.Type: GrantFiled: November 20, 1998Date of Patent: November 9, 1999Assignee: SmithKline Beecham CorporationInventors: Juan I. Luengo, James A. Chan, Ann L. Breen
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Patent number: 5958933Abstract: A method for treating a mammal having a damaged central nervous system, as the result of trauma or disease, for reestablishing previously destroyed neurological functions in a traumatized or diseased mammal, or for controlling spasticity and for providing protection from such injury to the central nervous system. The method comprises administering to the mammal at least one neurologically active compound comprising two groups, one group providing alpha-adrenergic agonist activity, specifically a guanidino group, and the second group providing agonist activity selected from the group consisting of beta-adrenergic agonist activity, serotinergic agonist activity, and GABA-ergic agonist activity (for example a methylated xanthine group, having beta-adrenergic agonist activity) as the primary therapeutic agent. The neurologically active compound is administered in a dosage amount and at a dosage rate sufficient to at least partially restore the lost neurological function or to control spasticity.Type: GrantFiled: June 6, 1995Date of Patent: September 28, 1999Inventor: N. Eric Naftchi
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Patent number: 5939357Abstract: This invention provides a novel fungicide composition which has a bicarbonate-containing inorganic salt ingredient which enhances the efficacy of a fungicide ingredient for the treatment of cultivated crops. An invention fungicide composition also contains a surfactant ingredient, and a water-soluble organic compound which functions as a compatibility enhancing ingredient in aqueous formulations, and the ingredients improve the spreadability and adhesiveness of the composition when applied to foliage. An invention fungicide composition also contains a fertilizer-effective ratio of nitrogen, phosphorus and potassium.Type: GrantFiled: June 7, 1993Date of Patent: August 17, 1999Assignee: Church & Dwight Co., Inc.Inventors: Keith A. Jones, Anthony E. Winston, M. Stephen Lajoie, Amy L. Joseph
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Patent number: 5932600Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: March 14, 1997Date of Patent: August 3, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catharine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Patent number: 5929099Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide in combination with chemotherapeutic agents is disclosed. The particular fungicide used is a benzimidazole derivative. Potentiators can also be included in the composition.Type: GrantFiled: July 15, 1996Date of Patent: July 27, 1999Assignee: Procter & Gamble Co.Inventor: James Berger Camden